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Using Multi-fluorinated Bile Acids and In Vivo Magnetic Resonance Imaging to Measure Bile Acid Transport

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pH-Sensitive Mebeverine Microspheres for Colon Delivery.

P M Dandagi¹, V S Mastiholimath, A P Gadad

¹Department of Pharmaceutics, K. L. E. S's College of Pharmacy, J. N. M. C. Campus, Nehru Nagar, Belgaum-590 010, India.

Indian Journal of Pharmaceutical Sciences

|May 27, 2010

Summary

Mebeverine microspheres were developed to enhance oral bioavailability and colon-specific absorption. Formulation F-3 demonstrated optimal characteristics and significant anti-irritable bowel syndrome activity in a rat model.

Keywords:

Eudragit L100 Eudragit S100 emulsion solvent evaporation technique mebeverine hydrochloride pH-sensitive microspheres

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Flexible Colonoscopy in Mice to Evaluate the Severity of Colitis and Colorectal Tumors Using a Validated Endoscopic Scoring System

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Published on: October 16, 2013

Area of Science:

Pharmaceutical Sciences
Drug Delivery Systems

Background:

Mebeverine hydrochloride exhibits poor oral bioavailability due to extensive first-pass metabolism.
Developing colon-targeted drug delivery systems can improve therapeutic efficacy and reduce systemic side effects.

Purpose of the Study:

To prepare and characterize mebeverine microspheres for improved oral bioavailability and colon-specific absorption.
To evaluate the in vitro and in vivo performance of mebeverine microspheres.

Main Methods:

Microspheres were prepared using the emulsion solvent evaporation method with varying drug-to-polymer ratios.
Formulations underwent evaluation for practical yield, entrapment efficiency, particle size, and in vitro drug release.
In vivo anti-irritable bowel syndrome activity was assessed using a colorectal distention rat model.

Main Results:

Microspheres exhibited high practical yield (up to 89.59%) and encapsulation efficiency (up to 79.4%).
Scanning electron microscopy revealed smooth, spherical microspheres (200-300 µm).
In vitro drug release showed a biphasic pattern with non-Fickian diffusion over 12 hours.

Conclusions:

Formulation F-3 was identified as optimal based on comprehensive evaluation.
Mebeverine microspheres demonstrated significant potential for treating constipation-induced irritable bowel syndrome, showing improved fecal output in rats.