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Composition of valpromide sustained release tablets and preparation method thereof

A technology of valproamide and valproamide intestine, which is applied in the field of medicine, can solve the problems of no practical application significance, poor stability of natural protein, stability of slow and controlled release preparations that do not meet the requirements of druggability, etc.

Pending Publication Date: 2022-07-01
湖南省湘中制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, valproamide is an insoluble drug, and it is often difficult to obtain an ideal sustained and controlled release preparation for general insoluble drugs using simple sustained and controlled release technology (skeleton or membrane control technology). Patent US 4913906 uses natural proteins to control the release of valproamide. release speed to prepare its sustained and controlled release preparations, but due to the poor stability of natural protein (soybean protein), the stability of the slow and controlled release preparations prepared in this way does not meet the requirements of druggability, and has no practical application significance

Method used

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  • Composition of valpromide sustained release tablets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] 300mg Valpromide Sustained Release Tablets

[0044] Skeleton Chip

[0045] Valpromide 300mg

[0046] HPMC-K4M 70mg

[0047] MCC 30 mg

[0048] Lactose 40mg

[0049] PVP-K30 12mg

[0050] MS 7mg

[0051] Docusate Sodium 15mg

[0052] normal film coat

[0053] Gastric Dissolved HPMC 25mg

[0054] PEG 2.0mg

[0055] Talc (100 mesh) 5mg

[0056] Enteric coating

[0057] Enteric acrylic resin 20mg

[0058] Phthalates 2.5mg

[0059] Talc (100 mesh) 7mg

[0060] production method:

[0061] (1): Mix valproamide, HPMC-K4M, MCC, lactose, docusate sodium, etc., granulate with PVP-K30 ethanol or aqueous solution, dry, and sieve;

[0062] (2): mixing the particles obtained in step (1) with MS;

[0063] (3): compress the mixture obtained in step (2) on a tablet press to obtain a round or oval tablet with a hardness of 6-8kg;

[0064] (4): Or mix the main drug with a variety of excipients and directly compress it.

[0065] (5): mix gastric-soluble HPMC, PEG, and talc...

Embodiment 2

[0069] 300mg Valpromide Sustained Release Tablets

[0070] Skeleton Chip

[0071] Valpromide 300mg

[0072]HPMC-K4M 90mg

[0073] MCC 20mg

[0074] Lactose 30mg

[0075] PVP-K30 15mg

[0076] MS 10mg

[0077] Tween-80 20mg

[0078] normal film coat

[0079] Gastric Dissolved HPMC 35mg

[0080] PEG 2.5mg

[0081] Talc (100 mesh) 8mg

[0082] Enteric coating

[0083] Enteric acrylic resin 60mg

[0084] Triethyl citrate 4mg

[0085] Talc (100 mesh) 10mg

[0086] production method:

[0087] (1): Mix valproamide, HPMC-K4M, MCC, lactose, etc., adopt the ethanol or aqueous solution of PVP-K30 and Tween-80 to granulate, dry, and sieve;

[0088] (2): mixing the particles obtained in step (1) with MS;

[0089] (3): compress the mixture obtained in step (2) on a tablet press to obtain round or oval tablets with a hardness of 7-9kg;

[0090] (4): Or mix the main drug with a variety of excipients and directly compress it.

[0091] (5): mix gastric-soluble HPMC, PEG, and t...

Embodiment 3

[0095] 300mg Valpromide Sustained Release Tablets

[0096] Skeleton Chip

[0097] Valpromide 300mg

[0098] HPMC-K4M 70mg

[0099] MCC 30 mg

[0100] Lactose 40mg

[0101] PVP-K30 12mg

[0102] MS 7mg

[0103] Sodium Lauryl Sulfate 25mg

[0104] normal film coat

[0105] Gastric Dissolved HPMC 25mg

[0106] PEG 2.0mg

[0107] Talc (100 mesh) 5mg

[0108] Enteric coating

[0109] Enteric acrylic resin 20mg

[0110] Glycerin 3.0mg

[0111] Talc (100 mesh) 7mg

[0112] production method:

[0113] (1): Mix valproamide, HPMC-K4M, MCC, lactose, sodium lauryl sulfate, etc., granulate with ethanol or aqueous solution of PVP-K30, dry, and sieve;

[0114] (2): mixing the particles obtained in step (1) with MS;

[0115] (3): compress the mixture obtained in step (2) on a tablet press to obtain round or oval tablets with a hardness of 5-7kg;

[0116] (4): Or mix the main drug with a variety of excipients and directly compress it.

[0117] (5): mix gastric-soluble HPMC, P...

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Abstract

The invention belongs to the technical field of pharmaceutical preparations. The invention provides an enteric sustained-release preparation of antiepileptic drug valpromide, which is taken once a day. The preparation is in a form of a sustained-release matrix tablet core and an enteric coated sustained-release tablet. Wherein the tablet core skeleton sustained-release material is a cellulose derivative, especially cellulose ether, such as HPMC, CMC, MC and HPC, the coating isolation layer contains one or more of gastric-soluble HPMC, HPC, PEG, PVP and AEA, and the enteric layer contains one or more of enteric HPMC, acrylic resin, PAP, CAP and the like. The preparation is convenient for patients to take and has few side effects.

Description

technical field [0001] The invention belongs to the field of medicine and relates to a composition of valpromide sustained-release tablets and a preparation method thereof. Background technique [0002] Valpromide is a prodrug of valproic acid, which is metabolized into valproic acid in the body to play a therapeutic role, so its clinical use is the same as that of valproic acid, and it is also used for the treatment of epilepsy. The reported half-life of valproic acid is 6-17 hours in adults and 4-14 hours in children. This results in considerable fluctuations in the plasma concentration of the drug, especially during chronic administration. Frequent dosing is required to maintain adequate and stable plasma concentrations, often making patients less accustomed to the prescribed dosing regimen. In addition, the wide fluctuations in plasma concentrations of the drug may result in lower than therapeutic amounts of the drug administered in conservative dosing regimens, or amo...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K9/36A61K47/02A61K47/32A61K47/10A61K47/20A61K47/26A61K47/38A61K31/16A61P25/08
CPCA61K9/2095A61K9/2813A61K9/2846A61K9/2853A61K9/2013A61K9/2018A61K9/2054A61K9/2866A61K9/2886A61K31/16A61P25/08
Inventor 谢向明杨贞皓尹文乐
Owner 湖南省湘中制药有限公司