Intestinal permeability and role of P-glycoprotein in intestinal absorption of novel triethylamine containing thiophene S006–830 using single-pass intestinal perfusion in rats. (July 2017)

• Record Type: Journal Article
• Authors: Hidau, Mahendra Kumar; Singh, Yeshwant; Singh, Shio Kumar
• Is Part Of: International journal of pharmacokinetics. Volume 2:Number 3(2017)
• Page Start: 163
• Page End: 171
• Publication Date: 2017-07
• Subjects: absorption rate -- accuracy -- bioanalytical method -- chromatography and absorbance. -- intestinal perfusate -- permeability -- precision -- recovery -- tuberculosis; Pharmacokinetics -- Periodicals; 615.705
• DOI: 10.4155/ipk-2017-0003
• Languages: English
• ISSNs: 2053-0846

Abstract

Aim: Study was designed to develop ultra-fast liquid chromatography method of antitubercular compound S006–830 in rat intestinal perfusate and apply method for determination of effective permeability coefficient (Peff ), absorption rate (Ka ) and role of P-glycoprotein (P-gp) in the absorption.Methods: Chromatography was performed. Peff, Ka of S006–830, role of P-gp in the absorption of S006–830 were determined by single-pass intestinal perfusion studies.Results: Method was found sensitive, reproducible. Recoveries of S006–830 were found around 60%. Method was applied for determination of Peff and Ka . Peff and Ka values indicated that S006–830 possesses high permeability and high absorption rate.Conclusion: Co-infusion of S006–830 with verapamil in single pass intestinal perfusion study demonstrated that P-gp do not have any significant role in the absorption of S006–830.