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Preparation method of ritonavir solid dispersion

A technology of solid dispersion and ritonavir, which is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, and pharmaceutical formulas, which can solve problems such as adverse reactions and ineffectiveness

Active Publication Date: 2022-05-31
乐普制药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Acid hydrolyzed impurities not only have no effect on clinical efficacy, but too high content may cause some adverse reactions

Method used

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  • Preparation method of ritonavir solid dispersion
  • Preparation method of ritonavir solid dispersion
  • Preparation method of ritonavir solid dispersion

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Embodiment 1 screens different carrier types and prepares solid dispersion

[0020] experiment procedure:

[0021] (1) Ritonavir was mixed with polyethylene glycol 3000, polyvinylpyrrolidone K30, and copovidone at a ratio of 1:5, respectively, and then placed in an autoclave.

[0022] (2) The temperature in each kettle is set to 45°C, and carbon dioxide is introduced until the pressure reaches 25Mpa. After the preparation time is 5 hours, the solid dispersion is taken out, ground, and the crystal form is detected by X-ray diffraction method together with the raw materials, and the The HPLC method was used to detect the content of acid hydrolyzed impurities. The results showed that the solid dispersion prepared by polyethylene glycol 3000 and ritonavir had a large content of acid hydrolysis impurities, and polyvinylpyrrolidone K30 or copovidone could be used.

[0023] Table 1 adopts the crystal form and impurity situation of solid dispersion prepared by different carri...

Embodiment 2

[0036] Embodiment 2 investigates the different ratios of ritonavir and copovidone in carbon dioxide under the critical state

[0037] experiment procedure:

[0038] (1) Mix ritonavir and copovidone at a ratio of 1:1, 1:3, 1:5, 1:7, and 1:9, respectively, and place them in an autoclave.

[0039] (2) The temperature in each kettle was set to 45°C, and carbon dioxide was introduced until the pressure reached 25Mpa. After the preparation time was 5 hours, the solid dispersion was taken out, and the crystal form was detected by X-ray diffraction method after grinding.

[0040] (3) The test results show that when the ratio of ritonavir and copovidone is 1:5-1:9, ritonavir is amorphous in solid dispersion.

[0041] Table 2 prepares the crystal form of solid dispersion at different temperatures

[0042] Ratio of ritonavir and copovidone 1:1 1:3 1:5 1:7 1:9 Crystal form of ritonavir partially crystalline partially crystalline not finalized not finalized n...

Embodiment 3

[0043] Embodiment 3 screening critical carbon dioxide prepares the temperature of solid dispersion

[0044] experiment procedure:

[0045] (1) After mixing ritonavir and copovidone evenly according to the ratio of 1:5, divide them into 5 parts on average, and put 4 parts in the autoclave respectively.

[0046] (2) Set 35°C, 40°C, 45°C, and 50°C respectively, and feed carbon dioxide until the pressure reaches 25Mpa. After the preparation time is 5 hours, take out the solid dispersion, grind it, and use it together with the mixture before preparing the solid dispersion The crystal form was detected by X-ray diffraction method, and the acid hydrolysis impurity content was detected by HPLC method. Tests show that the set temperature for preparing the solid dispersion should be 40-50°C.

[0047] (3) Adopt the hot-melt extruder of different direction conical screw to prepare solid dispersion, after ritonavir and copovidone are mixed according to 1:5 ratio, screw speed is set to be...

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Abstract

The invention provides a preparation method of a ritonavir solid dispersion. According to the invention, the solid dispersion of ritonavir is prepared by adopting a critical carbon dioxide method, and the solid dispersion is prepared at a relatively low temperature. Compared with an existing ritonavir hot-melt extrusion process for preparing the solid dispersion, the preparation method disclosed by the invention has the advantage that the generation of impurities in the preparation process can be remarkably avoided.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a preparation method of ritonavir solid dispersion. [0002] technical background [0003] Ritonavir is an anti-human immunodeficiency virus (HIV) drug and an HIV protease inhibitor. The indication is to treat advanced or non-progressive AIDS patients alone or in combination with antiretroviral nucleoside drugs. HIV protease is an enzyme found in infectious HIV that cleaves viral polymeric protein precursors into individual functional proteins. This action blocks cleavage of viral aggregated proteins, leading to the formation of immature, non-infectious virions. [0004] [0005] Ritonavir soft capsules and oral solutions were listed by the US FDA in 1996, and have been listed in the United States, Europe, Japan and many other countries in the world. Ritonavir Soft Capsules was approved by the Chinese Food and Drug Administration on December 1...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/20A61K9/48A61K31/427A61K47/32A61P31/18
CPCA61K31/427A61K47/32A61K9/1635A61K9/2027A61K9/4866A61P31/18Y02P20/54
Inventor 潘裕生宋林奇张玉俞悦王海翔洪华斌
Owner 乐普制药科技有限公司
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