Bialer M, Friedman M, Dubrovsky J, Raz I, Abramsky O
Biopharm Drug Dispos. 1985 Oct-Dec;6(4):401-11. doi: 10.1002/bdd.2510060406.
Five new sustained-release dosage forms of valproic acid (VPA) were developed. The new sustained-release formulations were administered to six healthy subjects for comparison with a standard tablet and an i.v. preparation of the drug. Three of the formulations exhibited a more prolonged and uniform absorption rate and yielded more sustained serum levels after ingestion. These three formulations maintained serum therapeutic levels of VPA for 24 h after a single oral administration of 1 g, and were bioequivalent to a marketed standard tablet of VPA. The absorption profile of the various oral formulations was analysed pharmacokinetically, using the Loo-Riegelman procedure.
开发了五种新型丙戊酸（VPA）缓释剂型。将这些新型缓释制剂给予六名健康受试者，以与标准片剂和该药物的静脉注射制剂进行比较。其中三种制剂表现出更持久且均匀的吸收速率，摄入后产生更持久的血清水平。这三种制剂在单次口服1 g后可维持VPA血清治疗水平达24小时，并且与市售的VPA标准片剂具有生物等效性。使用Loo-Riegelman方法对各种口服制剂的吸收情况进行了药代动力学分析。
