Abstract:
:Literature data pertaining to the decision to allow a waiver of in vivo bioequivalence testing for the approval of immediate-release (IR) solid oral dosage forms containing efavirenz as the only active pharmaceutical ingredient (API) are reviewed. Because of lack of conclusive data about efavirenz's permeability and its failure to comply with the "high solubility" criteria according to the Biopharmaceutics Classification System (BCS), the API can be classified as BCS Class II/IV. In line with the solubility characteristics, the innovator product does not meet the dissolution criteria for a "rapidly dissolving product." Furthermore, product variations containing commonly used excipients or in the manufacturing process have been reported to impact the rate and extent of efavirenz absorption. Despite its wide therapeutic index, subtherapeutic levels of efavirenz can lead to treatment failure and also facilitate the emergence of efavirenz-resistant mutants. For all these reasons, a biowaiver for IR solid oral dosage forms containing efavirenz as the sole API is not scientifically justified for reformulated or multisource drug products.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Cristofoletti R,Nair A,Abrahamsson B,Groot DW,Kopp S,Langguth P,Polli JE,Shah VP,Dressman JBdoi
10.1002/jps.23380subject
Has Abstractpub_date
2013-02-01 00:00:00pages
318-29issue
2eissn
0022-3549issn
1520-6017pii
S0022-3549(15)31214-4journal_volume
102pub_type
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