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Sodium valproate sustained release tablet as well as preparation process and application thereof

A technology of sodium valproate and valproic acid, which is applied in non-active ingredients medical preparations, anhydride/acid/halide active ingredients, nervous system diseases, etc. Poor uniformity and other problems, to achieve the effect of less type and dosage of excipients, low equipment requirements, and stable drug release rate

Active Publication Date: 2015-11-04
SICHUAN CREDIT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the strong hygroscopicity of sodium valproate, the production conditions are very strict when used in the preparation of solid preparations (environmental temperature and humidity need to be strictly controlled), and the humidity must be controlled at at least about 20%. Such harsh production conditions will lead to production Significant increase in link energy consumption and process difficulty, and high energy consumption will lead to high cost, which is very unfavorable for industrialized mass production;
[0008] 2. The prescription is complex, with many types of excipients and large dosage
In the existing technology, in order to achieve a better drug release effect, it is often necessary to use a variety of release-retarding materials to adjust the drug release performance of the drug, which will lead to complex prescriptions or large dosages of preparations, and more opportunities to introduce impurities , increase preparation cost and preparation difficulty;
[0009] 3. The drug release time does not reach 24 hours, and it still needs to be taken several times a day
In the prior art, there is no bibliographical report of 24-hour sodium valproate sustained-release tablet, and only 8-hour drug release is reported in open literature;
[0010] 4. The drug release effect is not ideal, and the drug release uniformity is poor
The drug release uniformity of the sustained-release tablets of the existing technology is not ideal, and the blood drug concentration fluctuates greatly, which is not conducive to clinical treatment;

Method used

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  • Sodium valproate sustained release tablet as well as preparation process and application thereof
  • Sodium valproate sustained release tablet as well as preparation process and application thereof
  • Sodium valproate sustained release tablet as well as preparation process and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041]Preparation process: mix sodium valproate, hydroxypropylmethylcellulose and microcrystalline cellulose through a 60-mesh sieve according to the dosage in Table 1. Add liquid valproic acid and 95% ethanol to the above mixture to make a soft material, pass through a 20-mesh sieve to make wet granules, dry at 60°C for 2 hours, and sizing the granules with a 20-mesh sieve. The obtained granules are added with micropowder silica gel and a lubricant, mixed evenly, and compressed into tablets to obtain slow-release tablets.

[0042] Table 1 Sodium valproate sustained-release tablets (1000 tablets)

[0043]

[0044] In vitro release assay:

[0045] The first method of release measurement method in appendix XD of the Chinese Pharmacopoeia 2010 edition was selected, using 900ml phosphate buffer solution (pH6.8) as the release medium, and the rotation speed was 60 rpm, at the predetermined time points (1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 20, 24h) samples were taken to determine t...

Embodiment 2

[0050] Adopt the sodium valproate slow-release tablet among the embodiment 1 to carry out stability study, investigate the sodium valproate slow-release tablet that makes with this prescription process at 40 ℃ ± 2 ℃, under the condition of relative humidity 75% ± 5% Placed for 6 months of stability. Measured by the items in Table 9 in the 0th, 1st, 2nd, 3rd, and 6th months respectively, the measurement results are the mean values ​​of the measurement results of the samples selected under each prescription in Example 1.

[0051] Table 3 Example 1 Prescription Stability Investigation

[0052]

[0053] The above stability test results show that the slow-release tablet prepared according to the prescription in Example 1 has been subjected to an accelerated test for 6 months, and all indicators are up to the standard, and its stability meets the requirements.

Embodiment 3

[0055] Preparation process: According to the dosage in Table 4 and Table 7, sodium valproate, blocking agent and filler are passed through a 60-mesh sieve for mixing. Add liquid valproic acid and 95% ethanol to the above mixture to make a soft material, pass through a 20-mesh sieve to make wet granules, dry at 60°C for 2 hours, and sizing the granules with a 20-mesh sieve. The obtained granules are added with micropowder silica gel and magnesium stearate, mixed evenly, and compressed into tablets to obtain slow-release tablets.

[0056] Table 4 Prescription of Sodium Valproate Sustained Release Tablets (1000 Tablets)

[0057] prescription

7

8

9

10

11

Sodium valproate (g)

333

333

333

333

333

Valproic acid (g)

145

145

145

145

145

HPMC E5 (g)

-

-

-

-

-

HPMC K4M (g)

100

-

-

-

-

HPMC K10M (g)

-

100

-

-

-

HPMC K15M...

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Abstract

The invention discloses a sodium valproate sustained release tablet and also discloses a prescription and preparation process of the sustained release tablet. The sustained release tablet can continuously and stably release drugs in 24 hours, so that more stable blood concentration is obtained after patients take the drug, side effects are reduced and the compliance of the patients is increased. The preparation process of the sustained release tablet is simple and is convenient for industrial production.

Description

technical field [0001] The invention relates to a sodium valproate sustained-release tablet, a preparation process and application thereof. Background technique [0002] Valproic acid and its derivatives belong to the first-line antiepileptic drugs, and they all act in the form of valproic acid after being absorbed by the body. Partial motor seizures, absence seizures, and infantile spasms. Today, the therapeutic field of valproic acid and its derivatives is still expanding. In addition to anti-epilepsy, the FDA-approved indications include bipolar disorder and migraine. [0003] Clinically, the effective blood concentration of valproic acid and its related salts is usually in the range of 40-100 μg / ml, but due to its short biological half-life, it usually requires multiple doses a day for treatment with this drug (eg three times a day) to maintain adequate blood levels. However, due to the frequent administration, the patient's compliance with taking the medicine will be...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K31/19A61K47/38A61P25/08A61P25/00A61P25/06
Inventor 何勤况其方林科名李文婕陈刚
Owner SICHUAN CREDIT PHARMA
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