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A kind of entecavir pharmaceutical composition and preparation method thereof

A technology of entecavir and composition, which is applied in the direction of drug combination, pharmaceutical formula, heterocyclic compound active ingredients, etc., can solve the problems such as failure to eliminate the influence of drug absorption, and achieve improved bioavailability, good fluidity, and compressibility high effect

Active Publication Date: 2017-11-17
山东希力药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

And there are many domestic patent applications about its oral preparations such as: CN201110404318.2, CN201210040363.9, CN201210131581.3, CN201310066806.6, CN201310216745.7, CN201210321702.0, but none of them can eliminate the influence of normal diet on drug absorption , need to take medicine on an empty stomach

Method used

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  • A kind of entecavir pharmaceutical composition and preparation method thereof
  • A kind of entecavir pharmaceutical composition and preparation method thereof
  • A kind of entecavir pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025]

[0026] making process

[0027] Get entecavir bulk drug, povidone K-30, P85 and add (180mL) 50% (v / v) ethanol, stir to dissolve, and set aside; Take the lactose of recipe quantity, microcrystalline cellulose PH-101 mix evenly, adopt Wet granulation or fluidized bed granulation, drying for 15 minutes after granulation. Cross 40 mesh sieves for granulation, then take by weighing the crospovidone XL-10 and magnesium stearate of prescription quantity, add in the above-mentioned granules, mix homogeneously. The entecavir preparation is obtained by directly compressing tablets or filling capsules. Tablet products may be film-coated if necessary.

Embodiment 2

[0029]

[0030] making process

[0031] Get entecavir bulk drug, hydroxypropyl methylcellulose E15, P85 and add (180mL) 50% ethanol, stir to dissolve, and set aside; take the lactose of prescription quantity, microcrystalline cellulose PH-101 and mix evenly, adopt wet granulation or Fluidized bed granulation, drying for 15 minutes after granulation. Pass through a 40-mesh sieve for granulation, then weigh the prescribed amount of crospovidone XL-10 and magnesium stearate, add them to the above granules, and mix well. The entecavir preparation is obtained by directly compressing tablets or filling capsules. Tablet products may be film-coated if necessary.

Embodiment 3

[0033]

[0034] making process

[0035] Get entecavir bulk drug, povidone K-30, LABRASOL and add (180mL) 50% ethanol, stir to dissolve, and set aside; take the lactose of recipe quantity, microcrystalline cellulose PH-101 and mix evenly, adopt wet granulation or fluid flow Bed granulation, drying for 15 minutes after granulation. Pass through a 40-mesh sieve for granulation, then weigh the prescribed amount of crospovidone XL-10 and magnesium stearate, add them to the above granules, and mix well. The entecavir preparation is obtained by directly compressing tablets or filling capsules. Tablet products may be film-coated if necessary.

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PUM

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Abstract

The invention relates to an entecavir pharmaceutical composition and a preparation method thereof, which contain entecavir, a penetration enhancer and pharmaceutically acceptable auxiliary materials, wherein the mass ratio of the membrane penetration enhancer to the entecavir is 1-100:1. The membrane penetration enhancer is selected from alcohols, propylene glycols, fatty alcohols, fatty acids, fatty acid esters, alkyl esters, polyols, sulfoxides, amides, nonionic surfactants, terpenes, One or more of alkanones and skin penetration enhancer compounds. The peak concentration and linear area of ​​the composition formulations are significantly improved, and the Cmax of entecavir in the new formulation of entecavir increases by about 53.9%, and the AUC increases by about 69.5%, which significantly improves the bioavailability of the drug in the fed state.

Description

technical field [0001] The invention relates to a pharmaceutical composition of entecavir, a drug for treating hepatitis B, and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Entecavir is a nucleoside analog independently developed by Bristol-Myers Squibb, and its chemical name is 2-amino-9-[(1S,3R,4S)-4-hydroxy-3-hydroxymethyl- 2-Methylenecyclopentyl]-1,9-dihydro-6H-purin-6-one hydrate, the structural formula is shown in the following formula: [0003] [0004] It is slightly soluble in water, and its solubility is 2.4 mg / mL. In 2005, it was approved for marketing by the FDA in the United States, and its dosage forms include tablets and oral solutions; Entecavir tablets were approved for marketing in China in February 2006. [0005] Pharmacokinetic studies have found that after oral administration of Entecavir Tablets in healthy people, this product is rapidly absorbed and reaches its peak concentration (Cmax) ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/14A61K47/10A61K31/522A61P1/16A61P31/20
Inventor 赵忠熙杨民姜晓燕田婷婷邢玉仁张建强董爱梅
Owner 山东希力药业有限公司