Enhancing Dissolution Rates of Gliclazide via Co-crystallization with Nicotinamide

Authors

  • Wardiyah S. Prawiro Politeknik Kesehatan Kemenkes Jakarta II
  • Gloria Murtini
  • Tati Suprapti
  • Harpolia Cartika

Keywords:

gliclazide, nicotinamide, co-crystallization, dissolution rate

Abstract

Gliclazide is a drug with poor water solubility and high permeability (BCS II), The absorption rate of this drug, when taken orally is controlled by dissolution rate in the gastrointestinal tracts. Co-crystallization method is widely used to improve the dissolution rate of this type of drug. This study aims to improve the dissolution rate of gliclazide by Co-crystallization method with nicotinamide as a coformer. Co-crystallization were prepared by solvent evaporation methods using methanol. Pure gliclazide, co-crystal gliclazide-nicotinamide in molar ratio 1:0,5, 1:1, 1:2, 1:2,5, 1:3, 1:3,5, 1:4, 1:5, and 1:7 and physical mixtures were characterized by DSC, FTIR, XRD and dissolution testing. Characterization by DSC and XRD in ratio 1:0,5, 1:1, and 1:2 showed a lower  endothermic peak of gliclazide, and decrease in the intensity of the diffraction pattern by XRD. Characterization by FTIR virtually showed no shift  of absorption peaks of gliclazide in ratio 1:0,5, 1:1, and 1:2. FTIR spectrum of cocrystal in ratio 1:7 showed a shift of absorption peaks for C=O and N-H. Results of dissolution testing for cocrystal in ratio 1:0,5, 1:3, 1:7, and physical mixture in ratio  1:7 showed higher dissolution rate than pure gliclazide. The highest of dissolution rate is cocrystal gliclazide-nicotinamide in ratio 1:7. Similarity analysis (f2) showed no similarity of dissolution rate for pure gliclazide, cocrystal gliclazide-nicotinamide in ratio 1:0,5, 1:3, 1:7 and  physical mixture in ratio  1:7.

 

 

Author Biography

Wardiyah S. Prawiro, Politeknik Kesehatan Kemenkes Jakarta II

Department of Pharmacy

References

Abdou H. Dissolution, Bioavailability, and Bioequivalence. Pennsylvania: Mack Publishing Company; 1989. 53,72 p.

Mirza S, Heinämäki J, Miroshnyk I, Yliruusi J. L24 Co-crystals: An emerging approach to improving properties of pharmaceutical solids. Eur J Pharm Sci. 2008;34(1):S16–7.

Sekhon BS. Pharmaceutical Co-Crystals - an Update. 2009;1(2):24–39.

Saharan VA, Kukkar V, Kataria M, Gera1 M, Choudhury PK. of Health Research. Int J Heal Res. 2008;1(March):3–14.

Fda U. Guidance for Industry, Waiver of in vivo bioavailability and bioequivalence studies for immediate release solid oral dosage forms based on a biopharmaceutics classification system. Washington DC US Dep Heal Hum Serv [Internet]. 2000;(May 2015):1–2. Available from: http://scholar.google.com/scholar?hl=en&btnG=Search&q=intitle:Guidance+for+Industry+Waiver+of+In+Vivo+Bioavailability+and+bioequivalence+studies#0

Davis N. Insulin, Oral Hypoglycemic Agents and The Pharmacology of The Endocrine Pancreas, in  Goodman and Gilman’s : The Pharmacological Basic of Therapeutics, 11th ed. New York: Mc Graw-Hill Inc; 2006. 1634 – 1637 p.

Sarkar A, Tiwari A, Bhasin PS, Mitra M. Pharmacological and pharmaceutical profile of gliclazide: A review. J Appl Pharm Sci. 2011;1(04):11–9.

European Directorate for Quality of Medicines & Health Care (EDQM). European Pharmacopoeia, 6th ed.vol 2. Strasbourg: Council of Europe; 2008.

Agustin R, Sari N, Zaini E. Pelepasan Ibuprofen dari Gel Karbomer 940 Co-Crystal . 2014;01(01):79–88.

Skoog DA, Holler FJ, Nieman TA. Instrumental Analysis Fifth Edition Contents Overview. Orlando: Harcourt Brace & Co; 1997;294, 380, 805 p.

Criterion P-F, Gray V. Determining Similarity of Products Variability of Dissolution Test Bioequivalence Testing , using the Dissolution Profile Bioequivalence Tool. 2010;1–26.

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Published

2016-08-15

How to Cite

Prawiro, W. S., Murtini, G., Suprapti, T., & Cartika, H. (2016). Enhancing Dissolution Rates of Gliclazide via Co-crystallization with Nicotinamide. Asian Journal of Applied Sciences, 4(4). Retrieved from https://www.ajouronline.com/index.php/AJAS/article/view/3820

Issue

Vol. 4 No. 4 (2016): August 2016

Section

Articles

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