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A kind of lobaplatin crystal, preparation method and pharmaceutical application

A technology of lobaplatin and crystals, which is applied in the field of new crystal forms and their preparation methods and applications in medicine, can solve the problems of difficulty in making preparations and poor stability, and achieve 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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preparation example Construction

[0048] 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.

[0049] In a preferred embodiment, the preparation method of lobaplatin new crystal form of the present invention comprises the steps of:

[0050] 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;

[0051] Wherein, the organic solvent is selected from methyl tert-butyl ether, toluene, diethyl ether, butyl acetate, 1,4-dioxane or n-heptane.

[0052] b. Preparation of the target crystal form: Weigh the lobaplatin dihydrate obtained in step a, put it in a container, add isobutanol or n-propanol, suspend and stir at room temperature for 45-50h, precipitate crystals, and separ...

Embodiment 1

[0056] Embodiment 1: Screening analysis of each crystal form

[0057] 1.1 Screening by room temperature volatile crystallization method

[0058] Take 20mg of lobaplatin trihydrate sample and put it into a 10ml sample bottle, add 3ml of absolute ethanol or absolute methanol, after fully dissolving, place it in an environment of 25°C for slow volatilization, obtain a solid dry product, and carry out PXRD determination. The results are shown in Table 2 below:

[0059] Table 2 The test results of volatilization and crystallization at room temperature

[0060] serial number

solvent

PXRD (possible crystal number)

1-1

Absolute ethanol

B

1-2

Anhydrous Methanol

B

[0061] The results show that: the crystal forms obtained in absolute methanol and absolute ethanol are compared and known to be the same crystal form, tentatively named as crystal form B.

[0062] 1.2 Screening by suspension crystallization method

[0063] Take 20mg of ...

Embodiment 2

[0105] Example 2: Preparation of a new crystal form of lobaplatin named Form C

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Abstract

The invention relates to a lobaplatin crystal, a preparing method and a medicine application. The crystal form of the lobaplatin crystal is C, and the melting point Tm.p.. is 228+ / -5 DEG C; in a PXRD pattern of the lobaplatin crystal, diffraction peaks exist when the 2theta value is 6.79, 8.07, 12.24, 12.61, 13.50, 16.50, 17.83, 18.32, 18.79, 20.09, 21.64, 22.27, 23.19, 24.73, 27.34, 28.35, 29.12 and 31.92, and the error range of the 2theta value is 0.2. The preparing method for the crystal form C includes the steps that isobutanol or normal propyl alcohol is added into lobaplatin dihydrate, the mixture is stirred in a suspension mode, and the crystal is dissolved out, separated out, dried and then obtained. Compared with existing lobaplatin and lobaplatin trihydrate, better stability and better solubility are achieved, and the lobaplatin crystal can be better suitable for preparing medicine preparations in various forms, can be better stored and used and can be better used for treating cancers such as the breast cancer, the small cell lung cancer and the 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 medicine, 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, molecular weight is 397.34, and chemical structural formula is as shown in 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, low toxic...

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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