Propofol: the challenges of formulation.

Abstract:

:Propofol is a potent lipophilic anesthetic that was initially formulated in Cremophor El for human use. Because of the occurrence of Cremophor EL anaphylaxis and improvements in the quality of lipid emulsions, it was ultimately brought to market as 1% propofol formulated in 10% soybean oil emulsion. Emulsions represent complex formulation compositions whose suitability for intravenous administration is dependent on a number of factors. Despite the success of propofol emulsions, drawbacks to such formulations include inherent emulsion instability, injection pain, a need for antimicrobial agents to prevent sepsis, and a concern of hyperlipidemia-related side effects. Efforts to overcome such drawbacks have involved the development of propofol emulsions with altered propofol and lipid contents, the addition of different excipients to emulsions for antimicrobial activity, and study of nonemulsion formulations including propofol-cyclodextrin and propofol-polymeric micelle formulations. In addition, a number of propofol prodrugs have been made and evaluated.

journal_name

Anesthesiology

journal_title

Anesthesiology

authors

Baker MT,Naguib M

doi

10.1097/00000542-200510000-00026

subject

Has Abstract

pub_date

2005-10-01 00:00:00

pages

860-76

issue

4

eissn

0003-3022

issn

1528-1175

pii

00000542-200510000-00026

journal_volume

103

pub_type

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