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Entecavir soft capsule

A technology of entecavir and soft capsules, applied in the field of entecavir soft capsules, can solve problems such as low penetration rate, achieve low penetration rate, ensure rapid release, and stabilize the composition system

Active Publication Date: 2010-05-12
杭州浙中医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] In order to solve the technical problems existing in the existing Entecavir soft capsules, the object of the invention is to provide a kind of Entecavir soft capsules with high solubility, low penetration rate and stable properties.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Weigh 1975.0 mg of polyethylene glycol 400, heat it in a water bath to 70°C and keep it warm, then add 5.0 mg of entecavir into it, and stir until dissolved. Form a solution ①, then add 20mg of povidone K30 into the solution ①, stir and dissolve. If adding preservatives, add preservatives and stir to dissolve. Serve the content composition of entecavir soft capsule, inject this composition in the soft capsule preparation machine, regulate the injection rate of machine, make the content composition of entecavir soft capsule of every soft capsule 0.2g, entecavir active component content is 0.5mg.

Embodiment 2

[0029] Prepare the following soft capsules with the following composition by synchronously synchronizing according to embodiment 1, just as the povidone consumption of solubilizing agent is different or increases preservative:

[0030] 2-a Component Content (mg / capsule)

[0031] Entecavir 0.5

[0032] Polyethylene glycol 400 197.0

[0033] Povidone K30 2.5

[0034] Total 200.0

[0035] 2-b Component Content (mg / capsule)

[0036] Entecavir 0.5

[0037] Polyethylene glycol 400 198.5

[0038] Povidone K30 1.0

[0039] Total 200.0

[0040] 2-c Component Content (mg / capsule)

[0041] Entecavir 0.5

[0042] Polyethylene glycol 400 196.5

[0043] Povidone K30 3.0

[0044] Total 200.0

[0045] 2-d Component Content (mg / capsule)

[0046] Entecavir 0.5

[0047] Polyethylene glycol 400 196....

Embodiment 3

[0052]Weigh 1969 mg of polyethylene glycol 400, heat it in a water bath to 70°C and keep it warm, then add 5.0 mg of entecavir into it, and stir until dissolved. into a solution ①, then add 20 mg of povidone K30 into the solution ①, stir, dissolve, and form a solution ②, add poloxamer 188 6 mg, stir at a high speed, and stir until it becomes a milky white liquid. If preservatives are added, add preservatives, Stir, dissolve. Serve the content composition of entecavir soft capsule, this composition is injected in the soft capsule preparation machine, regulate the injection rate of machine, make the content composition of entecavir soft capsule of every soft capsule 0.2g, entecavir active ingredient content is 0.5mg.

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PUM

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Abstract

The invention relates to a soft capsule with an active component inhibiting hepatitis virus, in particular to an Entecavir soft capsule with high dissolubility, low penetration rate and stable property. The Entecavir soft capsule comprises a soft capsule shell and a content composition, wherein the content composition comprises the following components by 100 percent of total weight of the composition: 0.05-1.0 percent of Entecavir, 80-99.85 percent of filling solvent and 0.10-5.0 percent of povidone; and the total weight of all components in the composition is 100 percent. The invention improves the dissolubility and stability of the Entecavir and can maintain a stable composition system under various conditions without precipitation; the Entecavir active component can not be changed along with the change of time and has uniform and consistent content and high storage stability, and impurities of the Entecavir active component can not increase by long-time storage. Compared with propylene glycol, the Entecavir soft capsule has low penetration rate and more stable composition system without sediment precipitation of the active component for long-time storage under a certain condition.

Description

technical field [0001] The invention relates to a soft capsule with an active ingredient for inhibiting hepatitis virus, in particular to an entecavir soft capsule with high solubility, low penetration rate and stable properties. technical background [0002] Entecavir (entecavir), its chemical name is 2-amino-9-[(1S,3S,4S)-4-hydroxy-3-hydroxymethyl-2-methylenepentyl]-1,9-hydrogen-6- H-purin-6-one-hydrate. The structural formula is as follows: [0003] [0004] Molecular formula: C 12 h 15 N 5 o 3 ·H 2 O molecular weight: 295.3. [0005] This product is white to off-white powder, slightly soluble in water, and its solubility increases in acid or alkaline aqueous solution. [0006] This product is a guanosine nucleoside analogue, which has inhibitory effect on hepatitis B virus (HBV) polymerase. It can become active triphosphate through phosphorylation, and the half-life of triphosphate in the cell is 15 hours. By competing with the natural substrate of HBV polym...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K31/522A61K47/32A61K47/34A61K47/44A61P31/20A61K47/10
Inventor 金三九
Owner 杭州浙中医药科技有限公司
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