Preparation method of paliperidone palmitate

A technology of paliperidone and palmitic acid, applied in the field of medicine, can solve problems such as large particle size, and achieve the effects of small particle size, high yield and small damage

Active Publication Date: 2019-03-01
CHIA TAI TIANQING PHARMA GRP CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The particle diameters obtained by the methods of the prior art are all relatively large, so it is necessary to develop a preparation method for the paliperidone palmitate bulk drug, which requires the resulting product to have a small particle diameter and a good shape, and is easy to be homogeneously pulverized in the follow-up, and also requires High yield, no solvent residue, thus meeting the needs of preparation and industrial production

Method used

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  • Preparation method of paliperidone palmitate
  • Preparation method of paliperidone palmitate
  • Preparation method of paliperidone palmitate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] 15g of paliperidone palmitate was dissolved in 150mL of dichloromethane at room temperature to obtain a dichloromethane solution of paliperidone palmitate, which was added dropwise to 2.25L of n-heptane, and the temperature was controlled at 3°C. Acceleration 2mL / min, stirring speed 250 rpm / min. After the dropwise addition was completed, keep stirring for 30 min to crystallize, filter, rinse the filter cake with 160 mL of n-heptane, and dry under reduced pressure at 50° C. for more than 6 h to constant weight to obtain 14 g of paliperidone palmitate (yield 93%). SEM topography ( figure 1 ) shows flaky crystals with particle size distribution d 10 : 1.00, d 50 : 3.59, d 90 : 11.24. The average particle size of FBRM is 9.16 μm. Dichloromethane and n-heptane solvent residues were not detected.

[0043]Examples 2-4 refer to the operation process of Example 1, and the conditions in Table 1 are used for the corresponding replacement to prepare paliperidone palmitate cry...

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Abstract

The invention belongs to the technical field of medicines and relates to a preparation method of paliperidone palmitate. The method disclosed by the invention comprises the step of precipitating paliperidone palmitate in a mixed solvent of dichloromethane and n-heptane. Paliperidone palmitate particles obtained by the invention are small in particle sizes, flaky, easy to homogenize and grind, andshort in grinding time, have little damage to instruments and equipments, and are short in crystallization time, high in yield and free of solvent residues and particularly suitable for needs of industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a preparation method of paliperidone palmitate. Background technique [0002] Paliperidone palmitate (paliperidone palmitate) is a long-acting injection of the second-generation antipsychotic drug paliperidone, which is mainly used for the treatment of schizophrenia. The active ingredient is paliperidone. The water solubility of paliperidone palmitate is extremely low. During the preparation process, the raw material medicine needs to be crushed into fine particles by homogenizer and other equipment to improve its water solubility, and prepared into a nanocrystal suspension, so as to form a suitable intramuscular injection. The aqueous suspension preparation of the drug increases the absorption rate and bioavailability of the drug. [0003] The particle size and crystal form of paliperidone palmitate raw material before pulverization have a great influence on the subsequent pulve...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/04
CPCC07D471/04
Inventor 徐文卫张爱明高鹏徐洋平孟庆义
Owner CHIA TAI TIANQING PHARMA GRP CO LTD
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