Iloperidone-benzoic acid organic pharmaceutical co-crystal and preparation method thereof
A technology of iloperidone and organic drugs, applied in the field of iloperidone-benzoic acid organic drug co-crystal and its preparation, to achieve the effect of improving bioavailability and stability
Inactive Publication Date: 2015-02-18
苏州纳埃净化科技有限公司
View PDF3 Cites 0 Cited by
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Drug crystal form research and solid-state characterization of drugs are relatively mature and highly valued fields in the European and American pharmaceutical industry, but they are still in their infancy in the domestic pharmaceutical industry
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 moreImage
Smart Image Click on the blue labels to locate them in the text.
Smart ImageViewing Examples
Examples
Experimental program
Comparison scheme
Effect test
Embodiment 1
[0027] Synthesis of new crystal forms of drugs using iloperidone and phenyl acids:
[0028] Weighing:
[0029] Weigh respectively 20 mg of iloperidone and benzoic acid with an analytical balance in a colorless transparent vial;
[0030] Dissolution of API:
[0031] Use a 5ml pipette to measure 3ml of ethanol and 3ml of dichloromethane into a colorless transparent vial.
[0032] Room temperature evaporation method:
[0033] (1) Place the colorless transparent vial on a mechanical stirrer and stir for 30 minutes;
[0034] (2) After the stirring stopped, seal the mouth of the bottle with tin foil and place it in a quiet place around the environment. After 12 hours, it was found that there were colorless and transparent polyhedral massive microcrystals at the bottom of the colorless and transparent vial, and the crystals were completely precipitated after 72 hours;
[0035] (3) Put the obtained crystal into a vacuum drying oven and weigh it to 25 mg after drying to obtain the ...
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
Login to View More Abstract
The invention belongs to the technical field of an organic pharmaceutical new crystal form, and in particular relates to an iloperidone-benzoic acid organic pharmaceutical co-crystal and a preparation method thereof. Iloperidone is used as a crude drug, and benzoic acid is used as a precursor; a basic structure unit of the pharmaceutical co-crystal consists of two iloperidone molecules, two benzoic acid molecules and two water molecules; on a Y direction, accumulation exists in aromatic six-membered ring containing fluorine in one iloperidone molecule and six-membered ring containing an ester group in the other iloperidone molecule along a Z direction, and hydrogen-bond interaction exists in benzoic acid and water molecules; and the space group of the pharmaceutical co-crystal is a monoclinic system. The solvent selected by the iloperidone-benzoic acid organic pharmaceutical co-crystal is ethanol and dichloromethane, and the iloperidone-benzoic acid organic pharmaceutical co-crystal is prepared by a method of solvent evaporation; and due to low boiling point of the selected organic solvent, the crystal is separated out in the process of solvent evaporation.
Description
technical field [0001] The invention belongs to the technical field of new crystal forms of organic medicines, and in particular relates to an iloperidone-benzoic acid organic medicine co-crystal and a preparation method thereof. Background technique [0002] In 1894, E. Fischer of Germany proposed the "lock-key" model based on the idea of "selective interaction between molecules", which was the prototype of modern supramolecular science theory. In 1937, German K.L.Wolf et al. created the term "supramolecular" to describe highly ordered entities formed by the association of molecules. In a general sense, any collection of molecules has interactions, so people often refer to them as The structural level of matter aggregation state is called "supramolecular". It was not until 1978 that Professor J.M.Lehn of France finally proposed the complete concept of "supramolecular chemistry" based on the traditional research on the host-guest system rooted in organic chemistry. Supra...
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
Login to View More Patent Type & Authority Patents(China)
IPC IPC(8): C07D413/04C07C51/43C07C63/06A61P25/18
Inventor 张婷罗亚楠贾江涛苏红敏贺鸿明
Owner 苏州纳埃净化科技有限公司