Liensinine suppository and preparation method and purpose thereof

A liensinine suppository and 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, serious liver first-pass effect, and the inability to achieve expected ideal pharmacological activity of liensinine , to avoid the effect of poor oral absorption

Active Publication Date: 2016-03-30
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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  • Liensinine suppository and preparation method and purpose thereof
  • Liensinine suppository and preparation method and purpose thereof
  • Liensinine suppository and preparation method and purpose thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

Embodiment 2

[0035] Weigh 0.35 g of liensinine (extracted and refined in the laboratory), micronize 1 to 3 times with a pulverizer, pass through a 100-mesh sieve, and mix 99.5 g of semi-synthetic mixed fatty acid lipids (model 36, purchased from Chengdu Lutianhua) and spit After heating and melting 0.1g of Wen-80 (purchased from Sichuan Jinshan Pharmaceutical) at 50°C, add micronized liensinine, stir to make it evenly mixed, pour it into a preheated plug mold, and cool at 2-8°C for 1-3 Take it out after 1 hour, and each plug weighs 1.0g.

Embodiment 3

[0037] Weigh 1.0 g of liensinine (extracted and refined in the laboratory), micronize 1 to 3 times with a pulverizer, pass through a 100-mesh sieve, and mix 98.5 g of semi-synthetic mixed fatty acid lipids (model 34, purchased from Chengdu Lutianhua) into Wen-80 (purchased from Sichuan Jinshan Pharmaceutical) 0.5g was heated and melted at 50°C, added liensinline, stirred to mix evenly, poured into a preheated plug mold, cooled at 2-8°C for 1-3 hours, and then taken out That is, each bolt 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 its preparation method and application. Background technique [0002] Liensinine is a bisbenzylisoquinoline alkaloid extracted from the green germ of the mature seeds of the Nymphaeaceae plant lotus (Nelumbonucifera Gaertn). Its chemical structure is shown in the following formula. [0003] [0004] Liensinine has antihypertensive, anti-arrhythmia, anti-hyperlipidemia, anti-lipid peroxidation, protection of cerebral ischemia and other cardiovascular and cerebrovascular system activities. 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...

Claims

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Application Information

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Patent Type & Authority Applications(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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