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Compound medicine compounds containing adefovir dipivoxil, preparing method and uses thereof

A technology of adefovir dipivoxil and composition, applied in the direction of medical preparations containing active ingredients, drug combinations, active ingredients of heterocyclic compounds, etc., can solve the problems of reduced antiviral activity, low sensitivity, drug resistance, etc.

Inactive Publication Date: 2008-07-30
BEIJING RUNDEKANG MEDICAL TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Entecavir inhibits replication of lamivudine-resistant strains but has reduced antiviral activity
In vitro experiments show that the sensitivity of lamivudine-resistant strains to entecavir is lower than that of wild strains, and the mutation sites of HBV are rt184, rt202, and rt250, which may lead to drug resistance by limiting the combination of entecavir and HBV polymerase

Method used

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  • Compound medicine compounds containing adefovir dipivoxil, preparing method and uses thereof
  • Compound medicine compounds containing adefovir dipivoxil, preparing method and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1 Compound adefovir dipivoxil lamivudine tablets

[0031] prescription:

[0032] components

Dosage

adefovir dipivoxil

Lamivudine

microcrystalline cellulose

CMS-Na

Magnesium stearate

Co-made

10g

100g

80g

6g

4g

1000 pieces

[0033] Preparation:

[0034] Pass adefovir dipivoxil and lamivudine through 80-mesh sieves respectively, and mix them uniformly by the method of equal increments, and set aside; add microcrystalline cellulose, CMS-Na, and magnesium stearate to them, mix them well, and powder wood Direct compression tablet, that is.

Embodiment 2

[0035] Embodiment 2: compound adefovir dipivoxil lamivudine capsules

[0036] prescription:

[0037] components

Dosage

adefovir dipivoxil

Lamivudine

pregelatinized starch

Talc powder

Co-made

20g

100g

20g

5g

1000 capsules

[0038] Preparation:

[0039] Pass adefovir dipivoxil and pregelatinized starch through a 80-mesh sieve respectively, and mix them uniformly by using an equal-volume increasing method, and set aside; add them to the lamivudine that has passed through an 80-mesh sieve, mix well, and finally add talcum powder, Subpackage, that is.

Embodiment 3

[0040] Embodiment 3: compound adefovir dipivoxil telbivudine chewable tablet

[0041] prescription:

[0042] components

Dosage

adefovir dipivoxil

Telbivudine

Xylitol

Mannitol

Sweet Orange Flavor

aspartame

2% PVP-k30 ethanol solution

Magnesium stearate

Co-made

20g

600g

250g

250g

15g

15g

Appropriate amount

10g

1000 capsules

[0043] Preparation:

[0044] Pass adefovir dipivoxil and other raw and auxiliary materials through 80-mesh sieves respectively, and mix them evenly by the method of equal increments, and set aside; add 2% PVP-k30 ethanol solution to make soft materials, granulate with 16-mesh sieves, dry, and sieve with 20-mesh sieves Granules, add other flavoring agents, sweeteners, and glidants, mix evenly, and compress into tablets.

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PUM

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Abstract

The invention relates to a medical composition with active components of adefovir dipivoxil and another rnucleotide (acid) anti-virus medicine and the preparation method and usage thereof. The adefovir dipivoxil and anther rnucleotide (acid) anti-virus medicine are taken as the active components, and mixed with a plurality of pharmaceutically acceptable supplements to prepare the medical composition; and the invention can be applied in treatment of viral hepatitis B. The adefovir dipivoxil and anther rnucleotide (acid) anti-virus medicine are taken as raw materials of the invention content, a plurality of supplements with special type and proportion are added, and various kinds of oral preparations such as tablet, capsule, dispersion, chewable tablet, oral disintegrating tablet, buccal tablet, dropping pill and soft capsule are prepared and developed according to the technical method described by the invention.

Description

technical field [0001] The invention relates to a pharmaceutical composition with adefovir dipivoxil and another nucleoside (acid) antiviral drug as active components, a preparation method and application thereof, and belongs to the technical field of medicine. Background technique [0002] One of the main problems faced by long-term nucleoside (acid) analog therapy is the selection of antiviral drug-resistant mutants. The incidence of drug-resistant mutant strains being screened is related to factors such as serum HBV DNA level before treatment, speed of virus suppression, course of treatment, and previous nucleoside (acid) analogue treatment history. The incidence of genotypic drug resistance is also related to the sensitivity of the drug resistance mutation detection method and the tested patient population. [0003] HBV resistance to antiviral drugs can be divided into phenotype resistance and genotype resistance. Phenotypic drug resistance refers to the increase in vi...

Claims

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Application Information

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IPC IPC(8): A61K31/675A61K31/7068A61K31/7072A61K45/06A61K9/20A61K9/48A61P1/16A61P31/20A61K31/52
Inventor 陈瑞晶
Owner BEIJING RUNDEKANG MEDICAL TECH CO LTD
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