生物等效性和生物利用度杂志

抽象的

A Review of Novel Formulation Strategies to Enhance Oral Delivery of Zaleplon

Narendar Dudhipala

Zaleplon is a pyrrazolopyrimidine which is recommended for the treatment of insomnia and pentylenetetrazole/ electroshock-induced convulsions is an effective anticonvulsant which potential acts on the GABA receptor. The poor oral bioavailability of zaleplon (~30%) is due to the low solubility which in turn amputates the dissolution of the drug, restricts gastric absorption and first-pass metabolism. It is now withdrawn from the market due to the high dose and inefficient therapeutic activity. This review focuses on the various drug systems of zaleplon such as solid dispersions, self-nanoemulsifying, solid dispersions, proliposomes and solid lipid nanoparticles to enhance the oral bioavailability.