Compound tablet containing atazanavir and ritonavir and preparation method of compound tablet

A technology of compound tablet and ritonavir, which is applied in the field of compound tablet containing atazanavir and ritonavir and its preparation, can solve problems such as low solubility and poor thermal stability of ritonavir, and achieve Simple effect of process parameter control

Inactive Publication Date: 2020-11-17
SHANGHAI DESANO PHARMA INVESTMENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Although atazanavir and ritonavir compound preparation is a kind of good anti-HIV virus medicine, some difficult problems still exist, and ritonavir heat stability is poor, and solubility in neutral media such as water is low, and Water is precisely the most suitable medium for evaluating non-bioequivalence in dissolution testing

Method used

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  • Compound tablet containing atazanavir and ritonavir and preparation method of compound tablet
  • Compound tablet containing atazanavir and ritonavir and preparation method of compound tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Name Dosage (g)

[0061] Atazanavir sulfate 341.7

[0062] Lactose monohydrate 142.0

[0063] Pregelatinized starch 55.0

[0064] Crospovidone 55.0

[0065] Calcium silicate 40.0

[0066] Yellow iron oxide 0.5

[0067] Magnesium Stearate 5.8

[0068] Ritonavir 100.0

[0069] Copovidone 560.0

[0070] Colloidal silica 23.0

[0071] Sorbitan monolaurate (Span 20) 60.0

[0072] Calcium hydrogen phosphate anhydrous 100.0

[0073] Sodium stearyl fumarate 7.0

[0074] Appropriate amount of purified water

[0075] Preparation of atazanavir blend granules

[0076] Weigh the raw materials and sieve them for later use: pass lactose monohydrate, pregelatinized starch and crospovidone together through a 30-mesh sieve, and then pass the above-mentioned sieved mixture through a 20-mesh sieve with atazanavir sulfate. Pass the yellow iron oxide through a 100-mesh sieve, then pass the sieved yellow iron oxide, lactose monohydrate, pregelatinized starch, crospovidone and calci...

Embodiment 2

[0084] Name Dosage (g)

[0085] Atazanavir sulfate 341.7

[0086] Microcrystalline cellulose 162.0

[0087] Pregelatinized starch 40.0

[0088] Croscarmellose Sodium 50.0

[0089] Calcium silicate 40.0

[0090] Yellow iron oxide 0.5

[0091] Ritonavir 100.0

[0092] Copovidone 560.0

[0093] Colloidal silica 23.0

[0094] Sorbitan monolaurate (Span 20) 80.0

[0095] Dibasic calcium phosphate anhydrous 80.0

[0096] Magnesium stearate 12.8

[0097] Appropriate amount of purified water

[0098] Preparation of Atazanavir Granules

[0099] Weigh the raw materials and sieve them for later use: pass lactose monohydrate, pregelatinized starch and croscarmellose sodium together through a 30-mesh sieve, and then pass the above-mentioned sieved mixture with atazanavir sulfate for 20 Mesh sieve, pass yellow iron oxide through 100 mesh sieve, then pass sieved yellow iron oxide, lactose monohydrate, pregelatinized starch, microcrystalline cellulose, copovidone and calcium silic...

Embodiment 3

[0107] Name Dosage (g)

[0108] Atazanavir sulfate 341.7

[0109] Lactose monohydrate 140.0

[0110] Pregelatinized starch 60.0

[0111] Hypromellose 55.0

[0112] Calcium silicate 40.0

[0113] Yellow iron oxide 0.5

[0114] Magnesium Stearate 5.8

[0115] Ritonavir 100.0

[0116] Copovidone 560.0

[0117] Colloidal silica 23.0

[0118] Sodium lauryl sulfate 60.0

[0119] Calcium hydrogen phosphate anhydrous 100.0

[0120] Sodium stearyl fumarate 7.0

[0121] Appropriate amount of purified water

[0122] Preparation of atazanavir blend granules

[0123] Weigh the raw materials, and sieve them for later use: pass lactose monohydrate, pregelatinized starch and hydroxypropyl cellulose together through a 30-mesh sieve, and then pass the above-mentioned sieved mixture through a 20-mesh sieve with atazanavir sulfate. Pass the yellow iron oxide through a 100-mesh sieve, then pass the sieved yellow iron oxide, lactose monohydrate, pregelatinized starch, hydroxypropyl cel...

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PUM

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Abstract

The invention relates to the field of pharmaceutical preparations, in particular to a compound tablet containing atazanavir and ritonavir and a preparation method of the compound tablet. According tothe method, the problems of poor thermal stability and poor water solubility of ritonavir in the compound tablets are solved by utilizing a hot melt extrusion technology, and the atazanavir and ritonavir compound tablet which is simpler in process difficulty, equipment conditions and process description control and better in bioavailability is researched and designed and is bioequivalent to singleatazonavir and ritonavir; and therefore, the medication mode is simplified, the patient compliance is improved, and the drug resistance risk is reduced.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a compound tablet containing atazanavir and ritonavir and a preparation method thereof. Background technique [0002] Atazanavir was developed by Bristol-Myers Squibb, ritonavir was developed by ABBVIE, the compound of atazanavir and ritonavir was developed by MATRIX LABS LTD and EMCURE PHARMS LTD, and has been approved by FDA Conditionally approved for marketing as part of combination therapy for the treatment of newly diagnosed HIV-1 infection. [0003] It is reported that about 40% of the active substances that play the main pharmacological activity in drugs are insoluble in water. Poorly water-soluble drugs (poorly water-soluble drugs) are difficult to be absorbed by the body because of their low solubility in water, and the elimination speed in the body is fast and the bioavailability is poor. At present, it is more and more difficult to find drugs with new chemi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K9/20A61K31/551A61K31/427A61P31/18
CPCA61K9/2077A61K9/209A61K9/2095A61K9/2866A61K31/427A61K31/551A61P31/18A61K2300/00
Inventor 王琳李金亮宁江松赵楠张静
Owner SHANGHAI DESANO PHARMA INVESTMENT
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