FORMULATION, OPTIMIZATION, AND EVALUATION OF SITAGLIPTIN AND SIMVASTATIN RAPIDLY DISSOLVING TABLETS


Asmaa A. Bayoumi

Abstract


Objective: The scope of this work was to formulate sitagliptin and simvastatin rapidly dissolving tablets. However, simvastatin is practically insoluble in water. For improving its poor oral bioavailability and with the aim of facilitating administration to patients facing problems with swallowing rapidly dissolving tablets were prepared

Methods: Tablets were prepared using superdisintegrant addition technique using croscarmellose sodium (Ac-di-sol), sodium starch glycolate (explotab) and crospovidone in different percentages. Evaluation tests such as weight variation, thickness, and content variation, and friability, disintegration, wetting time, in vitro dispersion and in vitro dissolution were carried out.

Results: The results showed that the presence of crospovidone could enhance the dissolution rate of simvastatin greatly. The best-optimized formulae found were that F8, F9, and F10 which showed good disintegration and the dissolution rate of simvastatin and sitagliptin was more than 90% after 10 min while the dissolution rate for simvastatin and sitagliptin pure standards was 12% and 30%, respectively after 10 min.

Conclusion: Some tablet formulae showed acceptable pharmacotechnical properties and complied with compendium requirements. Results of dissolution studies revealed that F8-F10 showed an increase in the dissolved sitagliptin and simvastatin to be more than 90% after 10 min. 


Keywords


Simvastatin, Sitagliptin, Rapidly dissolving tablets, Superdisintegrants, Crospovidone

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References


Chundawat SL, Sharma V. Formulation evaluation, and optimization of orodispersible tablets of pantoprazole sodium by the using of different superdisintegrants. Asian J Pharm Clin Res 2018;11:84-9.

Kumar S, Garg KRS. Fast dissolving tablets (Fdts): current status, new market opportunities, recent advances in manufacturing technologies and future prospectsissn. Int J Pharm Pharm Sci 2014;6:22-35.

Ramadan WH, Kabbara WK. Sitagliptin/Simvastatin: a first combination tablet to treat type 2 diabetes and hypercholesterolemia–a review of its characteristics. Vasc Health Risk Manag 2015;11:125–32.

"The Pharmacopoeia of United States of America". 35th Ed. National Formulary 30, Mack Publishing Co. Easton. Vol. 2. Electronic version; 2012.

Yunxia B, Hisakazu S, Yorinobu Y, Kazumi D, Akinobu O, Kotaro I. Preparation and evaluation of compressed tablet rapidly disintegrating in the oral cavity. Chem Pharm Bull 1996;44:2121-7.

Hari K, Rajeswari S, Ramanamurthy VK. Preparation and evaluation of orally disintegrating tablets of drotaverine hydrochloride using sublimation technique. Int J Pharm Pharm Sci 2018;10:85-95.

Ashish P, Mishra P, Main P, Harsoliya M, Agrawal S. A review on recent advancement in the development of the rapid disintegrating tablet. Int J Life Sci Pharm Res 2011;1:7-16.

https://www.accessdata.fda.gov/scripts/cder/dissolution/dsp_SearchResults. cfm. [Last accessed on 20 May 2018]

Aronson H. Correction factor for dissolution profile calculations. J Pharm Sci 1993;82:1190.

Battu SK, Repka MA, Majumdar S, Rao YM. Formulation and evaluation of rapidly disintegrating fenoverine tablets: effect of superdisintegrants. Drug Dev Ind Pharm 2007;33:1225–32.

Makiko F, Hideko O, Yu Suke S, Honami T, Masuo K, Yoshiteru W. Preparation, characterization, and tableting of a solid dispersion of indomethacin with crospovidone. Int J Pharm 2005;293:145-53.

Prasanthi S, Prasad RA, Kumar GY, Babu NR. formulation and evaluation of sitagliptin phosphate and simvastatin bilayered tablets. Indo Am J Pharm Res 2015;5:3654-66.




About this article

Title

FORMULATION, OPTIMIZATION, AND EVALUATION OF SITAGLIPTIN AND SIMVASTATIN RAPIDLY DISSOLVING TABLETS

Keywords

Simvastatin, Sitagliptin, Rapidly dissolving tablets, Superdisintegrants, Crospovidone

DOI

10.22159/ijap.2018v10i5.28122

Date

08-09-2018

Additional Links

Manuscript Submission

Journal

International Journal of Applied Pharmaceutics
Vol 10, Issue 5 (Sep-Oct), 2018 Page: 270-273

Online ISSN

0975-7058

Authors & Affiliations

Asmaa A. Bayoumi
Pharmacy Department, Ibn Hayyan University College, Karbala, Iraq
Iraq


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