Formulation development of multi unit particulate system(MUPS)for anti-diabetic drugs

Surendra Agrawal,Ketaki Joshi,Ram Gaud

SPPSPTM,SVKMs NMIMS,Vile Parle(W),Mumbai 400056,India

Formulation development of multi unit particulate system(MUPS)for anti-diabetic drugs

Surendra Agrawal*,Ketaki Joshi,Ram Gaud

SPPSPTM,SVKMs NMIMS,Vile Parle(W),Mumbai 400056,India

A R T I C L E I N F O

Article history:

Available online 23 November 2015

Sitagliptin

Metformin sustain release matrix pellets

MUPs

Metformin hydrochloride and sitagliptin phosphate is the common combination among diabetic drugs.Available dosage forms cannot avoid the dose dumping which leads to the complication such as lactic acidosis,gastrointestinal complication, and severe hypoglycemia.Metformin hydrochloride has a very short half-life,i.e.4 hrs,and thus fails to give action for the long period.This leads to the increase number of dosings per day.Single-unit formulations contain the active ingredient within the single tablet or capsule,whereas multiple-unit dosage forms comprise a number of discrete particles that are combined into one dosage unit.Other advantages of this divided dose include ease of adjustment of the strength,administration of incompatible drugs in a single dosage unit by separating them in different multiparticulates and different drug-release rates to obtain the desired overall release profle[1].

Metformin has small half-life compared to Sitagliptin phosphate;therefore,enteric coated sustained release matrix pellets were formulated for Metformin to improve the release pattern while immediate release pellets were formulated for Sitagliptin. The excipients chosen showed maximum utility even in lesser quantities,which served their purpose in the formulation of both types of pellets by extrusion spheronization process.The process parameters were controlled and the pellets were characterized for Aspect ratio and sphericity.Based on the drug release studies,batch MET/F/5 was observed to be showing 97.4%of release without coating for 12 hrs and shows less than 10%of drug release in 0.1 N HCl,and thus it was concluded that enteric coating of sustained release matrix pellets of Metformin was optimized.Along with this optimized batch of immediate release sitagliptin phosphate STG/F/8 showed 99.58% of release within 60 minutes.

The tablets formulated of these immediate release and sustained release pellets are observed to have 95%of content uniformity.The 8%–10%of coating with Eudragit S 100 and L 100-55 was considered optimum for coating of the pellets. The scanning electron microscopy of pellets revealed thatimmediate release pellets were with very smooth surface and sustained release matrix pellets without coating revealed slightly rough surface.The pellets were compressed in tablets and the compressed tablets were optimized based on the friability,hardness and thickness.The tablets were evaluated for the release pattern and optimized batch showed release of 96.4% of Sitagliptin in 1 hour while 97.3%of Metformin in 12 hrs.

Fig.1–Immediate and sustained release pellets.(A)Immediate release Sitagliptin phosphate pellets.(B)Sustained release Metformin hydrochloride pellets.

The developed dosage form of Metformin and Sitagliptin is expected to control glucose level through controlled release of drugs.

Acknowledgements

The authors acknowledge Dr.P.G Shrotriya,Research Director,and Dr.R.S.Gaud,Dean(Pharm.Sciences),for their support and encouragement in carrying out this work.

R E F E R E N C E

[1]Reddy S,Das P,Das H,et al.MUPS(multiple unit pellet system)tablets–a brief review.J Pharm Biomed Sci 2011;12(2):1–5.

*E-mail address:Surendra.agrawal80@gmail.com;sagrawal80@gmail.com.

Peer review under responsibility of Shenyang Pharmaceutical University.

http://dx.doi.org/10.1016/j.ajps.2015.10.060

1818-0876/©2016 The Authors.Production and hosting by Elsevier B.V.on behalf of Shenyang Pharmaceutical University.This is an open access article under the CC BY-NC-ND license(http://creativecommons.org/licenses/by-nc-nd/4.0/).