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, in situ 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.

中文翻译：

---

阿塞那平制剂开发的最新进展。

摘要

介绍

马来酸阿塞那平（AM）是一种非典型抗精神病药，已被广泛指定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，在开发新的制剂以解决AM的生物利用度问题方面取得了长足的进步。

覆盖区域

这篇综述文章深入探讨了研究人员为提高AM的生物利用度而采取的所有制剂方法，包括利用超声介导的透皮递送，鼻至脑递送，肠淋巴系统靶向，原位植入物等的工作。与该专利相关的所有专利AM配方也已被讨论和总结。

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着提高。我们还提到了可用于进一步增强AM生物利用度的未开发领域。尽管如此，这些研究大多数仍限于研究实验室水平，并且在进入市场之前面临多个障碍。需要获得可控制性和可重复性以生产新型制剂，以使其能够从工作台过渡到床边。