Salt compound of tenofovir disoproxil fumarate and preparation method and medicinal application thereof

A technology of tenofovir disoproxil and phosphoric acid, which is applied in the field of medicine and can solve problems such as differences in bioavailability

Active Publication Date: 2010-07-21
FUJIAN COSUNTER PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Different crystalline forms of the same drug may have significantly different bioavailability

Method used

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  • Salt compound of tenofovir disoproxil fumarate and preparation method and medicinal application thereof
  • Salt compound of tenofovir disoproxil fumarate and preparation method and medicinal application thereof
  • Salt compound of tenofovir disoproxil fumarate and preparation method and medicinal application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1. New crystal form of tenofovir disoproxil phosphate and its preparation

[0036] In a 50ml reaction bottle, add 2.0g of tenofovir disoproxil and 20.0ml of isopropanol, heat to 50°C, stir, add phosphoric acid dropwise to the solution pH2-3, drop it, react for 30min, cool to 0°C and place for 8hr, Suction filtration to obtain a white crystalline powder, washed twice with a small amount of isopropanol, and vacuum-dried to obtain the new crystal form of tenofovir disoproxil phosphate of the present invention.

[0037] Its X-ray diffraction diagram, infrared absorption spectrum diagram and differential thermal analysis diagram are shown in the appendix figure 1 , 2 and 3.

Embodiment 2

[0038] Embodiment 2. tenofovir disoproxil phosphate tablet

[0039] Prescription: 300 g of the new crystal form of tenofovir disoproxil phosphate of the present invention, 100 g of hydroxypropyl cellulose, and 50 g of sodium carboxymethyl starch.

[0040] Preparation method: The above-mentioned two kinds of materials were crushed through 100 mesh respectively, dried under reduced pressure at 100°C for more than 10 hours, cooled to room temperature, mixed with the new crystal form of tenofovir disoproxil phosphate, granulated by a dry granulator, and pressed into 1000 tablets, that is.

Embodiment 3

[0041] Example 3. Tenofovir Disoproxil Phosphate Capsules

[0042] Prescription: 300g of the new crystal form of tenofovir disoproxil phosphate of the present invention, 65g of lactose, 70g of microcrystalline cellulose, 15g of sodium carboxymethyl starch, and 1.5g of magnesium stearate.

[0043] Preparation method: the above-mentioned lactose, microcrystalline cellulose, and sodium carboxymethyl starch were respectively crushed through 100 meshes, dried under reduced pressure at 100°C for more than 10 hours, cooled to room temperature, and mixed evenly with the new crystal form of tenofovir disoproxil phosphate , granulated by a dry granulator, added magnesium stearate, mixed evenly, filled into 1000 empty capsules, and obtained tenofovir disoproxil phosphate capsules.

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Abstract

The invention relates to a salt compound of tenofovir disoproxil fumarate and a preparation method and medicinal application thereof. The preparation method comprises the following steps: heating to dissolve the tenofovir disoproxil fumarate with isopropanol in an amount which is 5 to 20 times the weight of the tenofovir disoproxil fumarate, stirring, regulating pH with phosphoric acid to between 2 and 3, and performing reaction for 30 minutes; and cooling to 0 DEG C, standing for crystallization, filtering, washing twice with a small amount of isopropanol, and performing vacuum drying.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to a new salt compound of tenofovir disoproxil, its preparation method and pharmaceutical application, specifically the phosphate and new crystal form of tenofovir disoproxil, its preparation method and pharmaceutical application . technical background [0002] Tenofovir disoproxil, usually tenofovir disoproxil fumarate, is a drug used to treat HIV and HBV infections. Its pharmacology and toxicology are similar to those of nucleoside reverse transcriptase inhibitors. Inhibits reverse transcriptase, thereby possessing potential anti-HIV-1 activity. Tenofovir bisphosphate, the active ingredient of tenofovir, can inhibit viral polymerase by directly competitively binding to natural deoxyribose substrates, and terminate the chain by inserting into DNA. Pharmacokinetics: Tenofovir is almost not absorbed through the gastrointestinal tract, so it undergoes esterification and salt formation to becom...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/6561A61K31/675A61P31/18A61P31/20
Inventor 康惠燕陈国华
Owner FUJIAN COSUNTER PHARMA
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