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Vaginal contraception thermosensitive gelata of econazole nitrate and preparation method thereof

A technology of econazole nitrate and temperature-sensitive gel, which is applied in the directions of pharmaceutical formulations, medical preparations of inactive ingredients, and drug delivery, can solve problems such as destroying the vaginal mucosa, and achieve good safety, high-efficiency contraceptive effect, and rapid action. Effect

Inactive Publication Date: 2012-05-30
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] Therefore, the technical problem to be solved in the present invention is to provide a kind of econazole nitrate vaginal contraceptive temperature-sensitive gel and a preparation method thereof for existing contraceptives that have the defect of destroying the vaginal mucosa. The present invention also provides a kind of econazole nitrate water soluble clathrate

Method used

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  • Vaginal contraception thermosensitive gelata of econazole nitrate and preparation method thereof
  • Vaginal contraception thermosensitive gelata of econazole nitrate and preparation method thereof
  • Vaginal contraception thermosensitive gelata of econazole nitrate and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0094] Example 1 Sulfobutyl ether-β-cyclodextrin (inclusion in liquid)

[0095] In the prescription, econazole nitrate is 0.5%, P407 is 17.4%, P188 is 6.25%, SBE-β-CD is 6.9%, and the proportion of buffer is 69%.

[0096] Add 720mg of econazole nitrate to 100ml of pH3.7 phosphoric acid-citric acid buffer, 10g of SBE-β-CD, stir at about 25°C until the drug is dissolved, then add 25g of P407, 9g of P188, and stir at low temperature (0-5°C) for 24 hours Above, a clear and transparent gel solution is obtained, the measured pH is 4.0±0.1 at room temperature, and the phase transition temperature is about 35±2°C.

Embodiment 2

[0097] Example 2 Sulfobutyl ether-β-cyclodextrin (inclusion in liquid)

[0098] In the prescription, econazole nitrate is 0.3%, P407 is 17.8%, P188 is 7.9%, SBE-β-CD is 8.5%, and the proportion of buffer is 66%.

[0099] Add 456mg of econazole nitrate to 100ml of pH 3.2 phosphoric acid-citric acid buffer, 13g of SBE-β-CD, stir at about 25°C until the drug is dissolved, then add 27g of P407, 12g of P188, and stir at low temperature (0-5°C) for more than 24 hours , to obtain a clear and transparent gel solution, the measured pH at room temperature is 3.5±0.1, and the phase transition temperature is about 34±2°C.

Embodiment 3

[0100] Example 3 sulfobutyl ether-β-cyclodextrin (inclusion in liquid)

[0101] In the prescription, econazole nitrate is 0.2%, P407 is 17.5%, P188 is 4.4%, SBE-β-CD is 5.1%, and the proportion of buffer is 73%.

[0102] Add 274mg of econazole nitrate to 100ml of pH 4.3 phosphoric acid-citric acid buffer, 8g of SBE-β-CD, stir at about 25°C until the drug dissolves, then add 24g of P407, 6g of P188, and stir at low temperature (0-5°C) for more than 24 hours , a clear and transparent gel solution was obtained, the pH of which was measured at room temperature was 4.6±0.1, and the phase transition temperature was about 36±2°C.

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Abstract

The invention provides a water-soluble cyclodextrin derivative clathrate of econazole nitrate, a vaginal contraception thermosensitive gelata containing the clathrate and a preparation method of the gelata. According to the invention, water-indissoluble econazole nitrate is clathrated by a water-soluble cyclodextrin derivative to improve the solubility of econazole nitrate in water, so the vaginal thermosensitive gelata is prepared by treating econazole nitrate as a sperm killing active component for an external contraceptive, and the vaginal thermosensitive gelata which is a novel external contraception preparation comprises the water-soluble cyclodextrin derivative clathrate of econazole nitrate, a thermosensitive gel skeletal material and an acidic buffer. The contraception thermosensitive gelata which is a liquid when it is at the outside of a body can be rapidly and uniformly coated on vaginal surfaces, and becomes a semisolid gel when it is in the body to immobilizedly capture sperms until the sperms are killed. The contraception thermosensitive gelata of econazole nitrate has the advantages of use convenience, rapid action, reliability, and good safety. The gelata which is a novel dosage form and has the characteristics of easy preparation and low material cost is in favor of the family planning work in such a world's most populous country China.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a water-soluble cyclodextrin derivative inclusion complex of econazole nitrate, a vaginal contraceptive temperature-sensitive gel containing the same and a preparation method. Background technique [0002] The most widely used external contraceptive drug at home and abroad is mainly nonoxynol-9 (NP-9), and its traditional preparations include suppositories, gels, films and vaginal tablets. The contraceptive effect of nonoxynol-9 has been fully affirmed clinically. Since the drug came out in the 1960s, it has played a major role in the world's family planning. [0003] Nonoxynol-9 is a powerful nonionic surfactant. Its contraceptive mechanism is to reduce the surface tension of sperm cell membranes and change the osmotic pressure of sperm cells, thereby killing sperm or immobilizing sperm, so as to achieve the purpose of contraception. Nonoxynol-9 is also a strong cytot...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/4174A61K47/48A61P15/18
Inventor 张春霞谢淑武陈庆华包泳初潘峰韩蕾李然然房超朱焰曹霖
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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