Tenofovir dipivoxil fumarate capsule and preparation method thereof

A technology of tenofovir fumarate and dipyrfurate, which is applied in the field of medicine, can solve the problems of blocked DNA extension and achieve the effect of simple and easy process, high bioavailability and remarkable drug effect

Active Publication Date: 2014-01-29
FUJIAN COSUNTER PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The main mechanism of action of tenofovir disoproxil fumarate is that it is hydrolyzed to tenofovir after oral administration, and tenofovir is phosphorylated by cellular kinases to produce a pharmacologically active metab

Method used

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  • Tenofovir dipivoxil fumarate capsule and preparation method thereof
  • Tenofovir dipivoxil fumarate capsule and preparation method thereof
  • Tenofovir dipivoxil fumarate capsule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Take 300 g of tenofovir disoproxil fumarate, 55 g of lactose, 20 g of microcrystalline cellulose, 1 g of micropowdered silica gel, and 4 g of magnesium stearate, and fill them into hollow capsules.

[0058] The preparation method of above-mentioned tenofovir disoproxil fumarate capsules comprises the following process steps:

[0059] (1) Weigh the above mass parts of tenofovir disoproxil fumarate, lactose, microcrystalline cellulose, and micropowder silica gel and pass through an 80-mesh sieve;

[0060] (2) Put the sieved tenofovir disoproxil fumarate, lactose, microcrystalline cellulose, and micropowder silica gel in an oven, and dry at 85-90°C for 4 hours;

[0061] (3) Mix lactose, microcrystalline cellulose and micropowder silica gel evenly, and then mix tenofovir disoproxil fumarate with it;

[0062] (4) Use a dry granulator for dry granulation, pass the obtained granules through a 100-mesh sieve, and collect 20-60 mesh dry granules;

[0063] (5) After re-crushing...

Embodiment 2

[0067] Take 300 g of tenofovir disoproxil fumarate, 50 g of lactose, 25 g of microcrystalline cellulose, 1.5 g of micropowdered silica gel, and 3 g of magnesium stearate, and fill them into hollow capsules. 1000 tenofovir disoproxil fumarate capsules can be prepared, and each capsule contains 300 mg of active ingredient tenofovir disoproxil fumarate. All the other are with embodiment 1.

Embodiment 3

[0069] Get tenofovir disoproxil fumarate 300g, lactose 60g, microcrystalline cellulose 15g, micropowder silica gel 2g, magnesium stearate 4g, fill into hollow capsules. 1000 tenofovir disoproxil fumarate capsules can be prepared, and each capsule contains 300 mg of active ingredient tenofovir disoproxil fumarate. All the other are with embodiment 1.

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Abstract

The invention relates to the field of medicines, and particularly relates to a tenofovir dipivoxil fumarate capsule and a preparation method thereof. The capsule disclosed by the invention is prepared from the following components in parts by mass: 300 parts of tenofovir dipivoxil fumarate, 40-60 parts of milk sugar, 10-40 parts of microcrystalline cellulose, 0.5-2 parts of superfine silica powder and 2-5 parts of magnesium stearate, which are filled into 1000 empty capsules.

Description

technical field [0001] The invention relates to the field of medicine, more specifically, to tenofovir disoproxil fumarate capsules and a preparation method thereof. Background technique [0002] Tenofovir disoproxil fumarate, chemical name 9-((R)-2-(bis(isopropoxycarbonyl)oxy(methoxy)phosphinyl)-propyl)adenine rich Maleate, its chemical structural formula is as follows: [0003] [0004] Tenofovir disoproxil fumarate (Tenofovir disoproxil fumarate) is an ester prodrug of tenofovir, which is a 5'-monophosphate nucleotide, which can inhibit HIV-1, HIV-2 and liver Replication of DNA viruses, the first nucleotide reverse transcriptase inhibitor licensed in the United States and Europe for the treatment of HIV infection. The main mechanism of action of tenofovir disoproxil fumarate is that it is hydrolyzed to tenofovir after oral administration, and tenofovir is phosphorylated by cellular kinases to produce a pharmacologically active metabolite, tenofovir diphosphate, which...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K31/675A61K47/38A61P1/16A61P31/20A61P31/18
Inventor 陈国华杨喜鸿林心镇苏葳张燕华陈仕魁
Owner FUJIAN COSUNTER PHARMA
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