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Total cucurbitacin phosphatidyl cholate mixed micelle oral quick-absorption membrane and preparation method thereof

A technology of mixing micelles and phospholipids, which is applied in the direction of drug combinations, pharmaceutical formulas, medical preparations of non-active ingredients, etc., can solve the problems of low solubility, low oral bioavailability, and difficult absorption of cucurbitacin compounds, and achieve Reduce the first-pass effect, improve bioavailability, and increase the effect of permeation

Active Publication Date: 2014-04-23
THE FIFTH MEDICAL CENT OF CHINESE PLA GENERAL HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Domestically marketed preparations with total cucurbitacin as the main component include total cucurbitacin tablets produced by Beijing Tongrentang Science and Technology Development Co., Ltd. Pharmaceutical Factory, Beijing Sanjiu Pharmaceutical Co., Ltd. and Chongqing Hanhua Pharmaceutical Co., Ltd. The name is cucurbitacin tablets, which are common oral preparations. They are mainly used for the treatment of chronic hepatitis B and primary liver cancer. The oral bioavailability is low, mainly because the solubility of cucurbitacin compounds is low and the dissolution is poor. poorly absorbed in the gastrointestinal tract

Method used

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  • Total cucurbitacin phosphatidyl cholate mixed micelle oral quick-absorption membrane and preparation method thereof
  • Total cucurbitacin phosphatidyl cholate mixed micelle oral quick-absorption membrane and preparation method thereof
  • Total cucurbitacin phosphatidyl cholate mixed micelle oral quick-absorption membrane and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0033] Embodiment 1: Preparation of total cucurbitacin phospholipid bile salt mixed micelles

[0034] (1) Add 16.67g of soy lecithin to 100ml of petroleum ether to make a standard solution with a mass concentration of 30-70mmol / L, dry most of the solvent under nitrogen, and then place it in a vacuum oven at room temperature for 12 hours to remove trace amounts of Organic solvent, made into lipid film;

[0035] (2) Dissolve 2 g of sodium taurocholate in 100 ml of phosphate buffer (pH=7.2) to prepare a bile salt solution with a mass concentration of 5-20 mmol / L;

[0036] (3) Mix the lipid film and the bile salt solution ultrasonically in a 45°C water bath for 45 minutes to obtain a blank phospholipid bile salt mixed micelle solution;

[0037] (4) Add 8g of total cucurbitacin powder into phospholipid bile salt blank micelles, fill with nitrogen and seal, place on a constant temperature magnetic stirrer, and stir evenly at 40°C for 24 hours to obtain drug-loaded micelles, namely ...

Embodiment 2

[0038] Example 2: Preparation of total cucurbitacin phospholipid bile salt mixed micelles

[0039] (1) Add 16.67g of soybean lecithin into 80ml of chloroform to make a standard solution with a mass concentration of 30-70mmol / L, dry most of the solvent under nitrogen, and then place it in a vacuum oven at room temperature for 12 hours to remove traces of Organic solvent, made into lipid film;

[0040] (2) Dissolve 2 g of sodium deoxycholate in 100 ml of phosphate buffer (pH=7.2) to prepare a bile salt solution with a mass concentration of 5-20 mmol / L;

[0041] (3) Ultrasonically mix the lipid film and bile salt solution in a 45°C water bath for 45 minutes to obtain a blank phospholipid / bile salt mixed micelle solution;

[0042] (4) Add 8g of total cucurbitacin powder into phospholipid bile salt blank micelles, fill with nitrogen and seal, place on a constant temperature magnetic stirrer, and stir evenly at 40°C for 24 hours to obtain drug-loaded micelles, that is, total cucurb...

Embodiment 3

[0043] Example 3: Preparation of total cucurbitacin phospholipid bile salt mixed micelles

[0044] (1) Add 16.67g of soy lecithin into 90ml of ether to make a standard solution with a mass concentration of 30-70mmol / L, dry most of the solvent under nitrogen, and then place it in a vacuum oven at room temperature for 12 hours to remove trace organic Solvent, made of lipid film;

[0045] (2) Dissolve 2 g of sodium chenodeoxycholate in 100 ml of phosphate buffer (pH=7.2) to prepare a bile salt solution with a mass concentration of 5-20 mmol / L;

[0046] (3) Mix the lipid film and the bile salt solution ultrasonically in a 45°C water bath for 45 minutes to obtain a blank phospholipid bile salt mixed micelle solution;

[0047] (4) Add 8 g of total cucurbitacin powder into phospholipid bile salt blank micelles, fill with nitrogen and seal, place on a constant temperature magnetic stirrer, and stir evenly at 40°C for 24 hours to obtain drug-loaded micelles, namely total cucurbitacin ph...

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Abstract

The invention provides a total cucurbitacin phosphatidyl cholate mixed micelle oral quick-absorption membrane and a preparation method thereof, and belongs to the technical field of traditional Chinese medicinal preparations and preparation methods thereof. The preparation method comprises the following steps: preparing a lipid membrane from phospholipid; dissolving cholate into a phosphate buffer solution to prepare a cholate liquid; performing ultrasonic mixing on the lipid membrane and the cholate liquid in a water bath to obtain a phosphatidyl cholate blank micelle liquid; adding total cucurbitacin powder into the phosphatidyl cholate blank micelle liquid to obtain phosphatidyl cholate mixed micelle of total cucurbitacin; sequentially adding hydroxypropyl methyl cellulose, low substituted hydroxyprepyl cellulose, microcrystalline cellulose and PEG400 (polyethylene glycol 400) into the phosphatidyl cholate mixed micelle of total cucurbitacin to obtain the total cucurbitacin phosphatidyl cholate mixed micelle oral quick-absorption membrane. The oral quick-absorption membrane has the advantages of improving the solubility of total cucurbitacin, increasing adhesive and penetrating effect of the oral quick-absorption membrane to oral mucosa, avoiding irritation of total cucurbitacin to gastrointestinal tracts, remarkably improving the bioavailability of total cucurbitacin and reducing adverse response.

Description

technical field [0001] The invention belongs to the technical field of traditional Chinese medicine preparations and preparation methods thereof, and in particular relates to a total cucurbitacin phospholipid bile salt mixed micelle oral fast-absorbing membrane and a preparation method thereof. Background technique [0002] Cucurbitacins are a class of tetracyclic triterpenoids that obtain bitter or sweet taste from various plants in Cucurbitaceae and other families and genera. They are all highly oxidized compounds, characterized by 18-methyl at C-9. Including more than 100 kinds of compounds such as cucurbitacin A, B, C, D, E, F, G, H, I, J, K, L, eschobilis, and escobilis. Among them, cucurbitacin B is the one with the highest content and the strongest physiological activity. It has various biological activities such as anti-tumor, liver protection, anti-inflammation, improving immunity, and gastrointestinal effects. Its structural formula is as follows [0003] [...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K36/42A61K31/575A61K47/24A61K47/28A61K47/38A61P35/00A61P1/16A61P29/00A61P37/04
Inventor 袁海龙韩晋于超徐和申宝德徐平华
Owner THE FIFTH MEDICAL CENT OF CHINESE PLA GENERAL HOSPITAL
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