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Method for preparing flupirtine maleate capsule

A technology of flupirtine maleate capsules and flupirtine maleate, which is applied in the field of preparation of flupirtine maleate capsules, can solve the problems of gastrointestinal corrosion and not recommend large-scale use, and achieve improved dissolution rate and improved dissolution rate and dissolution rate, the effect is obvious

Active Publication Date: 2012-11-14
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 method for preparing a flupirtine maleate capsule. The method comprises the following steps of: (A) weighting calcium hydrophosphate, crosslinking polyvinylpyrrolidone, lauryl sodium sulfate, magnesium stearate and superfine silica powder according to a formula and sieving through a sieve of 100 meshes; (B) performing superfine grinding on a flupirtine maleate raw material according to the formula until the particle size is 10 to 25 mu m, and uniformly mixing the treated flupirtine maleate raw material with the auxiliary materials in the step (A) according to an equivalent adding method; (C) granulating 50 percent of ethanol solution with the volume of 80 to 100 ml serving as an adhesive preparation soft material after sieving through a sieve of 20 meshes; (D) drying the wet particles prepared in the step (C) at the temperature of 55 to 65 DEG C for 2 to 4 hours, and arranging the particles after sieving through the sieve of 20 meshes; and (E) uniformly mixing the magnesium stearate and the superfine silica powder according to the formula, and filling to obtain the flupirtine maleate capsule. The method is ingenious in concept and simple in flow; the flupirtine maleate capsule is high in blood concentration, small in medicine amount and high in bioavailability; and the pain treating effect is obvious.

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 Applications(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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