Crystallization type Entecavir formulation as well as preparation method and use thereof

A technology of entecavir and crystalline form, which is applied in the field of crystalline entecavir preparations, can solve problems such as complicated process and unfavorable product quality control

Inactive Publication Date: 2009-02-25
ZHEJIANG MEDICINE CO LTD XINCHANG PHAMACEUTICAL FACTORY
View PDF1 Cites 7 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although R.J. Colonno et al. disclose a kind of low-dose entecavir and its composition preparation with other pharmaceutically active substances for the treatment of hepatitis B virus infection in CN1310999, the active ingredient it uses is amorphous entecavir, and its Oral preparations, especially tablets and capsules, adopt the preparation process of boiling granulation. Although this method can ensure the uniform distribution of active ingredients, it is not conducive to the quality control of the product because it needs to go through a humid and hot process and the process is complicated.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Crystallization type Entecavir formulation as well as preparation method and use thereof
  • Crystallization type Entecavir formulation as well as preparation method and use thereof
  • Crystallization type Entecavir formulation as well as preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] formula:

[0030]

[0031] Preparation:

[0032] First pass the crystalline entecavir and stearic acid through a 120-mesh sieve, then fully mix them, then mix them with sucrose, calcium sulfate, poloxamer, and hyprolose, and then press them into shape.

Embodiment 2

[0034] formula:

[0035]

[0036]

[0037] Preparation:

[0038] First pass the crystalline entecavir, silicon dioxide, and magnesium stearate through a 120-mesh sieve, and then fully mix them, and then mix them with lactose, povidone, and sodium carboxymethyl starch, and then press to form.

Embodiment 3

[0040] formula:

[0041]

[0042] Preparation:

[0043] First pass the crystalline entecavir and sucrose fatty acid lipid through a 120-mesh sieve, and then fully mix them, and then mix them with starch, alginic acid, hydroxypropyl cellulose, and sodium starch glycolate, and then press to form.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

Abstract

The invention relates to a medical composition used for treating hepatitis B virus infective diseases; the composition comprises a medicinally active component, crystallized Entecavir, and a medicinal excipient. The tablets and capsules prepared by the medical composition is obviously superior in stability to similar medicinal preparations by using amorphous Entecavir as the active component under the conditions of illumination, high temperature, high moisture, and the like.

Description

technical field [0001] The invention relates to a crystalline entecavir preparation and its clinical application in treating hepatitis B. Background technique [0002] Chronic hepatitis B inflammatory disease is the most serious liver disease in terms of morbidity and mortality worldwide. Currently, drugs for the treatment of chronic hepatitis B (CHB) can be divided into two categories. One is interferon α, and the other is nucleoside / nucleotide analogues, namely lamivudine and adefovir. However, because these drugs have their own limitations, they are far from meeting the needs of doctors and patients for the treatment of chronic hepatitis B. Entecavir (entecavir, ETV) is epoxy hydroxycarbodeoxyguanosine, which is a guanine nucleotide analogue. It becomes an active triphosphate through phosphorylation in vivo. Entecavir triphosphate passes through the natural substrate triphosphate of HBV polymerase. Deoxyguanosine competes to inhibit HBV polymerase, so as to achieve the...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/513A61K9/20A61K9/48A61P1/16A61P31/12
CPCA61K9/2013A61K9/2054A61K9/2866A61K9/2018A61K9/2027A61K31/522A61K9/2009A61K9/2059A61P1/16A61P31/12A61P31/20
Inventor 易德平田治科叶伟东
Owner ZHEJIANG MEDICINE CO LTD XINCHANG PHAMACEUTICAL FACTORY
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap