Biowaiver Monographs for Immediate-Release Solid Oral Dosage Forms: Enalapril.
Cast your vote
You can rate an item by clicking the amount of stars they wish to award to this item.
When enough users have cast their vote on this item, the average rating will also be shown.
Your vote was cast
Thank you for your feedback
Thank you for your feedback
AuthorsVerbeeck, Roger K
Groot, D W
Polli, James E
Shah, Vinod P
Dressman, Jennifer B
MetadataShow full item record
TitleBiowaiver Monographs for Immediate-Release Solid Oral Dosage Forms: Enalapril.
Published inJ Pharm Sci 2017; 106(8):1933-43
PubliekssamenvattingLiterature data relevant to the decision to allow a waiver of in vivo bioequivalence testing for the marketing authorization of immediate-release, solid oral dosage forms containing enalapril maleate are reviewed. Enalapril, a prodrug, is hydrolyzed by carboxylesterases to the active angiotensin-converting enzyme inhibitor enalaprilat. Enalapril as the maleate salt is shown to be highly soluble, but only 60%-70% of an orally administered dose of enalapril is absorbed from the gastrointestinal tract into the enterocytes. Consequently, enalapril maleate is a Biopharmaceutics Classification System class III substance. Because in situ conversion of the maleate salt to the sodium salt is sometimes used in production of the finished drug product, not every enalapril maleate-labeled finished product actually contains the maleate salt. Enalapril is not considered to have a narrow therapeutic index. With this background, a biowaiver-based approval procedure for new generic products or after major revisions to existing products is deemed acceptable, provided the in vitro dissolution of both test and reference preparation is very rapid (at least 85% within 15 min at pH 1.2, 4.5, and 6.8). Additionally, the test and reference product must contain the identical active drug ingredient.
- Stability and in vitro release profile of enalapril maleate from different commercially available tablets: possible therapeutic implications.
- Authors: Lima DM, dos Santos LD, Lima EM
- Issue date: 2008 Aug 5
- Enhanced intestinal permeability and oral bioavailability of enalapril maleate upon complexation with the cationic polymethacrylate Eudragit E100.
- Authors: Ramírez-Rigo MV, Olivera ME, Rubio M, Manzo RH
- Issue date: 2014 May 13
- Biowaiver monographs for immediate release solid oral dosage forms: piroxicam.
- Authors: Shohin IE, Kulinich JI, Ramenskaya GV, Abrahamsson B, Kopp S, Langguth P, Polli JE, Shah VP, Groot DW, Barends DM, Dressman JB
- Issue date: 2014 Feb
- Bioequivalence of enalapril oral solution for treatment of pediatric hypertension and enalapril tablets.
- Authors: Moffett BS, DiSanto AR, Espinosa O, Hou J, Colabuono P
- Issue date: 2014 Nov
- Bioequivalence study of two enalapril maleate tablet formulations in healthy male volunteers. Pharmacokinetic versus pharmacodynamic approach.
- Authors: Ribeiro W, Muscará MN, Martins AR, Moreno H Jr, Mendes GB, de Nucci G
- Issue date: 1996