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Acidic biological adhesion heat-variable gelling agent, its preparing method and uses

A bioadhesive and sensitive gel technology, applied in diseases, drug combination, drug delivery, etc., can solve problems such as inability to form a barrier, stickiness, and difficulty in accurate loading

Active Publication Date: 2010-07-14
上海市生物医药技术研究院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these preparations are not bioadhesive enough to truly form a barrier on the vaginal mucosal surface and thus do not adequately capture STD-causing microorganisms and / or spermatozoa, nor prevent sperm from entering
[0005] At present, all gels remain gelatinous and viscous at room temperature, so it is difficult to accurately fill the amount in production, and GMP large-scale production is extremely difficult

Method used

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  • Acidic biological adhesion heat-variable gelling agent, its preparing method and uses
  • Acidic biological adhesion heat-variable gelling agent, its preparing method and uses
  • Acidic biological adhesion heat-variable gelling agent, its preparing method and uses

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preparation example Construction

[0070] Preparation of Acidic Bioadhesive Thermosensitive Gel

[0071] The acidic bioadhesive thermosensitive gel provided by the invention can be obtained by mixing and dissolving a matrix excipient, a bioadhesive agent, a dispersant and an acidic buffer.

[0072] In a preferred example of the present invention, 15-20wt% Poloxamer127, 2-8wt% Poloxamer188, 0.5-10wt% polydimethylsiloxane and 1.0-2.5wt% acetic acid buffer are mixed and dissolved to form the above-mentioned acid bioglue Comes with thermosensitive gel.

[0073] In another preferred embodiment of the present invention, 0.6-10wt% wetting agent and 0.1-10wt% preservative can also be added.

[0074] liquid preparation

[0075] In view of the above-mentioned characteristics of the acidic bioadhesive thermosensitive gel provided by the present invention, it can be used to prepare a liquid preparation, and the liquid preparation contains: (i) the acidic bioadhesive thermosensitive gel provided by the present invention ...

Embodiment 1

[0113] Preparation of acidic bioadhesive thermosensitive gels

[0114] Put 19.5 kilograms of Poloxamer127 (purchased from Shanghai Changwei Pharmaceutical Excipient Technology Co., Ltd.) and 8 kilograms of F68 (purchased from Shanghai Changwei Pharmaceutical Excipient Technology Co., Ltd.) Stir well at 25°C and stir at 100-300rpm to make it completely dissolve. The process takes about 3-4 hours. After finishing, add 0.5L polydimethylsiloxane (purchased from Shanghai Yangjia Economic and Trade Development Co., Ltd.) and stir for 1 ~2 hours, let it stand overnight, centrifuge for 15 minutes, and remove air bubbles. Measure the pH and viscosity of the gel.

[0115] Results: The pH was 3.5, and the viscosity measured by NDJ-1 rotary viscometer (purchased from Shanghai Hengping Instrument Factory) was 11-22 Pa·s.

Embodiment 2

[0117] Preparation of acidic bioadhesive thermosensitive gels

[0118] Put 18.5 kilograms of Poloxamer127 (purchased from Shanghai Changwei Pharmaceutical Excipient Technology Co., Ltd.) and 10 kilograms of F68 (purchased from Shanghai Changwei Pharmaceutical Excipient Technology Co., Ltd.) Stir well at 25°C and stir at 100-300rpm to make it completely dissolve. The process takes about 3-4 hours. After finishing, add 0.5L polydimethylsiloxane (purchased from Shanghai Yangjia Economic and Trade Development Co., Ltd.) and stir for 1 ~2 hours, let it stand overnight, centrifuge for 15 minutes, and remove air bubbles. Measure the pH and viscosity of the gel.

[0119] Results: The pH was 3.7, and the viscosity measured by NDJ-1 rotary viscometer (purchased from Shanghai Hengping Instrument Factory) was 11-22 Pa·s.

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Abstract

The invention discloses acidic biologic adhesion heat-variable gelling agent, which includes (a) 12-20 wt percent of polyoxy ethylene polyoxy propylene polymer, (b) 0.5-10wt percent of polydimethyl siloxane and (c) 1.0-2.5 wt percent of acidity buffering agent. The invention is characterized in that a pH value is 3.0 to 4.5, the gelling agent is under a liquid state at the temperature less than and equal to 28 DEG C, and is under a gel state at the temperature more than and equal to 32 DEG C. The acidic biologic adhesion heat-variable gelling agent is used to prepare liquid preparation with the function of both contraception and preventative spread disease (STDs / HIV). The acidic biologic adhesion heat-variable gelling agent provides reformation and convenience for a production process, the loading and filling operation of the liquid medicine is convenient, the filling amount is accurate, and the invention particularly is suitable for GMP scale production and becomes an optimal substitute of a contraceptive sheath or lubricating additive.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to a pharmaceutical excipient gel and its preparation method and application. Background technique [0002] Gels have been used clinically for several years. At first, they were mostly prepared in small quantities for hospital preparations. Due to the continuous expansion of the application range and the continuous improvement of industrial production levels in recent years, more varieties of gels have been mass-produced. The requirement for commercially available gels is to keep the gel shape at room temperature without drying or liquefying. [0003] For example, there is a commercially available vaginal pH control gel, Aci-Jel™ (Ortho-McNeil Pharmaceutical Corp., Raitan, NJ), which is a water dispersible buffered gel with a pH of 3.9-4.1 and is used to restore And maintain normal vaginal acidity. It becomes a gel no matter in the normal temperature outside the body or in the temperature ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/34A61K47/36A61K9/00A61K45/00A61K31/085A61P15/02A61P15/18A61P31/00
Inventor 李卫华王健王强毅丁训诚
Owner 上海市生物医药技术研究院
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