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Open AccessArticle

Improved Stability of Rifampicin in the Presence of Gastric-Resistant Isoniazid Microspheres in Acidic Media

1
Division of Pharmaceutics, Faculty of Pharmacy, Rhodes University, Grahamstown 6140, South Africa
2
School of Health Sciences, Department of Pharmacy, University of Zambia, Lusaka 10101, Zambia
*
Author to whom correspondence should be addressed.
Pharmaceutics 2020, 12(3), 234; https://doi.org/10.3390/pharmaceutics12030234
Received: 10 January 2020 / Revised: 20 February 2020 / Accepted: 3 March 2020 / Published: 5 March 2020
(This article belongs to the Special Issue Encapsulation Techniques Applied to Pharmaceutics)
The degradation of rifampicin (RIF) in an acidic medium to form 3-formyl rifamycin SV, a poorly absorbed compound, is accelerated in the presence of isoniazid, contributing to the poor bioavailability of rifampicin. This manuscript presents a novel approach in which isoniazid is formulated into gastric-resistant sustained-release microspheres and RIF into microporous floating sustained-release microspheres to reduce the potential for interaction between RIF and isoniazid (INH) in an acidic environment. Hydroxypropyl methylcellulose acetate succinate and Eudragit® L100 polymers were used for the manufacture of isoniazid-loaded gastric-resistant sustained-release microspheres using an o/o solvent emulsification evaporation approach. Microporous floating sustained-release microspheres for the delivery of rifampicin in the stomach were manufactured using emulsification and a diffusion/evaporation process. The design of experiments was used to evaluate the impact of input variables on predefined responses or quality attributes of the microspheres. The percent degradation of rifampicin following 12 h dissolution testing in 0.1 M HCl pH 1.2 in the presence of isoniazid gastric-resistant sustained-release microspheres was only 4.44%. These results indicate that the degradation of rifampicin in the presence of isoniazid in acidic media can be reduced by encapsulation of both active pharmaceutical ingredients to ensure release in different segments of the gastrointestinal tract, potentially improving the bioavailability of rifampicin. View Full-Text
Keywords: isoniazid; rifampicin; gastric-resistant microspheres; solvent evaporation; microporous microspheres; design of experiments; stability; optimization isoniazid; rifampicin; gastric-resistant microspheres; solvent evaporation; microporous microspheres; design of experiments; stability; optimization
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MDPI and ACS Style

Mwila, C.; Walker, R.B. Improved Stability of Rifampicin in the Presence of Gastric-Resistant Isoniazid Microspheres in Acidic Media. Pharmaceutics 2020, 12, 234.

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