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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
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  • 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

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  • 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.

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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

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Application Information

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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
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