Liposome ointment containing heparin kind medicine and its preparation method

A liposome and ointment technology, applied in the field of medicine, can solve the problems of only local treatment, unsatisfactory effect and inconvenient medication

Inactive Publication Date: 2004-03-03
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Injection is mainly used as therapeutic medicine and short-term preventive medicine. As long-term preventive medicine, such as preventing thrombosis in patients with thrombosis tendency, it has the disadvantages of inconvenient medication and high risk of bleeding.
Due to the action of digestive tract enzymes and the first-pass action of the liver after absorption, although the tablet is convenient to take, the effect is not ideal
The common ointment currently used has only heparin sodium ointment (Drug Standards of the People's Republic of China, Yao Jian An Han [2002] No. 157), and its preparation method is to dissolve heparin sodium and fat-soluble components in water, and then mix and emulsify with the ointment base Therefore, since the ointment is not specially designed to solve the problem of transdermal absorption, it only plays a local therapeutic role, such as being used for soft tissue contusion, frostbite, burn, superficial phlebitis, chapped, eczema, etc.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Embodiment 1: Get 2 grams of phospholipids, add cholesterol as 2: 1 by the molar ratio of phospholipids and cholesterol, add 4ml of ethanol, after dissolving completely, make medicinal solution I; Get heparin sodium 0.1 gram, sodium cholate 0.1 gram and dissolve in 10ml distilled water , as the medicinal solution II; slowly add the medicinal solution I to the medicinal solution II, stir while adding, continue to stir for 1 hour after the addition, and then use a high-speed stirrer at 10000r / min to vigorously stir for 3 minutes to obtain heparin sodium liposomes Suspension: take 0.1 g of carbomer, add 6 ml of distilled water, and adjust the pH to 6.5 with 1 mol / L sodium hydroxide; take another 1 g of vitamin E, 0.1 g of ethyl paraben, and 1 ml of propylene glycol, dissolve and mix with carbomer Add it into the heparin liposome suspension together and stir evenly.

Embodiment 2

[0025] Embodiment 2: get 4 grams of phospholipids, 0.8 grams of cholesterol, be dissolved in 30ml chloroform, remove organic solvent by rotary evaporation in 37 ℃ of constant temperature water baths, make film-forming materials such as phospholipids form uniform lipid film on the beaker wall. Dissolve 0.1 g of low-molecular-weight heparin sodium and 0.1 g of sodium cholate in 20 ml of distilled water, add them to a round-bottomed flask, and wash the membrane by rotation for 2 hours to obtain a suspension of low-molecular-weight heparin sodium liposomes. Probe-type ultrasound for 3 minutes, filter through a 0.15 μm microporous membrane to remove impurities such as titanium particles released by the probe; take 0.3 g of carbomer, add 10 ml of distilled water, and adjust the pH to 6.5 with 1 mol / L sodium hydroxide after completely dissolving; Take 0.2 g of ethyl paraben, 2 ml of propylene glycol, and 2 g of vitamin E, mix and dissolve them, add them together with carbomer into the...

Embodiment 3

[0026] Embodiment 3: Get 2 grams of phospholipids, add cholesterol according to the molar ratio of phospholipids and cholesterol as 2: 1, add 3 ml of ethanol to dissolve, as medicinal solution I; 0.5 grams of low-molecular-weight heparin sodium, 0.1 grams of sodium cholate are dissolved in 3 ml of distilled water , as liquid II; mix liquid I and liquid II, grind for 30 minutes, stand for 1 hour, then add 5ml of distilled water and mix to obtain low molecular weight heparin sodium liposome suspension; add 0.1 g of sodium hyaluronate, add 10 ml of distilled water Dissolve: Take 1 gram of vitamin E, 0.1 gram of ethylparaben, and 1 ml of propylene glycol, mix and dissolve, add to the low-molecular-weight heparin liposome suspension together with the sodium hyaluronate solution, and stir evenly.

[0027] Effect of low molecular weight heparin liposome ointment on thrombus formation in rabbits in vitro. Take 30 rabbits and divide them into 5 groups randomly, 6 rabbits in each group....

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Abstract

A lipid ointment for treating thrombotic diseases, cold injury, burn, superficial phlebitis and eczema contains heparin medicines, auxiliary, phosphatide, cholesterin, sodium cholate and hydrophilic high-molecular polymer. Its preparing process is also disclosed.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to a liposome ointment containing heparin drugs for preventing and treating various thromboembolic diseases, frostbite, burns, superficial phlebitis, eczema and the like and a preparation method thereof. Background technique [0002] Heparin drugs are mucopolysaccharide drugs, which refer to a class of substances composed of hexuronic acid, hexosamine sugar and their sulfated, acetylated and other derivatives as structural units, including heparin, low molecular weight heparin and ultra low molecular weight heparin heparin. Heparin is extracted from the small intestinal mucosa, lung and other tissues of pigs, cattle, sheep and other animals, with a molecular weight distribution of 3000D to 50000D and an average molecular weight of about 15000D; low molecular weight heparin is a low molecular weight component obtained from heparin by fractionation, or For the low molecular weight h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K9/127A61K31/727A61K47/30A61P17/02
Inventor 王凤山俞淑文翟光喜姬胜利崔慧斐曹吉超张天民
Owner SHANDONG UNIV
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