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A kind of preparation method of eslicarbazepine acetate tablet

A technology of eslicarbazepine acetate and tableting, applied in the field of preparation of eslicarbazepine acetate tablets, can solve problems such as differences in prescription composition

Active Publication Date: 2019-12-17
YANGTZE RIVER PHARMA GRP BEIJING HAIYAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Though also have the report about the prescription composition of eslicarbazepine acetate sheet in the prior art, its prescription composition is all the same as There is a big difference

Method used

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  • A kind of preparation method of eslicarbazepine acetate tablet
  • A kind of preparation method of eslicarbazepine acetate tablet
  • A kind of preparation method of eslicarbazepine acetate tablet

Examples

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preparation example Construction

[0050] The invention provides a preparation method of eslicarbazepine acetate tablets, wherein the raw materials of said eslicarbazepine acetate tablets are composed of 400 parts by weight of eslicarbazepine acetate, 28-28 parts by weight of croscarmellose sodium 32 parts by weight, 34 to 36 parts by weight of povidone, and 3 to 4 parts by weight of magnesium stearate; wherein, 16 to 20 parts by weight of croscarmellose sodium are added, and the balance is added externally; Add 18 parts by weight, and the balance is added;

[0051] Described preparation method comprises the steps:

[0052] I. Grinding of active ingredients

[0053] Eslicarbazepine acetate is pulverized with a hammer mill. When the loading capacity is 400-500g each time, pulverize for 3-4 seconds each time, repeat 3 times, so that the particle size D50<20μm, D90<80μm and D(4, 3) <40 μm, passing through a 40-mesh sieve to obtain crushed and sieved eslicarbazepine acetate, which is set aside;

[0054] II. Mixi...

Embodiment 1

[0083] Example 1 Eslicarbazepine Acetate Tablets Determination of disintegration time and dissolution

[0084] According to the above method, determine The disintegration time and dissolution in the acidic medium of pH=1.2, the results are shown in Table 1.

[0085] Table 1 Disintegration time and dissolution measurement results

[0086]

[0087] As the basis of bringing into play biological activity, the eslicarbazepine acetate tablet prepared by the present invention should be as close as possible to that in disintegration time and dissolution. slices remain consistent.

Embodiment 2

[0088] Example 2 Research and optimization of crushing method of eslicarbazepine acetate

[0089] The inventors have found that after crushing eslicarbazepine acetate, the phenomenon of electrostatic agglomeration is serious, which is not suitable for further processing and needs to be sieved before agglomeration. This example studies the impact of crushing and sieving methods on the tabletability and dissolution of granulated granules.

[0090] The prescription of the eslicarbazepine acetate sheet of the present embodiment is composed as follows, wherein 0.1g=1 weight part:

[0091]

[0092] Prepared through the following steps:

[0093] According to the above prescription, prepare 6 parts of raw and auxiliary materials, numbered 1-6; then process eslicarbazepine acetate respectively according to the crushing and sieving methods shown in Table 2, to obtain eslicarbazepine acetate after crushing and sieving, Determination of bulk density and particle size (D10, D50, D90...

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Abstract

The invention relates to a preparation method of eslicarbazepine acetate tablets; the eslicarbazepine acetate tablets comprise the raw materials: 400 parts by weight of eslicarbazepine acetate, 28-32 parts by weight of croscarmellose sodium, 34-36 parts by weight of povidone, and 3-4 parts by weight of magnesium stearate, wherein 16 parts by weight of the croscarmellose sodium is internally added, and the remaining croscarmellose sodium is externally added; 18 parts by weight of the povidone is internally added, and the remaining povidone is externally added. The preparation method comprises the steps: I, active ingredient crushing; II, mixing of granulating materials; III, granulation; IV, drying; V, size stabilization; VI, external addition of accessories and mixing; and VII, tabletting.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a preparation method of eslicarbazepine acetate tablets. Background technique [0002] Eslicarbazepine acetate (ESL), also known as eslicarbazepine acetate, chemical name (S)-10-acetyl-10,11 dihydro-5H-dibenzo[b,f] Azepine-5-carboxamide, the structural formula is as shown in I. It is indicated for the adjunctive treatment of partial-onset seizures in adult patients with epilepsy with or without secondary generalized seizures. ESL is similar to carbamazepine and oxcarbazepine in chemical structure, and its advantage is that it can avoid the formation of toxic metabolites such as epoxides, and at the same time reduce the proportion of inactive components in metabolites, reduce the incidence of adverse reactions, improve pharmacological activity. Phase I-III clinical trials have shown that ESL has good efficacy and tolerability for adults with partial-onset epilepsy who...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K31/55A61K47/38A61K47/32A61P25/08
CPCA61K9/2027A61K9/2054A61K9/2095A61K31/55
Inventor 陈东王芳刘文东袁峰泉刘晓丽
Owner YANGTZE RIVER PHARMA GRP BEIJING HAIYAN PHARMA