![ Kadam N. R,et.al,(2015)[28]: Microspheres are
multiparticulate drug delivery systems which are prepared
to obtain prolonged or controlled drug delivery to improve
bioavailability, stability and to target the drug to specific
site at a predetermined rate. They are made from
polymeric waxy or other protective materials such as
natural, semi synthetic and synthetic polymers.
Microspheres are characteristically free flowing powders
having particle size ranging from 1-1000 μm consisting of
proteins or synthetic polymers. The range of techniques for
the preparation of microspheres provides multiple options
to control as drug administration aspects and to enhance
the therapeutic efficacy of a given the drug.
Literature Review](https://image.slidesharecdn.com/metforminepowerpointpresentation-180426113024/85/Metformine-power-point-presentation-slide-share-7-320.jpg)
Metformine power point presentation .. .slide share
- 1. FORMULATIONAND CHARACTERIZATION OF THE METFORMINHCL MICROSPHERES prepared by Kota.sriram & vanguri anil
- 2. INTRODUCTION To obtain maximum therapeutic efficacy, it becomes necessary to deliver the agent to the target tissue in the optimal amount in the right period of time there by causing little toxicity and minimal side effects. There are various approaches in delivering a therapeutic substance to the target site in a sustained controlled release fashion. One such approach is using microspheres as carriers for drugs. The development of new delivery systems for the controlled release of drugs is one of the most interesting fields of research in pharmaceutical sciences
- 3. A well designed controlled drug delivery system can overcome some of the problems of conventional therapy and enhance the therapeutic efficacy of a given drug. To obtain maximum therapeutic efficacy, it becomes necessary to deliver the agent to the target tissue in the optimal amount in the right period of time there by causing little toxicity and minimal side effects. There are various approaches in delivering a therapeutic substance to the target site in a sustained controlled release fashion. .
- 4. Microsphere can be used for the controlled release of drugs, vaccines, antibiotics, and hormones. advantage of the characteristics of microspheres, beyond the basic benefits, the microspheres could provide a larger surface area and possess an easier esti Albumin and gelatins are natural polymers , and poly lactic acid and polyglycolic acids are synthetic polymers. Microspheres are admistered orally to sustain drug release, and to reduce or eliminate gastrointestinal tract irritation.
- 5. Showing the picture of microspheres
- 6. Type of microspheres Bio adhesive Microspheres Magnetic Microspheres Floating microspheres Polymeric Microspheres
- 7. Kadam N. R,et.al,(2015)[28]: Microspheres are multiparticulate drug delivery systems which are prepared to obtain prolonged or controlled drug delivery to improve bioavailability, stability and to target the drug to specific site at a predetermined rate. They are made from polymeric waxy or other protective materials such as natural, semi synthetic and synthetic polymers. Microspheres are characteristically free flowing powders having particle size ranging from 1-1000 μm consisting of proteins or synthetic polymers. The range of techniques for the preparation of microspheres provides multiple options to control as drug administration aspects and to enhance the therapeutic efficacy of a given the drug. Literature Review
- 8. These delivery systems offer numerous advantages compared to conventional dosage forms, which include improved efficacy, reduced toxicity, improved patient compliance and convenience. Such systems often use macromolecules as carriers for the drugs. The present review highlights various types of microspheres, different methods of preparation, its applications and also various parameters to evaluate their efficiency. Microspheres are various types like Bioadhesive microspheres, Magnetic microspheres, Floating microspheres, Radioactive microspheres etc...
- 9. AIMAND OBJECTIVES Aim: formulation and characterization of the metformin hcl microspheres Objectives: The main objective of the present study is to design various types of Microspheres of Metformin hcl using polymers in various ratios. These different types of microspheres are prepared with respect to enhance the drug release to attain site specific drug delivery of the dosage form.
- 10. To obtain controlled drug release for prolonged period of time which in turn enhance bioavailability and therapeutic efficacy of the dosage forms. Improvement of Patient compliance by reducing dosing frequency.
- 11. DRUGPROFILE Name: Metformin hydrochloride Molecular weight: 129.16 g/mol Molecular formula: C4H11N5 IUPACname: 1,1-Dimethylbiguanide
- 12. Mechanismof action Metformin's mechanisms of action differ from other classes of oral antihyperglycemic agents. Metformin decreases blood glucose levels by decreasing hepatic glucose production, decreasing intestinal absorption of glucose, and improving insulin sensitivity by increasing peripheral glucose uptake and utilization. These effects are mediated by the initial activation by metformin of AMP-activated protein kinase (AMPK), a liver enzyme that plays an important role in insulin signaling, whole body energy balance, and the metabolism of glucose and fats.
- 13. Activation of AMPK is required for metformin's inhibitory effect on the production of glucose by liver cells. Increased peripheral utilization of glucose may be due to improved insulin binding to insulin receptors. Bioavailability: 50-60% hours Half-life: 2hrs Protein binding: Minimal Metabolism: Hepatic Elimination: Urine Uses: Metformin is primarily used for type 2 diabetes,
- 14. MATERIALS AND EQUIMENTS • Materials: Metformin hcl Sodium alginate Cacl2 • Equipments UV/VIS Double beam Spectrophotometer FTIR Weighing balance Franze diffusion cell
- 15. PLAN OF THE WORK Literature survey Pre formulation studies A. Preformulation study of metformin hcl a) Organoleptic Properties b) Determination of solubility c) Calibration curve d) Drug –excipient compatability studies by FTIR Preparation Microspheres by using various concentrations of Polymers Evaluation of Microspheres
- 16. METHADOLOGY Physical properties: Colour, odour, taste and appearance Determination of solubility Construction of Calibration Curve Preparation of Stock Solution
- 17. procedure • Procedure: Metformin HCl microspheres developed by ionotropic gelation technique. In this technique the sodium alginate is used as polymer in different ratios in different trails. The drug dissolved in respective solvents such as water . First to disperse polymer in respective solvent such as water and it is kept on magnatic stirrar for stirring for 1 hour at 100-500 rpm. Then add the drug to the polymer solution. After formation polymeric viscous solution kept stirring for 30 mins on magnetic stirring. After solution is added dropwise to the cacl2 solution with a needle and kept for stirring till formation of the microspheres for 1 hour. After development of the microspheres filtered and dried in a oven.
- 18. Ingridien ts Metformi n hcl Sodium alginate water Cacl2 F1 100 600 q.s 5% F2 100 700 q.s 5% F3 100 800 q.s 5% F4 100 900 q.s 5% F5 100 1000 q.s 5% FORMULATIONTABLE
- 19. RESULTS • Organoleptic characters Description - White crystalline powder Taste - Taste less Odour - Odour less Colour - White
- 20. Solubility soluble in DMSO ,whater and methanol Calibration curve y = 0.0187x + 0.01 R² = 0.9988 0 0.1 0.2 0.3 0.4 0.5 0.6 0.7 0.8 0 20 40 60 Absorbance concentration abs(nm) Linear (abs(nm))
- 21. Evaluationstudies: • Particle size determination showing the figure of microspheres
- 22. %of drug content studies Swelling index In-vitro drug release studies • Stability samples are stored at • Accelerated: 40±20C/75±5% RH • Intermediate: 30±20C/65±5% RH • Long term: 25±20C/60±5% RH
- 23. All comparative drug release profile 0 20 40 60 80 100 120 0 2 4 6 8 10 DR1 DR2 DR3 DR4 DR5 TIME %OFDRUGRELEASE
- 24. Conclusion The development and characterisation of Metformin hcl microspheres by applying method of ionotropic gelation method. Before going develop the formulation the pre formulation studies are carried out that are calibration , FTIR, physical properties of drugs such as appearance, taste, odour, solubility. The FTIR conducted between drug and excipients there is no incompatable matter is present. The formulation is developed by using ionotropic gelation technique the sodium alginate is used as the polymer in different concentration. F1-F5 formulations are developed .
- 25. The developed formulations are kept under evaluation parameters such as %of drug content,swelling index, SEM analysis ,In-vitro drug release studies. The In-vitro drug release studies carried out by franse diffusion cell up to 8hours. The optimised formulation under kept stability studies for 1month there is no degradation takes place.
- 26. References • 1. N. K. Jain, Controlled and Novel drug delivery, 04 Edition, CBS Publishers New Delhi, India; 21, 236-237. • 2. P.M. Dandagi, VS. Mastiholimath, M.B. Patil, M.K. Gupta, Biodegradable microparticulate system of captopril. International Journal of Pharmaceutics. 307, 2006, 83-88. • 3. Chinna Gangadhar B, Shyam Sunder R., Vimal Kumar Varma. M., Sleeva Raju M., Sai Kiran M, Formulation and Evaluation of Indomethacin Microspheres using natural and synthetic polymers as Controlled Release Dosage Forms. International Journal of Drug Discovery, 2(1), 2010,8-16. • 4. Imran Abdul Kayyum Tadwee*, Sadhana Shahi, M. Thube, Ankit S. Review on Microspheres. International Journal of Pharmaceutical Research Allied Sciences, 1(1), 2012, 24-33. • 5. Saravana Kumar K., Jayachandra Reddy P., Chandra Sekhar K.B., A Review on Microsphere for Novel drug delivery System. Journal of Pharmacy Research, 5(1), 2012, 420-424.