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Rifapentine-containing pharmaceutical composition and preparation method thereof

A technology of rifapentine and rifapentine layer, which is applied in the field of pharmaceutical preparations, can solve the problems such as the impurity content cannot be reduced, and achieve the effect of improving safety and drug efficacy

Pending Publication Date: 2022-04-12
JIANGSU SIMCERE PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Sanofi disclosed a pharmaceutical composition in the form of coated tablets containing isoniazid granules and rifapentine granules in the patent application WO2015011161. The applicant found that there were a large number of impurities in the pharmaceutical composition disclosed in the application, especially There is a high level of genotoxic impurity 1-cyclopentyl-4-nitrosopiperazine, and it was found that even eliminating the effect of oxygen (such as increasing the amount of antioxidants) can not reduce the content of the above impurities

Method used

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  • Rifapentine-containing pharmaceutical composition and preparation method thereof
  • Rifapentine-containing pharmaceutical composition and preparation method thereof
  • Rifapentine-containing pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059]Embodiment 1 rifapentine crude drug

[0060] The method disclosed in the patent application CN111018886A was adopted, wherein the process of crystallization, recrystallization and purification in step 5 was repeated many times to obtain the raw material drug of rifapentine, which was tested for 1-cyclopentyl-4-nitrosopiper The content of oxazine was 1.33 ppm.

Embodiment 2

[0062] prescription

[0063] Rifapentine layer

[0064] Intragranular Weight (mg / tablet) Rifapentine 300.0 Microcrystalline Cellulose PH112 150 Sodium carboxymethyl starch 20 pregelatinized starch 30 Calcium stearate 3 Extragranular Microcrystalline Cellulose PH112 60 sodium ascorbate 10 Sodium carboxymethyl starch 26 Calcium stearate 4 total 603

[0065] Isoniazid layer

[0066] Isoniazid 300.0 Microcrystalline Cellulose PH102 150.0 Microcrystalline Cellulose KG802 40.0 Sodium carboxymethyl starch 20.0 Calcium stearate 0.25 total 510.25

[0067] Preparation process (dry granulation)

[0068] (1) Micronize the prescribed amount of rifapentine in advance, mix with microcrystalline cellulose PH112, sodium carboxymethyl starch, and pregelatinized starch for 10 minutes, and then add calcium stearate passed through a 60-mesh sieve and mix 3 minutes, wher...

Embodiment 3

[0076] prescription

[0077] Rifapentine layer

[0078] Intragranular Weight (mg / tablet) Rifapentine 300.0 Microcrystalline Cellulose PH102 145.5 Low-substituted hydroxypropyl cellulose LC21 10 pregelatinized starch 20 Sodium dodecyl sulfate 2.5 Calcium stearate 3 Extragranular Microcrystalline Cellulose KG802 40 sodium ascorbate 10 Sodium carboxymethyl starch 5 Calcium stearate 4 total 540

[0079] Isoniazid layer

[0080] Isoniazid 300.0 Microcrystalline Cellulose PH102 159.75 Microcrystalline Cellulose KG802 40.0 Sodium carboxymethyl starch 30.0 Low-substituted hydroxypropyl cellulose LC21 15.0 Calcium stearate 0.25 total 545

[0081] Preparation process (dry granulation)

[0082] According to the prescription in the table above, the rifapentine-containing composition was prepared by the preparation method of Example 2.

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Abstract

The invention relates to a rifapentine-containing pharmaceutical composition and a preparation method thereof, rifapentine-containing particles are prepared through dry granulation, the content of impurities in the pharmaceutical composition in the prior art is reduced, especially the content of genotoxic impurity 1-cyclopentyl-4-nitrosopiperazine is reduced, and the safety of medication and the curative effect of the medicine are improved.

Description

[0001] The present invention claims the priority of the previous application submitted to the State Intellectual Property Office of China on September 27, 2020, with the patent application number 202011036278.6, and the title of the invention being "a pharmaceutical composition containing rifapentine and its preparation method". The entirety of the aforementioned prior application is incorporated herein by reference. technical field [0002] The application relates to the field of pharmaceutical preparations, in particular to a pharmaceutical composition containing rifapentine and a preparation method thereof. Background technique [0003] Tuberculosis is a common chronic infectious disease in clinic. In recent years, the incidence and mortality of tuberculosis in China have shown a sharp upward trend, posing a serious threat to the health and quality of life of the people. Clinically, the principle of anti-tuberculosis treatment is based on the combination of regular drugs...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/20A61K9/28A61K47/38A61K47/36A61K47/12A61K31/496A61K31/4409A61P31/06
Inventor J·巴拉穆鲁甘潘云高晓芳魏菁文董静李毅
Owner JIANGSU SIMCERE PHARMA
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