Method for preparing flupirtine maleate capsule

The technology of flupirtine acid capsules and flupirtine maleate is applied in the field of preparation of flupirtine maleate capsules, which can solve the problems of gastrointestinal corrosion, and it is not recommended to use it in large quantities, so as to improve the dissolution rate and the dissolution rate. And the dissolution rate, the effect is obvious

Active Publication Date: 2014-09-03
SICHUAN BAILI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, in the preparation process of flupirtine maleate capsules, sodium lauryl sulfate is usually added to increase the solubility of flupirtine maleate. Sodium dialkyl sulfate is an anionic surfactant with severe foaming. Although it can speed up the melting speed of drugs, once it exceeds the standard, it will corrode the human stomach and intestines. It is not recommended to use it in large quantities

Method used

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  • Method for preparing flupirtine maleate capsule
  • Method for preparing flupirtine maleate capsule
  • Method for preparing flupirtine maleate capsule

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1: the preparation method of flupirtine maleate capsule, comprises the following steps:

[0032] 1. Weigh and crush 186.2g of calcium hydrogen phosphate and 12.0g of cross-linked polyvinylpyrrolidone through a 100-mesh sieve;

[0033] 2. Weigh 100g (10um) of flupirtine maleate superfine powder after superfine pulverization treatment, and mix it with the above-mentioned auxiliary materials evenly according to the method of equal addition;

[0034] 3. Use an appropriate amount of 50% ethanol solution as a binder to make soft materials, and pass through a 20-mesh sieve to granulate;

[0035] 4. Dry the wet granules at 60°C by blowing air, pass through a 20-mesh sieve, and granulate;

[0036] 5. Add 0.75g of magnesium stearate through a 100-mesh sieve, 0.75g of micropowder silica gel, and mix well;

[0037] 6. Detection of intermediate content;

[0038] 7. Filling, polishing, and blistering to obtain flupirtine maleate capsules.

[0039] The dissolution relea...

Embodiment 2

[0042] 1. Weigh and crush 186.2g of calcium hydrogen phosphate and 12.0g of cross-linked polyvinylpyrrolidone through a 100-mesh sieve;

[0043] 2. Weigh 100g (15um) of flupirtine maleate superfine powder after superfine pulverization, and mix it with the above-mentioned excipients evenly according to the method of equal volume addition;

[0044] 3. Use an appropriate amount of 50% ethanol solution as a binder to make soft materials, and pass through a 20-mesh sieve to granulate;

[0045] 4. Dry the wet granules at 60°C by blowing air, pass through a 20-mesh sieve, and granulate;

[0046] 5. Add 0.75g of magnesium stearate through a 100-mesh sieve, 0.75g of micropowder silica gel, and mix well;

[0047] 6. Detection of intermediate content;

[0048] 7. Filling, polishing, and blistering to obtain flupirtine maleate capsules.

[0049] The dissolution release data are as follows:

[0050] time (min) Dissolution rate of No.1 sample (%) Dissolution rate of No. 2 ...

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Abstract

The invention discloses a preparation method of flupirtine maleate capsules, comprising the following steps: A, taking the prescribed amount of calcium hydrogen phosphate, cross-linked polyvinylpyrrolidone, sodium lauryl sulfate, magnesium stearate, and micropowder silica gel , pass through 100 mesh sieves respectively; B, take the prescribed amount of flupirtine maleate raw material and carry out ultrafine pulverization treatment to 10-25um, then mix it with the auxiliary materials in step A according to the equal amount incremental method; C, take 80-100ml 50% ethanol solution is used as a binder to make soft materials, and granulated through a 20-mesh sieve; D. Dry the wet granules prepared in step C at a temperature of 55-65°C for 2-4 hours, and granulate through a 20-mesh sieve E. Add magnesium stearate and micropowder silica gel in the prescribed amount, mix well, and fill to obtain the required flupirtine maleate capsules. The invention has ingenious concept and simple process, and the prepared flupirtine maleate capsule has high blood drug concentration, small drug dose, high bioavailability and obvious pain treatment effect.

Description

technical field [0001] The invention belongs to the technical field of chemical pharmacy and relates to a preparation method of flupirtine maleate capsules. Background technique [0002] Flupirtine maleate (Chemical name: 2-amino-6-[(4-fluorobenzyl)amino]-3-pyridine carbamate ethyl ester maleate) opens selective neuronal potassium channels It is a non-opioid analgesic that acts on the central nervous system and does not produce dependence and tolerance. [0003] Flupirtine maleate capsules are reddish-brown hard capsules, and the contents are white or off-white granules and powder, suitable for acute mild and moderate pain: such as pain caused by exercise-induced muscle spasm. Flupirtine maleate is a drug with low solubility. For insoluble drugs or drugs with a very slow dissolution rate, the dissolution process of the drug often becomes the rate-limiting process of absorption. [0004] At present, in the preparation process of flupirtine maleate capsules, sodium lauryl su...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/48A61K31/44A61P25/04A61P21/02
Inventor 王一茜李芳
Owner SICHUAN BAILI PHARM CO LTD
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