Lurasidone hydrochloride oral preparation and preparing method of lurasidone hydrochloride oral preparation

A technology of lurasidone hydrochloride and oral preparations, which is applied in the field of medicine, can solve the problems of large static electricity of raw materials, inability to obtain sufficient immediate release and solubility, and large loss, and achieve small intra-batch differences, small losses, and high yields Effect

Active Publication Date: 2015-02-11
SHIJIAZHUANG NO 4 PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since lurasidone is a poorly soluble drug, sufficient immediate release and solubility cannot be obtained under many prescription preparation conditions
[0006] At present, in order to solve the above problems, some researchers micronize the raw materials to control the particle size of the raw materials in the preparation process of lurasidone hydrochloride p

Method used

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  • Lurasidone hydrochloride oral preparation and preparing method of lurasidone hydrochloride oral preparation
  • Lurasidone hydrochloride oral preparation and preparing method of lurasidone hydrochloride oral preparation
  • Lurasidone hydrochloride oral preparation and preparing method of lurasidone hydrochloride oral preparation

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0035] The preparation method of lurasidone hydrochloride tablet in following each embodiment is as follows:

[0036] (1) Weigh the prescription amount of lurasidone hydrochloride raw material and optional silicon dioxide, mix them, pulverize and control the particle size to 0.1-20 μm, and set aside;

[0037] (2) Preparation of an aqueous solution of a water-soluble polymer binder: a water-soluble polymer binder was dissolved in pure water. The amount of water-soluble polymer binder is for example 1 to 20wt% of pure water weight, preferably 2 to 8wt%, the water-soluble polymer binder that can be used is for example hypromellose, polyvinylpyrrolidone or polyvinyl alcohol .

[0038] (3) Preparation of granules containing lurasidone hydrochloride: adding a mixture containing lurasidone hydrochloride and optional silicon dioxide, mannitol, lactose, low-substituted hydroxypropyl cellulose, Croscarmellose Sodium, mix well. Add the aqueous binder solution prepared in (2) to make s...

Embodiment 1 and comparative example 1 and 2

[0044] (1) embodiment 1 and comparative example 1 and 2 raw materials and proportioning ratio as shown in table 1:

[0045] Table 1. Embodiment 1 and comparative examples 1 and 2 raw materials and proportioning (batch: 1000)

[0046]

Example 1

Comparative example 1

Comparative example 2

Lurasidone Hydrochloride

80.0g

80.0g

80.0g

Mannitol

116.0g

116.0g

144.0g

lactose

58.0g

58.0g

72.0g

[0047] Low-substituted hydroxypropyl cellulose (hydroxypropyl content%)

42.0g(11％)

50.0g(11％)

-

Croscarmellose Sodium

8.0g

-

8.0g

silica

6.0g

6.0g

6.0g

hypromellose

7.0g

7.0g

7.0g

Magnesium stearate

3.2g

3.2g

3.2g

Opadry Film Coating Premix

8.3g

8.3g

8.3g

[0048] (2), test

[0049] (2.1) Dissolution test: According to the research results of the dissolution curve of the reference prepar...

Embodiment 1-4

[0065] (1) embodiment 1-4 raw material and proportioning ratio as shown in table 6:

[0066] Table 6. Embodiment 1-4 raw material and proportioning (batch: 1000 pieces)

[0067]

[0068]

[0069] (2), test

[0070] Embodiment 1-4 dissolution rate result is as table 8

[0071] Table 7 Dissolution test results

[0072]

[0073] As shown in Table 7, the f2 values ​​in Examples 2-4 show similarities to Example 1. That is, as shown in Table 7 and Figure 4 As shown, in Examples 1-4, the f2 value representing the similarity of dissolution properties is in the range of 50≤f2≤100, and preparations with similar dissolution properties are obtained.

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Abstract

The invention provides a lurasidone hydrochloride oral preparation and a preparing method of the lurasidone hydrochloride oral preparation. The lurasidone hydrochloride oral preparation comprises lurasidone hydrochloride accounting for 20 to 45 weight percent of the oral preparation and cellulose derivatives accounting for 5 to 30 weight percent of the oral preparation, wherein the cellulose derivatives are a mixture of low-substituted hydroxypropyl cellulose and croscarmellose sodium. The lurasidone hydrochloride oral preparation has the advantages that the low-substituted hydroxypropyl cellulose and the croscarmellose sodium are simultaneously used as disintegrating agents, so that lurasidone hydrochloride tablets can be fast dissolved out, even when the content of active ingredients in the preparation is changed, the dissolution characteristics are also identical to the reference preparation, and the in-batch differences are small. In addition, according to the raw material processing mode, the raw material yield is higher, and the loss is less.

Description

technical field [0001] The invention belongs to the technical field of medicines, in particular to a lurasidone hydrochloride oral preparation and a preparation method thereof. Background technique [0002] Lurasidone (lurasidone) is a kind of atypical antipsychotic drug developed by Japan's Sumitomo Pharmaceutical Company, which has been marketed in the United States in the form of film-coated tablets (20mg, 40mg, 80mg, 120mg / tablet). On October 28, 2010, the U.S. Food and Drug Administration (FDA) approved Latuda (lurasidone hydrochloride) for the treatment of schizophrenia; on June 28, 2013, two new indications approved by FDA, One as monotherapy and the other as adjunctive drug therapy to lithium or sodium valproate for major depressive episodes associated with bipolar I disorder in adult patients. [0003] Lurasidone was significantly more effective than placebo in patients with schizophrenia. Lurasidone has no gender, age, and race differences in the treatment of sch...

Claims

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Application Information

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IPC IPC(8): A61K9/36A61K31/496A61K47/38A61P25/18
Inventor 曲继广刘芳菊袁广峰杨帆曹柳李彪赵晓雷程彦超袁兴利孙伶
Owner SHIJIAZHUANG NO 4 PHARMA
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