Comparative evaluation of in vitro efficacy of colesevelam hydrochloride tablets*. (September 2014)

• Record Type: Journal Article
• Authors: Krishnaiah, Yellela S. R.; Yang, Yongsheng; Bykadi, Srikant; Sayeed, Vilayat A.; Khan, Mansoor A.
• Is Part Of: Drug development and industrial pharmacy. Volume 40:Number 9(2014:Sep.)
• Page Start: 1173
• Page End: 1179
• Publication Date: 2014-09
• Subjects: Pharmaceutical chemistry -- Periodicals; Pharmaceutical industry -- Periodicals; Drug Industry -- Periodicals; Technology, Pharmaceutical -- Periodicals; 615.05
• DOI: 10.3109/03639045.2013.809534
• Languages: English
• ISSNs: 0363-9045

Abstract

<abstract> <title>Abstract</title> <p> <italic>Context</italic>: Colesevelam hydrochloride is used as an adjunct to diet and exercise to reduce elevated low-density lipoprotein (LDL) cholesterol in patients with primary hyperlipidemia as well as to improve glycemic control in patients with type 2 diabetes. This is likely to result in submission of abbreviated new drug applications (ANDA).</p> <p> <italic>Objective</italic>: This study was conducted to compare the efficacy of two tablet products of colesevelam hydrochloride based on the <italic>in vitro</italic> binding of bile acid sodium salts of glycocholic acid (GC), glycochenodeoxycholic acid (GCDA) and taurodeoxycholic acid (TDCA).</p> <p> <italic>Methods</italic>: Kinetic binding study was carried out with constant initial bile salt concentrations as a function of time. Equilibrium binding studies were conducted under conditions of constant incubation time and varying initial concentrations of bile acid sodium salts. The unbound concentration of bile salts was determined in the samples of these studies. Langmuir equation was utilized to calculate the binding constants <italic>k<sub>1</sub></italic> and <italic>k<sub>2</sub></italic>.</p> <p> <italic>Results</italic>: The amount of the three bile salts bound to both the products reached equilibrium at 3 h. The similarity factor (<italic>f<sub>2</sub></italic>) was 99.5 based on the binding profile of total bile salts to the test and reference colesevelam tablets as a function of time. The 90% confidence interval for the test to reference ratio of <italic>k<sub>2</sub></italic> values were 96.06–112.07 which is within the acceptance criteria of 80–120%.</p> <p> <italic>Conclusion</italic>: It is concluded from the results that the test and reference tablets of colesevelam hydrochloride showed a similar <italic>in vitro</italic> binding profile and capacity to bile salts.</p> </abstract>