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Lobaplatin crystal, and preparation method thereof and pharmaceutical application thereof

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 high fluidity, good stability and high solubility. Effect

Active Publication Date: 2016-01-06
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 thereof and pharmaceutical application thereof
  • Lobaplatin crystal, and preparation method thereof and pharmaceutical application thereof
  • Lobaplatin crystal, and preparation method thereof and pharmaceutical application thereof

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preparation example Construction

[0047] 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.

[0048] In a preferred embodiment, the preparation method of lobaplatin new crystal form E of the present invention comprises the following steps:

[0049] 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;

[0050] Wherein, the organic solvent is selected from methyl tert-butyl ether, toluene, diethyl ether, butyl acetate, 1,4-dioxane or n-heptane.

[0051] b. Preparation of the target crystal form: Weigh the lobaplatin dihydrate obtained in step a, place it in a container, add ethylene glycol dimethyl ether, suspend and stir at room temperature for 45-50 hours, precipita...

Embodiment 1

[0055] Embodiment 1: Screening analysis of each crystal form

[0056] 1.1 Screening by room temperature volatile crystallization method

[0057] 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:

[0058] Table 2 normal temperature volatilization and crystallization test results

[0059] Numbering

solvent

PXRD (possible crystal number)

1-1

Absolute ethanol

B

1-2

Anhydrous Methanol

B

[0060] 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.

[0061] 1.2 Screening by suspension crystallization method

[0062] Take 20mg of lobaplatin t...

Embodiment 2

[0104] Example 2: Preparation of a new crystal form of lobaplatin named as crystal form E

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Abstract

The invention relates to a lobaplatin crystal, and a preparation method thereof and a pharmaceutical application thereof. The crystal has a crystal form of E, and has a melting point Tm.p.. of 214+ / -5 DEG C. In an X-ray powder diffraction PXRD pattern of the crystal, diffraction peaks appear when 2theta angle values are 6.61, 8.09, 12.38, 13.03, 15.40, 16.66, 17.47 and 19.07, wherein an 2theta value error range is 0.2. The crystal form E is obtained through the following steps: glycol dimethyl ether is added into lobaplatin dihydrate; suspension stirring is carried out, and crystals are precipitated; the crystals are separated and dried, such that white powder is obtained. Therefore, the novel crystal form E of lobaplatin is obtained. Compared with existing lobaplatin trihydrate, the crystal form provided by the invention has better stability and solubility. The crystal form is suitable to be used for preparing various forms of pharmaceutical preparations, and is suitable for storage and application. The crystal can be better used for treating cancers such as 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 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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