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Efavirenz tablet and preparation method thereof

A technology for efavirenz and velen tablets, applied in the field of efavirenz tablets and their preparation, can solve the problems of slow absorption and inability to completely absorb active ingredients and the like

Active Publication Date: 2013-03-27
ANHUI BIOCHEM BIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It can be seen that the absorption of traditional efavirenz tablets in the body is slow, and when the dose becomes larger, the active ingredients cannot be completely absorbed

Method used

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  • Efavirenz tablet and preparation method thereof
  • Efavirenz tablet and preparation method thereof
  • Efavirenz tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] (1) Weigh the raw materials according to the weights listed in Table 1.

[0026] (2) Dissolve the weighed sodium lauryl sulfate in water to make an aqueous solution of sodium lauryl sulfate; then mix the weighed efavirenz, microcrystalline cellulose, hydroxypropyl cellulose and Add 3 / 10 croscarmellose sodium into the prepared sodium lauryl sulfate aqueous solution and stir to form a soft material. The soft material is granulated in a 18-24 mesh granulation screen. After granulation The granules are sized through a 18-24 mesh screen. Then the magnesium stearate taken by weighing and the remaining croscarmellose sodium and the granulated granules are mixed uniformly and compressed into tablets to obtain 1000 tablets;

[0027] (3) Prepare the weighed hydroxypropyl methylcellulose into a 5% solution with 85% ethanol, and use this solution to coat the tablet prepared in S2 to obtain the finished efavirenz tablet. The average mass of the measured single efavirenz tablet is ...

Embodiment 2

[0031] (1) Weigh the raw materials according to the weights listed in Table 2.

[0032] (2) Dissolve the weighed sodium lauryl sulfate in water to make an aqueous solution of sodium lauryl sulfate; then mix the weighed efavirenz, microcrystalline cellulose, hydroxypropyl cellulose and Add 1 / 2 of the croscarmellose sodium into the prepared sodium lauryl sulfate aqueous solution and stir to form a soft material. The soft material is granulated in a 18-24 mesh granulation screen. After granulation, The granules are sized through a 18-24 mesh screen. Then the magnesium stearate taken by weighing and the remaining croscarmellose sodium and the granulated granules are mixed uniformly and compressed into tablets to obtain 1000 tablets;

[0033] (3) Prepare the weighed hydroxypropyl methylcellulose into a 5% solution with 85% ethanol, and use this solution to coat the tablet prepared in S2 to obtain the finished efavirenz tablet. The measured average mass of a single efavirenz table...

Embodiment 3

[0037] (1) Weigh the raw materials according to the weights listed in Table 3.

[0038] Table 3 Formula Composition of Efavirenz Tablets (C)

[0039]

[0040] (2) Dissolve the weighed sodium lauryl sulfate in water to make an aqueous solution of sodium lauryl sulfate; then mix the weighed efavirenz, microcrystalline cellulose, hydroxypropyl cellulose and Add 1 / 2 of the croscarmellose sodium into the prepared sodium lauryl sulfate aqueous solution and stir to form a soft material. The soft material is granulated in a 18-24 mesh granulation screen. After granulation, The granules are sized through a 18-24 mesh screen. Then, the weighed magnesium stearate and the remaining croscarmellose sodium were uniformly mixed with the granulated granules and compressed into 1000 tablets.

[0041] (3) Prepare the weighed hydroxypropyl methylcellulose into a 5% solution with 85% ethanol, and use this solution to coat the tablet prepared in S2 to obtain the finished efavirenz tablet. The...

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Abstract

The invention discloses an efavirenz tablet which is prepared from the following raw materials in parts by weight: 65-75 parts of efavirenz, 10-15 parts of croscarmellose sodium, 7-9 parts of microcrystalline cellulose and 7-12 parts of lauryl sodium sulfate, hydroxy propyl cellulose, magnesium stearate and hydroxypropyl methyl cellulose in total. The dispersibility of the efavirenz tablet in the intestinal tract is improved and the dissolution speed of efavirenz is improved by increasing the using amount of the croscarmellose sodium, and therefore the efavirenz can be rapidly absorbed and utilized.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to an efavirenz tablet and a preparation method thereof. Background technique [0002] Efavirenz is a new generation of anti-HIV-1 virus non-nucleoside reverse transcriptase inhibitors, clinically used alone or in combination with other drugs for the treatment of HIV infection. The single tablet of traditional commercially available efavirenz tablets weighs 1.2g, which contains 50% efavirenz, 5% croscarmellose sodium, 20% microcrystalline cellulose, and the balance as auxiliary additives. Because the weight of its single tablet is 1.2g, the volume of the efavirenz tablets obtained by it is relatively large, which is not conducive to taking by patients. For some younger patients, it may even block the throat, causing safety accidents . [0003] Pharmacokinetic experiments show that healthy volunteers take 100-1600 mg of traditional efavirenz tablets once orally, the time to peak (Tmax) is ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/536A61K47/38A61P31/18
Inventor 邢怀阳沈蔡月
Owner ANHUI BIOCHEM BIO PHARMA
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