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Tenofovir microcapsule and preparation method thereof

A technology of tenofovir and microcrystalline cellulose, applied in the field of tenofovir microcapsules and preparation thereof, can solve the problems of insufficient absorption and utilization, difficult absorption of tenofovir, etc., and achieve good absorption and strong HBV The effect of copying, improving stability

Inactive Publication Date: 2019-08-30
南京望知星医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The technical problem to be solved by the present invention is that the existing tenofovir is not easy to be absorbed by the gastrointestinal tract, and cannot be optimally absorbed and utilized by the human body.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1: A tenofovir microcapsule, wherein tenofovir comprises the following components in a weight fraction ratio: R-propylene oxide: 56 parts, diethyl p-toluenesulfonyloxymethylphosphonate: 32 parts, adenine: 2 parts, bromotrimethylsilane: 12 parts, dimethoxyethoxy aluminum hydride: 7 parts;

[0022] Microcapsules include the following components in a weight fraction ratio: chitin: 22-25 parts, microcrystalline cellulose: 15 parts, sodium alginate: 14 parts, hydrolase: 3 parts, mercaptoacetic acid: 4-6 parts, Glucose: 6 parts, epichlorohydrin: 4 parts, oil phase: 3 parts, curing agent: 1 part, dispersant: 2 parts.

[0023] The preparation method of microcapsules is as follows:

[0024] Add chitin, microcrystalline cellulose and hydrolase in the above proportions to the reaction kettle, and heat to 30°C and stir for 7-9 minutes to obtain mixture A;

[0025] Add mixture A, sodium alginate and glucose into a stirring tank, heat to 45-50°C, stir for 25-28 minutes, and adjust t...

Embodiment 2

[0032] Example 2: A tenofovir microcapsule, which is different from Example 1 in that the tenofovir includes the following components in a weight fraction ratio: R-propylene oxide: 58 parts, p-toluenesulfonate Diethyl acyloxymethylphosphonate: 33.5 parts, adenine: 3 parts, bromotrimethylsilane: 13.5 parts, dimethoxyethoxy aluminum hydride: 8 parts.

[0033] The microcapsules include the following components in a weight fraction ratio: chitin: 23.5 parts, microcrystalline cellulose: 16 parts, sodium alginate: 15 parts, hydrolase: 4.5 parts, mercaptoacetic acid: 5 parts, glucose: 7 parts , Epichlorohydrin: 4.5 parts, oil phase: 6 parts, curing agent: 2 parts, dispersant: 2.5 parts.

Embodiment 3

[0034] Example 3: A tenofovir microcapsule, which is different from Example 1 in that the tenofovir includes the following components in a weight fraction ratio: R-propylene oxide: 60 parts, right Diethyl tosyloxymethylphosphonate: 35 parts, adenine: 4 parts, trimethylsilyl bromide: 15 parts, dimethoxyethoxy aluminum hydride: 9 parts.

[0035] The microcapsules include the following components in a weight fraction ratio: chitin: 25 parts, microcrystalline cellulose: 17 parts, sodium alginate: 16 parts, hydrolase: 6 parts, mercaptoacetic acid: 6 parts, glucose: 8 parts , Epichlorohydrin: 5 parts, oil phase: 9 parts, curing agent: 3 parts, dispersant: 3 parts.

[0036] After tests, the absorption rate of tenofovir on the market is 47-49%, and the absorption rate of tenofovir microcapsules in Examples 1 to 3 of the present invention reaches 57-59%, which is much improved, and Judging from the smell, the tenofovir of the present invention has a small odor, while the tenofovir on the m...

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PUM

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Abstract

The present invention discloses a tenofovir microcapsule and a preparation method thereof, and relates to the technical field of tenofovir. The tenofovir comprises the following components according to parts by weight: 56-60 parts of R-propylene oxide, 32-35 parts of diethyl p-toluenesulfonyloxymethylphosphonate, 2-4 parts of adenine, 12-15 parts of trimethyl bromo-silicane and 7-9 parts of dimethoxyethoxy aluminum hydride; and the microcapsule comprises the following components in parts by weight: 22-25 parts of chitin, 15-17 parts of microcrystalline cellulose, 14-16 parts of sodium alginate, 3-6 parts of hydrolase, 4-6 parts of thioglycolic acid, 6-8 parts of glucose, 4-5 parts of epichlorohydrin, 3-9 parts of an oil phase, 1-3 parts of a curing agent and 2-3 parts of a dispersing agent. The tenofovir capsule is improved in absorption rate and also relatively small in smell.

Description

Technical field [0001] The invention relates to the technical field of tenofovir microcapsules, in particular to a tenofovir microcapsule and a preparation method thereof. Background technique [0002] Tenofovir, the chemical name is (R)-{[2-(6-amino-9H-purin-9-yl)-1-methylethoxy]methyl}phosphonic acid, or (R)-9 -(2-phosphonomethoxypropyl) adenine, tenofovir disoproxil fumarate is a first-line antiviral drug for the treatment of HIV and HBV, tenofovir is the preparation of tenofovir fumarate The key intermediate of esters. The existing tenofovir is not easily absorbed by the gastrointestinal tract, and cannot achieve the purpose of being optimally absorbed and utilized by the human body. Summary of the invention [0003] The technical problem to be solved by the present invention is that the existing tenofovir is not easily absorbed by the gastrointestinal tract and cannot achieve the purpose of being optimally absorbed and utilized by the human body. [0004] In order to solve t...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K47/38A61K47/36A61K47/44A61K31/675A61P31/18A61P31/20C07F9/6561
CPCA61K9/5015A61K9/5036A61K9/5042A61K31/675A61P31/18A61P31/20C07F9/65616
Inventor 朱立中
Owner 南京望知星医药科技有限公司
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