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New tenofovir disoproxil fumarate crystal and preparation method thereof
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A tenofovir disoproxil fumarate and crystallization technology, applied in the field of medicine, can solve problems such as differences in bioavailability, and achieve the effects of good stability, high bioavailability and stable stability
Active Publication Date: 2014-01-15
FUJIAN COSUNTER PHARMA CO LTD
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Problems solved by technology
Different crystalline forms of the same drug may have significantly different bioavailability
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Embodiment 1
[0036] Embodiment 1. tenofovir disoproxil fumarate crystal form and its preparation
[0037] In a 10ml reaction bottle, add 1.0g tenofovir disoproxil fumarate, 4.0ml methanol and 1.0ml petroleum ether, heat to 50°C, stir for 30min, cool to 0°C for 8hr, and filter with suction to obtain a white crystalline powder , washed twice with a small amount of petroleum ether, and vacuum-dried to obtain the new crystal form of tenofovir disoproxil fumarate of the present invention.
[0038] Its X-ray diffraction diagram, infrared absorption spectrum diagram and differential thermal analysis diagram are shown in the appendix figure 1 , 2 and 3.
[0040] Prescription: 300 g of the new crystal form of tenofovir disoproxil fumarate of the present invention, 100 g of hydroxypropyl cellulose, and 50 g of sodium carboxymethyl starch.
[0041] Preparation method: The above-mentioned two kinds of materials were crushed through 100 mesh respectively, dried under reduced pressure at 100°C for more than 10 hours, cooled to room temperature, mixed with the new crystal form of tenofovir disoproxil fumarate, and granulated by a dry granulator. Compressed into 1000 pieces, that is.
[0043] Prescription: 300g of the new crystal form of tenofovir disoproxil fumarate of the present invention, 65g of lactose, 70g of microcrystalline cellulose, 15g of sodium carboxymethyl starch, and 1.5g of magnesium stearate.
[0044] Preparation method: the above-mentioned lactose, microcrystalline cellulose, and sodium carboxymethyl starch were respectively crushed through 100 meshes, dried under reduced pressure at 100°C for more than 10 hours, cooled to room temperature, and mixed with the new crystal form of tenofovir disoproxil fumarate Mix evenly, granulate with a dry granulator, add magnesium stearate, mix evenly, fill into 1000 empty capsules, and obtain tenofovir disoproxil fumarate capsules.
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Abstract
The invention relates to a new tenofovir disoproxil fumarate crystal and a preparation method thereof. The method for preparing the new tenofovir disoproxil fumarate crystal comprises the following steps of: dissolving the tenofovir disoproxil fumarate by mixed solution with the weight of 2-20 times of the tenofovir disoproxil fumarate by heating; stirring for 30 min, cooling to 0 DEG C, placing for crystallization, filtering, washing twice with a small amount of petroleum ether, and vacuum drying. The mixed solution is a mixed solution of methanol and petroleum ether in the volume ratio of (3.5-5):1, that is to say, the mixed solution contains 3.5-5 ml of methanol and 1 ml of petroleum ether.
Description
technical field [0001] The invention belongs to the field of medicine, in particular to a new crystal form of tenofovir disoproxil fumarate and a preparation method thereof. technical background [0002] Tenofovir disoproxil, English name: Tenofovir Disoprox, is a kind of medicine that is used for the treatment of HIV, HBV infection, and its pharmacology and toxicology: be to inhibit reverse transcriptase with the similar method of nucleoside reverse transcriptase inhibitor, thereby Has potential anti-HIV-1 activity. Tenofovir bisphosphate, the active ingredient of tenofovir, can inhibit viral polymerase by directly competitively binding to natural deoxyribose substrates, and terminate the chain by inserting into DNA. Pharmacokinetics: Tenofovir is almost not absorbed through the gastrointestinal tract, so it undergoes esterification and salt formation to become tenofovir disoproxil fumarate. Tenofovir disoproxil is water-soluble and can be rapidly absorbed and degraded in...
Claims
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