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Emtricitabine and tenofovir medicine composition

A technology of emtricitabine and tenofovir fumarate, applied in the field of medicine, can solve the problems of easy degradation, high viscosity, affecting drug dissolution, etc.

Active Publication Date: 2019-09-20
海思科制药(眉山)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In addition, the study found that emtricitabine has good solubility, but its viscosity is relatively large after dissolution. Emtricitabine prepared by conventional tablet preparation process dissolves slowly, and the dissolution decreases after long-term storage.
Emtricitabine is highly viscous when it meets water, and it is easy to form a thin film on the surface of the drug to prevent the entry of water molecules. It is difficult for the disintegrant to work quickly, resulting in slow disintegration of the tablet, which in turn affects the dissolution of the drug.
Tenofovir disoproxil fumarate is unstable in contact with water and heat, and is easy to degrade. If the excipients used in the preparation of tablets are improperly selected and the preparation process is unreasonable, the stability of the tablet and the release of active ingredients will be affected.

Method used

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  • Emtricitabine and tenofovir medicine composition
  • Emtricitabine and tenofovir medicine composition
  • Emtricitabine and tenofovir medicine composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030]

[0031] Preparation method: Isopropanol is used as a granulation wetting agent, removed during the drying process, and floats within the range of 80% to 120% of the theoretical value according to specific conditions during the soft material production process. Special requirements for production environment: The following production environments require relative humidity below 50%. Disperse tenofovir disoproxil fumarate through a 40-mesh sieve for later use; crush emtricitabine and pass through an 80-mesh sieve for later use; dry mannitol at 85±5°C until the water content is less than 0.5 %, dry pregelatinized starch and croscarmellose sodium at 90±5°C until the moisture is less than 1.5%; dry magnesium stearate at 70±5°C until the moisture is less than 2.5%, and set aside; Starch, croscarmellose sodium, emtricitabine, tenofovir disoproxil fumarate, and mannitol were put into a multi-directional motion mixer and mixed to obtain a premixed medicinal powder. Put the ...

Embodiment 2

[0032] Example 2 (prepared with reference to comparative document CN1738628A)

[0033]

[0034]

[0035] Preparation method: Purified water is used as a granulation wetting agent, removed during the drying process, and floats within the range of 80% to 120% of the theoretical value according to specific conditions during the soft material production process. Special requirements for production environment: The following production environments require relative humidity below 50%. Disperse tenofovir disoproxil fumarate through a 40-mesh sieve for subsequent use; pulverize emtricitabine and pass through an 80-mesh sieve for subsequent use; mix lactose monohydrate, pregelatinized starch, microcrystalline cellulose and Sodium carboxymethyl cellulose is dried at 90±5°C until the water content is less than 1.5%; magnesium stearate is dried at 70±5°C until the water content is less than 1.5%, and it is ready for use; croscarmellose sodium, emtricitabine, Put tenofovir disoprox...

Embodiment 3

[0037] Get the sample prepared according to Examples 1-2 and the original research product, according to the dissolution assay method (Chinese Pharmacopoeia 2015 edition four general rules 0931 second method), the dissolution comparative results in the hydrochloric acid solution of 900ml 0.01mol / L are shown in Table 1 ~2.

[0038] Emtricitabine dissolution curve result in the present invention and commercially available product Truvada in table 1

[0039]

[0040] Table 2 Dissolution curve results of tenofovir disoproxil in the present invention and commercially available product Truvada

[0041]

[0042]

[0043] The results show that the present invention releases faster than the original research product, and has a faster dissolution advantage as an immediate release preparation.

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Abstract

The invention provides a stable emtricitabine and tenofovir medicine composition. The prepared medicine composition can effectively control degradation of effective components in the preparation and storage process, and the physical and chemical stability of medicines is improved. The invention further relates to a preparation method and an application of the medicine composition.

Description

technical field [0001] The invention relates to the field of medicine, in particular to an emtricitabine tenofovir pharmaceutical composition and a preparation method thereof. Background technique [0002] Emtricitabine and Tenofovir Disoproxil Tablets are compound preparations of emtricitabine and tenofovir disoproxil fumarate, each tablet contains 200mg emtricitabine and 300mg tenofovir Pifurate, trade name , developed by Gilead Sciences Inc. (Gilead Sciences Inc.), initially marketed in the United States in 2004, is suitable for use in combination with other antiretroviral drugs to treat HIV-1 infection in adults and children aged 12 and over , and was approved by the FDA on May 11, 2012 for pre-exposure prophylaxis in adults to reduce the risk of high-risk individuals acquiring HIV-1 infection through sexual transmission (prevention of HIV-1 infection). [0003] CN1738628A discloses the pharmaceutical composition of emtricitabine and tenofovir disoproxil fumarate, thi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K47/38A61K47/36A61K47/26A61K31/513A61K31/675A61P31/18
CPCA61K9/2866A61K9/2095A61K9/2059A61K9/2054A61K9/2018A61K31/513A61K31/675A61P31/18A61K2300/00
Inventor 周仕川江智勇李方群曾琴雷有成曹燕贾晓曼向志祥
Owner 海思科制药(眉山)有限公司
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