Heavy-load valproic acid drug sustained release tablet and preparation method thereof

A technology for valproic acid and sustained-release tablets, which is applied in directions such as pharmaceutical formulations, drug combinations, and drug delivery, can solve the problems of complex preparation process, unstable release and high production cost, and achieves simple preparation process, convenient swallowing, Easy-to-operate effects

Active Publication Date: 2014-11-19
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] Although there are many slow-release preparations prepared with valproic acid and its derivatives as active ingredients in the prior art to control the release of drugs, there are certain defects, such as film-controlled slow-release preparations due to its complicated preparation process, The production cost is high, and the problem of solvent residue is easy to occur during the coating process. Due to the complex process...

Method used

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  • Heavy-load valproic acid drug sustained release tablet and preparation method thereof
  • Heavy-load valproic acid drug sustained release tablet and preparation method thereof
  • Heavy-load valproic acid drug sustained release tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Sodium valproate extended-release tablets:

[0049]

[0050] Tablet weight is 824mg, made into 1000 pieces

[0051] Preparation Process:

[0052] Sodium valproate and auxiliary materials are passed through an 80-mesh sieve, the molecular weight of chitosan is 400kDa, and the degree of deacetylation is 50%, and each component except the lubricant magnesium stearate and the anti-adhesive micropowder silica gel is mixed in equal amounts Evenly, add an appropriate amount of 70% ethanol solution as a binder, make a soft material, granulate, dry at 55°C, granulate, add lubricant magnesium stearate and anti-sticking agent micro-powder silica gel to mix evenly, place Compressed into tablets in a tablet machine.

[0053] The self-made sustained-release tablet was placed in the dissolution vessel for dissolution test, and the in vitro release results were as follows: figure 1 shown.

Embodiment 2

[0055] Compound Sodium Valproate Sustained Release Tablets:

[0056]

[0057]

[0058] Tablet weight is 882mg, made into 1000 pieces

[0059] Preparation Process:

[0060] The sodium valproate and auxiliary materials are passed through an 80-mesh sieve, and the liquid valproic acid is adsorbed by adsorbent micropowder silica gel, so that it is adsorbed into a uniform powder, and then chitosan (400kDa, deacetylation degree 75%), alginic acid Add sodium, sodium carboxymethylcellulose, and sodium valproate in sequence, and mix well. Add an appropriate amount of 70% ethanol solution as a binder, make soft materials, granulate, dry at 55°C, granulate, add lubricant magnesium stearate and anti-sticking agent micro-powder silica gel, mix well, place Compressed into tablets in a tablet machine.

[0061] The self-made sustained-release tablet was placed in the dissolution vessel for dissolution test, and the in vitro release results were as follows: figure 1 shown.

Embodiment 3

[0063] Compound Sodium Valproate Sustained Release Tablets

[0064]

[0065] The tablet weight is 902mg to make 1000 tablets

[0066] Preparation Process:

[0067] The sodium valproate and auxiliary materials are passed through 80 mesh sieves, and the liquid valproic acid is adsorbed by adsorbent pregelatinized starch, so that it is absorbed into a uniform powder, and then chitosan (200kDa, deacetylation degree 75%), Add sodium alginate, carrageenan, and sodium valproate in sequence, and mix well. Add an appropriate amount of 50% ethanol solution as a binder, make soft materials, granulate, dry at 80°C, granulate, add lubricant magnesium stearate and anti-sticking agent micro-powder silica gel, mix well, place Compressed into tablets in a tablet machine.

[0068] The self-made sustained-release tablet was placed in the dissolution vessel for dissolution test, and the in vitro release results were as follows: figure 1 shown.

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Abstract

The invention relates to a heavy-load valproic acid drug sustained release tablet and a preparation method of a heavy-load valproic acid drug sustained release tablet and belongs to the field of pharmaceutical preparations. The heavy-load valproic acid drug sustained release tablet is mainly used for treating clinically primary generalized epilepsy. A valproic acid drug comprises valproic acid and pharmaceutically acceptable salt, ester or amide. According to the invention, a novel hydrophilic gel skeleton controlled release system is applied; in polymer matrix selection, a novel controlled release matrix material with good biocompatibility is selected; and the controlled release matrix is a composition of chitosan and one or more of, but not limited to, sodium alginate, sodium carboxymethylcellulose, carrageenan, xanthan gum, hyaluronic acid, polyacrylic resin and an acrylic polymer. Synergic control of slow release of a drug composite is achieved through joint application of different polymers and the chitosan and by employing property difference of the different polymers and intelligent interaction with the chitosan, a combined action of different drug release mechanisms is realized, and a slow release effect of the drug composite up to 24h can be achieved.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a high-loaded valproic acid sustained-release tablet and a preparation method thereof, and also relates to the application of the sustained-release tablet in the preparation of drugs for treating primary generalized epilepsy. Background technique [0002] Valproic acid, the chemical name is 2-propylpentanoic acid, the structural formula is [0003] [0004] Certain salts of this acid such as sodium valproate and esters and its amide form valproamide (VPO) are effective in the treatment of seizures or as antipsychotics. [0005] Valproic acid and its derivatives, as first-line antiepileptic drugs, have been widely used in the treatment of epilepsy and as antipsychotic drugs. + Channel-related: It inhibits γ-aminobutyric acid (GABA) metabolic enzymes, accumulates GABA in the brain, inhibits excessive discharge of focal neurons, and inhibits the spread of discharge. V...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K31/19A61K47/36A61K47/38A61P25/08
Inventor 毛世瑞邵杨
Owner SHENYANG PHARMA UNIVERSITY
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