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Magnesium valproate sustained-release tablet and preparing method thereof

A technology of magnesium valproate and sustained-release tablets, which is used in pharmaceutical formulations, anhydride/acid/halide active ingredients, and pill delivery, etc., can solve the problems of packaging, transportation, storage inconvenience, low drug release stability, and gastrointestinal tract. The problem of high irritation, etc., to achieve stable therapeutic effect, simple and easy preparation method, and easy absorption.

Inactive Publication Date: 2016-04-06
HEILONGJIANG ZHICHENG MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, among the magnesium valproate drugs for the treatment of epilepsy and mania on the market, there are shortcomings such as low drug release stability, high irritation to the gastrointestinal tract, low bioavailability, inconvenient packaging, transportation, and storage, and complicated preparation methods.

Method used

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  • Magnesium valproate sustained-release tablet and preparing method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] A sustained-release magnesium valproate tablet is characterized in that: it is made of the following raw materials: 250 mg magnesium valproate, 150-245 mg hypromellose, and 5-20 mg lubricant.

[0026] The preferred weight ratio of the raw materials is: 250mg magnesium valproate, 140mg hypromellose, 10mg lubricant.

[0027] The hypromellose can be one or two of the following models: 75hd100cr hypromellose, 75hd4000cr hypromellose, 75hd15000cr hypromellose, 100000cr hypromellose.

[0028] The lubricant is one or both of magnesium stearate, talcum powder and silicon dioxide.

[0029] Its production method includes the following steps:

[0030] Step 1: material preparation: according to the above mass ratio, magnesium valproate is pulverized with a pulverizer, and passed through a 100-mesh sieve;

[0031] Step 2: Mixing: Weigh magnesium valproate and hypromellose according to the above mass ratio, put them into a three-dimensional mixer and mix for 30 minutes to make medi...

Embodiment 2

[0038] Indications:

[0039] 1. Antiepileptic: for the treatment of generalized or partial epilepsy, especially the following types: absence seizures, myoclonic seizures, tonic-clonic seizures, atonic seizures and mixed seizures and partial epilepsy: simple or complex seizures; secondary generalized seizures; special types of syndromes (West, Lennox-Gastaut).

[0040] 2. Anti-mania: It is mainly used for the treatment of acute mania, bipolar mania and schizoaffective mania.

Embodiment 3

[0042] medicine interactions:

[0043] 1. Drinking alcohol can increase the sedative effect.

[0044] 2. When general anesthetics or central nervous system depressants are used together with valproic acid, the clinical effect of the former may be more obvious.

[0045] 3. Combined with anticoagulant drugs such as warfarin or heparin, and thrombolytic drugs, the risk of bleeding increases.

[0046] 4. When combined with aspirin or dipyridamole, the bleeding time is prolonged due to the reduction of platelet aggregation.

[0047] 5. When used in combination with phenobarbitals, the metabolism of the latter slows down and the blood concentration increases, thus increasing the sedative effect and causing drowsiness.

[0048] 6. Combined use with primidone can also cause an increase in blood concentration and lead to poisoning, and the dosage of primidone should be reduced if necessary.

[0049] 7. Combined with clonazepam to prevent and treat absence seizures, it has been repor...

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Abstract

The invention discloses a magnesium valproate sustained-release tablet and a preparing method thereof. The magnesium valproate sustained-release tablet is prepared from magnesium valproate, hydroxypropyl methylcellulose and a lubricating agent through the process steps of material preparing, mixing, granulating, total mixing, tabletting, aluminum-plastic packaging and the like. The magnesium valproate sustained-release tablet mainly has the antiepileptic and anti-mania treatment effects. A novel sustained release preparation is adopted, according to the definition of sustained release, the absorption efficiency of a drug entering an organism is reduced by reducing the drug release speed of the drug in the dosage form, and therefore a more stable treatment effect is achieved; the effective blood concentration can be kept in a long time, the toxic and side effects of the drug can be reduced, and drug use safety is improved. The drug is convenient to use and particularly suitable for patients with chronic diseases and improves compliance of patients. The magnesium valproate sustained-release tablet has the advantages of being high in stability, convenient to package, transport and store and the like, and the preparing method is simple, easy to implement and suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of chemical drug sustained-release preparations, and in particular relates to a magnesium valproate sustained-release tablet and a preparation method thereof. Background technique [0002] Epilepsy, commonly known as "shorn wind" or "epilepsy", is a chronic disease in which the sudden abnormal discharge of brain neurons leads to transient brain dysfunction. According to the latest epidemiological data in China, the overall prevalence rate of epilepsy in China is 7.0‰, the annual incidence rate is 28.8 / 100,000, and the prevalence rate of active epilepsy with seizures within one year is 4.6‰. Based on this, it is estimated that there are about 9 million epilepsy patients in China, of which 5 to 6 million are active epilepsy patients, and about 400,000 new epilepsy patients are added every year. In China, epilepsy has become the second most common disease in neurology after headache. sick. [0003] Mania is listed as a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K47/38A61P25/08A61P25/18
CPCA61K9/2054A61K9/0002A61K31/19
Inventor 张昕
Owner HEILONGJIANG ZHICHENG MEDICAL TECH
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