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Dual-functional vaginal composite temperature-sensitive hydrogel preparation with effects of contracepting and killing microbes and preparation method thereof

A temperature-sensitive hydrogel and microbe-killing technology, applied in the field of medicine and health, can solve the problems of large side effects and inconvenient use, and achieve the effects of prolonging the residence time, good spermicidal effect and convenient use.

Active Publication Date: 2015-05-13
WEIFANG MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical problem to be solved by the present invention is to provide a contraceptive and microbiocidal dual-functional vaginal compound temperature-sensitive hydrogel preparation and its preparation method in view of the above deficiencies, so as to achieve the following invention objectives: longer action time, mucoadhesive, local retention Non-irritating, self-degradable and non-irritating to the vaginal mucosa, the contraceptive effect is better, and the compound temperature-sensitive hydrogel with anti-inflammatory and anti-viral effects overcomes the defects of relatively large side effects and inconvenient use in the existing contraceptive methods

Method used

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  • Dual-functional vaginal composite temperature-sensitive hydrogel preparation with effects of contracepting and killing microbes and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] The preparation of microspheres comprises the following steps:

[0042] a. Preparation of raw material solution

[0043] Accurately weigh 5 g each of chitosan and bletilla striata polysaccharide, and 1 g of tenofovir, which were vacuum-dried to constant weight at room temperature, and dissolved in 1000 mL of 0.5% acetic acid solution;

[0044] b. Filtration, spray drying

[0045] After being filtered through a 0.45 μm microporous membrane, the filtrate was introduced into the double-flow spiral nozzle of a Büchi 290 small spray dryer through a peristaltic pump. The inlet temperature was controlled at 110 °C, the feed rate was 1.5 mL / min, and the air flow rate was 300 L / h, the mass ratio of chitosan / Bletilla striata polysaccharide / tenofovir is 5:5:1;

[0046] c. Preparation of microsphere powder

[0047] Spray drying "one-step" to prepare PD / TFV / CTS / BSP microsphere powder, collect the microsphere powder in a desiccator for later use.

Embodiment 2

[0049] The preparation of microspheres comprises the following steps:

[0050] a. Preparation of raw material solution

[0051] Accurately weigh 5 g of chitosan, 10 g of Bletilla striata polysaccharide, and 1 g of tenofovir that were vacuum-dried to constant weight at room temperature, and dissolve them in 1000 mL of 0.5% acetic acid solution;

[0052] b. Filtration, spray drying

[0053] After being filtered through a 0.45 μm microporous membrane, the filtrate was introduced into the double-flow spiral nozzle of the Büchi 290 small spray dryer through a peristaltic pump. The inlet temperature was controlled at 110°C, the feed rate was 4 mL / min, and the air flow rate was 400 L / h , the mass ratio of chitosan / Bletilla striata polysaccharide / tenofovir is 5:10:1;

[0054] c. Preparation of microsphere powder

[0055] Spray drying "one-step" to prepare PD / TFV / CTS / BSP microsphere powder, collect the microsphere powder in a desiccator for later use.

Embodiment 3

[0057] The preparation of microspheres comprises the following steps:

[0058] a. Preparation of raw material solution

[0059] Accurately weigh 5 g of chitosan, 20 g of Bletilla striata polysaccharide, and 1 g of tenofovir that were vacuum-dried to constant weight at room temperature, and dissolve them in 1000 mL of 0.5% acetic acid solution.

[0060] b. Filtration, spray drying

[0061] After being filtered through a 0.45 μm microporous membrane, the filtrate was introduced into the double-flow spiral nozzle of the Büchi 290 small spray dryer through a peristaltic pump. The inlet temperature was controlled at 110°C, the feed rate was 6.5 mL / min, and the air flow rate was 500 L / h , the mass ratio of chitosan / Bletilla striata polysaccharide / tenofovir is 5:20:1;

[0062] c. Preparation of microsphere powder

[0063] Spray drying "one-step" to prepare PD / TFV / CTS / BSP microsphere powder, collect the microsphere powder in a desiccator for later use.

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Abstract

The invention discloses a dual-functional vaginal composite temperature-sensitive hydrogel preparation with effects of contracepting and killing microbes. The hydrogel preparation comprises the following components in parts by weight: 32.21-58.57 parts of platycodin D, 2.04 parts of tenofovir, 10.2-40.8 parts of bletilla striata polysaccharide, 11.51 parts of chitosan, 13-17 parts of alpha, sodium beta-glycerophosphate, 0.04-0.08 part of sodium alginate and 0.40-0.60 part of CaCl2. The invention also discloses a method for preparing the composite temperature-sensitive hydrogel preparation. The composite temperature-sensitive hydrogel prepared by the method has the functions of contracepting and promoting HIV pre-exposure prophylaxis, is non-irritating to vagina mucosa and is good in spermicidal effect. The medicines in the gel exist in the body in the microsphere form so as to prolong the retention time of the medicines in the treatment part, and the bioavailability and treatment effect of the medicine are improved.

Description

technical field [0001] The invention relates to a composite temperature-sensitive hydrogel, in particular to a contraceptive and antimicrobial dual-function vaginal composite temperature-sensitive hydrogel preparation and a preparation method thereof, which belong to the field of medicine and health. Background technique [0002] Population explosion has become a major global problem. Each year, more than 120 million couples cannot meet their contraceptive needs, resulting in 46 million abortions worldwide. At the same time, more than 40 million people are living with HIV worldwide, with about 18,000 new infections every day. The infection rate of sexually transmitted diseases is also rising rapidly, with about 340 million new infections every year, resulting in a heavy social public health burden. In recent years, the development of dual-function external contraceptives has become an international development trend and focus, and the World Health Organization (WHO) and the...

Claims

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Application Information

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IPC IPC(8): A61K31/704A61K9/06A61P15/18A61P31/02A61P31/18A61K31/675
Inventor 张维芬孙玉卿商洪才郑增娟
Owner WEIFANG MEDICAL UNIVERSITY
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