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A method of producing a co-crystal and a product formed through the method

A technology of products and substances, applied in the selection of auxiliary crystallization conditions, drug combination, solution crystallization, etc., to achieve the effect of high yield and not easy to wear

Inactive Publication Date: 2016-07-20
UNIVERSITY OF BRADFORD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, easily oxidized APIs or guests cannot be processed using this technique

Method used

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  • A method of producing a co-crystal and a product formed through the method
  • A method of producing a co-crystal and a product formed through the method
  • A method of producing a co-crystal and a product formed through the method

Examples

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Effect test

example 1

[0154] A physical mixture of ibuprofen and niacinamide was prepared by mixing 41.2 g of ibuprofen and 26 g of niacinamide (1:1 molar ratio) in a Turbula mixer for 30 minutes. An extruder (ThermoPrism TSE16TC) with an L:D ratio of 15:1 and a screw diameter of 16 mm was used. This incorporated screw configuration 1 mainly consists of a forward feed section and a small distributive mixing zone. The detailed screw configuration has been described previously. The barrel temperature was set at 80°C. Once the temperature stabilized for 15 min, the physical mixture was slowly fed to the extruder with the screw rotating at 20 rpm. Fine agglomerated product was collected at the exit of the extruder. The residence time of the material through the extruder was about 3 minutes. The powder was cooled to room temperature and then characterized by powder X-ray diffraction (PXRD).

[0155] figure 2 The PXRD pattern of a physical mixture comprising ibuprofen-nicotinamide is shown. The c...

example 2

[0158] A physical mixture of ibuprofen and niacinamide was prepared by mixing 41.2 g of ibuprofen and 26 g of niacinamide (1:1 molar ratio) in a Turbula mixer for 30 minutes. An extruder (ThermoPrism Eurolab) with an L:D ratio of 40:1 and a screw diameter of 16 mm was used. This incorporated screw configuration number 2 consists of feed and distributive mixing zones. The detailed screw configuration has been described previously. The barrel temperature was set at 80°C. Once the temperature stabilized for 15 min, the physical mixture was slowly fed to the extruder with the screw rotating at 20 rpm. The residence time of the material through the extruder was about 20 minutes. Fine agglomerated product was collected at the exit of the extruder. The powder was cooled to room temperature and then characterized by powder X-ray diffraction (PXRD).

[0159] As mentioned above, figure 2 The PXRD pattern of a physical mixture comprising ibuprofen-nicotinamide is shown. The chara...

example 3

[0162] A physical mixture of ibuprofen and niacinamide was prepared by mixing 41.2 g of ibuprofen and 26 g of niacinamide (1:1 molar ratio) in a Turbula mixer for 30 minutes. with an L:D ratio of 40:1, (ThermoPrismEurolab) with replaceable feed, distribution and dispersive mixing screw zones, and with a reverse feed screw section before the last feed zone (configuration 3) The temperature of the extruder was set at 80°C. Once the temperature stabilized for 15 min, the physical mixture was slowly fed to the extruder with the screw rotating at 20 rpm. The residence time of the material through the extruder was about 33 minutes. Fine agglomerated product was collected in the terminal region. The powder was cooled to room temperature and then characterized by powder X-ray diffraction (PXRD).

[0163] As mentioned above, figure 2 The PXRD pattern of a physical mixture comprising ibuprofen-nicotinamide is shown. The characteristic peak of ibuprofen can be observed at 6°2theta....

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Abstract

The present invention provides a method of producing a co-crystal and a product formed through the method, the method comprising the steps of, providing a first substance and a second substance, wherein the first and second substances are compatible to form a co-crystal, mixing said first and second substances together, and exposing the mixture of said first and second substances to prolonged and sustained conditions of pressure and shear, sufficient to form a co-crystal of said first and second substance.The prolonged and sustained conditions of pressure and shear are preferably applied in an extrusion process. Associated compositions and uses thereof are also provided.

Description

[0001] This application is a divisional application of the application dated July 27, 2009, the application number is 200980138138.5, and the invention name is "method and product". technical field [0002] The present invention relates to methods for the formation of products useful in traditional Chinese medicine, and to products formed by such methods. The present invention relates particularly, but not exclusively, to methods of forming co-crystal products using extrusion, and products obtained or obtainable by such methods. Background technique [0003] Crystal engineering is currently being investigated as a method to tune the physicochemical properties of active agents. By rethinking the types of molecules and intermolecular reactions that can be used to form crystal complexes with the help of pharmaceuticals, the application of crystal engineering to pharmaceuticals opens up the possibility for the development of a wider range of multicomponent structures containing ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): B01D9/02A61K45/06A61K31/192A61K31/522A61K31/60A61K31/55A61K47/22A61K47/12
CPCA61K31/192A61K31/445A61K31/55A61K45/06B01D9/005A61P1/04A61P17/00A61P21/00A61P25/00A61P25/04A61P29/00A61K2300/00
Inventor 阿南特·帕拉德卡艾德里安·凯利菲尔·科茨彼得·约克
Owner UNIVERSITY OF BRADFORD
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