#205 Development and characterization of Sitagliptin microsphere for controlled release and better patient compliance

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Jana, A. .; De, P. K. .; Maity, B. . #205 Development and Characterization of Sitagliptin Microsphere for Controlled Release and Better Patient Compliance. J Pharm Chem 2022, 8.

Abstract

In the last few decades, it has been observed that the diabetes population is increasing around the world. Apart from insulin injections, various oral antihyperglycemic medications are available, like sitagliptin, to increase insulin production to control diabetic conditions. But sitagliptin has a very short biological half-life of 8-14 h, and only 38% drug binds to plasma protein; also, 79% drug is eliminated from the body unchanged from the urine, due to which patients required multiple dosing. The objective of the present study was to develop a microsphere with a hydrophobic primary polymer like ethyl cellulose (EC) and hydrophilic secondary polymer HPMC to sustain the drug release and to control the desired release rate with an increase in the duration of drug action. With the primary polymer, another copolymer is used to fabricate a controlled release microsphere. For microsphere preparation emulsion solvent evaporation (ESE) method was used here; in this method, drug and polymer first dissolved in organic phase then added in oil with constant stirring to evaporate organic phase.ESE method provides %yield from a range of 72% to 95% in different variable batches. Entrapment efficiency (EE) is also studied to have in-between 69% to 80% range. Formulation F5 polymer copolymer ratio of 1:1 showing 30% burst release within 15 min on dissolution study which is quite effective to reach the faster onset of action and releases 69% drug up to 6 h of study. FTIR data indicates selected polymers are not interacting with sitagliptin which otherwise can deteriorate its therapeutic efficacy. Microspheres are further characterized on various tests like Scanning electron microscopy (SEM), dissolution kinetics, floating capacity, micromeritics property. EE data and % yield data showing ESE method is suitable for making microspheres with minimum loss of raw materials. Dissolution study showing burst release for faster onset of action followed by sustained release of the drug.

Fig. Dissolution data comparison for different formulation

References

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