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Tenofovir disoproxil fumarate tablet that is easy to dissolve and preparation method thereof

A technology of tenofovir fumarate and disoproxil, which is applied in the directions of non-active ingredient medical preparations, active ingredients-containing medical preparations, pharmaceutical formulas, etc., can solve the problem of reducing the biological activity of new drug compounds. Affecting drug absorption and metabolism process, unfavorable to bioavailability and other problems, to achieve the effect of improving bioavailability, efficient and fast process, and uniform size

Active Publication Date: 2019-02-05
SHANDONG WEIFANG PHARMA FACTORY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Oral tablets control product quality through dissolution. Tenofovir disoproxil fumarate tablets have relatively large specifications, and each tablet contains 300 mg of the main drug. The viscosity of the main drug is relatively high, resulting in a low dissolution rate of the final product. Reduces the selection of biological activity of new drug compounds, which is not conducive to improving bioavailability and poor clinical efficacy
Different preparation methods of the same pharmaceutical preparation may have significant differences in the dissolution rate of the drug, which will affect the absorption and metabolism process of the drug in the body, so that its bioavailability may also have significant differences

Method used

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  • Tenofovir disoproxil fumarate tablet that is easy to dissolve and preparation method thereof
  • Tenofovir disoproxil fumarate tablet that is easy to dissolve and preparation method thereof
  • Tenofovir disoproxil fumarate tablet that is easy to dissolve and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Using fluidized bed granulation and tableting process:

[0035]Preparation method: weigh tenofovir disoproxil fumarate, lactose, pregelatinized starch, microcrystalline cellulose, croscarmellose sodium, magnesium stearate, Cellactose80, tenofovir fumarate Fovir dipivoxil, lactose, pregelatinized starch, and microcrystalline cellulose are passed through a 100-mesh sieve, croscarmellose sodium is passed through a 80-mesh sieve, and magnesium stearate is passed through a 60-mesh sieve. Mix tenofovir disoproxil fumarate, lactose, pregelatinized starch, microcrystalline cellulose and croscarmellose sodium added inside, and prepare in a fluidized bed with water as a wetting agent Granules, the air inlet temperature is controlled at 45°C to 55°C. After granulation, add additional croscarmellose sodium Cellactose80 and magnesium stearate to mix evenly, detect the content of the intermediate, and determine the tablet weight according to the content, and adjust the tableting pre...

Embodiment 2

[0037] Using fluidized bed granulation and tableting process:

[0038] Preparation method: weigh tenofovir disoproxil fumarate, lactose, pregelatinized starch, microcrystalline cellulose, croscarmellose sodium, magnesium stearate, Cellactose80, tenofovir fumarate Fovir dipivoxil, lactose, pregelatinized starch, and microcrystalline cellulose are passed through a 100-mesh sieve, croscarmellose sodium is passed through a 80-mesh sieve, and magnesium stearate is passed through a 60-mesh sieve. Mix tenofovir disoproxil fumarate, lactose, pregelatinized starch, microcrystalline cellulose and croscarmellose sodium added inside, and prepare in a fluidized bed with water as a wetting agent Granules, the air inlet temperature is controlled at 45°C to 55°C. After granulation, add additional croscarmellose sodium Cellactose80 and magnesium stearate to mix evenly, detect the content of the intermediate, and determine the tablet weight according to the content, and adjust the tableting pr...

Embodiment 3

[0040] Using fluidized bed granulation and tableting process:

[0041] Preparation method: weigh tenofovir disoproxil fumarate, lactose, pregelatinized starch, microcrystalline cellulose, croscarmellose sodium, magnesium stearate, Cellactose80, tenofovir fumarate Fovir dipivoxil, lactose, pregelatinized starch, and microcrystalline cellulose are passed through a 100-mesh sieve, croscarmellose sodium is passed through a 80-mesh sieve, and magnesium stearate is passed through a 60-mesh sieve. Mix tenofovir disoproxil fumarate, lactose, pregelatinized starch, microcrystalline cellulose and croscarmellose sodium added inside, and prepare in a fluidized bed with water as a wetting agent Granules, the air inlet temperature is controlled at 45°C to 55°C. After granulation, add additional croscarmellose sodium Cellactose80 and magnesium stearate to mix evenly, detect the content of the intermediate, and determine the tablet weight according to the content, and adjust the tableting pr...

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Abstract

The invention belongs to the technical field of medicinal preparations and in particular relates to readily soluble tenofovir disoproxil fumarate tablets and a preparation method thereof. The readily soluble tenofovir disoproxil fumarate tablets are prepared by taking tenofovir disoproxil fumarate as a raw material and a pharmaceutically acceptable auxiliary component as an auxiliary material, and adopting a fluidized bed granulation tabletting process and a wet activity dry granulation tabletting process, wherein the auxiliary material comprises microcrystalline cellulose, pregelatinized starch, lactose, crosslinking carboxymethyl cellulose sodium, Cellactose 80 and magnesium stearate. The readily soluble tenofovir disoproxil fumarate tablets provided by the invention have the advantages of relatively good intermediate fluidity, mellow and full granules, uniform size, high dissolution rate and the like, and can obviously improve the dissolution rate of a medicament in water, and by virtue of significantly improving the dissolution rate of the medicament, the biological utilization degree of an oral administration medicament is improved.

Description

(1) Technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to a tenofovir disoproxil fumarate tablet which is easy to dissolve and a preparation method thereof. (2) Background technology [0002] Tenofovir disoproxilfumarateTDF (Viread) is a new type of nucleotide reverse transcriptase inhibitor developed by Gilead, which was approved by the US FDA in October 2001 and 2008 for the treatment of AIDS and Chronic hepatitis B (CHB) in adults. At present, more than 100 countries including China have approved TDF for the treatment of AIDS, and more than 30 countries and regions including the United States have obtained indications for TDF to treat CHB. [0003] Tenofovir disoproxil fumarate (English name: Tenofovir disoproxil fumarate, abbreviation: TDF or TFV DF) is the ester precursor of tenofovir (tenofovir), which is quickly hydrolyzed into tenofovir after oral administration , and is phosphorylated by cellular kinas...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K31/675A61K47/38A61K47/32A61K47/26A61P31/20A61P31/18
Inventor 李昕皓王在利冉东升王淑霞
Owner SHANDONG WEIFANG PHARMA FACTORY
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