Document Detail


Slow release formulations of inhaled rifampin.
MedLine Citation:
PMID:  18584334     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Intira Coowanitwong; Vikram Arya; Poj Kulvanich; Günther Hochhaus
Related Documents :
15451544 - Cytotoxicity of anticancer drugs incorporated in solid lipid nanoparticles on ht-29 col...
16842944 - Self-assembled nanoparticles of poly(lactide)--vitamin e tpgs copolymers for oral chemo...
12176274 - Caffeine microparticles for nasal administration obtained by spray drying.
22041704 - Comparison of dissolution behavior of scopolamine butylbromide between ethical and over...
1760904 - Chronic lung fibrosis following carmustine (bcnu) chemotherapy: radiological features.
25331194 - Determining the polymer threshold amount for achieving robust drug release from hpmc an...
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    
Affiliation:
Department of Pharmaceutics, College of Pharmacy, University of Florida, Gainesville, Florida, 32610, USA.
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Descriptor/Qualifier:
Administration, Inhalation
Animals
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
Male
Mice
Microspheres
Particle Size
Rats
Rats, Sprague-Dawley
Rifampin / administration & dosage*,  adverse effects,  blood,  chemistry
Solubility
Surface Properties
Chemical
Reg. No./Substance:
0/Antibiotics, Antitubercular; 0/Delayed-Action Preparations; 0/Drug Carriers; 13292-46-1/Rifampin
Comments/Corrections

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


Previous Document:  A novel approach to optimize and formulate fast disintegrating tablets for nausea and vomiting.
Next Document:  Inhibitors of GSK-3 prevent corticosterone from inducing COX-1 expression in cardiomyocytes.