Lobaplatin dihydrate, preparation method and drug application

A lobaplatin and drug technology, applied in the field of lobaplatin dihydrate and its preparation, can solve the problems of poor stability and difficulty in making lobaplatin, achieve good stability, not easy to deliquescence, and improve the quality of drug production

Active Publication Date: 2015-12-30
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 had the problems of deliquescence, difficulty in making preparations and poor stability.

Method used

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  • Lobaplatin dihydrate, preparation method and drug application
  • Lobaplatin dihydrate, preparation method and drug application
  • Lobaplatin dihydrate, preparation method and drug application

Examples

Experimental program
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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, comprising the following steps:

[0049] Weigh lobaplatin trihydrate in a container, add an organic solvent, suspend and stir at room temperature for 45-50h, filter, wash with ether, and vacuum dry to obtain a white powder, which is lobaplatin dihydrate; the organic solvent is selected from From methyl tert-butyl ether, toluene, diethyl ether, butyl acetate, 1,4-dioxane or n-heptane, the mass volume ratio is lobaplatin trihydrate: organic solvent = 1:15-30.

Embodiment 1

[0052] Example 1: Screening analysis of various crystal forms of lobaplatin

[0053] 1.1 Screening by room temperature volatile crystallization method

[0054] 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:

[0055] Table 2 normal temperature volatilization and crystallization test results

[0056] Numbering

solvent

PXRD (possible crystal number)

1-1

Absolute ethanol

B

1-2

Anhydrous Methanol

B

[0057] The results show that the crystal forms obtained in anhydrous methanol and absolute ethanol are the same crystal form through PXRD diffraction pattern analysis and comparison, and are named as crystal form B.

[0058] 1.2 Screening by suspension crystallization m...

Embodiment 2

[0101] Example 2: Preparation of Lobaplatin Dihydrate Named Crystal Form A

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Abstract

The invention relates to lobaplatin dihydrate, a preparation method and drug application. The melting point Tm.p.. of the lobaplatin dihydrate is 220+ / -5 DEG C, and the crystal form of the lobaplatin dihydrate is A. An X-ray powder diffraction PXRD pattern has diffraction peaks when the 2theta value is 11.04, 12.32, 12.61, 13.85, 15.14, 15.55, 16.68, 17.67, 17.86, 19.03, 20.06, 21.00, 22.68, 22.92, 23.76, 25.39, 25.58, 26.37, 26.77, 27.00, 27.71, 28.13, 29.71, 31.42, 31.94, 32.89, 34.29, 34.60, 36.10, 36.93, 37.66, 40.78 and 43.41, wherein the error range of the 2theta value is 0.2. The lobaplatin dihydrate is obtained by adding lobaplatin trihydrate into suspension crystallization solvent and performing suspension crystallization. Compared with the prior art lobaplatin and lobaplatin trihydrate, the lobaplatin dihydrate has better stability and solubility, is more suitable for preparation of drug preparations of different forms, storage and usage and can be better used for treating breast cancer or small cell lung cancer or chronic myeloid leukemia or the like.

Description

technical field [0001] The invention relates to the field of medicines, in particular to a dihydrate 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, low to...

Claims

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Application Information

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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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