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Crystal form of penehyclidine hydrochloride racemic mixture I and preparation method thereof

A technology of penehyclidine hydrochloride and racemate, which is applied to the crystal form of penehyclidine hydrochloride racemate I and the field of preparation thereof, and can solve the problem that no reports of penehyclidine hydrochloride racemate have been seen, etc. problem, to improve the stability of the drug, reduce the hygroscopicity, and avoid the effect of deliquescence

Active Publication Date: 2014-01-01
CHENGDU ZIHAO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, there is no relevant report on the related crystal form of penehyclidine hydrochloride racemate

Method used

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  • Crystal form of penehyclidine hydrochloride racemic mixture I and preparation method thereof
  • Crystal form of penehyclidine hydrochloride racemic mixture I and preparation method thereof
  • Crystal form of penehyclidine hydrochloride racemic mixture I and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1 Preparation of Penhyclidine Hydrochloride Racemate I Crystal Form of the Present Invention

[0033] Take 25g of 3-(2-hydroxy-2-cyclopentyl-2-phenylethoxy)quinuclidane hydrochloride (also known as penhyclidine hydrochloride), add 75ml of ethanol to reflux to dissolve, then add 25ml of petroleum The ether was naturally cooled, crystals were precipitated, filtered, and the filtrate was set aside for later use. The crystals were penehyclidine hydrochloride racemate I crystal form, 8.4 g in total, and the optical rotation was determined to be 0.

Embodiment 2

[0037] Example 2 Detection of Penhyclidine Hydrochloride Racemate I and II Crystal Forms

[0038] 1. Powder X-ray Diffraction Determination

[0039] Powder X-ray diffraction measurement conditions: CuKα line, (monochromator), tube voltage 40KV, tube current 30mA. The powder X-ray diffraction measurement results of the racemate I crystal form obtained in Example 1 are shown in figure 1 , the crystal form of racemate II obtained in the comparative example is shown in figure 2 , see the table below for specific data:

[0040] Table 1

[0041]

[0042] 2. DSC detection of penehyclidine hydrochloride racemate Ⅰ and Ⅱ crystal forms

[0043] The racemate I and II crystal forms were taken respectively for DSC determination. Among them, the determination results of the racemate I crystal form are shown in image 3 ; Racemate II crystal form determination results see Figure 4 .

[0044] 3. HPLC detection of racemate I crystal form and mixture of two racemate crystal forms...

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Abstract

The invention provides a crystal form of a penehyclidine hydrochloride racemic mixture I. In a powder X-ray diffraction pattern of the crystal form, characteristic peaks are achieved when a diffraction angle 2 theta is within the ranges of 9.46-9.86 degrees, 16.39-16.79 degrees, 18.82-19.22 degrees and 19.13-19.53 degrees. The invention further provides a preparation method for the crystal form. According to the invention, the prepared crystal form of the penehyclidine hydrochloride racemic mixture I can obviously reduce the hygroscopicity of the compound, avoids deliquescence, deformation, mildewing or degradation of the compound, which are caused by the fact that water is absorbed by the compound, provides convenience for storage and transportation of the compound, and provides a basis for improvement on the drug stability.

Description

technical field [0001] The invention relates to the crystal form of penehyclidine hydrochloride racemate I and a preparation method thereof. Background technique [0002] Penehyclidine hydrochloride is 3-(2-hydroxy-2-cyclopentyl-2-phenylethoxy)quinuclidane hydrochloride, the molecular formula is: C 20 h 29 NO 2 .HCl [0003] [0004] The compound is a potent anticholinergic drug designed and developed by the Chinese Academy of Military Medical Sciences, with selective M 1 , M 3 and N 1 , N 2 Receptor antagonism, showing a strong anticholinergic effect on the central and peripheral, but on M 2 The receptor has no obvious effect, which can avoid the tachycardia caused by atropine lack of M receptor subtype selectivity and block the presynaptic membrane M 2 Receptor regulation function, so long-acting and less side effects, in 1999, Chengdu Lisite Pharmaceutical Co., Ltd. exclusively marketed under the trade name of Chang Tuo Ning, has been widely used clinically in ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D453/02A61K31/439A61P9/06A61P11/00A61P11/02
CPCC07D453/02
Inventor 刘忠荣余建红叶兵严强
Owner CHENGDU ZIHAO PHARMA
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