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Gossypol acetate-containing thermosensitive gel preparation and preparation method and application thereof

A technology of gossypol acetate and sensitive gel, which is applied in the field of heat-sensitive gel and its preparation, can solve problems such as hindering popularization and use, and achieve the effects of avoiding toxic and side effects, convenient administration, and reducing irritation

Inactive Publication Date: 2017-05-24
UNIV OF SHANGHAI FOR SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the severe hypokalemia toxicity of gossypol acetate has hindered its clinical promotion and use for a long time.

Method used

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  • Gossypol acetate-containing thermosensitive gel preparation and preparation method and application thereof
  • Gossypol acetate-containing thermosensitive gel preparation and preparation method and application thereof
  • Gossypol acetate-containing thermosensitive gel preparation and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Step 1: adding an organic solvent into the container, dissolving 17.5% by mass poloxamer and 1.0% by mass gossypol acetate in the organic solvent to obtain a mixed solution. In this embodiment, the organic solvent is chloroform, and the model of the poloxamer is poloxamer 407.

[0022] Step 2, the mixed solution was ultrasonically oscillated for 5 minutes.

[0023] Step 3: spin-dry the mixed solution after shaking, and stop after the mixed solution in the container forms a film along the container wall, and the rotation speed of the spin-dry is 100-150 r / min. In this embodiment, the rotating speed of spin drying is 120r / min.

[0024] Step 4, place the container with the film under vacuum condition for 3-4 hours. In this embodiment, the standing time is 3 hours.

[0025] Step 5, add 1.0% by mass lactic acid solution, 0.05% by mass preservative and 80.45% by mass deionized water to the container for hydration by oscillating in an ice bath. The temperature range for osc...

Embodiment 2

[0040] Step 1: adding an organic solvent into the container, dissolving 20.0% by mass poloxamer and 1.0% by mass gossypol acetate in the organic solvent to obtain a mixed solution. In this embodiment, the organic solvent is chloroform, and the model of the poloxamer is poloxamer 407.

[0041] Step 2, the mixed solution was ultrasonically oscillated for 5 minutes.

[0042] Step 3: spin-dry the mixed solution after shaking, and stop after the mixed solution in the container forms a film along the container wall, and the rotation speed of the spin-dry is 100-150 r / min. In this embodiment, the rotating speed of spin drying is 120r / min.

[0043] Step 4, place the container with the film under vacuum condition for 3-4 hours. In this embodiment, the standing time is 3 hours.

[0044] Step five, add 0.5% lactic acid solution by mass percentage, 0.05% preservative by mass percentage and deionized water with 78.45% mass percentage to the container, carry out ice bath shock hydration, t...

Embodiment 3

[0049] Step 1: adding an organic solvent into the container, dissolving 20.0% by mass poloxamer and 1.0% by mass gossypol acetate in the organic solvent to obtain a mixed solution. In this embodiment, the organic solvent is chloroform, and the model of the poloxamer is poloxamer 407.

[0050] Step 2, the mixed solution was ultrasonically oscillated for 5 minutes.

[0051] Step 3: spin-dry the mixed solution after shaking, and stop after the mixed solution in the container forms a film along the container wall, and the rotation speed of the spin-dry is 100-150 r / min. In this embodiment, the rotating speed of spin drying is 120r / min.

[0052] Step 4, place the container with the film under vacuum condition for 3-4 hours. In this embodiment, the standing time is 3 hours.

[0053] Step 5: Add 0.1% by mass lactic acid solution, 0.05% by mass preservative and 78.85% by mass deionized water to the container for hydration by oscillating in an ice bath. The temperature range for osc...

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Abstract

The invention provides a gossypol acetate-containing thermosensitive gel preparation. The gossypol acetate-containing thermosensitive gel preparation is characterized by comprising the following components: gossypol acetate accounting for 0.02-1 percent by mass of the gossypol acetate-containing thermosensitive gel preparation, poloxamer accounting for 16-25 percent by mass of the gossypol acetate-containing thermosensitive gel preparation, a preservative accounting for 0.05-0.3 percent by mass of the gossypol acetate-containing thermosensitive gel preparation, deionized water accounting for 72.7-83.83 percent by mass of the gossypol acetate-containing thermosensitive gel preparation and lactic acid accounting for 0.1-1.0 percent by mass of the gossypol acetate-containing thermosensitive gel preparation, wherein the PH of the gossypol acetate-containing thermosensitive gel preparation is 4.5-5.5. The gossypol acetate-containing thermosensitive gel preparation is in a liquid state at room temperature and is convenient for drug administration; after the gossypol acetate-containing thermosensitive gel preparation is administrated into a vagina, phase transformation occurs due to the temperature rise, and in-situ gelation occurs in the vagina, so that close contact between the preparation and a mucosal tissue can be achieved; and the gossypol acetate-containing thermosensitive gel preparation can penetrate into vaginal mucosal folds to be fully spread and can stay in the vagina for some time to achieve a long-lasting effect.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a heat-sensitive gel containing gossypol acetate and a preparation method and application thereof. Background technique [0002] Gossypol is a yellow polyphenolic compound isolated from cottonseed of Malvaceae plant, which is widely used in the field of medicine in the form of gossypol acetate. Oral gossypol acetate is mainly used for male contraception in the early stage, and has anti-tumor, anti-viral and other activities. However, the severe hypokalemia toxicity of gossypol acetate has hindered its clinical promotion and use for a long time. Contents of the invention [0003] The present invention is carried out in order to solve the above problems, and the purpose is to provide a heat-sensitive gel containing gossypol acetate and its preparation method and application. [0004] The invention provides a heat-sensitive gel containing gossypol acetate, which has su...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K31/11A61K47/10A61K47/12A61K47/14A61P15/00
CPCA61K31/11A61K9/0034A61K9/06A61K47/10A61K47/12A61K47/14
Inventor 次丽倩刘瑜刘哲鹏
Owner UNIV OF SHANGHAI FOR SCI & TECH
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