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NS5A inhibitor composition

A composition and compound technology, applied in the direction of antiviral agents, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve problems such as preclinical research in the early stage

Pending Publication Date: 2021-05-28
YICHANG HEC CHANGJIANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Prior art CN105693700B provides compounds (I), (II) and pharmaceutically acceptable salts thereof, which have good biological properties, but this prior art research is still in the early stage of preclinical research, in order to help The development of clinical research requires further research on the properties of the drug, and the search for drug salts and drug dosage forms suitable for human consumption

Method used

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  • NS5A inhibitor composition
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0160] Compound III capsules were prepared according to the recipe shown below, and the dissolution rate was determined.

[0161] Preparation:

[0162] (1) The drug particle size D of compound III 50 =47.1μm, microcrystalline cellulose, mannitol, croscarmellose sodium, micropowder silica gel, magnesium stearate passed through a 60-mesh sieve;

[0163] (2) Weigh the components according to the prescription ratio:

[0164] Compound III: 29.27;

[0165] Microcrystalline cellulose: 22.24;

[0166] Mannitol: 44.49;

[0167] Croscarmellose sodium: 2.00;

[0168] Micropowder silica gel: 1.00;

[0169] Magnesium stearate: 1.00;

[0170] Total: 100.

[0171] (3) Mix the microcrystalline cellulose, mannitol, croscarmellose sodium and compound III in the prescribed amount for 20 minutes until uniform, to obtain a mixture;

[0172] (3) The magnesium stearate of the sieved prescription ratio added in the mixture, after total mixing 5min to evenly, is filled into 100mg specificatio...

Embodiment 2

[0175] Compound III capsules were prepared according to the recipe shown below, and the dissolution rate was determined.

[0176] Preparation:

[0177] (1) The drug particle size D of compound III 50 =35.9μm, microcrystalline cellulose, mannitol, croscarmellose sodium, micropowder silica gel, magnesium stearate passed through a 60-mesh sieve;

[0178] (2) Weigh the components according to the prescription ratio:

[0179] Compound III: 29.27;

[0180] Microcrystalline cellulose: 22.24;

[0181] Mannitol: 44.49;

[0182] Croscarmellose sodium: 2.00;

[0183] Micropowder silica gel: 1.00;

[0184] Magnesium stearate: 1.00;

[0185] Total: 100.

[0186] (3) Mix the microcrystalline cellulose, mannitol, croscarmellose sodium and compound III in the prescribed amount for 20 minutes until uniform, to obtain a mixture;

[0187] (3) The magnesium stearate of the sieved prescription ratio added in the mixture, after total mixing 5min to evenly, is filled into 100mg specificatio...

Embodiment 3

[0190] Compound III capsules were prepared according to the recipe shown below, and the dissolution rate was determined.

[0191] Preparation:

[0192](1) The drug particle size D of compound III 50 =22.5μm, microcrystalline cellulose, mannitol, croscarmellose sodium, micropowder silica gel, magnesium stearate passed through a 60-mesh sieve;

[0193] (2) Weigh the components according to the prescription ratio:

[0194] Compound III: 29.27;

[0195] Microcrystalline cellulose: 22.24;

[0196] Mannitol: 44.49;

[0197] Croscarmellose sodium: 2.00;

[0198] Micropowder silica gel: 1.00;

[0199] Magnesium stearate: 1.00;

[0200] Total: 100.

[0201] (3) Mix the microcrystalline cellulose, mannitol, croscarmellose sodium and compound III in the prescribed amount for 20 minutes until uniform, to obtain a mixture;

[0202] (3) The magnesium stearate of the sieved prescription ratio added in the mixture, after total mixing 5min to evenly, is filled into 100mg specification...

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Abstract

The invention provides a composition. The composition comprises a compound shown in a formula (I) or a formula (II) or a pharmaceutically acceptable salt thereof as an active ingredient, or a compound shown in a formula (III) or a formula (IV) as an active ingredient. The particle size of the active component satisfies the following condition: D50 is greater than or equal to 20 [mu]m and D50 is less than or equal to 50 [mu]m. The composition can be used for effectively treating the hepatitis C virus, and is high in safety and quick in effect.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to a composition for treating hepatitis C and capsules thereof. Background technique [0002] Viral hepatitis C is a global infectious disease caused by hepatitis C virus (Hepatitis C virus, HCV). It progresses to chronic hepatitis, and 20 years after infection, about 5% to 15% develop liver cirrhosis, the annual incidence of liver cirrhosis decompensation is 3% to 4%, and 2% to 4% of liver cirrhosis patients develop liver cancer every year ( HCC), HCV is a serious hazard to the health and life of patients, and the symptoms of CHC patients are hidden, the diagnosis rate of HCV infection and the rate of antiviral treatment are low, there are many hidden sources of infection in the crowd, and it has become a serious social problem. and public health issues. [0003] According to the updated data of the World Health Organization (WHO) in April 2016, the global chronic HCV infection rate is ab...

Claims

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Application Information

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IPC IPC(8): A61K31/4178A61K9/48A61K47/32A61K47/38A61K47/36A61K47/26A61K47/02A61P31/14
CPCA61K31/4178A61K9/4866A61K9/4858A61K9/485A61P31/14A61K2300/00
Inventor 欧金来郭朕谢洪明张英俊
Owner YICHANG HEC CHANGJIANG PHARMA CO LTD
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