Next Article in Journal
Identifizierung und Unterscheidung von H2-Antihistaminika und Thioharnstoffderivaten durch Farbreaktionen mit Kupfer(II)-Salzen in stark saurer Lösung
[ Identification and differentiation of H2-antihistamines and thiourea derivatives by colour reaction with Copper(II)-salts in acidic solutions ]
Previous Article in Journal
Investigation of the Direct Effects of the Alcoholic Extract of Elaeagnus angustifolia L. (Elaeagnaceae) on Dispersed Intestinal Smooth Muscle Cells of Guinea Pig
Article Menu

Article Versions

Export Article

Open AccessArticle
Sci. Pharm. 2006, 74(1), 31-51; doi:10.3797/scipharm.2006.74.31 (registering DOI)

In-vitro and in-vivo availability of mebeverine hydrochloride suppositories

Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O.Box 22452, Riyadh 11459, Saudi Arabia
*
Author to whom correspondence should be addressed.
Received: 10 May 2005 / Accepted: 2 February 2006 / Published: 1 March 2006
Download PDF [476 KB, uploaded 27 December 2016]

Abstract

Mebeverine hydrochloride suppositories were prepared using Witepsol H15 suppository base. The effect of different concentrations of various enhancers (surfactants, amino acids and osmotic modifiers) on the drug release form the prepared suppositories was studied. The results showed that mebeverine hydrochloride suppositories containing Brij 35 (2%) and urea (10%) were superior to the other formulations containing the tested enhancers. These formulae showed the highest release rates (K = 0.083 ± 0.004 min-1 and 0.111 ± 0.005 min-1 , respectively) that followed first-order kinetics with t50% of 8.35 ± 0.45 min and 6.24 ± 0.33 min, respectively. Therefore, these two formulae with the control suppositories were subjected to in vivo study in albino rabbits compared to the commercial Duspatalin® tablets and intravenous injection. Higher Cmax (1770.26 ± 165.46 ng.ml-1) within shorter Tmax (0.75 ± 0.20 h) was observed after rectal administration of the control suppositories compared to that of commercially available film-coated tablets (Duspatalin® – 135 mg). A significant difference (p≤0.05) between the absolute bioavailability of Duspatalin® tablets (27.09 ± 3.80%) and control suppositories (46.66 ± 1.72%) was detected. Statistically (p≤0.05), the mean residence time (MRT) after oral administration of Duspatalin® tablets (3.16 ± 0.30 h) was significantly longer than that after the rectal administration of control suppositories (2.73 ± 0.30 h). suppositories containing 2% Brij 35 showed higher plasma levels of the drug (2766.11± 339.50 ng.ml-1) with an absolute bioavailability of 70.50 ± 10.51% compared to 27.09 ± 3.80% for Duspatalin® tablets.
Keywords: Mebeverine hydrochloride; suppositories; in vitro and in vivo availability; enhancers; HPLC Mebeverine hydrochloride; suppositories; in vitro and in vivo availability; enhancers; HPLC
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

Scifeed alert for new publications

Never miss any articles matching your research from any publisher
  • Get alerts for new papers matching your research
  • Find out the new papers from selected authors
  • Updated daily for 49'000+ journals and 6000+ publishers
  • Define your Scifeed now

SciFeed Share & Cite This Article

MDPI and ACS Style

Al-Dossary, B.N.; Al-Gohary, O.M.; El-Khawaas, M.M. In-vitro and in-vivo availability of mebeverine hydrochloride suppositories. Sci. Pharm. 2006, 74, 31-51.

Show more citation formats Show less citations formats

Article Metrics

Article Access Statistics

1

Comments

[Return to top]
Sci. Pharm. EISSN 2218-0532 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top