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Tenofovir and preparation technology thereof

A tenofovir and capsule material technology, applied in the field of tenofovir and its preparation technology, can solve the problems of inability to absorb and utilize, and the tenofovir is not easily absorbed, and achieves improved absorption rate and high packaging stability. , the effect of prolonging the half-life

Inactive Publication Date: 2019-08-09
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

[0022] Embodiment 1: a kind of tenofovir, tenofovir comprises capsule material and capsule core, and wherein capsule core comprises the following components according to weight and number ratio: R-methyl lactate: 23 parts, adenine: 7 parts , diisopropyl-p-toluenesulfonyloxymethyl-phosphonate: 13 parts, sodium borohydride: 3 parts.

[0023] The capsule material includes the following components according to the ratio of parts by weight: glycerol phosphorylcholine: 17 parts, palmitic acid: 17 parts, sodium hydroxide: 2 parts, diisopropylethylamine: 4 parts, paraformaldehyde: 6 parts, acetic acid: 4 parts, polyacrylic acid resin: 7 parts, deionized water: 12 parts, absolute ethanol: 8 parts, surfactant: 3 parts, water-soluble dispersant: 4 parts, solvent: 5 parts.

[0024] Specifically, the surfactant includes a water-soluble anionic surfactant and a water-soluble nonionic surfactant, and the weight ratio of the water-soluble anionic surfactant to the water-soluble nonionic surfa...

Embodiment 2

[0032] Embodiment 2: A kind of tenofovir, differs from embodiment 1 in that tenofovir comprises capsule material and capsule core, and capsule core comprises the following components according to weight and number ratio: R-methyl lactate: 24 parts, adenine: 8 parts, diisopropyl-p-toluenesulfonyloxymethyl-phosphonate: 14 parts, sodium borohydride: 4 parts;

[0033] The capsule material includes the following components according to the ratio of parts by weight: glycerol phosphorylcholine: 18 parts, palmitic acid: 18 parts, sodium hydroxide: 2.5 parts, diisopropylethylamine: 5 parts, paraformaldehyde: 7.5 parts, acetic acid: 5.5 parts, polyacrylic acid resin: 8 parts, deionized water: 15.5 parts, absolute ethanol: 10 parts, surfactant: 5 parts, water-soluble dispersant: 5 parts, solvent: 7.5 parts.

Embodiment 3

[0034] Embodiment 3: A kind of tenofovir, differs from Example 1 in that tenofovir includes a capsule material and a capsule core, and the capsule core comprises the following components according to the ratio in parts by weight: R-methyl lactate: 25 parts, adenine: 9 parts, diisopropyl-p-toluenesulfonyloxymethyl-phosphonate: 15 parts, sodium borohydride: 5 parts;

[0035] The capsule material includes the following components according to the ratio of parts by weight: glycerol phosphorylcholine: 19 parts, palmitic acid: 19 parts, sodium hydroxide: 3 parts, diisopropylethylamine: 6 parts, paraformaldehyde: 9 parts, acetic acid: 7 parts, polyacrylic acid resin: 9 parts, deionized water: 19 parts, absolute ethanol: 12 parts, surfactant: 7 parts, water-soluble dispersant: 6 parts, solvent: 10 parts.

[0036] The tenofovir prepared by the invention is composed of a capsule core and a capsule material, which improves the physical properties of the tenofovir and is easy to be absorb...

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PUM

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Abstract

The invention discloses tenofovir and a preparation technology thereof, and relates to the technical field of the tenofovir. The tenofovir comprises a capsule wall material and a capsule core, whereinthe capsule core is prepared from, by weight, 23-25 parts of R-methyl lactate, 7-9 parts of adenine, 13-15 parts of diisopropyl-p-tosyloxymethylphosphonate and 3-5 parts of sodium borohydride; the capsule wall material is prepared from, by weight, 17-19 parts of choline glycerophosphate, 17-19 parts of palmitic acid, 2-3 parts of sodium hydroxide, 4-6 parts of ethyldiisopropylamine, 6-9 parts ofparaformaldehyde, 4-7 parts of acetic acid, 7-9 parts of polyacrylic resin, 12-19 parts of deionized water, 8-12 parts of absolute ethyl alcohol, 3-7 parts of a surface active agent, 4-6 parts of a water-soluble dispersing agent and 5-10 parts of a solvent. The tenofovir prepared by using the technology is composed of the capsule core and the capsule wall material, the physical properties of the tenofovir are improved, the tenofovir is easily absorbed by the human body, and therefore, the pharmaceutical effect of the tenofovir is improved.

Description

technical field [0001] The invention relates to the technical field of tenofovir, in particular to a tenofovir and a preparation process thereof. Background technique [0002] Tenofovir, chemical name (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, HBV, tenofovir is the preparation of tenofovir fumarate Key intermediates of esters. Oral administration and rectal administration are two common administration methods. The drug is absorbed by the stomach or rectal mucosa and enters the blood, and is transported to the whole body through blood circulation, so as to achieve the purpose of treating diseases. The existing tenofovir is not easy to Absorbed by the gastrointestinal tract, the purpose of optimal absorption and utilization by the human body cannot be achieved. Contents of the invention [0003] The technical prob...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K31/675A61K47/34A61K47/32A61P31/18A61P31/20C07F9/6561
CPCA61K9/5026A61K9/5031A61K31/675A61P31/18A61P31/20C07F9/65616
Inventor 朱立中
Owner 南京望知星医药科技有限公司
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