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Lurasidone crystal, preparation method thereof and application of lurasidone crystal in injection drug delivery system

A technology for lurasidone pamoate and crystals, applied in the field of medicine, can solve the problems of large differences, non-compliance with pH and no dependence, undisclosed solubility of lurasidone hydrochloride crystals, and the like, so as to improve solubility and solubility. The absolute change value is small and the effect of increasing the drug load

Active Publication Date: 2019-07-12
HUBEI UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

For example, the Chinese invention patent application 201310066819.3 discloses the crystal form of lurasidone hydrochloride and its preparation method and use, but the patent only discloses the characteristic parameters of the prepared lurasidone hydrochloride crystal and no transformation during storage and grinding. Crystallization phenomenon, no data on solubility improvement disclosed
Chinese invention patent application 201310071135.2 discloses three new crystal forms of lurasidone hydrochloride A, B, and C and their preparation methods. The solubilities of the prepared lurasidone hydrochloride crystals in water and pH2.0 acidic conditions are respectively 3.4mg / ml and 8.0mg / ml, the difference in solubility is about 4.6mg / ml, which is very different, which does not meet the characteristics that the release rate of ideal injection raw materials should not be dependent on pH
Secondly, the solubility of lurasidone hydrochloride crystals in the pH range of the gastrointestinal tract is not disclosed, so it cannot fully reflect its release, absorption process and the influence of diet on it and the real improvement of bioavailability

Method used

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  • Lurasidone crystal, preparation method thereof and application of lurasidone crystal in injection drug delivery system
  • Lurasidone crystal, preparation method thereof and application of lurasidone crystal in injection drug delivery system
  • Lurasidone crystal, preparation method thereof and application of lurasidone crystal in injection drug delivery system

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preparation example Construction

[0052] The preparation method of pamoic acid lurasidone crystal of the present invention comprises the following steps:

[0053] (1) dissolving lurasidone and pamoic acid in tetrahydrofuran to obtain the first mixed solution;

[0054] (2) adding ethyl acetate to the first mixed solution, stirring, heating and reacting and then cooling down to room temperature to obtain a second mixed solution;

[0055] (3) After spinning the second mixed solution to dryness, ethyl acetate was added, dichloromethane crystallized, and the crystals were precipitated and filtered to obtain lurasidone pamoic acid crystals.

[0056] In step (1), the molar ratio of lurasidone and pamoic acid can be 1:1-1.2, most preferably 1:1.

[0057] In step (2), preferably, heating to 55-60° C. for 2-3 hours.

[0058] The preparation method of pamoic acid lurasidone nanocrystal of the present invention comprises the following steps:

[0059] (a) preparing pamoic acid lurasidone crystals according to the above ...

Embodiment 1

[0075] This example is used to illustrate the preparation method of pamoic acid lurasidone crystals.

[0076] Dissolve 1g of lurasidone and 788mg of pamoic acid in 20ml of tetrahydrofuran, then add 20ml of ethyl acetate, react at 60°C for 2h and then spin dry. Add 10ml of ethyl acetate and 5ml of dichloromethane, and filter to obtain the product lurasidone pamoate A1 after crystallization.

Embodiment 2

[0078] This example is used to illustrate the preparation method of pamoic acid lurasidone crystals.

[0079] Dissolve 1g of lurasidone and 788mg of pamoic acid in 30ml of tetrahydrofuran, then add 10ml of ethyl acetate, react at 55°C for 3h and spin dry. Add 15ml of ethyl acetate and 8ml of dichloromethane, and filter to obtain the product lurasidone pamoate A2 after crystallization. The product was vacuum-dried at 50°C, and stored in a glass bottle at room temperature, dry, and protected from light.

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Abstract

The invention relates to the technical field of medicine, and discloses a lurasidone crystal, a preparation method thereof and application of the lurasidone crystal in an injection drug delivery system. The method comprises the steps: dissolving lurasidone and plmoxiric acid in tetrahydrofuran so as to obtain a first mixed solution, adding ethyl acetate to the first mixed solution, performing stirring and heating for a reaction, then performing cooling to room temperature so as to obtain a second mixed solution, performing spin-drying on the second mixed solution, adding ethyl acetate, performing crystallization by means of dichloromethane, precipitating the crystal, and then performing filtration. The equilibrium solubility of the plmoxiric acid-lurasidone crystal is 0.12-73 [mu]g / ml at apH value of 2.0-7.8, the absolute change value of the solubility is small, the overall trend is stable, and no influences from the pH value and no dependence on the pH value are achieved.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a pamoic acid lurasidone crystal, a pamoic acid lurasidone nanocrystal and a preparation method and application thereof. Background technique [0002] Lurasidone hydrochloride (Lurasidone hydrochloride) is a new type of anti-schizophrenia drug discovered by Dainippon Sumitomo Pharmaceutical Co., Ltd. In October 2010, FDA approved its oral tablet for marketing. Lurasidone hydrochloride has high affinity to dopamine D2 receptor and 5-HT2A receptor, and also has high affinity to 5-HT7, 5-HT1A and α2c adrenoceptor subtype. Lurasidone hydrochloride has shown good therapeutic effects on both positive and negative symptoms of schizophrenic patients. While effectively treating schizophrenia, adverse reactions such as weight gain, extrapyramidal reaction, and QT interval prolongation are avoided. Due to the antagonistic effect of lurasidone hydrochloride on 5-HT7 receptors, it has a go...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D417/12A61K31/496A61P25/18
CPCA61K9/0019A61P25/18C07B2200/13C07D417/12
Inventor 卢山
Owner HUBEI UNIV OF CHINESE MEDICINE
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