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Deoxidized podophyllotoxin polymer micelle freeze-drying preparation

A technology of deoxypodophyllotoxin and polymer glue, which is applied in the direction of drug combination, microcapsules, and capsule delivery, and can solve the problems of inability to solubilize and the solubility of deoxypodophyllotoxin

Active Publication Date: 2014-04-02
ZHEJIANG JIANFENG PHARM CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] In order to improve the druggability of deoxypodophyllotoxin, we tried to study other ways to solubilize deoxypodophyllotoxin, however, the solubility of deoxypodophyllotoxin could not be solved by adding co-solvents such as ethanol, isopropanol and glycerol; further research Attempts to solubilize via micelles have been attempted with other block polymers such as poloxamers or surfactants such as Tween 80, respectively. but precipitated immediately
[0009] In further research, we were surprised to find that deoxypodophyllotoxin has greater solubility and better stability in the polymer micelles of mPEG-PDLLA, while other drug-loading systems cannot achieve the same purpose

Method used

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  • Deoxidized podophyllotoxin polymer micelle freeze-drying preparation
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Examples

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Effect test

Embodiment 1

[0036] Example 1 Preparation and compounding of deoxypodophyllotoxin solution with ethanol as cosolvent

[0037] 150 mg of deoxypodophyllotoxin and 10 mL of ethanol were placed in an eggplant-shaped bottle, and heated to dissolve completely. The above solution was added to 500 mL of sodium chloride solution with a concentration of 0.9%, and crystal precipitation was immediately visible.

Embodiment 2

[0038] Example 2 Preparation and reconstitution of deoxypodophyllotoxin polymer micelles using polysorbate 80 as solubilizer

[0039] 150 mg of deoxypodophyllotoxin and 80-1500 mg of polysorbate were placed in an eggplant-shaped flask, 20 ml of ethanol was added to dissolve completely, and the ethanol was removed under reduced pressure. An oily product was obtained.

[0040]Take 1000 mg of this product, add it to 500 mL of 0.9% sodium chloride solution, shake it, and it can be seen that a large amount of crystals are precipitated and turbid.

Embodiment 3

[0041] Example 3 Preparation and reconstitution of deoxypodophyllotoxin polymer micelles using poloxamer 188 as solubilizer

[0042] Put 150 mg of deoxypodophyllotoxin and 1,884,000 mg of poloxamer in an eggplant-shaped bottle, add 20 ml of ethanol to dissolve completely, and remove the ethanol under reduced pressure. The product was obtained as a white block.

[0043] Take 2000 mg of this product, add it to 500 mL of 0.9% sodium chloride solution, shake it, and it can be seen that a large number of crystals are precipitated and turbid.

[0044] All the above are comparative examples, which cannot reach the purpose of the present invention.

[0045] The present invention adopts mPEG-PDLLA as carrier material, specific examples are as follows:

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Abstract

The invention provides a deoxidized podophyllotoxin polymer micelle freeze-drying preparation. Polymer micelle consists of an amphiphilic block polymer, and a polyethylene glycol monomethyl ether-poly (D,L) lactide block copolymer is optimal. A preparation method of the preparation comprises the steps that deoxidized podophyllotoxin and the block polymer are dissolved in an organic solvent; the solvent is flooded to be gel; the gel is hydrated; the micelle is obtained; and the freeze-drying preparation is prepared further. The freeze-drying preparation can be used for treating a tumor; a medicine carrying encapsulation rate is above 90%; the particle size of the redissolved micelle is 40-70nm; and a redissolved micelle solution can be stabilized for 4-24h at 25 DEG C.

Description

technical field [0001] The invention relates to a freeze-dried pharmaceutical composition and a preparation method thereof, in particular to a composition, a preparation method and a freeze-dried preparation of a deoxypodophyllotoxin micelle. Background technique [0002] Deoxypodophyllotoxin is a compound extracted and purified from lignin plants, the structural formula is as follows: [0003] [0004] In the 1990s, experiments have shown that deoxypodophyllotoxin has an in vitro inhibitory effect on P-388 leukemia, human lung cancer A-549 and colon cancer HT-29 cell lines. Since deoxypodophyllotoxin is insoluble in water, it cannot be used to prepare preparations for intravenous injection, which limits its application in preparation industry and clinical practice. In order to improve its water solubility, various methods have been adopted in the prior art. [0005] Chinese patent CN101693112A discloses an inclusion compound of deoxypodophyllotoxin and β-cyclodextrin; ...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K31/365A61K47/34A61P35/00A61P35/02
Inventor 朱雄吴葆金黄金龙史继峰孙如宁涂家生吴建梅
Owner ZHEJIANG JIANFENG PHARM CO LTD
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