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A kind of antiretroviral pharmaceutical composition

A composition and drug technology, applied in the field of medicine, can solve the problems of water and heat instability, decreased dissolution, easy degradation, etc., and achieve the effects of increasing yield and drug loading, improving stability, and reducing degradation

Active Publication Date: 2020-02-14
ANHUI BIOCHEM BIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The study found that the direct contact of the three drugs would also lead to a significant drop in the content of tenofovir disoproxil fumarate during storage, affecting the therapeutic effect
[0007] The patent No. is that CN101222914A patent document also discloses this triple preparation Efeentretinol pharmaceutical composition and production method thereof, and points out to make emtricitabine and tenofovir DF stabilizer with dry granulation, wet granulation Prepare efavirenz granules and compress the two granules to solve the problems that wet granulation fails to produce chemically stable tablets, and dry granulation omits the low bioequivalence of surfactants
[0008] In addition, the study found that although emtricitabine is a soluble raw material, it is viscous after dissolution, which is easy to cause tablet adhesion. The phenomenon of decline
Because emtricitabine is highly viscous when it meets water, it is easy to form a thin film on the surface of the drug to prevent the entry of water molecules, and 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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  • A kind of antiretroviral pharmaceutical composition
  • A kind of antiretroviral pharmaceutical composition
  • A kind of antiretroviral pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Prescription: as shown in Table 1-2

[0030] The formula of table 1 efavirenz pellet

[0031] Element weight Efavirenz 600g Sodium dodecyl sulfate 25g microcrystalline cellulose 18g Croscarmellose sodium (additional) 48g

[0032] The formula of table 2 triple preparation

[0033]

[0034]

[0035] The preparation method is as follows:

[0036] (1) Preparation of tenofovir disoproxil fumarate-β-cyclodextrin inclusion compound (saturated aqueous solution method)

[0037] Weigh 300g of β-cyclodextrin in 1.8L water, stir to dissolve it, and make a saturated solution, weigh 300g of tenofovir disoproxil fumarate to the β-cyclodextrin saturated solution at a mass ratio of 1:1 , the stirring temperature was 35°C, and the stirring was continued for 4 h at a rotational speed of 1000 r / min. After cooling and standing for 2 h, the filtrate was dried to constant weight, and the obtained white substance was the desired clathrate.

[00...

Embodiment 2

[0045] Prescription: as shown in Table 3-4

[0046] The formula of table 3 efavirenz pellets

[0047]

[0048]

[0049] The formula of table 4 triple preparation

[0050] Element weight Efavirenz pellets about 700g Emtricitabine 200g tenofovir disoproxil fumarate 300g pregelatinized starch 130g Croscarmellose sodium (externally added) 40g Magnesium stearate 20g Micropowder silica gel 12g β-cyclodextrin 300g

[0051] (1) Preparation of tenofovir disoproxil fumarate-β-cyclodextrin inclusion compound (saturated aqueous solution method)

[0052] Weigh 300g of β-cyclodextrin in 1.8L water, stir to dissolve it, and make a saturated solution, weigh 300g of tenofovir disoproxil fumarate to the β-cyclodextrin saturated solution at a mass ratio of 1:1 , the stirring temperature was 35°C, and the stirring was continued for 4 h at a rotational speed of 1000 r / min. After cooling and standing for 2 h, the filtrate was d...

Embodiment 3

[0060] Prescription: with embodiment 1

[0061] The preparation method is as follows:

[0062] (1) Preparation of tenofovir disoproxil fumarate-β-cyclodextrin inclusion compound (grinding method)

[0063] Weigh tenofovir disoproxil fumarate 300g, weigh 300g β-cyclodextrin according to the mass ratio of 1:1 and place it in a mortar, add 10L ethanol as a wetting agent, grind in a grinder for 1h, ethanol It is ready for use after being removed by volatilization.

[0064] (2) Preparation of efavirenz pellets

[0065] Dissolve 25g sodium lauryl sulfate in 120g pure water, premix 600g efavirenz, 18g microcrystalline cellulose and prepared sodium lauryl sulfate under stirring, add 48g cross-linked carboxymethyl cellulose to the premix Sodium plain, adding water to make soft materials into balls to obtain efavirenz drug-containing pill cores, passing through a 50-60 mesh sieve for later use;

[0066] (3) Preparation of Emtricitabine Microparticles

[0067] First get 25g of crosca...

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Abstract

The invention provides an antiretroviral pharmaceutical composition in the form of tablets. The antiretroviral pharmaceutical composition comprises main drugs efavirenz, emtricitabine and tenofovir disoproxil fumarate, as well as pharmaceutically acceptable excipients microcrystalline cellulose, croscarmellose sodium, sodium lauryl sulfate, magnesium stearate and the like. A preparation method of the antiretroviral pharmaceutical composition comprises the steps of (1) preparation of a tenofovir disoproxil fumarate-beta-cyclodextrin inclusion complex; (2) preparation of efavirenz pellets; (3) preparation of emtricitabine microparticles; and (4) preparation of tables from the three preparations through one-step granulation. The prepared pharmaceutical composition can effectively avoid the degradation of active ingredients in the preparation process and improve the dissolution and stability of drugs.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to an antiretroviral pharmaceutical composition and a preparation method thereof. Background technique [0002] Efavirenz (trade name Sustival, also known as EFV), emtricitabine (trade name Emtrival, also known as FTC), and tenofovir disoproxil fumarate (also known as tenofovir fumarate The above three are antiretroviral drugs, which can be used in combination with other antiretroviral drugs to treat viral infections, especially for the treatment of HIV infection and chronic Hepatitis B treatment. [0003] Among them, the chemical name of emtricitabine is: 5-fluoro-1-(2R,5S)-[2-hydroxymethyl-1,3-oxathione-5-yl]cytosine. Emtricitabine is a soluble raw material, its appearance is white, off-white powder or crystalline powder, tasteless and odorless, and easily soluble in water. [0004] Tenofovir bisphosphate, the active ingredient of tenofovir, can inhibit viral polymerase by d...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/675A61K47/69A61P31/18A61P1/16A61P31/20A61K31/536A61K31/513
CPCA61K31/513A61K31/536A61K31/675A61K2300/00
Inventor 王志邦郭立新钟晓锋沈蔡月朱礼根夏玉明陈小峰刘安友
Owner ANHUI BIOCHEM BIO PHARMA
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