Document Detail

Slow release formulations of inhaled rifampin.
MedLine Citation:
PMID:  18584334     Owner:  NLM     Status:  MEDLINE    
Rifampin microspheres were prepared by spray drying using either polylactic acid (PLA) or poly(lactic-co-glycolic acid) (PLGA) polymers in different drug to polymer ratios (90:10 to 5:95, w/w). The in-vitro release characteristics, particle-size distribution, and cytotoxicity (in an alveolar macrophage cell line) and pharmacokinetics in rats after pulmonary instillation were evaluated. Increasing the polymer content from 10% to 95% slowed down the in vitro drug release with PLGA particles showing a steeper change with increasing polymer content (100% to 20% drug release over 6 h) than PLA particles (88% to 42% drug release over 6 h). PLA microsphere formulations revealed lack of cytotoxicity and a mass median aerodynamic diameter (MMDA) of 2.22-2.86 mum, while PLGA particles were larger (MMDA of 4.67-5.11 mum). Pharmacokinetics differed among the formulations with the 10% PLA formulation showing a distinct sustained release (t (max) of 2 h vs 0.5 h of free drug) and a systemic bioavailability similar to that of free drug. Formulations with high polymer content showed a lower relative bioavailability (30%). This suggested that an optimal release rate existed for which a distinct amount of drug was delivered over an extended period of time.
Intira Coowanitwong; Vikram Arya; Poj Kulvanich; Günther Hochhaus
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Publication Detail:
Type:  Journal Article     Date:  2008-06-27
Journal Detail:
Title:  The AAPS journal     Volume:  10     ISSN:  1550-7416     ISO Abbreviation:  AAPS J     Publication Date:  2008 Jun 
Date Detail:
Created Date:  2008-09-10     Completed Date:  2008-11-03     Revised Date:  2010-09-21    
Medline Journal Info:
Nlm Unique ID:  101223209     Medline TA:  AAPS J     Country:  United States    
Other Details:
Languages:  eng     Pagination:  342-8     Citation Subset:  IM    
Department of Pharmaceutics, College of Pharmacy, University of Florida, Gainesville, Florida, 32610, USA.
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MeSH Terms
Administration, Inhalation
Antibiotics, Antitubercular / administration & dosage*,  adverse effects,  blood,  chemistry
Cell Line
Cell Survival / drug effects
Delayed-Action Preparations
Drug Carriers / chemistry*
Drug Compounding
Macrophages, Alveolar / drug effects
Particle Size
Rats, Sprague-Dawley
Rifampin / administration & dosage*,  adverse effects,  blood,  chemistry
Surface Properties
Reg. No./Substance:
0/Antibiotics, Antitubercular; 0/Delayed-Action Preparations; 0/Drug Carriers; 13292-46-1/Rifampin

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