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最近在阿塞那平制剂开发方面的进展。

Recent advances in the development of asenapine formulations.

机构信息

Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education , Manipal, India.

出版信息

Expert Opin Drug Deliv. 2020 Oct;17(10):1377-1393. doi: 10.1080/17425247.2020.1792439. Epub 2020 Jul 16.

DOI:10.1080/17425247.2020.1792439
PMID:32633149
Abstract

INTRODUCTION

Asenapine maleate (AM) is an atypical antipsychotic agent, that has been widely prescribed for the management of schizoaffective disorders. However, the bioavailability of AM is extremely poor due to the extensive first-pass metabolism. With the advancement in pharmaceutical technologies, significant strides have been made to create novel formulations to address the bioavailability problem of AM.

AREAS COVERED

This review article provides an insight into all the formulation approaches undertaken by researchers to increase the bioavailability of AM encompassing the works utilizing ultrasound mediated transdermal delivery, nose to brain delivery, intestinal lymphatic system targeting, implants, etc. All the patents associated with AM formulation have also been discussed and summarized.

EXPERT OPINION

Numerous studies have been carried out on AM formulations over the recent years, many of these studies have shown significant improvement in bioavailability. We have also mentioned the unexplored domains which can be exploited for further enhancing the bioavailability of AM. Nonetheless, most of these studies are still limited to the research laboratory level and face multiple hurdles before making into the market. Attaining controllability and reproducibility for the production of novel formulations is needed to enable its transition from bench to bedside.

摘要

简介

马来酸阿塞那平(AM)是一种新型抗精神病药物,已广泛用于治疗分裂情感障碍。然而,由于广泛的首过代谢,AM 的生物利用度极差。随着制药技术的进步,为解决 AM 的生物利用度问题,已经取得了重大进展,创造了新的制剂。

涵盖领域

本文综述了研究人员为提高 AM 的生物利用度而采用的所有制剂方法,包括利用超声介导的经皮给药、脑靶向鼻内给药、肠道淋巴系统靶向、植入物等。还讨论并总结了与 AM 制剂相关的所有专利。

专家意见

近年来,已经对 AM 制剂进行了许多研究,其中许多研究表明生物利用度有了显著提高。我们还提到了尚未开发的领域,可以进一步提高 AM 的生物利用度。然而,这些研究大多仍局限于研究实验室水平,在进入市场之前还面临着多重障碍。需要控制和重现新型制剂的生产,才能使其从实验室过渡到临床。

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