SlideShare a Scribd company logo
International Journal of Trend in Scientific Research and Development (IJTSRD)
Volume: 3 | Issue: 4 | May-Jun 2019 Available Online: www.ijtsrd.com e-ISSN: 2456 - 6470
@ IJTSRD | Unique Paper ID - IJTSRD23863 | Volume – 3 | Issue – 4 | May-Jun 2019 Page: 739
Formulation and Evaluation of Nimodipine
Tablet by Liquisolid Technique
Neha Durge1, Kirti Parida2
1Student, 2Assistant Manager
1Department of Pharmaceutics, Smt. Kishoritai Bhoyar College of Pharmacy,
1New Kamptee, Nagpur, Maharastra, India
2Getz Pharma Research Private Limited, Ambarnath, Maharashtra, India
How to cite this paper: Neha Durge |
Kirti Parida "Formulation and
Evaluation of Nimodipine Tablet by
Liquisolid Technique" Published in
International Journal of Trend in
Scientific Research and Development
(ijtsrd), ISSN: 2456-
6470, Volume-3 |
Issue-4, June 2019,
pp.739-745, URL:
https://www.ijtsrd.c
om/papers/ijtsrd23
863.pdf
Copyright © 2019 by author(s) and
International Journal of Trend in
Scientific Research and Development
Journal. This is an Open Access article
distributed under
the terms of the
Creative Commons
Attribution License (CC BY 4.0)
(http://creativecommons.org/licenses/
by/4.0)
ABSTRACT
Liquisolid technique is novel concept of the drug delivery via theoralroute.This
technique is applied to poorly water soluble , water insolubleor lipophilicdrugs.
According to the new formulation method of liquisolid compact, liquid
medication such as solution or suspensions of water insoluble drug in suitable
non- volatile solvent can be converted into acceptably flowingandcompressible
powders by blending with selected powder excipients. The present work
endeavour is directed towards the development of liquisolid compact for
production of immediate releasetabletof waterinsolubleNimodipine.Liquisolid
compacts were prepared by using polyethylene glycol 300 as the liquid vehicle
or non volatile solvent. Crospovidone was used as a superdisintegrating agent
and PVP K30 as a binder. Microcrystalline cellulose was used as a absorbing
carrier and silicone dioxide as adsorbing coating material. The prepared
liquisolid system were evaluated for their micromeretic propertiesand possible
drug-excipients interaction . The FTIR spectra study ruled out any interaction
between the drug and excipients in preparation of Nimodipine liquisolid
compact. The in-vitro dissolution study confirmed enhance drug release from
liquisolid compacts by using USP type I basket in 0.5 % SLS in water. The
selected optimal formula released 93.86 % of its content in 30 min which is
showing immediate release. The results showed that use of superdisintegrants
had remarkable impact on the release rate of Nimodipine from Liquisolid
compact, enhancing the release rate of the drug from liquisolid compact.
Keywords: Nimodipine, Liquisolid technique, immediate release, Crospovidone
INTRODUCTION
Oral route is most common and popular route of
administration of drug because of its systemic effect,patient
compliance, less expensivetomanufacture,safeandeffective
etc. Tablet form is the most widely used dosage form
because of self-administration and ease in manufacturing.
Tablet provides high precision dosing. In most of the cases
immediate on set of action is required as compare to
conventional therapy. To achieve the rapid onset of action
and eliminate the drawbacks of conventional therapy
immediate release dosage form is now a days popular and
used as a alternative oral dosage form. Immediate release
tablets are very quickly absorbed after administration. Basic
approach used in development is the use of
superdisintegrants which provide rapid disintegration of
tablet after administration.1
Nimodipine
belongs to the class of pharmacological agents known as a
calcium channel blockers. Nimodipine is used as a anti-
hypertensive and in subarachnoid hemorrhage and
Arrhythmias. It increases blood flow to injured brain tissues.
The bioavailability is 13% by oral route were95%of protein
binding. It get metabolise in liver and biological half life
having 8-9 hours and drug is excretedfromFacesandurine2.
Many techniques are being employed for the solubility
enhancement of poorly soluble drugs to resolve the
bioavailability issue due to inadequate dissolution rate.
Various approaches make use of hydrophilic polymers as
solubility enhancers acting through a varietyofmechanisms
such as amorphization, co-solvency, micelle formation or
inclusion complexes3,4,5. These techniques impart many
advantageous effects in the formulation development. But
usually these approaches show lack of stability and
decreasing success rate over a period of storage. One of the
remarkable demerits of solid dispersions, glass solutions,
eutectic mixtures and inclusion complexes is formation of
sticky and hygroscopic mass resulting in the poor flow
characteristics. Due to this set-back, industrial feasibility of
the final dosage form becomes very difficult6,7,8.
The liquisolid technology emerged as a new drug delivery
system distinguished by its characteristics and ability to
deliver variety of drugs9,10. Liquisolid drug delivery system
has gained attentionofpharmaceuticalresearchersduetoits
contribution in the solubility enhancement as well as
dissolution retardingapproachesdependingon theneed and
design of the formulation11,12,13.
IJTSRD23863
International Journal of Trend in Scientific Research and Development (IJTSRD) @ www.ijtsrd.com eISSN: 2456-6470
@ IJTSRD | Unique Paper ID - IJTSRD23863 | Volume – 3 | Issue – 4 | May-Jun 2019 Page: 740
Three major components in the formulation of liquisolid
compacts are liquid medication, carrier and coat material14.
Fig.1: Concept of Liquisolid formulation
The aim of the present work is to increase the solubility and
in-vitro dissolution of water insoluble drug Nimodipine by
formulating it into liquisolid tablets. The liquisolid tablets
are prepared by using Avicel PH 101, Avicel PH 102, Avicel
PH 200 as carrier material, Aerosil as coating material, PEG
300 as liquid vehicle
MATERIALS AND METH.ODS
Nimodipine was purchased from Maxwell Life Science Pvt.
Ltd. Mumbai, India. Avicel PH101, Avicel PH102, Avicel
PH200 were purchased from FMC Biopolymer, Aerosil from
Evonik, PEG 300 from Colorcon Asia ,Propylene Glycol from
Sigma Aldrich, Tween 80 from Merck, Crosspovidone from
Nanhang, Sodium Laury Sulphate from Loba Chemical,
Methanol from BP Chemicals, Magnesium stearate from
Peter Greven. All other materials used were of
Pharmaceutical grade.
Solubility studies
For the selection of best non-volatile solvents, solubility
studies were performed. In this procedure, pure drug was
dissolved in non-volatile solvents (propylene glycol and
polyethylene glycol, Tween 80) . Excessamountof puredrug
was added to the above solvents. Obtained saturation
solutions were shaken on sonicator for 1 hours at 250C
under constant vibration. After 1 hours saturated solution
were filtered and analyzed by UV spectrophotometer.
Calculation of loading factor (Lf) and “q” value
Loading factors were calculated for different carriers, using
various solvents. By using Lf = W/Q formula (W: Amount of
liquid medication and Q: Amount of carrier material), the
drug loading factors were obtained and used for calculating
the amount of carrier and coating materials in each
formulation. The results showed that if the viscosity of the
solvent is higher, lower amounts of carrier and coating
materials are needed to produce flowable powder. Based on
R value used, the corresponding q (amount of coating
material) can be calculated for all formulations using the
equation R =Q/q.
Table 1 represents the exact qualitative and quantitative composition for each formulation.
Ingredients
Formulation code ( mg)
(1:1 Ratio of drug +
different vehicle)
Formulation code (mg)
(1:2 Ratio of drug
+ different vehicle )
Formulation code (mg)
(1: 3, 1:4, 1:5 Ratio
of drug + PEG 300)
Nimodipine
F1 F2 F3 F4 F5 F6 F7 F8 F9
30 30 30 30 30 30 30 30 30
Tween 80 30 - - 60 - - - - -
Propylene glycol - 30 - - 60 - - - -
Polyethylene glycol 300 - - 30 - - 60 90 120 150
MCC 101 55 55 55 110 110 80 140 110 110
MCC102 140 140 140 140 140 140 - - 110
MCC200 - - - - - - 220 220 110
PVP k30 - - - - - 30 10 20 20
Aerosil 1.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5
Crosspovidone 2 2 2 2 2 2 2 2 2
Magnesium stearate 1.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5
Total weight of Tablet 260 345 500 510 540
Manufacturing Procedure:-
1. Dispense all the materials as per formula.
2. Nimodipine API was mixed with different vehiclesuchas tween80,Propyleneglycol,PEG300with1:1.1:2,1:3.1:4,1:5ratio.
3. Nimodipine was dispersed in Tween 80 or PG, PEG300, then added Microcrystalline cellulose 101 , 102 ,200 it absorbed
the liquid and get converted into powder form.
4. Then add PVP K30 binder and Crosspovidone and mix properly.
5. After that it get dried in hot air oven at 60ᵒC for 1 hour.
6. Then the blend is pass through sieve no 20.
7. To this blend add aerosil as a coating agent and mix with Magnesium stearate to enhance the flow.
8. After complete mixing compression of the tablet with punch pressure having size 7.5mm or 10mm.
International Journal of Trend in Scientific Research and Development (IJTSRD) @ www.ijtsrd.com eISSN: 2456-6470
@ IJTSRD | Unique Paper ID - IJTSRD23863 | Volume – 3 | Issue – 4 | May-Jun 2019 Page: 741
1. POST COMPRESSION ASSESMENT OF SUBLINGUAL TABLET
The tablets of all the batches were evaluated for weight variation, drug content, hardness, thickness, disintegration time,
wetting time, water absorption ratio, moisture content and in-vitro dissolution study.
Weight Variation: 10 tablets were selected randomly from each batch and weighed individually to check for weight
variation. The following percentage deviation in weight variation is allowed as per USP.
Table No.4: Weight variation tolerances
Average weight of a tablet Percentage deviation
130 mg or less 10
> 130 mg and < 324 mg 7.5
324 mg or more 5
Thickness and Diameter: The thickness and diameter of 4 tablets from each formulation were recorded during the
process of compression using Vernier caliper.
Hardness: Pharmatorn hardness tester was used for the determination of hardness of tablets. Tablet was placed in
between the plungers and the force of the fracture was recorded.
Friability: 6.5 gm. of tablets were accurately weighed and placed in the friabilator (Electrolab, EF-2 Friabilator) and
operated for 100 revolutions. The tablets were de-dusted and reweighed. Percentage friability was calculated using the
following formula
F = (1- W0 / W) × 100
Where,
W0 is the weight of the tablets before the test and W is the weight of the tablet after the test. The tablets that loose less
than 1% weight were considered to be satisfactory.
Disintegration Time: Six tablets were taken and introduced in each tube of disintegration apparatus, and the tablet rack
of the disintegration apparatus was positioned into a one liter beaker containing 900 ml of distilled water and the time of
disintegration was recorded. To discriminate between the formulationsdisintegrationwasdone atroomtemperature and
disk was not used for the study.
In-vitro Dispersion Time: Six tablets were taken for determination of dispersion time. Each tablet was placed in 6 ml
0.5% SDS in Water buffer solution, pH7.0 ± 0.5˚C. Time required for complete dispersion of a tablet was measured.
predetermined time interval 10,20,30,45 min and replaced with same volume of fresh medium 0.5% SDS Water buffer.
Absorbance of this solution was measured at 240 nm.
2. Identification tests for Nimodipine
A. Melting point: The melting point of the Nimodipine was found to be 125 °C which complies with melting point reported
one.
B. UV Scanning: The λmax of Nimodipine was found to be 240 nm. This complies with specified λmax.
Fig.No.2. Scanning of Nimodipine
International Journal of Trend in Scientific Research and Development (IJTSRD) @ www.ijtsrd.com eISSN: 2456-6470
@ IJTSRD | Unique Paper ID - IJTSRD23863 | Volume – 3 | Issue – 4 | May-Jun 2019 Page: 742
C. Infrared Absorption Spectrophotometry:
Fig.No. 3 FTIR spectrum of Nimodipine
Table No.5 FTIR peaks of Nimodipine
Sr. No. Observed Frequency (cm-1) Assignment
1. 1307.97 C-N
2. 1730.92 C=O
3. 745.86 C-H
4. 1747.93 C=C
5. 1541.14 N-H
6. 1646.84 C=N
7. 677.02 C-CI
8. 3903.41 O-H
9. 824.62 C-C
A. Drug-Exipients Compatability study
Drug-Excipients Compatibility Study was carried out with different excipients with different ratio for initial, 15 days, 30
days.
Table No.6 Drug-Excipients compatibility study
Sr.
no
Combination
Physical Appearance
Initial
15 days 30 days
Open closed Open Closed
1 Nimodipine
Off yellow
powder
Off yellow
powder
Off yellow
powder
Off yellow
powder
Off yellow
powder
2 Nimodipine +Mcc 101(1:1)
Off yellow
powder
Off yellow
powder
Off yellow
powder
Off yellow
powder
Off yellow
powder
3 Nimodipine+Mcc 102(1:1)
Off yellow
powder
Off yellow
powder
Off yellow
powder
Off yellow
powder
Off yellow
powder
4 Nimodipine+ Mcc 112(1:1)
Off yellow
powder
Off yellow
powder
Off yellow
powder
Off yellow
powder
Off yellow
powder
5 Nimodipine + 200(1:1)
Off yellow
powder
Off yellow
powder
Off yellow
powder
Off yellow
powder
Off yellow
powder
6 Nimodipine + Tween 80(1:0.5)
Off yellow
powder
Off yellow
powder
Off yellow
powder
Off yellow
powder
Off yellow
powder
7
Nimodipine + propylene
glycol(1:0.5)
Off yellow
powder
Off yellow
powder
Off yellow
powder
Off yellow
powder
Off yellow
powder
8
Nimodipine + Polyethylene
glycol(1:0.5)
Off yellow
powder
Off yellow
powder
Off yellow
powder
Off yellow
powder
Off yellow
powder
9
Nimodipine + PVP K
30(1:0.25)
Off yellow
powder
Off yellow
powder
Off yellow
powder
Off yellow
powder
Off yellow
powder
10
Nimodipine +
Crospovidone(1:0.5)
Off yellow
powder
Off yellow
powder
Off yellow
powder
Off yellow
powder
Off yellow
powder
11 Nimodipine + Aerosil(1:0.25)
Off yellow
powder
Off yellow
powder
Off yellow
powder
Off yellow
powder
Off yellow
powder
International Journal of Trend in Scientific Research and Development (IJTSRD) @ www.ijtsrd.com eISSN: 2456-6470
@ IJTSRD | Unique Paper ID - IJTSRD23863 | Volume – 3 | Issue – 4 | May-Jun 2019 Page: 743
3. PRECOMPRESSION EVALUATION OF LUBRICATED BLEND
Table No.7 Flowability parameter of Nimodipine Liquisolid compact.
Sr. No. Batch Code Bulk Volume Tap Volume Bulk density Tap Density
1. F1 2.1 1.9 0.9523 1.0526
2. F2 4.8 4.3 0.4166 0.4651
3. F3 4.7 4.1 0.4255 0.4878
4. F4 4.9 4.2 0.4081 0.4761
5. F5 5.1 4.4 0.3921 0.4545
6. F6 5.4 4.3 0.3703 0.4651
7. F7 6.1 5.0 0.3278 0.4000
8. F8 6.2 5.2 0.3225 0.3846
9. F9 6.4 5.5 0.3125 0.3636
Table No: 8. Flowability parameter of Nimodipine Liquisolid compact
Formulation code Angle of Repose (Ө) Carr's Index Hausner's Ratio
F1 29.03 12.18 1.13
F2 29.05 10.42 1.11
F3 26.86 12.77 1.14
F4 28.62 14.28 1.16
F5 29.08 13.72 1.15
F6 27.15 20.38 1.25
F7 28.17 18.05 1.22
F8 28.96 16.14 1.19
F9 29.63 14.05 1.16
4. Evaluation of Liquisolid tablets:
Table No:-9. Evaluation of Liquisolid tablets:-
Formulation Code
Thickness
(mm)
Diameter
(mm)
Hardness (kg/cm2) Disintegration time (min:sec)
F1 4.29±0.02 7.09±0.01 1.06±0.25 12 min 51 sec
F2 4.28±0.01 7.13±0.02 2.05±0.19 14 min 34 sec
F3 4.29±0.07 7.10±0.01 1.09±0.30 11 min 46 sec
F4 4.37±0.03 10.24±0.10 1.28±0.11 12 min 32 sec
F5 4.38±0.05 10.20±0.04 2.62±0.28 15 min 10 sec
F6 4.39±0.01 10.05±0.06 2.34±0.20 19 min 54 sec
F7 6.38±0.02 10.19±0.03 2.44±0.15 18 min 59 sec
F8 6.78±0.07 10.21±0.09 2.23±0.55 14 min 10 sec
F9 8.15±0.15 10.22±0.01 3.27±0.12 23 min 45 sec
Conventional Tablets 6.12±0.06 12.20±0.02 9.86±0.16 15 min 36 sec
Mean ±SD n=3
Table No:10. Evaluation of Liquisolid tablets
Formulation code Weight Variation (mg) Friability (%) % Drug content
F1 262.6 0.25 96.78
F2 260.0 0.83 95.26
F3 262.2 0.22 96.20
F4 342.1 0.66 93.58
F5 344.1 0.49 97.51
F6 345.1 0.86 92.26
F7 505.2 0.42 101.22
F8 512.7 0.18 99.24
F9 542.3 0.36 95.18
Conventional 547.3 0.16 94.96
5. In- vitro Drug Release from Nimodipine Liquisolid Compact.
In- Vitro dissolution studies were carried out using USP apparatus typeI at50rpm. Dissolutionmedium consistof 0.5 %SLSin
water maintained at 37ᵒC . Drug release at different time intervals was measured byUV- VisibleSpectrophotometerat240nm.
In- vitro drug release drug release profile of all batches was compared with conventional formulation for drug release.
International Journal of Trend in Scientific Research and Development (IJTSRD) @ www.ijtsrd.com eISSN: 2456-6470
@ IJTSRD | Unique Paper ID - IJTSRD23863 | Volume – 3 | Issue – 4 | May-Jun 2019 Page: 744
Table No: 11. In- vitro release profile of immediate release Liquisolid tablet
Time in min Cumulative % drug release
F1 F2 F3 F4 F5 F6 F7 F8 F9 Conventional Tablet
0 0 0 0 0 0 0 0 0 0 0
5 32.34 31.98 36.67 34.67 35.89 32.34 41.61 62.51 56.94 62.46
10 43.45 36.18 41.45 46.65 40.01 43.45 57.45 66.37 68.57 65.96
15 48.89 43.39 47.47 50.91 46.13 48.89 63.45 70.86 72.31 70.98
20 53.76 51.27 55.68 54.87 55.58 53.76 67.91 76.82 81.89 76.02
25 55.85 57.89 60.76 58.76 61.19 55.85 70.15 88.31 85.64 89.41
30 61.14 63.86 62.21 59.98 64.91 61.14 74.19 93.86 88.49 90.56
Figure No.4. In-Vitro release profile of tablet of batches F4, F5, F6 and Market product
It was observed that F4,F5,F6 prepared by liquisolid techniques using binder PVP K30 to gives 61.14%,63.86%,62.21% drug
release in 30 min and marketed preparation show 90.56% drug releae.F2 give better immediate action.
Figure No.5. In-Vitro release profile of tablet of batches F4, F5, F6 and Market product
It was observed that F4,F5,F6 prepared by liquisolid techniques using binder PVP K30 and disintegrants Crosspovidone to
gives 59.98%,64.91%,61.14 drug release in 30 min and marketed preparation show 90.56% drug releae.F5 give better
immediate action.
Figure No.6. In-Vitro release profile of tablet of batches F7, F8, F9 and Market product
International Journal of Trend in Scientific Research and Development (IJTSRD) @ www.ijtsrd.com eISSN: 2456-6470
@ IJTSRD | Unique Paper ID - IJTSRD23863 | Volume – 3 | Issue – 4 | May-Jun 2019 Page: 745
It was observed that F7,F8,F9 prepared by liquisolid
techniques using binder PVP K30 and disintegrants
Crosspovidonetogives74.19%,93.86%,88.49%drugrelease
in 30 min and marketed preparation show 90.56% drug
releae.F8 give better immediate action.
It was found that immediate release liquisolid tablet
prepared by using binder and disintegrate show immediate
action and greater bioavailability. Formulation no.F8 was
found to be optimized batch.
SUMMARY AND CONCLUSION
The present work showed that the liquisolid technique can
be used for the production of immediate release matrices of
water insoluble drug. PEG 300 was used as the liquid vehicle.
The prepared tablets were evaluated for tablet hardness,
friability, thickness, weight variation, in-vitro disintegration
time and dissolution. The hardness of all tablets was found
to be 1.06 ± 0.25-3.27± 0.12 Kg/cm2. The hardness of all
tablets were kept within the above mentioned range to
compare the disintegration time of tablets prepared using
different vehicle and their varying concentrations. The
friability values were found in the range of 0.5-1 %.
indicating that the tablets were mechanically stable and
could handle rigors of transportation and handling.
Thickness of all formulations was between 4.28±0.01 to
8.15±0.15 mm/inch showing fairly uniform tablets. Out of
the total formulations, the tablets made by using the Drug:
vehicle with ratio 1:4 complex with Crospovidone showed
faster disintegration and faster drug release.
From the study, it can be concluded that liquisolidtechnique
showed better disintegration time and drug release. It can
also be said that use of 7% crosspovidone as a disintegrating
agent gave tablet with faster disintegration time.
In the present work, release studies showed that batch F8 is
an optimized batch which gaves 62.51%, 66.37%, 70.86%,
76.82%, 88.31%, 93.86% drug release in 0, 5, 10, 15, 20, 25,
30 minutes respectively. On the other hand conventional
prepraion showed the 62.46%, 65.96%, 70.98%, 76.08%,
89.41%, 90.56% drug release in 30 minutes respectively.
Dissolution study was performed using USP Dissolution
apparatus I (basket type), using 900 ml dissolution medium
0.5% SLS in water with a rotation speed of 50 rpm.
The release of drug from these formulations provide
evidence that PEG 300 play anvitalrolein immediate release
of drug from liquisolid compact.
Thus, it can be concluded that formulation of Nimodipine
tablet by Liquisolid Technique with appropriate ratio
showed better disintegration time and percent drug release
than other formulation. As all parameters were found
satisfactory for small scale batch, it need to check
commercial feasibility at larger scale. Hence it can be very
well recommended for launching the proposed formulation
in market with some desirable changes if required.
REFERENCE
[1] Jaimini M., Rawat S., Research Journal of
Pharmaceutical, Biological and Chemical Sciences : A
Reviewon immediate drug delivery system, volume 4,
issue 2, 2013, page no.1722-1725
[2] https://en.wikipedia.org/wiki/Nimodipine
[3] Jarowski CI., Rohera BD., Spireas S., Pharmaceutical
Resesarch Powdered solution technology: Principles
and Mechanism, Volume 9, 1990, page no. 1351-1358
[4] Baby D N., Saroj S., Sabitha M., International Journal of
Pharmacy and Pharmaceutical Sciences Mechanism of
solubility of liquisolid formulation in non volatile
solvent: A Review. volume 4,2012, page no. 710-713
[5] Vemula S K., Katkum R ., Journal of Drug Research and
Development: Liquisolid Compact Technique for
improvement of the dissolution rate of flurbiprofen:
formulation and Evaluation, SciForschen., Volume 1.1,
2015, page no. 1-4
[6] Rao S A., Naga A T., International Journal ofResearchin
Pharmaceutical and Biomedical Sciences: Liquisolid
Technology: An Overview, Volume 2 , Issue ,2 2011,
page no. 401-408
[7] Patel H., Patel A , Patel V., International journal of
pharmaceutical research and bioscience, liquisolid
technique: a novel technique for enhancingdissolution
rate of poorly soluble drug. volume 3, issue 2, 2014,
page no. 437-445
[8] Spireas S., Sadu S., Grover R., Journal of Pharmaceutical
Science, In vitro release evaluation of hydrocortisone
liquisolid tables, Volume 87, 1998,page no.867- 876
[9] Spireas S., Saud S., International Journal of
Pharmaceutical Science, Enhancementof Prednisolone
dissolution properties using Liquisolid compact,
Volume 166, 1998, page no.177-88
[10] Anna B., Umashankar M S., Kavitha B., International
journal of applied Pharmaceutics, Liquisolid
Technology- A Latest Review. Academic Science,
Volume 6, Issue1, 2014, page no.11-1513. Karamkar A
B., Gonjari I D., Hosmani A H.,et al., International
Journal of Health Research: Liquisolid tablets: A novel
approach of drug delivery,Volume2,Issue1,2009, page
no.45-50.
[11] Kulkarni A S., Aloorkar N G., Mane M S et al.,
International Journal of Pharmaceutical science and
Nanotechnology,Liquisolid Systems:A Review,Volume
3, Issue 1, 2010, page no. 135-142
[12] Syed I A., Pavani E., International Journal of
Pharmaceutical Sciences and Drug Research The
Liquisolid Technique: Based Drug Delivery System.
Volume 4, Issue 2, 2012, page no. 88-93
[13] 13 Gavali S M., Pacharane S S., Sankpal S S et al.,
International journal of research in pharmacy and
chemistry: Liquisolid compact: A new technique for
enhancement of drug dissolution, Volume 1, Issue 3,
2011, page no. 705-710
[14] Beedha S., Meesa R., World journal of pharmacy and
pharmaceutical sciences: Liquisolid Technology for
enhancing the dissolution profileof Irbesartan byusing
different non volatile solvents and carrier materials,
Volume 3, Issue 10, 2014, page no. 839-843

More Related Content

PPT
Techniques for enhancement of dissolution rate
PPTX
Oral sustained and controlled release dosage forms
PDF
A Review on Dry-powder Inhaler
PPTX
Sustained and controlled drug delivery system
PPTX
Implantable Drug Delivery System
PPTX
Orodispersible tablets
PPTX
Selection of drug candidates cdds.pptx
Techniques for enhancement of dissolution rate
Oral sustained and controlled release dosage forms
A Review on Dry-powder Inhaler
Sustained and controlled drug delivery system
Implantable Drug Delivery System
Orodispersible tablets
Selection of drug candidates cdds.pptx

What's hot (20)

PPTX
Physicochemical and biological properties of sustained release formulations
PDF
Direct compression method..Mominul Islam
PPTX
buccal drug delivery system
PDF
WHO and ICH Guidelines for the Assessment of Herbal Drug
PPTX
Implant drug delivery system
DOCX
Microencapsulation methods
PPTX
Solid dispersion
PPTX
Buccal drug delivery system
PPTX
Bcs classification system
PPTX
Formulation and evaluation of transdermal delivery system
PPTX
Niosomes
DOCX
Implants
PPTX
Implantable Drug Delivery System
PPTX
Controlled release drug delivery system2
PPT
Evaluation of transdermal drug delivery system
PPTX
Buccal drug delivery system
PPTX
Evaluation of Parentrals
PPTX
Gastro Retentive Drug Delivery System
PPT
Aerosol's
PPTX
Dissolution models
Physicochemical and biological properties of sustained release formulations
Direct compression method..Mominul Islam
buccal drug delivery system
WHO and ICH Guidelines for the Assessment of Herbal Drug
Implant drug delivery system
Microencapsulation methods
Solid dispersion
Buccal drug delivery system
Bcs classification system
Formulation and evaluation of transdermal delivery system
Niosomes
Implants
Implantable Drug Delivery System
Controlled release drug delivery system2
Evaluation of transdermal drug delivery system
Buccal drug delivery system
Evaluation of Parentrals
Gastro Retentive Drug Delivery System
Aerosol's
Dissolution models
Ad

Similar to Formulation and Evaluation of Nimodipine Tablet by Liquisolid Technique (20)

PDF
liquisolid system- review
PDF
Formulation, Development and Evaluation of Fast Disintegrating Tablet of Piro...
PDF
Formulation Development and Evaluation of Mouth Dissolving Film of Ziprasidon...
PDF
Formulation and Evaluation of Floating Tablet of Metoprolol Succinate
PDF
Formulation Development and Evaluation of Self Nano Emulsifying Drug Delivery...
PDF
Formulation, Evaluation and Optimization of Fast Disintegrating Nifedipine 20...
PDF
Formulation, Development, Characterization and in Vitro Study of Rosuvastatin...
PDF
Formulation and Evaluation of Fast Disintegrating Tablet of Solid Dispersion ...
PDF
Research Article of Formulation and Evaluation of Fast Dissolving Tablet of N...
PDF
Formulation Development and Evaluation of Carbamazepine Fast Dissolving Tablets
PDF
Formulation and Evaluation of Solid dispersion for Dissolution Enhancement of...
PDF
Formulation Development and Evaluation of Mouth Dissolving Tablet of Thiocolc...
PDF
Formulation and Evaluation of Glimepiride Oral Capsules
PDF
Formulation of Rutin trihydrate Liposomes for Topical Delivery
PDF
Dissolution enhancement of glimepiride by solid dispersion technique.
PPTX
new Puneet PPT On Formulation & Evalution of Nano-Suspension of Carvedilol.pptx
PDF
Development of Gastroretentive Floating Tablets Quetiapine Fumarate
PDF
Formulation and Evaluation of Liquisolid Compact of Etoricoxib for Solubility...
PDF
Formulation development and invitro evaluation of lamotrigine fast dissolving...
PDF
Research Paper 4 (1).pdf.......................
liquisolid system- review
Formulation, Development and Evaluation of Fast Disintegrating Tablet of Piro...
Formulation Development and Evaluation of Mouth Dissolving Film of Ziprasidon...
Formulation and Evaluation of Floating Tablet of Metoprolol Succinate
Formulation Development and Evaluation of Self Nano Emulsifying Drug Delivery...
Formulation, Evaluation and Optimization of Fast Disintegrating Nifedipine 20...
Formulation, Development, Characterization and in Vitro Study of Rosuvastatin...
Formulation and Evaluation of Fast Disintegrating Tablet of Solid Dispersion ...
Research Article of Formulation and Evaluation of Fast Dissolving Tablet of N...
Formulation Development and Evaluation of Carbamazepine Fast Dissolving Tablets
Formulation and Evaluation of Solid dispersion for Dissolution Enhancement of...
Formulation Development and Evaluation of Mouth Dissolving Tablet of Thiocolc...
Formulation and Evaluation of Glimepiride Oral Capsules
Formulation of Rutin trihydrate Liposomes for Topical Delivery
Dissolution enhancement of glimepiride by solid dispersion technique.
new Puneet PPT On Formulation & Evalution of Nano-Suspension of Carvedilol.pptx
Development of Gastroretentive Floating Tablets Quetiapine Fumarate
Formulation and Evaluation of Liquisolid Compact of Etoricoxib for Solubility...
Formulation development and invitro evaluation of lamotrigine fast dissolving...
Research Paper 4 (1).pdf.......................
Ad

More from ijtsrd (20)

PDF
A Study of School Dropout in Rural Districts of Darjeeling and Its Causes
PDF
Pre extension Demonstration and Evaluation of Soybean Technologies in Fedis D...
PDF
Pre extension Demonstration and Evaluation of Potato Technologies in Selected...
PDF
Pre extension Demonstration and Evaluation of Animal Drawn Potato Digger in S...
PDF
Pre extension Demonstration and Evaluation of Drought Tolerant and Early Matu...
PDF
Pre extension Demonstration and Evaluation of Double Cropping Practice Legume...
PDF
Pre extension Demonstration and Evaluation of Common Bean Technology in Low L...
PDF
Enhancing Image Quality in Compression and Fading Channels A Wavelet Based Ap...
PDF
Manpower Training and Employee Performance in Mellienium Ltdawka, Anambra State
PDF
A Statistical Analysis on the Growth Rate of Selected Sectors of Nigerian Eco...
PDF
Automatic Accident Detection and Emergency Alert System using IoT
PDF
Corporate Social Responsibility Dimensions and Corporate Image of Selected Up...
PDF
The Role of Media in Tribal Health and Educational Progress of Odisha
PDF
Advancements and Future Trends in Advanced Quantum Algorithms A Prompt Scienc...
PDF
A Study on Seismic Analysis of High Rise Building with Mass Irregularities, T...
PDF
Descriptive Study to Assess the Knowledge of B.Sc. Interns Regarding Biomedic...
PDF
Performance of Grid Connected Solar PV Power Plant at Clear Sky Day
PDF
Vitiligo Treated Homoeopathically A Case Report
PDF
Vitiligo Treated Homoeopathically A Case Report
PDF
Uterine Fibroids Homoeopathic Perspectives
A Study of School Dropout in Rural Districts of Darjeeling and Its Causes
Pre extension Demonstration and Evaluation of Soybean Technologies in Fedis D...
Pre extension Demonstration and Evaluation of Potato Technologies in Selected...
Pre extension Demonstration and Evaluation of Animal Drawn Potato Digger in S...
Pre extension Demonstration and Evaluation of Drought Tolerant and Early Matu...
Pre extension Demonstration and Evaluation of Double Cropping Practice Legume...
Pre extension Demonstration and Evaluation of Common Bean Technology in Low L...
Enhancing Image Quality in Compression and Fading Channels A Wavelet Based Ap...
Manpower Training and Employee Performance in Mellienium Ltdawka, Anambra State
A Statistical Analysis on the Growth Rate of Selected Sectors of Nigerian Eco...
Automatic Accident Detection and Emergency Alert System using IoT
Corporate Social Responsibility Dimensions and Corporate Image of Selected Up...
The Role of Media in Tribal Health and Educational Progress of Odisha
Advancements and Future Trends in Advanced Quantum Algorithms A Prompt Scienc...
A Study on Seismic Analysis of High Rise Building with Mass Irregularities, T...
Descriptive Study to Assess the Knowledge of B.Sc. Interns Regarding Biomedic...
Performance of Grid Connected Solar PV Power Plant at Clear Sky Day
Vitiligo Treated Homoeopathically A Case Report
Vitiligo Treated Homoeopathically A Case Report
Uterine Fibroids Homoeopathic Perspectives

Recently uploaded (20)

PPTX
Renaissance Architecture: A Journey from Faith to Humanism
PDF
O5-L3 Freight Transport Ops (International) V1.pdf
PPTX
human mycosis Human fungal infections are called human mycosis..pptx
PPTX
school management -TNTEU- B.Ed., Semester II Unit 1.pptx
PDF
The Lost Whites of Pakistan by Jahanzaib Mughal.pdf
PDF
VCE English Exam - Section C Student Revision Booklet
PDF
O7-L3 Supply Chain Operations - ICLT Program
PDF
ANTIBIOTICS.pptx.pdf………………… xxxxxxxxxxxxx
PDF
Physiotherapy_for_Respiratory_and_Cardiac_Problems WEBBER.pdf
PDF
TR - Agricultural Crops Production NC III.pdf
PDF
Complications of Minimal Access Surgery at WLH
PDF
BÀI TẬP BỔ TRỢ 4 KỸ NĂNG TIẾNG ANH 9 GLOBAL SUCCESS - CẢ NĂM - BÁM SÁT FORM Đ...
PDF
Abdominal Access Techniques with Prof. Dr. R K Mishra
PDF
grade 11-chemistry_fetena_net_5883.pdf teacher guide for all student
PDF
3rd Neelam Sanjeevareddy Memorial Lecture.pdf
PPTX
Introduction to Child Health Nursing – Unit I | Child Health Nursing I | B.Sc...
PPTX
Week 4 Term 3 Study Techniques revisited.pptx
PDF
01-Introduction-to-Information-Management.pdf
PPTX
Cell Structure & Organelles in detailed.
PDF
Microbial disease of the cardiovascular and lymphatic systems
Renaissance Architecture: A Journey from Faith to Humanism
O5-L3 Freight Transport Ops (International) V1.pdf
human mycosis Human fungal infections are called human mycosis..pptx
school management -TNTEU- B.Ed., Semester II Unit 1.pptx
The Lost Whites of Pakistan by Jahanzaib Mughal.pdf
VCE English Exam - Section C Student Revision Booklet
O7-L3 Supply Chain Operations - ICLT Program
ANTIBIOTICS.pptx.pdf………………… xxxxxxxxxxxxx
Physiotherapy_for_Respiratory_and_Cardiac_Problems WEBBER.pdf
TR - Agricultural Crops Production NC III.pdf
Complications of Minimal Access Surgery at WLH
BÀI TẬP BỔ TRỢ 4 KỸ NĂNG TIẾNG ANH 9 GLOBAL SUCCESS - CẢ NĂM - BÁM SÁT FORM Đ...
Abdominal Access Techniques with Prof. Dr. R K Mishra
grade 11-chemistry_fetena_net_5883.pdf teacher guide for all student
3rd Neelam Sanjeevareddy Memorial Lecture.pdf
Introduction to Child Health Nursing – Unit I | Child Health Nursing I | B.Sc...
Week 4 Term 3 Study Techniques revisited.pptx
01-Introduction-to-Information-Management.pdf
Cell Structure & Organelles in detailed.
Microbial disease of the cardiovascular and lymphatic systems

Formulation and Evaluation of Nimodipine Tablet by Liquisolid Technique

  • 1. International Journal of Trend in Scientific Research and Development (IJTSRD) Volume: 3 | Issue: 4 | May-Jun 2019 Available Online: www.ijtsrd.com e-ISSN: 2456 - 6470 @ IJTSRD | Unique Paper ID - IJTSRD23863 | Volume – 3 | Issue – 4 | May-Jun 2019 Page: 739 Formulation and Evaluation of Nimodipine Tablet by Liquisolid Technique Neha Durge1, Kirti Parida2 1Student, 2Assistant Manager 1Department of Pharmaceutics, Smt. Kishoritai Bhoyar College of Pharmacy, 1New Kamptee, Nagpur, Maharastra, India 2Getz Pharma Research Private Limited, Ambarnath, Maharashtra, India How to cite this paper: Neha Durge | Kirti Parida "Formulation and Evaluation of Nimodipine Tablet by Liquisolid Technique" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456- 6470, Volume-3 | Issue-4, June 2019, pp.739-745, URL: https://www.ijtsrd.c om/papers/ijtsrd23 863.pdf Copyright © 2019 by author(s) and International Journal of Trend in Scientific Research and Development Journal. This is an Open Access article distributed under the terms of the Creative Commons Attribution License (CC BY 4.0) (http://creativecommons.org/licenses/ by/4.0) ABSTRACT Liquisolid technique is novel concept of the drug delivery via theoralroute.This technique is applied to poorly water soluble , water insolubleor lipophilicdrugs. According to the new formulation method of liquisolid compact, liquid medication such as solution or suspensions of water insoluble drug in suitable non- volatile solvent can be converted into acceptably flowingandcompressible powders by blending with selected powder excipients. The present work endeavour is directed towards the development of liquisolid compact for production of immediate releasetabletof waterinsolubleNimodipine.Liquisolid compacts were prepared by using polyethylene glycol 300 as the liquid vehicle or non volatile solvent. Crospovidone was used as a superdisintegrating agent and PVP K30 as a binder. Microcrystalline cellulose was used as a absorbing carrier and silicone dioxide as adsorbing coating material. The prepared liquisolid system were evaluated for their micromeretic propertiesand possible drug-excipients interaction . The FTIR spectra study ruled out any interaction between the drug and excipients in preparation of Nimodipine liquisolid compact. The in-vitro dissolution study confirmed enhance drug release from liquisolid compacts by using USP type I basket in 0.5 % SLS in water. The selected optimal formula released 93.86 % of its content in 30 min which is showing immediate release. The results showed that use of superdisintegrants had remarkable impact on the release rate of Nimodipine from Liquisolid compact, enhancing the release rate of the drug from liquisolid compact. Keywords: Nimodipine, Liquisolid technique, immediate release, Crospovidone INTRODUCTION Oral route is most common and popular route of administration of drug because of its systemic effect,patient compliance, less expensivetomanufacture,safeandeffective etc. Tablet form is the most widely used dosage form because of self-administration and ease in manufacturing. Tablet provides high precision dosing. In most of the cases immediate on set of action is required as compare to conventional therapy. To achieve the rapid onset of action and eliminate the drawbacks of conventional therapy immediate release dosage form is now a days popular and used as a alternative oral dosage form. Immediate release tablets are very quickly absorbed after administration. Basic approach used in development is the use of superdisintegrants which provide rapid disintegration of tablet after administration.1 Nimodipine belongs to the class of pharmacological agents known as a calcium channel blockers. Nimodipine is used as a anti- hypertensive and in subarachnoid hemorrhage and Arrhythmias. It increases blood flow to injured brain tissues. The bioavailability is 13% by oral route were95%of protein binding. It get metabolise in liver and biological half life having 8-9 hours and drug is excretedfromFacesandurine2. Many techniques are being employed for the solubility enhancement of poorly soluble drugs to resolve the bioavailability issue due to inadequate dissolution rate. Various approaches make use of hydrophilic polymers as solubility enhancers acting through a varietyofmechanisms such as amorphization, co-solvency, micelle formation or inclusion complexes3,4,5. These techniques impart many advantageous effects in the formulation development. But usually these approaches show lack of stability and decreasing success rate over a period of storage. One of the remarkable demerits of solid dispersions, glass solutions, eutectic mixtures and inclusion complexes is formation of sticky and hygroscopic mass resulting in the poor flow characteristics. Due to this set-back, industrial feasibility of the final dosage form becomes very difficult6,7,8. The liquisolid technology emerged as a new drug delivery system distinguished by its characteristics and ability to deliver variety of drugs9,10. Liquisolid drug delivery system has gained attentionofpharmaceuticalresearchersduetoits contribution in the solubility enhancement as well as dissolution retardingapproachesdependingon theneed and design of the formulation11,12,13. IJTSRD23863
  • 2. International Journal of Trend in Scientific Research and Development (IJTSRD) @ www.ijtsrd.com eISSN: 2456-6470 @ IJTSRD | Unique Paper ID - IJTSRD23863 | Volume – 3 | Issue – 4 | May-Jun 2019 Page: 740 Three major components in the formulation of liquisolid compacts are liquid medication, carrier and coat material14. Fig.1: Concept of Liquisolid formulation The aim of the present work is to increase the solubility and in-vitro dissolution of water insoluble drug Nimodipine by formulating it into liquisolid tablets. The liquisolid tablets are prepared by using Avicel PH 101, Avicel PH 102, Avicel PH 200 as carrier material, Aerosil as coating material, PEG 300 as liquid vehicle MATERIALS AND METH.ODS Nimodipine was purchased from Maxwell Life Science Pvt. Ltd. Mumbai, India. Avicel PH101, Avicel PH102, Avicel PH200 were purchased from FMC Biopolymer, Aerosil from Evonik, PEG 300 from Colorcon Asia ,Propylene Glycol from Sigma Aldrich, Tween 80 from Merck, Crosspovidone from Nanhang, Sodium Laury Sulphate from Loba Chemical, Methanol from BP Chemicals, Magnesium stearate from Peter Greven. All other materials used were of Pharmaceutical grade. Solubility studies For the selection of best non-volatile solvents, solubility studies were performed. In this procedure, pure drug was dissolved in non-volatile solvents (propylene glycol and polyethylene glycol, Tween 80) . Excessamountof puredrug was added to the above solvents. Obtained saturation solutions were shaken on sonicator for 1 hours at 250C under constant vibration. After 1 hours saturated solution were filtered and analyzed by UV spectrophotometer. Calculation of loading factor (Lf) and “q” value Loading factors were calculated for different carriers, using various solvents. By using Lf = W/Q formula (W: Amount of liquid medication and Q: Amount of carrier material), the drug loading factors were obtained and used for calculating the amount of carrier and coating materials in each formulation. The results showed that if the viscosity of the solvent is higher, lower amounts of carrier and coating materials are needed to produce flowable powder. Based on R value used, the corresponding q (amount of coating material) can be calculated for all formulations using the equation R =Q/q. Table 1 represents the exact qualitative and quantitative composition for each formulation. Ingredients Formulation code ( mg) (1:1 Ratio of drug + different vehicle) Formulation code (mg) (1:2 Ratio of drug + different vehicle ) Formulation code (mg) (1: 3, 1:4, 1:5 Ratio of drug + PEG 300) Nimodipine F1 F2 F3 F4 F5 F6 F7 F8 F9 30 30 30 30 30 30 30 30 30 Tween 80 30 - - 60 - - - - - Propylene glycol - 30 - - 60 - - - - Polyethylene glycol 300 - - 30 - - 60 90 120 150 MCC 101 55 55 55 110 110 80 140 110 110 MCC102 140 140 140 140 140 140 - - 110 MCC200 - - - - - - 220 220 110 PVP k30 - - - - - 30 10 20 20 Aerosil 1.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5 Crosspovidone 2 2 2 2 2 2 2 2 2 Magnesium stearate 1.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5 Total weight of Tablet 260 345 500 510 540 Manufacturing Procedure:- 1. Dispense all the materials as per formula. 2. Nimodipine API was mixed with different vehiclesuchas tween80,Propyleneglycol,PEG300with1:1.1:2,1:3.1:4,1:5ratio. 3. Nimodipine was dispersed in Tween 80 or PG, PEG300, then added Microcrystalline cellulose 101 , 102 ,200 it absorbed the liquid and get converted into powder form. 4. Then add PVP K30 binder and Crosspovidone and mix properly. 5. After that it get dried in hot air oven at 60ᵒC for 1 hour. 6. Then the blend is pass through sieve no 20. 7. To this blend add aerosil as a coating agent and mix with Magnesium stearate to enhance the flow. 8. After complete mixing compression of the tablet with punch pressure having size 7.5mm or 10mm.
  • 3. International Journal of Trend in Scientific Research and Development (IJTSRD) @ www.ijtsrd.com eISSN: 2456-6470 @ IJTSRD | Unique Paper ID - IJTSRD23863 | Volume – 3 | Issue – 4 | May-Jun 2019 Page: 741 1. POST COMPRESSION ASSESMENT OF SUBLINGUAL TABLET The tablets of all the batches were evaluated for weight variation, drug content, hardness, thickness, disintegration time, wetting time, water absorption ratio, moisture content and in-vitro dissolution study. Weight Variation: 10 tablets were selected randomly from each batch and weighed individually to check for weight variation. The following percentage deviation in weight variation is allowed as per USP. Table No.4: Weight variation tolerances Average weight of a tablet Percentage deviation 130 mg or less 10 > 130 mg and < 324 mg 7.5 324 mg or more 5 Thickness and Diameter: The thickness and diameter of 4 tablets from each formulation were recorded during the process of compression using Vernier caliper. Hardness: Pharmatorn hardness tester was used for the determination of hardness of tablets. Tablet was placed in between the plungers and the force of the fracture was recorded. Friability: 6.5 gm. of tablets were accurately weighed and placed in the friabilator (Electrolab, EF-2 Friabilator) and operated for 100 revolutions. The tablets were de-dusted and reweighed. Percentage friability was calculated using the following formula F = (1- W0 / W) × 100 Where, W0 is the weight of the tablets before the test and W is the weight of the tablet after the test. The tablets that loose less than 1% weight were considered to be satisfactory. Disintegration Time: Six tablets were taken and introduced in each tube of disintegration apparatus, and the tablet rack of the disintegration apparatus was positioned into a one liter beaker containing 900 ml of distilled water and the time of disintegration was recorded. To discriminate between the formulationsdisintegrationwasdone atroomtemperature and disk was not used for the study. In-vitro Dispersion Time: Six tablets were taken for determination of dispersion time. Each tablet was placed in 6 ml 0.5% SDS in Water buffer solution, pH7.0 ± 0.5˚C. Time required for complete dispersion of a tablet was measured. predetermined time interval 10,20,30,45 min and replaced with same volume of fresh medium 0.5% SDS Water buffer. Absorbance of this solution was measured at 240 nm. 2. Identification tests for Nimodipine A. Melting point: The melting point of the Nimodipine was found to be 125 °C which complies with melting point reported one. B. UV Scanning: The λmax of Nimodipine was found to be 240 nm. This complies with specified λmax. Fig.No.2. Scanning of Nimodipine
  • 4. International Journal of Trend in Scientific Research and Development (IJTSRD) @ www.ijtsrd.com eISSN: 2456-6470 @ IJTSRD | Unique Paper ID - IJTSRD23863 | Volume – 3 | Issue – 4 | May-Jun 2019 Page: 742 C. Infrared Absorption Spectrophotometry: Fig.No. 3 FTIR spectrum of Nimodipine Table No.5 FTIR peaks of Nimodipine Sr. No. Observed Frequency (cm-1) Assignment 1. 1307.97 C-N 2. 1730.92 C=O 3. 745.86 C-H 4. 1747.93 C=C 5. 1541.14 N-H 6. 1646.84 C=N 7. 677.02 C-CI 8. 3903.41 O-H 9. 824.62 C-C A. Drug-Exipients Compatability study Drug-Excipients Compatibility Study was carried out with different excipients with different ratio for initial, 15 days, 30 days. Table No.6 Drug-Excipients compatibility study Sr. no Combination Physical Appearance Initial 15 days 30 days Open closed Open Closed 1 Nimodipine Off yellow powder Off yellow powder Off yellow powder Off yellow powder Off yellow powder 2 Nimodipine +Mcc 101(1:1) Off yellow powder Off yellow powder Off yellow powder Off yellow powder Off yellow powder 3 Nimodipine+Mcc 102(1:1) Off yellow powder Off yellow powder Off yellow powder Off yellow powder Off yellow powder 4 Nimodipine+ Mcc 112(1:1) Off yellow powder Off yellow powder Off yellow powder Off yellow powder Off yellow powder 5 Nimodipine + 200(1:1) Off yellow powder Off yellow powder Off yellow powder Off yellow powder Off yellow powder 6 Nimodipine + Tween 80(1:0.5) Off yellow powder Off yellow powder Off yellow powder Off yellow powder Off yellow powder 7 Nimodipine + propylene glycol(1:0.5) Off yellow powder Off yellow powder Off yellow powder Off yellow powder Off yellow powder 8 Nimodipine + Polyethylene glycol(1:0.5) Off yellow powder Off yellow powder Off yellow powder Off yellow powder Off yellow powder 9 Nimodipine + PVP K 30(1:0.25) Off yellow powder Off yellow powder Off yellow powder Off yellow powder Off yellow powder 10 Nimodipine + Crospovidone(1:0.5) Off yellow powder Off yellow powder Off yellow powder Off yellow powder Off yellow powder 11 Nimodipine + Aerosil(1:0.25) Off yellow powder Off yellow powder Off yellow powder Off yellow powder Off yellow powder
  • 5. International Journal of Trend in Scientific Research and Development (IJTSRD) @ www.ijtsrd.com eISSN: 2456-6470 @ IJTSRD | Unique Paper ID - IJTSRD23863 | Volume – 3 | Issue – 4 | May-Jun 2019 Page: 743 3. PRECOMPRESSION EVALUATION OF LUBRICATED BLEND Table No.7 Flowability parameter of Nimodipine Liquisolid compact. Sr. No. Batch Code Bulk Volume Tap Volume Bulk density Tap Density 1. F1 2.1 1.9 0.9523 1.0526 2. F2 4.8 4.3 0.4166 0.4651 3. F3 4.7 4.1 0.4255 0.4878 4. F4 4.9 4.2 0.4081 0.4761 5. F5 5.1 4.4 0.3921 0.4545 6. F6 5.4 4.3 0.3703 0.4651 7. F7 6.1 5.0 0.3278 0.4000 8. F8 6.2 5.2 0.3225 0.3846 9. F9 6.4 5.5 0.3125 0.3636 Table No: 8. Flowability parameter of Nimodipine Liquisolid compact Formulation code Angle of Repose (Ө) Carr's Index Hausner's Ratio F1 29.03 12.18 1.13 F2 29.05 10.42 1.11 F3 26.86 12.77 1.14 F4 28.62 14.28 1.16 F5 29.08 13.72 1.15 F6 27.15 20.38 1.25 F7 28.17 18.05 1.22 F8 28.96 16.14 1.19 F9 29.63 14.05 1.16 4. Evaluation of Liquisolid tablets: Table No:-9. Evaluation of Liquisolid tablets:- Formulation Code Thickness (mm) Diameter (mm) Hardness (kg/cm2) Disintegration time (min:sec) F1 4.29±0.02 7.09±0.01 1.06±0.25 12 min 51 sec F2 4.28±0.01 7.13±0.02 2.05±0.19 14 min 34 sec F3 4.29±0.07 7.10±0.01 1.09±0.30 11 min 46 sec F4 4.37±0.03 10.24±0.10 1.28±0.11 12 min 32 sec F5 4.38±0.05 10.20±0.04 2.62±0.28 15 min 10 sec F6 4.39±0.01 10.05±0.06 2.34±0.20 19 min 54 sec F7 6.38±0.02 10.19±0.03 2.44±0.15 18 min 59 sec F8 6.78±0.07 10.21±0.09 2.23±0.55 14 min 10 sec F9 8.15±0.15 10.22±0.01 3.27±0.12 23 min 45 sec Conventional Tablets 6.12±0.06 12.20±0.02 9.86±0.16 15 min 36 sec Mean ±SD n=3 Table No:10. Evaluation of Liquisolid tablets Formulation code Weight Variation (mg) Friability (%) % Drug content F1 262.6 0.25 96.78 F2 260.0 0.83 95.26 F3 262.2 0.22 96.20 F4 342.1 0.66 93.58 F5 344.1 0.49 97.51 F6 345.1 0.86 92.26 F7 505.2 0.42 101.22 F8 512.7 0.18 99.24 F9 542.3 0.36 95.18 Conventional 547.3 0.16 94.96 5. In- vitro Drug Release from Nimodipine Liquisolid Compact. In- Vitro dissolution studies were carried out using USP apparatus typeI at50rpm. Dissolutionmedium consistof 0.5 %SLSin water maintained at 37ᵒC . Drug release at different time intervals was measured byUV- VisibleSpectrophotometerat240nm. In- vitro drug release drug release profile of all batches was compared with conventional formulation for drug release.
  • 6. International Journal of Trend in Scientific Research and Development (IJTSRD) @ www.ijtsrd.com eISSN: 2456-6470 @ IJTSRD | Unique Paper ID - IJTSRD23863 | Volume – 3 | Issue – 4 | May-Jun 2019 Page: 744 Table No: 11. In- vitro release profile of immediate release Liquisolid tablet Time in min Cumulative % drug release F1 F2 F3 F4 F5 F6 F7 F8 F9 Conventional Tablet 0 0 0 0 0 0 0 0 0 0 0 5 32.34 31.98 36.67 34.67 35.89 32.34 41.61 62.51 56.94 62.46 10 43.45 36.18 41.45 46.65 40.01 43.45 57.45 66.37 68.57 65.96 15 48.89 43.39 47.47 50.91 46.13 48.89 63.45 70.86 72.31 70.98 20 53.76 51.27 55.68 54.87 55.58 53.76 67.91 76.82 81.89 76.02 25 55.85 57.89 60.76 58.76 61.19 55.85 70.15 88.31 85.64 89.41 30 61.14 63.86 62.21 59.98 64.91 61.14 74.19 93.86 88.49 90.56 Figure No.4. In-Vitro release profile of tablet of batches F4, F5, F6 and Market product It was observed that F4,F5,F6 prepared by liquisolid techniques using binder PVP K30 to gives 61.14%,63.86%,62.21% drug release in 30 min and marketed preparation show 90.56% drug releae.F2 give better immediate action. Figure No.5. In-Vitro release profile of tablet of batches F4, F5, F6 and Market product It was observed that F4,F5,F6 prepared by liquisolid techniques using binder PVP K30 and disintegrants Crosspovidone to gives 59.98%,64.91%,61.14 drug release in 30 min and marketed preparation show 90.56% drug releae.F5 give better immediate action. Figure No.6. In-Vitro release profile of tablet of batches F7, F8, F9 and Market product
  • 7. International Journal of Trend in Scientific Research and Development (IJTSRD) @ www.ijtsrd.com eISSN: 2456-6470 @ IJTSRD | Unique Paper ID - IJTSRD23863 | Volume – 3 | Issue – 4 | May-Jun 2019 Page: 745 It was observed that F7,F8,F9 prepared by liquisolid techniques using binder PVP K30 and disintegrants Crosspovidonetogives74.19%,93.86%,88.49%drugrelease in 30 min and marketed preparation show 90.56% drug releae.F8 give better immediate action. It was found that immediate release liquisolid tablet prepared by using binder and disintegrate show immediate action and greater bioavailability. Formulation no.F8 was found to be optimized batch. SUMMARY AND CONCLUSION The present work showed that the liquisolid technique can be used for the production of immediate release matrices of water insoluble drug. PEG 300 was used as the liquid vehicle. The prepared tablets were evaluated for tablet hardness, friability, thickness, weight variation, in-vitro disintegration time and dissolution. The hardness of all tablets was found to be 1.06 ± 0.25-3.27± 0.12 Kg/cm2. The hardness of all tablets were kept within the above mentioned range to compare the disintegration time of tablets prepared using different vehicle and their varying concentrations. The friability values were found in the range of 0.5-1 %. indicating that the tablets were mechanically stable and could handle rigors of transportation and handling. Thickness of all formulations was between 4.28±0.01 to 8.15±0.15 mm/inch showing fairly uniform tablets. Out of the total formulations, the tablets made by using the Drug: vehicle with ratio 1:4 complex with Crospovidone showed faster disintegration and faster drug release. From the study, it can be concluded that liquisolidtechnique showed better disintegration time and drug release. It can also be said that use of 7% crosspovidone as a disintegrating agent gave tablet with faster disintegration time. In the present work, release studies showed that batch F8 is an optimized batch which gaves 62.51%, 66.37%, 70.86%, 76.82%, 88.31%, 93.86% drug release in 0, 5, 10, 15, 20, 25, 30 minutes respectively. On the other hand conventional prepraion showed the 62.46%, 65.96%, 70.98%, 76.08%, 89.41%, 90.56% drug release in 30 minutes respectively. Dissolution study was performed using USP Dissolution apparatus I (basket type), using 900 ml dissolution medium 0.5% SLS in water with a rotation speed of 50 rpm. The release of drug from these formulations provide evidence that PEG 300 play anvitalrolein immediate release of drug from liquisolid compact. Thus, it can be concluded that formulation of Nimodipine tablet by Liquisolid Technique with appropriate ratio showed better disintegration time and percent drug release than other formulation. As all parameters were found satisfactory for small scale batch, it need to check commercial feasibility at larger scale. Hence it can be very well recommended for launching the proposed formulation in market with some desirable changes if required. REFERENCE [1] Jaimini M., Rawat S., Research Journal of Pharmaceutical, Biological and Chemical Sciences : A Reviewon immediate drug delivery system, volume 4, issue 2, 2013, page no.1722-1725 [2] https://en.wikipedia.org/wiki/Nimodipine [3] Jarowski CI., Rohera BD., Spireas S., Pharmaceutical Resesarch Powdered solution technology: Principles and Mechanism, Volume 9, 1990, page no. 1351-1358 [4] Baby D N., Saroj S., Sabitha M., International Journal of Pharmacy and Pharmaceutical Sciences Mechanism of solubility of liquisolid formulation in non volatile solvent: A Review. volume 4,2012, page no. 710-713 [5] Vemula S K., Katkum R ., Journal of Drug Research and Development: Liquisolid Compact Technique for improvement of the dissolution rate of flurbiprofen: formulation and Evaluation, SciForschen., Volume 1.1, 2015, page no. 1-4 [6] Rao S A., Naga A T., International Journal ofResearchin Pharmaceutical and Biomedical Sciences: Liquisolid Technology: An Overview, Volume 2 , Issue ,2 2011, page no. 401-408 [7] Patel H., Patel A , Patel V., International journal of pharmaceutical research and bioscience, liquisolid technique: a novel technique for enhancingdissolution rate of poorly soluble drug. volume 3, issue 2, 2014, page no. 437-445 [8] Spireas S., Sadu S., Grover R., Journal of Pharmaceutical Science, In vitro release evaluation of hydrocortisone liquisolid tables, Volume 87, 1998,page no.867- 876 [9] Spireas S., Saud S., International Journal of Pharmaceutical Science, Enhancementof Prednisolone dissolution properties using Liquisolid compact, Volume 166, 1998, page no.177-88 [10] Anna B., Umashankar M S., Kavitha B., International journal of applied Pharmaceutics, Liquisolid Technology- A Latest Review. Academic Science, Volume 6, Issue1, 2014, page no.11-1513. Karamkar A B., Gonjari I D., Hosmani A H.,et al., International Journal of Health Research: Liquisolid tablets: A novel approach of drug delivery,Volume2,Issue1,2009, page no.45-50. [11] Kulkarni A S., Aloorkar N G., Mane M S et al., International Journal of Pharmaceutical science and Nanotechnology,Liquisolid Systems:A Review,Volume 3, Issue 1, 2010, page no. 135-142 [12] Syed I A., Pavani E., International Journal of Pharmaceutical Sciences and Drug Research The Liquisolid Technique: Based Drug Delivery System. Volume 4, Issue 2, 2012, page no. 88-93 [13] 13 Gavali S M., Pacharane S S., Sankpal S S et al., International journal of research in pharmacy and chemistry: Liquisolid compact: A new technique for enhancement of drug dissolution, Volume 1, Issue 3, 2011, page no. 705-710 [14] Beedha S., Meesa R., World journal of pharmacy and pharmaceutical sciences: Liquisolid Technology for enhancing the dissolution profileof Irbesartan byusing different non volatile solvents and carrier materials, Volume 3, Issue 10, 2014, page no. 839-843