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Lobaplatin crystal and preparation method and drug application thereof

A technology of lobaplatin trihydrate and lobaplatin, which is applied to a new crystal form and a preparation method thereof and the application field in medicine, can solve the problems of difficulty in preparing preparations, poor stability and the like, and achieves good fluidity and good stability. , the effect of high solubility

Active Publication Date: 2016-03-30
GUIZHOU YIBAI PHARMA CO LTD
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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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  • Lobaplatin crystal and preparation method and drug application thereof
  • Lobaplatin crystal and preparation method and drug application thereof
  • Lobaplatin crystal and preparation method and drug application thereof

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preparation example Construction

[0053] 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.

[0054] In a preferred embodiment, the preparation method of the new crystal form of lobaplatin of the present invention comprises the following steps:

[0055] a. Preparation of lobaplatin dihydrate: Weigh lobaplatin trihydrate in a container, add 15-30ml organic solvent to 1g lobaplatin trihydrate, suspend and stir at room temperature for 45-50h, filter and wash with ether , to obtain a white powder after vacuum drying, which is lobaplatin dihydrate;

[0056] Wherein, the organic solvent is selected from methyl tert-butyl ether, toluene, diethyl ether, butyl acetate, 1,4-dioxane or n-heptane.

[0057] b. Preparation of the target crystal form: Weigh the lobaplatin dihydrate obtained in step a, put it in a container, add anhydrous methanol, stir at room temperature until the solid d...

Embodiment 1

[0067] Embodiment 1: Screening analysis of each crystal form

[0068] 1.1 Screening by room temperature volatile crystallization method

[0069] 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:

[0070] Table 2 normal temperature volatilization and crystallization test results

[0071] Numbering

solvent

PXRD (possible crystal number)

1-1

Absolute ethanol

B

1-2

Anhydrous Methanol

B

[0072] 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.

[0073] 1.2 Screening by suspension crystallization method

[0074] Take 20mg of lobaplatin t...

Embodiment 2

[0116] Example 2: Preparation of a new crystal form of lobaplatin named Form B

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Abstract

The present invention relates to a lobaplatin crystal and a preparation method and drug application thereof, the lobaplatin crystal form is B, the melting point Tm. p. . is 230 + / -5 DEG C, diffraction peaks exist at the 2 theta angle values of 8.25, 9.77, 11.70, 13.13, 15.28, 16.48, 17.22, 17. 74, 19.01, 19.56, 22.28, 23.72, 24.04, 24.30, 25.62, 26.20, 28.57, 30.22 and 30.61 in an X-ray powder diffraction PXRD spectrum, wherein the 2 theta angle value error is in the range of 0.2. The crystal form B is obtained by solvent evaporation of lobaplatin trihydrate, or volatilization at room temperature after addition of a solvent in lobaplatin dihydrate or solvent-out crystallization, and drying. Compared with lobaplatin and the lobaplatin trihydrate in the prior art, the lobaplatin crystal in the crystal form B has better stability and solubility, is more suitable for the preparation of various forms of pharmaceutical preparations and storage and use, and can be better used to treat cancers such as breast cancer, small cell lung cancer or chronic granulocytic 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, the chemical structure formula is as shown in the following formula (1): [0003] [0004] Lobaplatin has alkylating effect and belongs to 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 Applications(China)
IPC IPC(8): C07F15/00A61K31/282A61P35/00A61P35/02
Inventor 窦啟玲隋东虎张圣贵
Owner GUIZHOU YIBAI PHARMA CO LTD
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