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A kind of lobaplatin crystal, preparation method and pharmaceutical application

A lobaplatin and crystal technology, which is applied to new crystal forms and their preparation methods and application fields in medicines, can solve the problems of difficulty in preparing preparations and poor stability, and achieves a product with good fluidity, good stability and high solubility. Effect

Active Publication Date: 2018-08-14
海南长安国际制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical problem to be solved by the present invention is that in the past, lobaplatin anhydrate had deliquescence, was difficult to make preparations, and had poor stability.

Method used

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  • A kind of lobaplatin crystal, preparation method and pharmaceutical application
  • A kind of lobaplatin crystal, preparation method and pharmaceutical application
  • A kind of lobaplatin crystal, preparation method and pharmaceutical application

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Experimental program
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preparation example Construction

[0049] On the other hand, the present invention provides a method for preparing a new crystal form of lobaplatin that is simple to prepare, easy to operate, and suitable for scale-up production.

[0050] In a preferred embodiment, the preparation method of the new crystal form of lobaplatin of the present invention comprises the following steps:

[0051] a. Preparation of lobaplatin dihydrate: Weigh lobaplatin trihydrate in a container, add 15-30ml of organic solvent, suspend and stir at room temperature for 45-50h, filter, wash with ether, and obtain a white powder after vacuum drying, namely Lobaplatin dihydrate;

[0052] Wherein, the organic solvent is selected from methyl tert-butyl ether, toluene, diethyl ether, butyl acetate, 1,4-dioxane or n-heptane.

[0053] b. Preparation of the target crystal form: Weigh the lobaplatin dihydrate obtained in step a, put it in a container, add methanol or ethanol, stir at room temperature until the solid dissolves, filter off the inso...

Embodiment 1

[0058] Embodiment 1: Screening analysis of each crystal form

[0059] 1.1 Screening by room temperature volatile crystallization method

[0060] Take 20 mg of lobaplatin trihydrate sample and put it into a 10 ml sample bottle, add 3 ml of absolute ethanol or absolute methanol, after fully dissolving, place it in an environment of 25°C and slowly volatilize to obtain a dry solid, which is then determined by PXRD. The results are shown in Table 2 below:

[0061] Table 2 The test results of volatilization and crystallization at room temperature

[0062] serial number

solvent

PXRD (possible crystal number)

1-1

Absolute ethanol

B

1-2

Anhydrous Methanol

B

[0063] The results showed that the crystal forms obtained in absolute methanol and absolute ethanol were compared and found to be the same crystal form, tentatively named as crystal form B.

[0064] 1.2 Screening by suspension crystallization method

[0065] Take 20mg of lob...

Embodiment 2

[0107] Example 2: Preparation of a new crystal form of lobaplatin named Form F

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Abstract

The invention relates to a lobaplatin crystal, a preparation method and a pharmaceutical application. The lobaplatin crystal form is F, the melting point Tm.p..=229±5°C, and the 2θ angle value in the X-ray powder diffraction PXRD spectrum is 8.21 、11.60、12.99、15.24、16.44、17.11、17.55、18.42、19.01、19.20、19.42、21.81、22.17、22.42、23.33、23.85、24.18、24.40、24.77、25.46、25.98、26.13、27.89、28.42、29.03、30.32 There are diffraction peaks at , 31.17, 31.94, 33.30, 36.20, 37.62, and 39.66, and the error range of the 2θ value is 0.2. The crystal form F is obtained by adding methanol or ethanol to lobaplatin dihydrate, stirring at room temperature until the solid is dissolved, filtering off the insoluble matter, and then slowly adding an organic solvent. After the crystal is separated, the crystal is separated and dried. get. Compared with the existing lobaplatin and lobaplatin trihydrate, the lobaplatin crystal of crystal form F has better stability and solubility, and is more suitable for the preparation, storage and use of various forms of pharmaceutical preparations, and can better For the treatment of cancer such as the treatment of breast cancer, small cell lung cancer or chronic myelogenous leukemia.

Description

technical field [0001] The invention relates to the field of medicines, in particular to a new crystal form of lobaplatin and its preparation method and application in medicines, belonging to the technical field of medicines. Background technique [0002] Lobaplatin (D19466), also known as Lobaplatin, is the third-generation platinum-based antineoplastic drug after cisplatin and carboplatin, and its chemical name is: cis-[trans-1,2-cyclobutane Alkanebis(methylamine)-N,N']-[(2S)-lactic acid-O1,O2]-platinum(II), the molecular formula is C 9 h 18 N 2 o 3 Pt, the molecular weight is 397.34, and the chemical structural formula is shown in the following formula (1): [0003] [0004] Lobaplatin has an alkylating effect and is an alkylating agent (broad sense). It has good anti-tumor effect, such as in vitro AH135-tumor, B16-melanoma, colon cancer 115, in vivo mouse P338 leukemia, etc. has a good inhibitory effect. Lobaplatin is characterized by strong anticancer activity,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F15/00A61K31/282A61P35/00A61P35/02
Inventor 窦啟玲隋东虎张圣贵
Owner 海南长安国际制药有限公司
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