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Method for preparing entecavir tablets

A Cavir tablet, Entecavir technology, applied in the directions of pill delivery, antiviral agents, pharmaceutical formulations, etc., can solve the problem of tablet uniformity and other problems, and achieve the solution of uniformity problem, simple and easy process, and reduction of production costs. Effect

Inactive Publication Date: 2012-04-18
NANJING YOKO PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Purpose of the invention: In view of the deficiencies in the prior art, the purpose of the present invention is to provide a method for preparing entecavir tablets, to solve the problem of uniformity of the tablets in the case of low drug content, and to realize that there is no need for a drying process operation, ready for direct compression

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] The components of the entecavir tablet are: 10g entecavir, 8.5kg microcrystalline cellulose PH-200LM, 300g Ac-Di-Sol, 500g povidone K30, 50g magnesium stearate.

[0015] Take by weighing 8.5kg microcrystalline cellulose PH-200LM, 3gAc-Di-Sol, 6g povidone K30 and mix uniformly with a three-dimensional mixer at room temperature, the mixing time is 10min, and set aside; disperse 10g entecavir with 500ml water for injection, and the dispersion time is 10 minutes, set aside; Spray the above-mentioned 500ml of water for injection containing the main drug on the above-mentioned excipients, then add 50g of magnesium stearate, mix evenly with a three-dimensional mixer, and the mixing time is 5min. Mix well. Die compression, a total of 50,000 pieces, to measure the content of intermediates; wherein, the compression hardness is 6kg, and the mold is 7mm.

Embodiment 2

[0017] The composition of entecavir tablet is: 70g entecavir, 9kg microcrystalline cellulose PH-200LM, 200g Ac-Di-Sol, 200g povidone K30, 100g magnesium stearate, 800ml water for injection.

[0018] Weigh 9kg of microcrystalline cellulose PH-200LM, 500g of Ac-Di-Sol, and 600g of povidone K30 and mix them uniformly with a three-dimensional mixer at room temperature for 5 minutes for later use; disperse 100g of entecavir with 800ml of water for injection for 5 minutes , set aside; the above-mentioned 800ml of water for injection containing the main drug is sprayed on the above-mentioned excipients, and then 50g of magnesium stearate is added, and mixed evenly with a three-dimensional mixer, and the mixing time is 2min. Mix well. Die compression, a total of 50,000 pieces, to measure the content of intermediates; wherein, the compression hardness is 7kg, and the mold is 8mm.

Embodiment 3

[0020] The components of the entecavir tablet are: 0.7g entecavir, 80g microcrystalline cellulose PH-200LM, 3g Ac-Di-Sol, 5g povidone K30, 0.9g magnesium stearate, 700ml water for injection.

[0021] Weigh 8kg of microcrystalline cellulose PH-200LM, 500g of Ac-Di-Sol, and 600g of povidone K30 and mix them uniformly with a three-dimensional mixer at room temperature for 30 minutes and set aside; disperse 80g of entecavir with 700ml of water for injection for 30 minutes , set aside; the above-mentioned 700ml of water for injection containing the main drug is sprayed on the above-mentioned excipients, and then 100g of magnesium stearate is added, and mixed evenly with a three-dimensional mixer for 10 minutes, and mixed evenly. Mold compression, a total of 50,000 pieces, to measure the content of intermediates; wherein, the compression hardness is 8kg, and the mold is 9mm.

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Abstract

The invention discloses a method for preparing entecavir tablets, which comprises: preparing an auxiliary material for later use by uniformly mixing a filling agent, a disintegrating agent and a bonding agent in formula amount; dispersing entecavir in a formula amount into injection water to obtain a main medicine for later sue; and uniformly spreading the main medicine into the auxiliary material, adding lubricating agent, uniformly mixing, measuring the content of an intermediate, tabletting and obtaining entecavir tablets. The preparation of the entecavir tablets adopts a spray gun to spray the main medicine into the pre-mixed medicinal auxiliary material, so the uniformity problem of the tablets under a condition of low medicine content is solved. In addition, as the low-water-content microcrystalline cellulose PH-200LM as the filling agent of the entecavir tablets, tabletting can be performed without using a drying process; and the direct tabletting process is simpler and easier to implement than a wet-process granulation, fluidized bed granulation and spray drying processes and other processes, is suitable for industrial production and favorable for product quality control, energy conservation and consumption reduction, can reduce production cost and has high practicality.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to a method for preparing entecavir tablets. Background technique [0002] Entecavir is a deoxyguanosine analog that can effectively inhibit the replication of hepatitis B virus and has a strong anti-HBV effect. It can inhibit the three stages of HBV DNA replication initiation, retrovirus and DNA positive strand synthesis. The effect of Entecavir is to inhibit HBV DNA polymerase and retrovirus, thereby inhibiting the replication of HBV by pre-gene RNA retrovirus DNA negative strand, thereby inhibiting the synthesis of the positive strand, thereby blocking the elongation and assembly of the HBV DNA chain. It has been clinically proven to have a good inhibitory effect on hepatitis B virus. It is currently clinically used to treat chronic hepatitis B infection in adults with active virus replication and persistently elevated serum transaminases, or active liver hi...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/522A61K47/38A61P1/16A61P31/20
Inventor 高建兴张峰陆军曹燕锋姜东成
Owner NANJING YOKO PHARMA GRP CO LTD
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