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新型格列美脲舌下片的制剂与评价

Formulation and Evaluation of New Glimepiride Sublingual Tablets.

作者信息

Al-Madhagi Wafa, Abdulbari Albarakani Ahmed, Khaled Alhag Abobakr, Ahmed Saeed Zakaria, Mansour Noman Nahlah, Mohamed Khaldon

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Sana'a University, Sana'a, Yemen; Department of Pharmacy, Faculty of Medicine and Health Sciences, Yemeni Jordanian University, Sana'a, Yemen.

Department of Pharmacy, Faculty of Medicine and Health Sciences, Yemeni Jordanian University, Sana'a, Yemen.

出版信息

J Pharm (Cairo). 2017;2017:3690473. doi: 10.1155/2017/3690473. Epub 2017 Feb 5.

Abstract

Oral mucosal delivery of drugs promotes rapid absorption and high bioavailability, with a subsequent immediate onset of pharmacological effect. However, many oral mucosal deliveries are compromised by the possibility of the patient swallowing the active substance before it has been released and absorbed locally into the systemic circulation. The aim of this research was to introduce a new glimepiride formula for sublingual administration and rapid drug absorption that can be used in an emergency. The new sublingual formulation was prepared after five trials to prepare the suitable formulation. Two accepted formulations of the new sublingual product were prepared, but one of them with disintegration time of 1.45 min and searching for preferred formulation, the binder, is changed with Flulac and starch slurry to prepare formula with disintegration time of 21 seconds that supports the aim of research to be used in an emergency. The five formulations were done, after adjusting to the binder as Flulac and aerosil with disintegration time of 21 seconds and accepted hardness as well as the weight variation. The assay of a new product (subglimepiride) is 103% which is a promising result, confirming that the formula succeeded. The new product (subglimepiride) is accepted in most quality control tests and it is ready for marketing.

摘要

药物的口腔黏膜给药可促进快速吸收和高生物利用度,随后药理作用迅速起效。然而,许多口腔黏膜给药方式存在一个问题,即患者可能在活性物质在局部释放并吸收进入体循环之前就将其吞咽。本研究的目的是推出一种用于舌下给药和快速药物吸收的新型格列美脲配方,可用于紧急情况。经过五次试验以制备合适的配方后,制备了新的舌下制剂。制备了两种被认可的新型舌下产品配方,但其中一种崩解时间为1.45分钟,为了寻找更优配方,将粘合剂改为氟拉克和淀粉浆,制备出崩解时间为21秒的配方,这符合该研究用于紧急情况的目标。在将粘合剂调整为氟拉克和气相二氧化硅后,制备了五种配方,其崩解时间为21秒,硬度和重量差异也符合要求。新产品(舌下格列美脲)的含量测定为103%,这是一个很有前景的结果,证实配方成功。新产品(舌下格列美脲)在大多数质量控制测试中都被认可,已准备好上市。

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