Document Detail


The tablet formulation of lopinavir/ritonavir provides similar bioavailability to the soft-gelatin capsule formulation with less pharmacokinetic variability and diminished food effect.
MedLine Citation:
PMID:  17224848     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Lopinavir, an HIV protease inhibitor, is coformulated with ritonavir to enhance the bioavailability and pharmacokinetics of lopinavir. The original solid oral formulation of lopinavir/ritonavir, a soft-gelatin capsule (SGC), requires refrigerated storage, is taken as 6 capsules daily at the recommended adult dose, and is administered with food to maximize the bioavailability of lopinavir. Melt extrusion technology was used to produce a tablet formulation reducing the number of dosage units administered per day and simplifying storage requirements. Three studies assessed the bioavailability of tablet doses of lopinavir/ritonavir at 800/200 mg or 400/100 mg under different meal conditions compared with equal doses of the SGC after a moderate-fat meal. The tablet was bioequivalent to the SGC after a moderate-fat meal with respect to lopinavir and ritonavir areas under the concentration-time curve. Compared with the SGC formulation, the tablet formulation resulted in more consistent lopinavir and ritonavir exposures within and across studies and across meal conditions. The diminished food effect and decreased variability of the tablet are likely to result in more consistent lopinavir and ritonavir exposures, minimizing the likelihood of extreme high or low values compared with the SGC.
Authors:
Cheri Enders Klein; Yi-Lin Chiu; Walid Awni; Tong Zhu; Renee S Heuser; Thao Doan; Joerg Breitenbach; John B Morris; Scott C Brun; George J Hanna
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Publication Detail:
Type:  Journal Article; Randomized Controlled Trial; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of acquired immune deficiency syndromes (1999)     Volume:  44     ISSN:  1525-4135     ISO Abbreviation:  J. Acquir. Immune Defic. Syndr.     Publication Date:  2007 Apr 
Date Detail:
Created Date:  2007-03-13     Completed Date:  2007-07-10     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  100892005     Medline TA:  J Acquir Immune Defic Syndr     Country:  United States    
Other Details:
Languages:  eng     Pagination:  401-10     Citation Subset:  IM; X    
Affiliation:
Abbott, Abbott Park, IL 60064, USA. cheri.klein@abbott.com
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MeSH Terms
Descriptor/Qualifier:
Adult
Area Under Curve
Biological Availability
Capsules
Dose-Response Relationship, Drug
Female
Food-Drug Interactions*
Gelatin / chemistry
HIV Protease Inhibitors / administration & dosage,  pharmacokinetics*
Humans
Male
Metabolic Clearance Rate
Middle Aged
Pyrimidinones / administration & dosage,  pharmacokinetics*
Ritonavir / administration & dosage,  pharmacokinetics*
Tablets
Chemical
Reg. No./Substance:
0/Capsules; 0/HIV Protease Inhibitors; 0/Pyrimidinones; 0/Ritonavir; 0/Tablets; 192725-17-0/lopinavir; 9000-70-8/Gelatin

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


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