Liansinline suppository and its preparation method and application

A liensinine suppository and the technology of liensinine are applied in the directions of suppository delivery, pharmaceutical formulation, cardiovascular system diseases, etc., and can solve the problems of no commercial listing of liensinine, the inability to achieve the expected ideal pharmacological activity, and serious liver first-pass effect, etc. , to avoid the effect of poor oral absorption

Active Publication Date: 2018-05-11
WUHAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the actual clinical application process, in many cases, liensinine cannot achieve the expected ideal pharmacological activity in vivo.
Some scholars have studied the pharmacokinetics and bioavailability of liensinine, and found that the oral absorption of liensinine is not good (about 17% of the drug can be absorbed into the liver through the gastrointestinal tract), and the first-pass effect of the liver is serious (into the liver). About 75% of the drug in the liver is metabolized by the liver), resulting in the absolute bioavailability of liensinine oral administration being only 4.39%
[0005] Liensinine is currently not on the market

Method used

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  • Liansinline suppository and its preparation method and application
  • Liansinline suppository and its preparation method and application
  • Liansinline suppository and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Weigh 0.35 g of Liensinine (extracted and refined in the laboratory), and heat 99.5 g of semi-synthetic mixed fatty acid ester (type 36, purchased from Lutianhua, Chengdu) and 0.1 g of Tween-80 (purchased from Sichuan Jinshan Pharmaceutical) at 50 °C After melting, add Liensinine, stir to make it evenly mixed, pour it into a preheated plug mold, cool it at 2 to 8°C for 1 to 3 hours, and then take it out. Each plug weighs 1.0 g.

Embodiment 2

[0035] Weigh 0.35 g of Liensinine (extracted and refined in the laboratory), micronized 1 to 3 times with a pulverizer, passed through a 100-mesh sieve, and mixed 99.5 g of semi-synthetic mixed fatty acid ester (model 36, purchased from Lutianhua, Chengdu) and vomited. After 0.1 g of Wen-80 (purchased from Sichuan Jinshan Pharmaceutical) was heated and melted at 50 °C, micronized Liensinine was added, stirred to make it evenly mixed, poured into a preheated plug mold, and cooled at 2 to 8 °C for 1 to 3 Take it out after an hour, and each plug weighs 1.0g.

Embodiment 3

[0037] Weigh 1.0 g of Liensinine (extracted and refined in the laboratory), micronized 1 to 3 times with a pulverizer, passed through a 100-mesh sieve, and mixed 98.5 g of semi-synthetic mixed fatty acid esters (model 34, purchased from Lutianhua, Chengdu) and spun out. After 0.5 g of Wen-80 (purchased from Sichuan Jinshan Pharmaceutical) was heated and melted at 50°C, Liensinine was added, stirred to make it evenly mixed, poured into a preheated plug mold, cooled at 2-8°C for 1-3 hours and taken out That is, each plug weighs 1.0g.

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Abstract

The invention provides a liensinine rectal administration suppository and a preparation method and a purpose thereof. The liensinine rectal administration suppository comprises liensinine, a fat-soluble suppository matrix and a surface active agent. The invention also provides the purpose of the liensinine suppository for preparing an anti-arrhythmia or anti-hypertension drug. The liensinine rectal administration suppository provided by the invention has the advantages that the low bioavailability caused by poor oral absorbing of the liensinine and severe first-pass effect of liver is avoided; the drug passes through inferior rectal veins and anus veins, bypasses the liver via internal iliac veins, enters inferior vena cava, and then enters large circulation, so as to realize the anti-arrhythmia or anti-hypertension function.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a liensinine suppository and a preparation method and application thereof. Background technique [0002] Liensinine is a bisbenzylisoquinoline alkaloid extracted from the green germ of the mature seeds of Nelumbo nucifera Gaertn. Its chemical structure is shown in the following formula. [0003] [0004] Liensinine has a variety of cardiovascular and cerebrovascular system activities such as antihypertensive, antiarrhythmic, antihyperlipidemia, antilipid peroxidation, and protection of cerebral ischemia. However, in the actual clinical application process, in many cases, liensinine cannot achieve the expected ideal pharmacological activity in vivo. Some scholars have studied the pharmacokinetics and bioavailability of Liensinine and found that Liensinine is poorly absorbed orally (about 17% of the drug can be absorbed into the liver through the gastroint...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/02A61K31/4725A61K47/44A61K47/14A61P9/06A61P9/12
CPCA61K9/02A61K31/4725A61K47/14A61K47/44
Inventor 宋金春宋杨一嫣彭燕黄岭张翔戴谆
Owner WUHAN UNIV
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