Medicinal composition and preparation method thereof

A composition and drug technology, which is applied in the direction of drug combination, pharmaceutical formula, non-active ingredients of polymer compounds, etc., can solve the problems of poor water solubility of drugs, achieve the effects of convenient operation, good solubility, and improved utilization efficiency

Inactive Publication Date: 2012-01-11
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In order to solve the shortcomings of poor water solubility of certain drugs in the prior art, the present invention provides a pharmaceutical composition capable of improving the water solubility of drugs and a preparation method thereof

Method used

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  • Medicinal composition and preparation method thereof
  • Medicinal composition and preparation method thereof
  • Medicinal composition and preparation method thereof

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preparation example Construction

[0046] According to the preparation method provided by the present invention, the contacting in step (a) is carried out under an inert atmosphere, and the contacting conditions include: the molar ratio of the ester to the cyclodextrin is 1-15:1, relatively For 1g of cyclodextrin, the amount of the organic amine is 0.01-5ml, the amount of the first organic solvent is 4-100ml, the contact temperature is 70-85°C, and the contact time is 10-15 hours.

[0047] Since lactide, glycolide and caprolactone are ring-opened under the action of the catalyst, they can directly react with -OH on the cyclodextrin. Therefore, in the present invention, one or both of lactide, glycolide and caprolactone are selected to be directly contacted with cyclodextrin to obtain the cyclodextrin-aliphatic polyester compound represented by formula (6). branch polymer. Lactide, glycolide, and caprolactone used in the present invention are all commercially available.

[0048] According to the preparation me...

Embodiment 1

[0068] Preparation of hydroxypropyl β-cyclodextrin-polylactic acid-dipalmitoylphosphatidylethanolamine grafted polymer nanoparticles loaded with paclitaxel

[0069](1) 5.64g of lactide (Alfar Aesar company, 97%, analytically pure) and 2.5g of hydroxypropyl β-cyclodextrin (Japan Sigma-Aldrich company) are placed in a three-necked flask and vacuumized for 1 hour Finally, add 10 mL of distilled dimethyl sulfoxide to dissolve, add 0.5 mL of triethylamine (Xilong Chemical Factory, Shantou City, Guangdong, analytically pure), and react at 80 ° C for 12 hours under nitrogen protection to obtain hydroxypropyl β - Cyclodextrin-polylactic acid graft polymer crude product. Then use 200mL water to precipitate, wash with water (100mL×4 times), dry in a vacuum oven at 20°C for 48 hours, then extract with toluene (20mL×2 times), and dry in a vacuum oven at 20°C for 48 hours. 6.11 g of solid product hydroxypropyl β-cyclodextrin-polylactic acid graft polymer was obtained. Calculated n=14.

...

Embodiment 2

[0086] Preparation of hydroxypropyl β-cyclodextrin-polylactic acid-dipalmitoylphosphatidylethanolamine grafted polymer nanoparticles loaded with paclitaxel

[0087] Steps (1) to (3) are carried out according to the method of Example 1, and the amounts, conditions and results of each substance involved in the method are shown in Table 1 to Table 3.

[0088](4) 20 mg of purified hydroxypropyl β-cyclodextrin-polylactic acid-dipalmitoylphosphatidylethanolamine graft polymer was dissolved in 3 mL of dichloromethane to obtain cyclodextrin-aliphatic polyester-phosphatidyl Ethanolamine grafted polymer solution, 0.2mg paclitaxel (Norui Pharmaceutical Technology Co., Ltd., Beijing, lot number: 090328) was dissolved in 0.2mL dichloromethane to obtain a paclitaxel solution, cyclodextrin-aliphatic polyester-phosphatidylethanolamine Graft polymer solution and paclitaxel solution were mixed, and the mixed solution was added to 20mL aqueous solution containing 0.4%wt surfactant polyvinyl alco...

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Abstract

The invention provides a medicinal composition and a preparation method thereof. The medicinal composition comprises a carrier and an active component loaded on the carrier, wherein the carrier is nano particles of cyclodextrin-aliphatic polyester-phosphatidyl ethanolamine graft polymer with the structural formula shown in a formula (1) in the specifications; and in the formula (1), m is an integer from 6 to 8, and G is an oxygen atom or has a formula shown in the specifications.

Description

technical field [0001] The invention relates to a pharmaceutical composition and a preparation method thereof. Background technique [0002] Some drugs have good curative effects on major diseases, but due to their poor water solubility, they cannot be effectively absorbed by the human body, making it difficult to fully exert their drug effects, which affects their clinical application. [0003] Paclitaxel (PTX for short) is a new type of broad-spectrum anticancer drug chemically modified from diterpenoid natural products extracted from Taxus brevifolia. It has attracted widespread attention due to its unique mechanism of action. Numerous studies have shown that paclitaxel is effective in the treatment of various tumors, such as ovarian cancer, breast cancer, non-small cell lung cancer, head-neck cancer, and Kaposi sarcoma caused by AIDS, etc., so it is used as a first-line broad-spectrum anticancer drug. However, its water solubility is extremely poor. In order to increase...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/40A61K31/337A61K9/14C08B37/16C08G63/91A61P35/00
Inventor 聂广军吴雁苗卿华韩思媛王欢
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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