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Cucurbitacin lipsome preparation method and formulation

A technology of cucurbitacin and body composition, which is applied in the field of medicine and can solve the problems of unsuitable for intravenous injection and low encapsulation rate

Inactive Publication Date: 2004-06-16
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are literatures to make it into liposome (Chinese herbal medicine 1991, 22 (2): 62), but the encapsulation efficiency is low, only 41.8%, and mixed surfactant is added in the prescription, it is not suitable for intravenous injection

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Embodiment 1: Preparation of cucurbitacin BE (cucurbitacin B content greater than 60%) liposomes

[0021] prescription:

[0022] Cucurbitacin BE 0.01g

[0023] Soy Lecithin 1g

[0024] Proper amount of ethanol

[0025] Phosphate buffer solution of pH 6.8

[0026] Makes 100ml

[0027] Preparation Process:

[0028] Weigh the prescribed amount of soybean lecithin and cucurbitacin BE, put them in a beaker, add an appropriate amount of ethanol to dissolve, add phosphate buffer, and hydrate for 1 to 2 hours to obtain a cucurbitacin liposome solution. The encapsulation efficiency of the obtained liposome was determined, and the encapsulation efficiency was 95.3%.

Embodiment 2

[0029] Embodiment 2: Preparation of cucurbitacin BE (cucurbitacin B content greater than 80%) liposomes

[0030] prescription:

[0031] Cucurbitacin BE 0.1g (10mmol)

[0032] Hydrogenated Soy Lecithin 1g

[0033] Proper amount of ethanol

[0034] Phosphate buffer at pH 7.4

[0035] Makes 100ml

[0036] Preparation process: same as above, encapsulation efficiency is 86.5%.

Embodiment 3

[0037] Embodiment 3: Preparation of cucurbitacin BE (cucurbitacin B content greater than 80%) liposomes

[0038] prescription:

[0039] Cucurbitacin BE 0.02g

[0040] Egg yolk lecithin 4g

[0041] Cholesterol 1g

[0042] Proper amount of ethanol

[0043] pH4 citrate buffer

[0044] Makes 100ml

[0045] Preparation process: same as above, encapsulation efficiency is 83.7%.

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PUM

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Abstract

The invention relates to a cucurbitacin liposome composition and its preparation, which has rather high encapsulation efficiency, and can be administered through vein, muscle, oral and nasal. The constituent percentage by weight of the composition are, cucurbitacin BE or cucurbitacin B 0.001-0.1%, phospholipids 0.1-10%, cholesterin 0-5%, the phospholipids can be lecithin, di-stearoyl phosphatidyl choline, di- palmityl phosphatidyl choline, di-oleoyl phosphatidyl choline, di- palmityl phosphatidyl ethanolamine, di-stearoyl phosphatidylglycerol. The preparation according to the invention can be prepared in the form of injection, oral liquid, syrup, drop and nasal spray

Description

Technical field: [0001] The invention relates to the technical field of medicine, specifically, it is a cucurbitacin liposome prescription and its preparation using phospholipids and cucurbitacin to form lipids. Background technique: [0002] Cucurbitacin is the extract of traditional Chinese medicine melon stalk (alias: bitter clove), which mainly contains cucurbitacin B, E, etc., and is an active ingredient for treating hepatitis and liver cancer. Cucurbitacin tablets are used to treat chronic hepatitis (Cucurbitacin Tablets Pharmacy Bulletin 1986, 21(6): 357). After clinical trials in 13 hospitals in Shanghai, Beijing, Chongqing and other places, the effective rate is 75.2%, and the marked rate is 44.6%. . It has been observed clinically that cucurbitacin tablets can comprehensively improve the common symptoms and main signs of chronic hepatitis, and have obvious effects of lowering enzyme (S-GPT), lowering turbidity (TTT, ZnTT) and lowering bilirubin. It can cause S-GP...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/57A61P1/16A61P31/12A61P35/00
Inventor 邓意辉王绍宁吴琼
Owner SHENYANG PHARMA UNIVERSITY
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