Tenofovir disoproxil fumarate tablets allowing direct powder compression and preparation method thereof

A technology for tenofovir fumarate and pyrifurate tablets is applied in the field of tablets and their preparation, and can solve the problems of high viscosity of tenofovir disoproxil fumarate, unfavorable stability and impurity content, Affecting drug efficacy and other issues, achieving the effect of being suitable for industrial-scale operation, good dissolution, and small difference in tablet weight

Inactive Publication Date: 2014-06-04
ANHUI BIOCHEM BIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the wet instability caused by the structure of the main drug tenofovir disoproxil fumarate, wet granulation will inevitably have an adverse effect on its stability and impurity content, thereby affecting the efficacy of the drug.
Therefore, the powder direct compression method in the prior art will be the preferred method, but because the viscosity of tenofovir disoproxil fumarate itself is relatively large, so far no direct powder compression method has been adopted to prepare fumarate. Report on Tenofovir Disoproxil Tablets

Method used

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  • Tenofovir disoproxil fumarate tablets allowing direct powder compression and preparation method thereof
  • Tenofovir disoproxil fumarate tablets allowing direct powder compression and preparation method thereof
  • Tenofovir disoproxil fumarate tablets allowing direct powder compression and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment

[0027] Example general method:

[0028] (1) Weigh microcrystalline cellulose, talc and component A with a limited weight percentage and mix them uniformly to obtain a premixed auxiliary material.

[0029] (2) Add tenofovir disoproxil fumarate to the premixed excipients in several times. After each addition of the main drug should be mixed with the premixed excipients, continue to add the main drug until the main drug is added. Add all tenofovir disoproxil fumarate and mix well. After the end of the divided addition, a mixture was obtained.

[0030] (3) The mixture was placed in a ZP-35 II tableting machine, and the powder was directly compressed into 1000 tablets.

[0031] The whole process is done in a dry environment.

[0032] The prescription amounts of the main drug and the premixed adjuvant in each example are listed in Table 1 below.

[0033] Table 1—the prescription content (g) of main drug and premixed adjuvant in each embodiment

[0034]

[0035]

Embodiment 7

[0037] Example 7 is a comparative example with reference to the prior art, which is the wet granulation method described in US Pat. No. 5,935,946.

[0038] Main Drugs and Excipients:

[0039]

[0040] The preparation method includes the following steps:

[0041] (1) Take the stated amounts of tenofovir disoproxil fumarate, lactose monohydrate, pregelatinized starch, croscarmellose sodium and purified water.

[0042] (2) Mix tenofovir disoproxil fumarate, lactose monohydrate, pregelatinized starch, and croscarmellose sodium evenly, then add purified water to prepare soft materials, and use a 20-mesh sieve to wet-process After drying at 50°C for 5 hours, granulate with a 20-mesh sieve.

[0043] (3) Adding additional lactose monohydrate, croscarmellose sodium and magnesium stearate to the above dry granules, and mixing them uniformly to obtain a mixture.

[0044] (4) Put the mixture in a tablet press and press it into 1000 tablets.

[0045] Comparative Results

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Abstract

The invention relates to tenofovir disoproxil fumarate tablets and a preparation method thereof. The tablets mainly contain a main drug tenofovir disoproxil fumarate and a premixing accessory, wherein the premixing accessory is a mixture of uniformly mixed microcrystalline cellulose, talc powder and a component A, and the component A is aerosil or poloxamer 188. The preparation method provided by the invention effectively overcomes the defects of the prior art that the tenofovir disoproxil fumarate has relatively high viscosity and consequently the tablets are difficult to prepare by a direct powder compression method, thereby avoiding the degradation of tenofovir disoproxil fumarate by the moisture introduced in a preparation process of wet granulation in the prior art, and further improving the quality of the tablets. The prepared tablets have the advantages of little difference in tablet weight, moderate hardness, good dissolubility and low impurity content. Moreover, the production process of the tablets is simple and convenient to operate and suitable for industrial-scale production.

Description

technical field [0001] The invention relates to a tablet and a preparation method thereof, in particular to a tenofovir disoproxil fumarate tablet and a preparation method thereof. Background technique [0002] Tenofovir Disoproxil Fumarate is a water-soluble diester prodrug of Tenofovir, a new type of nucleotide reverse transcriptase inhibitor, which can inhibit the replication of HIV virus. Its main mechanism of action is that it is hydrolyzed into tenofovir after oral administration into the human body to exert its efficacy. Clinical data show that tenofovir disoproxil fumarate has significant anti-HIV efficacy and little toxicity to normal human cells, and is expected to become a first-line drug against HIV. [0003] At present, tenofovir disoproxil fumarate tablets (trade name: Viread) have been marketed in China, the United States, New Zealand, Australia, Canada, Turkey and other countries for the treatment of HIV infection. [0004] CN 102198110A discloses tenofovir...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/675A61K47/38A61P31/18
Inventor 邢怀阳沈蔡月车富强王贺崔颖王辉
Owner ANHUI BIOCHEM BIO PHARMA
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