酒石酸唑吡坦在比格犬中的防滥用制剂与即刻释放制剂的口服应用

Amina Vazda, W. Xia, H. Engqvist
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引用次数: 1

摘要

目的:处方药物滥用的持续增加使开发一种防止滥用的制剂变得十分必要。地聚合物是一种很有前途的药物设计基础,因为它们可以调节药物释放,并且与传统的药物赋形剂相比具有优越的物理和化学性质。方法:以含酒石酸唑吡坦的地聚合物微丸为控释制剂,以市售速释产品Stilnoct®片为对照,口服给药于比格犬。结果:酒石酸唑吡坦为速释片剂,血浆速释谱升高,而地聚合物中的酒石酸唑吡坦为控释谱。药动学分析表明,与酒石酸唑吡坦地聚合物微丸给药相比,速释片给药可产生更高的血药浓度。另一方面,地聚合物制剂延长了药物释放时间。结论:口服含酒石酸唑吡坦的地聚合物微丸具有控释血浆特性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Oral Administration of Zolpidem Tartrate in an Abuse-deterrent Formulation Versus an Immediate Release Formulation in Beagle Dogs
Objective: The continuing rise of prescription drug abuse has greatly necessitated the development of an abuse-deterrent formulation. Geopolymers are a promising base for drug design as they allow for tuneable drug release and possess superior physical and chemical properties compared with conventional pharmaceutical excipients.Methods: Geopolymer pellets containing zolpidem tartrate were administrated orally to beagle dogs as a controlled-release formulation with the commercial immediate-release product, Stilnoct® tablets, as the control.Results: The administration of zolpidem tartrate as immediate-release tablets demonstrated an elevated immediate release plasma profile and the zolpidem tartrate in the geopolymers demonstrated a controlled-release plasma profile. The pharmacokinetic analysis demonstrated that immediate-release tablet administration generated much higher plasma concentration when compared with geopolymer pellets administration for zolpidem tartrate. On the other hand, the geopolymer formulation prolonged the time of drug release.Conclusion: Oral administration of zolpidem tartrate in geopolymer pellets demonstrated a controlled-release plasma profile.
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