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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, increase solubility and stability, and increase storage stability

Active Publication Date: 2011-05-11
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, place it in a water bath and heat it to 70°C to keep it warm, then add 5.0 mg of entecavir to it and stir until it dissolves. To form a solution ①, then add 20 mg of Povidone K30 to the solution ①, stir and dissolve. If preservative is added, add preservative and stir to dissolve. Serve the entecavir soft capsule content composition, inject this composition into the soft capsule preparation machine, adjust the injection volume of the machine, so that the content of the entecavir soft capsule content composition of 0.2g per soft capsule contains 0.5mg of the active ingredient of entecavir.

Embodiment 2

[0029] According to Example 1, the following soft capsules with the following components were prepared by simultaneous polymerization, except that the amount of povidone used as a solubilizer was different or the preservative was added:

[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 400 196.5

[0048] Propy...

Embodiment 3

[0052] Weigh 1969 mg of polyethylene glycol 400, place it in a water bath and heat it to 70°C to keep it warm, then add 5.0 mg of entecavir to it and stir until it is dissolved. To form a solution ①, then add 20 mg of Povidone K30 to the solution ①, stir and dissolve, to form a solution ②, add poloxamer 188 6 mg, stir at high speed, and stir until a milky white liquid. If adding preservative, add preservative, stir and dissolve. Serve the entecavir soft capsule content composition, inject this composition into the soft capsule preparation machine, adjust the injection volume of the machine, so that the content of the entecavir soft capsule content composition of 0.2g per soft capsule contains 0.5mg of the active ingredient of entecavir.

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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 active ingredients 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-hydro-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 solutions. [0006] This product is a guanine nucleoside analog, which has an inhibitory effect on hepatitis B virus (HBV) polymerase. It can be phosphorylated into active triphosphate, the half-life of triphosphate in the cell is 15 hours. By competing with deoxyguanosine triphosphate, the natural substrate of HBV polymerase, ...

Claims

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Application Information

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Patent Type & Authority Patents(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