Vilda+Metformin CR tablet.pptx

Useful in developing CR tablets

1. Development and evaluation of combined formulation for the immediate delivery of vildagliptin and sustained delivery of metformin hcl with comparison to the marketed formulation CONTENTS : Aim and objective Introduction Plan of work Literature review Drug profile Experimental methodology

2. Aim The aim of this study is to formulate and evaluate the bilayer tablet (immediate delivery of vildagliptin and sustained release of metformin hcl with comparison to marketed formulation Objectives Preparation of immediate release layer of vildagliptin 400mg (polymers used HPMC, PEO, Locust bean gum) Preparation of sustained release layer of metformin hcl 900mg (polymers used HPMC, Eutragid, PEO) Preparation of bilayer tablet by direct compression method. Evaluation studies of bilayer tablet of vildagliptin and metformin hcl. Optimization by using DOE (to find the best levels for input factors) Comparative studies by using dissolution and disintegration time.

3. Diabetes mellitus (DM) is a major public health issue affecting more than 400 million people worldwide. DM is caused either by deficiency of insulin secretion, damage of pancreatic β cell or insulin resistance related to non-use of insulin. Type 1 DM and type 2 DM are the 2 types of DM. Type 1 DM is an autoimmune disorder that affects pancreatic cells which reduces or impairs the production of insulin while type 2 DM is a result of impairment of pancreatic beta cells that hinder the individual’s ability to use insulin The multilayered tablet concept has been long utilized to develop sustained release formulations. Such a tablet has a fast releasing layer and may contain bi& or triple layers to sustain the drug release. The pharmacokinetic advantage relies on the fact that drug release from immediate release layer leads to a sudden rise in the blood concentration. However, the blood level is maintained at steady state as the drug is released from the sustained release layer. INTRODUCTION

4. Selection of drug-vildagliptin and metformin hcl Selection of polymers and excipients Method of preparation of bilayer tablet Evaluation of bilayer tablet Comparison with marketed bilayer tablets PLAN OF WORK

5. DRUG FORMULATION METHOD PURPOSE REFERENCE Vildagliptin and metformin HCL Bilayer tablet Direct compression method Treatment of patient with type II Diabetes. Twinkle K. Prajapati (IJCAR) research article LITERATURE REVIEW

6. DRUG FORMULATION EXCIPIENT METHOD PURPOSE REFERENCE Vildagliptin(IR)and metformin hcl(SR) Bilayer tablet IR-Microcrystalline cellulose, Magnesium stearate, Super disintegrant, SR-HPMC K4M, Carbopolol 934p, Lactose monohydrate IR- Direct compression SR- wet granulation Treatment for type II diabetes mellitus Nishit Gohel, Komal Patel, Jignasa Modi, Formulation development and evaluation of modified release tablet using a fixed dose combination of anti diabetic drugs

7. Metformin Summary: Metformin is a biguanide anti hyperglycemic used in conjunction with diet and exercise for glycemic control in type 2 diabetes mellitus. It is also used off-label for insulin resistance in polycystic ovary syndrome (PCOS). Brand Names: Actoplus Met, Avandamet, Fortamet, Glucophage, Glucovance, Glumetza, Glycon, Invokamet, Janumet, Jentadueto, Kazano, Kombiglyze, Komboglyze, Qternmet, Riomet, Segluromet, Synjardy, Trijardy, Velmetia, Xigduo Generic Name: Metformin Structure: BCS classification : class III Weight: Average: 129.1636 Chemical Formula: C4H11N5 DRUG PROFILE

8. Synonyms : Dimethyl biguanid Metformin combination products : DPP-4 inhibitors (sitagliptin,vildagliptin, linagliptin, alogliptin, or saxagliptin), combination with SGLT2 inhibitors (canagliflozin, empagliflozin, ertugliflozin, or dapagliflozin) or in combination with pioglitazone. Half-life : The plasma elimination half-life of metformin is 6.2 hours in the plasma. The elimination half-life in the blood is approximately 17.6 hours Clearance : Renal clearance is about 3.5 times greater than creatinine clearance, which indicates that tubular secretion is the major route of metformin elimination. Following oral administration, approximately 90% of the absorbed drug is eliminated via the renal route within the first 24 hours DOSE: 500mg – 1000mg

9. VILDAGLIPTIN Summary: Vildagliptin is a once-daily dipeptidyl peptidase 4 (DPP-4) inhibitor used in the management of type 2 diabetes mellitus . Brand Names : Galvus, Jalra, Xiliarx Weight Average : 303.3993 Structure: Chemical Formula: C 17 H 25 N 3 O 2 Half-life: The mean elimination half-life following intravenous administration is approximately two hours. The elimination half-life after oral administration is approximately three hours. Clearance: After intravenous administration to healthy subjects, the total plasma and renal clearance vildagliptin were 41 and 13 L/h, respectively Dosage : 50mg or 100 mg

10. VILDAGLIPTIN IR

11. Experimental methodology: SR-900MG S.no Materials 1. Drug ( metformin) 2. HPMC 3. Eutragid 4. PEO 5. Magnesium stearate 6. Aerosil 7. MCC 5OO mg 300mg, 270mg, 225mg, 180mg 3mg 3mg 94mg, 124mg, 169mg, 214mg

12. S.NO MATERIALS 1 Drug (vildagliptin) 2 HPMC 3 HPMC+PEO 4 Locust bean gum + PEO 5 HPMC+ Locust bean gum 6 Mg stearate 7 Aerosil 8 MCC Immediate Release: 400mg 100mg 100mg 75mg+ 75mg 75mg+75mg 75mg+ 75mg 2mg 2mg 196mg, 146mg

13. SR- drug (metformin is added to the polymers ( hpmc , eutragid and PEO) coshift and mix well magnesium stearate , aerosil and mcc is added. pass through 60 mesh Double compression ( tablet compression machine) Preparation of SR layer (metformin) and IR vildagliptin {double compression) Direct compression method IR- drug (vildagliptin) + hpmc , PEO, locust bean gum, mg stearate, aerosil , mcc

14. Hardness Angle of repose Disintegration Dissolution Friability Weight variation Bulk density Evaluation

15. Thank you