Gel matrix having bioadhesion and favorable biocompatibility, and preparation method and application thereof

A technology of biocompatibility and gel matrix, which is applied in the field of medicine, can solve the problems of misoprostol's unstable chemical properties, difficulty in controlling the dosage, and damage to the shape of suppositories, so as to achieve good biocompatibility and improve bioavailability degree, increase the effect of stability

Inactive Publication Date: 2017-05-17
CHUXIONG MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The disadvantage of this kind of medication is that some early pregnant women have adverse reactions such as mild nausea, vomiting, dizziness, fatigue, and lower abdominal pain after taking the tablet orally, and ordinary tablets are used in the vagina, and there is disintegration of the tablet, release and absorption of the drug. , resulting in its curative effect is not as good as suppositories and gels, and the dosage is not easy to control
According to information, there is currently a patent for misoprostol suppositories in China, but due to the melting properties of suppositories, the shape of suppositories may be destroyed when the room temperature is high in summer. The temperature is easily decomposed and destroyed. When preparing a suppository, it is necessary to heat the oil to a molten state, then cool it to 30-50°C under stirring, add the misoprostol drug, stir and mix evenly, and then fill the mold and cool it. Misoprostol is easily decomposed and destroyed at 30-50°C

Method used

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  • Gel matrix having bioadhesion and favorable biocompatibility, and preparation method and application thereof
  • Gel matrix having bioadhesion and favorable biocompatibility, and preparation method and application thereof

Examples

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preparation example Construction

[0023] The preparation method of the misoprostol pharmaceutical composition is to add the misoprostol-hydroxypropyl cellulose solid dispersion to the gel matrix with bioadhesion and good biocompatibility according to the formula ratio , grind and mix to obtain uniformity.

[0024] The preparation of the misoprostol pharmaceutical composition of the present invention is prepared into tablet, capsule, powder, granule, pill, gel by adding pharmaceutically acceptable adjuvants in the misoprostol pharmaceutical composition Potions and suppositories.

[0025] The present invention will be further described below with specific implementation case:

[0026] Misoprostol-hydroxypropyl methylcellulose solid dispersion (the mass ratio of misoprostol and hydroxypropyl methylcellulose is 1 to 99) and misoprostol reference substance in the embodiment of the present invention, by Purchased from Beijing Zhongxi Yuanda Technology Co., Ltd.; polyethylene glycol (PEG) 4000, polyethylene glycol ...

Embodiment 1

[0028] This example is to prepare a composition containing 0.1%-1% misoprostol-hypromellose and gel matrix.

[0029] The prescription composition of the gel base is: polyethylene glycol 400 (80g), polyethylene glycol 4000 (10g), glycerin 9.4g, 5% ethylparaben alcohol solution 0.6g, a total of 100g.

[0030] The preparation method of the gel matrix is ​​as follows: weigh polyethylene glycol 400, polyethylene glycol 4000, and glycerin respectively, mix them and heat them on a water bath, wait until the polyethylene glycol 4000 is completely dissolved and the solution is clear, stop heating, and keep stirring until Condensate to form a gel, add 5% ethylparaben alcohol solution and stir evenly to obtain a blank gel matrix.

[0031] The preparation method of the composition of misoprostol and gel base is as follows: add misoprostol-hydroxypropyl methylcellulose solid dispersion to the above gel base, fully grind and mix evenly, and obtain the medicine containing misoprostol of gel...

Embodiment 2

[0033] This example is to prepare a composition containing 0.1%-1% misoprostol-hypromellose and gel matrix.

[0034] The prescription composition of the gel base is: polyethylene glycol 400 (70g), polyethylene glycol 4000 (20g), glycerin 9.4g, 5% ethylparaben alcohol solution 0.6g, a total of 100g.

[0035] The preparation method of the gel matrix is ​​as follows: weigh polyethylene glycol 400, polyethylene glycol 4000, and glycerin respectively, mix them and heat them on a water bath, wait until the polyethylene glycol 4000 is completely dissolved and the solution is clear, stop heating, and keep stirring until Condensate to form a gel, add 5% ethylparaben alcohol solution and stir evenly to obtain a blank gel matrix.

[0036] The preparation method of the composition of misoprostol and gel base is as follows: add misoprostol-hydroxypropyl methylcellulose solid dispersion to the above gel base, fully grind and mix evenly, and obtain the medicine containing misoprostol of gel...

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Abstract

The invention discloses a gel matrix having bioadhesion and favorable biocompatibility, and a preparation method and application thereof. The gel matrix having bioadhesion and favorable biocompatibility comprises the following components in parts by weight: 60-90 parts of polyethyleneglycol 400, 0-20 parts of polyethyleneglycol 1000, 3-8 parts of polyethyleneglycol 4000, 7-12 parts of glycerol and 0.4-0.8 part of 5% ethylparaben alcohol solution. The preparation method comprises the following steps: mixing polyethyleneglycol 400, polyethyleneglycol 1000, polyethyleneglycol 4000 and glycerol conforming to the formula, heating on a water bath until completely dissolving, stopping heating, stirring until condensing to form a gel, adding 5% ethylparaben alcohol solution conforming to the formula, and uniformly mixing. The application refers to application of the gel matrix having bioadhesion and favorable biocompatibility in preparation of a medicinal composition with improved bioavailability and curative effect. The gel matrix disclosed by the invention has bioadhesion and favorable biocompatibility; and medicine can adhere to a vaginal mucosa to be slowly dispersed from the gel to the mucosa, thereby improving the bioavailability and curative effect of the medicine.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a gel matrix with bioadhesion and good biocompatibility, its preparation method and application. Background technique [0002] Misoprostol is a chemically synthesized derivative of prostaglandin E1, which can inhibit gastric acid secretion, protect gastric mucosa and have obvious contraction effect on pregnant uterus. peptic ulcer induced by anti-inflammatory drugs. At present, misoprostol is the most widely used in gynecology. It is mainly used in combination with mifepristone sequentially. It is administered orally to terminate early pregnancy within 49 days of menopause. The dosage is 36-48 days after taking mifepristone. Hours later, take a single fasting misoprostol tablet 0.6 mg or place the tablet 0.2 mg in the vagina. In addition, clinically, the softening and dilating of the cervix can relieve the pain of postmenopausal women undergoing artificial abortion...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K31/5575A61K47/10A61K47/14A61P1/04A61P15/04
CPCA61K9/06A61K9/0034A61K31/5575A61K47/10A61K47/14
Inventor 陆鸿奎张荷兰李蓉邹云川李新林
Owner CHUXIONG MEDICAL COLLEGE
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