Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

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
View PDF2 Cites 3 Cited by
  • 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 metabolite, tenofovir diphosphate, which Competing with 5'-deoxyadenosine triphosphate to participate in the synthesis of HIV and HBV viral DNA, after entering the viral DNA, DNA elongation is hindered due to the lack of 3'-OH

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • 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.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com