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Tailored release drug delivery system for rifampicin and isoniazid for enhanced bioavailability of rifampicin.
Pharm Dev Technol. 2011 Apr; 16(2):127-36.PD

Abstract

The front line antitubercular drugs rifampicin (RMP) and isoniazid (INH), when co-administered, face the problem of reduced bioavailability of RMP. Stabilization of RMP in the presence of INH under acidic environment may improve the bioavailability of RMP. In vitro degradation studies showed around 15-25% degradation of RMP under the aforesaid conditions if the ratio of RMP: INH is above 1:0.5.This degradation is reduced to less than 10% when the ratio of RMP: INH is below 1:0.25. Based on these findings, an innovative drug delivery system was designed with the immediate release of RMP and tailored prolonged release of INH. The bilayer tablets prepared with this concept were subjected to relative bioavailability studies in healthy human volunteers in an open label, balanced, randomized, single-dose, cross-over study under fasted state. A validated LC-MS/MS bioanalytical method was employed for estimation of RMP and INH in plasma. Bioavailability studies revealed that C(max) and AUC for RMP increased by 18 and 20%, respectively, confirming the above innovative concept. Even in the case of INH, AUC increased significantly by around 30% and thus time above minimum inhibitory concentration (MIC) would also increase, which may result in further improved clinical outcome.

Authors+Show Affiliations

Department of Pharmaceutics, Sinhgad College of Pharmacy, Pune, Maharashtra, India. prof_avachat@yahoo.comNo affiliation info available

Pub Type(s)

Journal Article
Randomized Controlled Trial

Language

eng

PubMed ID

20105081

Citation

Avachat, Amelia M., and Satish B. Bhise. "Tailored Release Drug Delivery System for Rifampicin and Isoniazid for Enhanced Bioavailability of Rifampicin." Pharmaceutical Development and Technology, vol. 16, no. 2, 2011, pp. 127-36.
Avachat AM, Bhise SB. Tailored release drug delivery system for rifampicin and isoniazid for enhanced bioavailability of rifampicin. Pharm Dev Technol. 2011;16(2):127-36.
Avachat, A. M., & Bhise, S. B. (2011). Tailored release drug delivery system for rifampicin and isoniazid for enhanced bioavailability of rifampicin. Pharmaceutical Development and Technology, 16(2), 127-36. https://doi.org/10.3109/10837450903511186
Avachat AM, Bhise SB. Tailored Release Drug Delivery System for Rifampicin and Isoniazid for Enhanced Bioavailability of Rifampicin. Pharm Dev Technol. 2011;16(2):127-36. PubMed PMID: 20105081.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Tailored release drug delivery system for rifampicin and isoniazid for enhanced bioavailability of rifampicin. AU - Avachat,Amelia M, AU - Bhise,Satish B, Y1 - 2010/01/27/ PY - 2010/1/29/entrez PY - 2010/1/29/pubmed PY - 2011/7/21/medline SP - 127 EP - 36 JF - Pharmaceutical development and technology JO - Pharm Dev Technol VL - 16 IS - 2 N2 - The front line antitubercular drugs rifampicin (RMP) and isoniazid (INH), when co-administered, face the problem of reduced bioavailability of RMP. Stabilization of RMP in the presence of INH under acidic environment may improve the bioavailability of RMP. In vitro degradation studies showed around 15-25% degradation of RMP under the aforesaid conditions if the ratio of RMP: INH is above 1:0.5.This degradation is reduced to less than 10% when the ratio of RMP: INH is below 1:0.25. Based on these findings, an innovative drug delivery system was designed with the immediate release of RMP and tailored prolonged release of INH. The bilayer tablets prepared with this concept were subjected to relative bioavailability studies in healthy human volunteers in an open label, balanced, randomized, single-dose, cross-over study under fasted state. A validated LC-MS/MS bioanalytical method was employed for estimation of RMP and INH in plasma. Bioavailability studies revealed that C(max) and AUC for RMP increased by 18 and 20%, respectively, confirming the above innovative concept. Even in the case of INH, AUC increased significantly by around 30% and thus time above minimum inhibitory concentration (MIC) would also increase, which may result in further improved clinical outcome. SN - 1097-9867 UR - https://www.unboundmedicine.com/medline/citation/20105081/Tailored_release_drug_delivery_system_for_rifampicin_and_isoniazid_for_enhanced_bioavailability_of_rifampicin_ L2 - http://www.tandfonline.com/doi/full/10.3109/10837450903511186 DB - PRIME DP - Unbound Medicine ER -