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Gossypol or liquid preparation of analogue thereof and preparation method and use thereof

A technology for liquid preparations and analogs, which can be used in non-active ingredients medical preparations, antiviral agents, drug combinations, etc., and can solve the problems of large-scale production difficulty, viscosity, and difficulty in accurate loading

Active Publication Date: 2008-12-24
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, at present, all gels remain colloidal 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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  • Gossypol or liquid preparation of analogue thereof and preparation method and use thereof
  • Gossypol or liquid preparation of analogue thereof and preparation method and use thereof
  • Gossypol or liquid preparation of analogue thereof and preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0089] Preparation of gossypol acid thermosensitive gel (liquid preparation I)

[0090] 18 kilograms of Poloxamer127 (purchased from Shanghai Changwei Pharmaceutical Excipient Technology Co., Ltd.) and 0.65 kilograms of F68 (purchased from Shanghai Changwei Pharmaceutical Excipient Technology Co., Ltd.) were placed in the stirrer, and 60 liters of 0.4M acetate buffer was added. Stir well at 25°C and stir at a speed of 100-300rpm to dissolve completely. The process takes about 3-4 hours. After completion, add 0.8 kg of pure gossypol, 10 liters of glycerin, 0.5 liters of polydimethylsiloxane and 0.1 liters of Benzoic acid (purchased from Shanghai Changwei Pharmaceutical Excipient Technology Co., Ltd.), stirred for another 1-2 hours, left to stand overnight, and centrifuged for 15 minutes to remove air bubbles. Finally, a total of 100 liters of this product was prepared with 0.4M acetic acid buffer. The pH and viscosity of the gel were measured (room temperature 23-25°C).

[00...

Embodiment 2

[0093] Preparation of 8-benzoyl-1,4-benzoquinone acidic thermosensitive gel (liquid preparation II)

[0094] 19.2 kilograms of Poloxamer127 (purchased from Shanghai Changwei Pharmaceutical Excipient Technology Co., Ltd.) and 0.5 kilograms of F68 (purchased from Shanghai Changwei Pharmaceutical Excipient Technology Co., Ltd.) were placed in the stirrer, and 60 liters of 0.2M acetate buffer was added. Stir well at 25°C and stir at 100-300rpm to dissolve completely. The process takes about 3-4 hours. After completion, add 0.2 kg of 8-benzoyl-1,4-benzoquinone, 10 liters of glycerin, and 0.5 liters of polydimethyl Siloxane and 0.1 liter of benzoic acid (purchased from Shanghai Changwei Pharmaceutical Excipient Technology Co., Ltd.), were stirred for 1-2 hours, left standing overnight, and centrifuged for 15 minutes to remove air bubbles. Finally, a total of 100 liters of this product was prepared with 0.2M acetic acid buffer. Measure the pH and viscosity of the gel.

[0095] The ...

Embodiment 3

[0097] Preparation of 8-benzoyl-1,4-phenol acid thermosensitive gel (liquid formulation III)

[0098] Put 18.5 kg of Poloxamer127 (purchased from Shanghai Changwei Pharmaceutical Excipient Technology Co., Ltd.) and 0.5 kg of Bohm 934P (Carbopol) (purchased from Shanghai Changwei Pharmaceutical Excipient Technology Co., Ltd.) into a stirrer, add 60 liters of 0.4M acetic acid buffer solution, stir well at 23-25°C, stirring speed 100-300rpm, to make it completely dissolved, the process is about 3-4 hours, after that, add 0.28 kg 8-benzoyl-1,4-phenol, 10 liters of glycerin, 0.5 liters Polydimethylsiloxane and 0.1 liter of benzoic acid (purchased from Shanghai Changwei Pharmaceutical Excipient Technology Co., Ltd.), stirred for 1-2 hours, left standing overnight, and centrifuged for 15 minutes to remove air bubbles. Finally, a total of 100 liters of this product was prepared with 0.4M acetic acid buffer. Measure the pH and viscosity of the gel.

[0099] The resulting pH was 3.5. ...

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Abstract

The invention discloses liquid preparation with gossypol or other analogs. The liquid preparation contains (a) 0.01to 10 weight percent of gossypol or other analogs; (b)12 to 20 weight percent of polyoxypropylene polymer, alginic acid or chitosan; (c) 0.5 to 10 weight percent of poly (dimethylsiloxane), poly (dimethylsiloxalkanol) or dimethylsiloxalkyl ether polymer; and (d) 1.0 to 2.5 weight percent of acidic buffering agent. The invention also discloses a preparation method and usage of the liquid preparation.

Description

technical field [0001] The invention relates to a pharmaceutical preparation, in particular to a liquid preparation of gossypol or its analogues, a preparation method and application thereof. Background technique [0002] Gossypol is a yellow polyphenolic toxic compound contained in the roots, stems and seeds of the Malvaceae plant cotton. The chemical structure of gossypol is 8,8'-dialdehyde-1,1,6,6'7,7'-hexahydroxy-5,5'-diisopropyl-3,3'-dimethyl- 2,2'-binaphthalene, as shown in formula 1: [0003] [0004] Formula 1 [0005] Gossypol has a sperm-inhibiting effect, but gossypol has effects on certain functions of the human or animal body. For example, gossypol may induce primary hypothyroidism; it can reduce serum motilin levels in mice and inhibit weight gain; it can reduce serum potassium and increase urinary potassium in patients with hypokalemia; some people who take gossypol After taking 0.5-4.5 years, there is still no sperm in the semen or the sperm in the sem...

Claims

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Application Information

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IPC IPC(8): A61K31/11A61K9/00A61K47/34A61K47/36A61P15/00A61P15/18A61P31/12A61P35/00A61P37/06A61K47/10
Inventor 李卫华吴国沛刘颖王健王玉柱丁训诚
Owner 上海市生物医药技术研究院
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