Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Lobaplatin crystal, preparation method and medical application thereof

A technology of lobaplatin trihydrate and lobaplatin, which is applied in the field of new crystal form and its preparation method and application in medicine, can solve the problems of difficulty in making preparations and poor stability, and achieve good fluidity and stability , Improving the effect of drug production quality

Active Publication Date: 2016-02-17
海南长安国际制药有限公司
View PDF6 Cites 3 Cited by
  • 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Lobaplatin crystal, preparation method and medical application thereof
  • Lobaplatin crystal, preparation method and medical application thereof
  • Lobaplatin crystal, preparation method and medical application thereof

Examples

Experimental program
Comparison scheme
Effect test

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 of the present invention, the preparation method of the new crystal form of lobaplatin 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, put it in a container, add 1,2-dichloroethane, suspend and stir at room temperature for 45-50h...

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 D

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention relates to a lobaplatin crystal, a preparation method and a medical application thereof. A crystal form of the crystal is D, its melting point Tm.p..is 218+ / -5 DEG C, in a PXRD pattern of the lobaplatin crystal, diffraction peaks exist when the 2theta value is 6.76, 11.07, 12.35, 12.65, 13.88, 15.18, 15.56, 16.68, 17.70, 17.90, 20.08, 21.02, 22.70, 22.92, 25.41, 25.64, 26.41, 26.79, 27.02, 28.15, 31.44, 31.96, 32.96, 34.34, 34.62, 36.93, 40.82 and 43.46, and the error range of the 2theta value is 0.2. The preparing method for the crystal form D includes the steps that 1,2-dichloroethane is added into lobaplatin dihydrate, a 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 medicines, belonging to the technical field of medicines. technical background [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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com