Entecavir crystalline compound and capsule preparation thereof

A crystalline compound, entecavir technology, applied in the direction of active ingredients of heterocyclic compounds, capsule delivery, organic chemistry, etc., can solve the problems of slow dissolution rate and slow onset of action, and achieve long maintenance time, fast release speed, and improved water solubility Effect

Inactive Publication Date: 2015-10-28
HUNAN SANQING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese patent application CN201210004946.6 discloses an entecavir capsule, its components include entecavir, pregelatinized starch and microcrystalline cellulose, 1000 capsules contain entecavir 0.5g, pregelatinized starch 30-100g, microcrystalline cellulose 30 ~100g, lubricant 0~2g, mixed with entecavir and microcrystalline cellulose by equal addition method, then mixed with pregelatinized starch, and put into the capsule shell, its dissolution rate is slow, so the onset of action is slow

Method used

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  • Entecavir crystalline compound and capsule preparation thereof
  • Entecavir crystalline compound and capsule preparation thereof
  • Entecavir crystalline compound and capsule preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Add 10g of entecavir solid into 100ml of mixed solvent of dimethylacetamide and methanol, the volume between dimethylacetamide and methanol is 2.0:1.5, and the temperature is at 40°C, all the entecavir solids are dissolved; control the temperature at Under the condition of 35~40 ℃, add the aqueous solution of isopropanol in the obtained solution, wherein, the mass percent of isopropanol is contained in the aqueous solution of isopropanol is 35%; After adding the aqueous solution of isopropanol, at a rate of Cool down to -5°C at 3.5°C / 10min, stand at -5°C for 13 hours, precipitate crystals, filter, wash the filter cake with ether, and dry in vacuo to obtain entecavir crystals. Carry out Cu-Kα to the obtained product entecavir crystal 1 Radiographic X-ray powder diffraction (eg figure 1 Shown), in 11.1 °, 13.9 °, 14.4 °, 21.1 °, 21.8 °, 22.1.9 °, 23.5 °, 25.2 °, 25.4 °, ° diffraction angle (2θ ± 0.1) shows diffraction peaks.

Embodiment 2

[0043] Add 15g of entecavir solid into 100ml of mixed solvent of dimethylacetamide and methanol, the volume between dimethylacetamide and methanol is 2.0:2.0, and the entecavir solid is completely dissolved at 35°C; control the temperature at Under the condition of 35-40°C, add an aqueous solution of isopropanol to the obtained solution, wherein the aqueous solution of isopropanol contains 30% by mass of isopropanol ethanol; after adding the aqueous solution of isopropanol, at a rate Cool down to -10°C at 2.5°C / 10min, stand at -10°C for 18 hours, precipitate crystals, filter, wash the filter cake with ether, and vacuum dry to obtain entecavir crystals. Show through powder XRD detector analysis, with attached figure 1 The results shown match.

Embodiment 3

[0045] Add 12 solids of Entecavir into 100ml of mixed solvent of dimethylacetamide and methanol, the volume between dimethylacetamide and methanol is 2.0:2.0, and the temperature is at 40°C, all solids of Entecavir are dissolved; control the temperature at Under the condition of 35-40°C, add an aqueous solution of isopropanol to the obtained solution, wherein the aqueous solution of isopropanol contains isopropanol with a mass percentage of 40% ethanol; after adding the aqueous solution of isopropanol, at a rate Cool down to 0°C at 3.0°C / 10min, stand at 0°C for 20 hours, precipitate crystals, filter, wash the filter cake with ether, and dry in vacuo to obtain entecavir crystals. Show through powder XRD detector analysis, with attached figure 1 The results shown match.

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PUM

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Abstract

An entecavir crystalline compound and a capsule preparation containing the entecavir crystalline compound are provided. The X-ray powder diffraction of the crystalline compound measured by Cu-K alpha1 is shown as Figure 1. The capsule preparation containing the entecavir crystalline compound comprises the components of an entecavir crystalline compound, a solubilizer, a filler, a disintegrating agent, a lubricant and a binder. The entecavir capsule provided by the invention uses pharmaceutical excipients almost with no side effects on the human body, and the in vivo and in vitro experiments show that the entecavir capsule can be released in a short time to achieve therapeutic plasma concentration and maintain therapeutic plasma concentration for a long time.

Description

technical field [0001] The invention relates to an anti-HBV oral nucleoside drug entecavir crystal compound and a capsule preparation thereof. Background technique [0002] Chronic viral hepatitis B (CH-B) is a common disease that seriously endangers human health. The prevention and treatment of chronic hepatitis B is a global public health problem, which has attracted the attention of all countries in the world. Hundreds of millions of people around the world have been infected with hepatitis B virus, among which there are about 400 million chronic hepatitis B virus carriers. Among infected patients, about 15% to 40% will develop cirrhosis, liver failure or liver cancer. Among the carriers of hepatitis B virus, 50% to 75% of them have chronic hepatitis B with active virus replication, and the estimated incidence rate of progression from chronic hepatitis B to cirrhosis in 5 years is 2% to 20%; from compensated cirrhosis to Liver decompensation is 20% to 23%; from compensa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D473/18A61K31/522A61K9/48
CPCA61K9/0053A61K9/4866C07B2200/13C07D473/18
Inventor 张舰李马理徐燕
Owner HUNAN SANQING PHARMA
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