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Memantine pamoate crystal as well as preparation method and application thereof

A technology of pamoate and pamoic acid, which is applied in the preparation of carboxylates, organic chemical methods, and the preparation of amino compounds from amines, etc., can solve the problems of poor medication compliance, missed doses and refusal of patients, and reduce the Solubility, overcoming the effect of high solubility

Pending Publication Date: 2022-02-08
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, at present, the administration frequency of the drug on the market is once to twice a day, and the patient's medication compliance is poor, and it is easy to miss and refuse to take it.

Method used

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  • Memantine pamoate crystal as well as preparation method and application thereof
  • Memantine pamoate crystal as well as preparation method and application thereof
  • Memantine pamoate crystal as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example

[0063] Put 4.669g of pamoic acid raw material in 32ml of water, stir at 60°C, and configure it as a suspension of pamoic acid, add 0.3mol / L NaOH solution dropwise to the pamoic acid suspension, dropwise Stir while adding, after the NaOH solution is added dropwise, continue to stir for 5 minutes, and sonicate for 5 minutes. If there is still an insoluble precipitate, continue stirring and add NaOH solution dropwise until the pamoic acid is completely dissolved and a clear pamoic acid solution is obtained. Put 5.1785g of memantine hydrochloride raw material in 300ml of water, stir at room temperature, add the above clarified pamoic acid solution into the memantine aqueous solution dropwise, after the dropwise addition, continue to stir for 5min to obtain a milky white powder, which is memantine Crystal form I of adamantine pamoate.

[0064] figure 1 For the powder X-ray diffraction pattern of the memantine pamoate crystals prepared above, from figure 1 It can be seen that the...

Embodiment 1

[0069] Put 2g of memantine pamoate crystal form I raw material (prepared in the preparation example) in 10mL of methanol, stir at 30°C, and configure the methanol solution of crystal form I, and 50mL of 1,4-epoxyhexacyclic solution Use a peristaltic pump to add dropwise to the methanol solution at a rate of 3mL / min, and stir at 200rpm while adding dropwise. After the dropwise addition is complete, filter the solution with suction to obtain a light yellow solid, which is the crystal form of memantine pamoate IV.

[0070] Figure 5 For the powder X-ray diffraction pattern of the memantine pamoate crystals prepared above, from Figure 5 It can be seen that there are characteristic peaks at 7.38, 9.92, 10.68, 11.74, 13.28, and 19.58 degrees according to the diffraction angle 2θ, indicating that the crystal is in the IV crystal form.

[0071] Image 6 For the TGA figure of the memantine pamoate crystals prepared above, from Image 6 It can be seen that memantine pamoate crystal...

Embodiment 2

[0075] Put 2g of memantine pamoate crystal form I raw material (prepared in the preparation example) in 10mL DMF, stir at 30°C, and configure the DMF solution of crystal form I, and use a peristaltic pump to 70mL of dichloromethane solution to Add dropwise to the DMF solution at a rate of 3 mL / min, and stir at 200 rpm while adding dropwise. After the dropwise addition is complete, the solution is suction-filtered to obtain a light yellow solid, which is memantine pamoate crystal form IV.

[0076] The product obtained in Example 2 was tested by PXRD, and it can be known that there are characteristic peaks at 7.38, 9.92, 10.68, 11.74, 13.28, and 19.58 when the diffraction angle is 2θ.

[0077] DSC test was carried out on Example 2, and the substance appeared a characteristic endothermic peak at 222.8°C.

[0078] The solubility test of the memantine pamoate type IV crystal prepared above shows that: at 37°C, the solubility in PBS buffer is about 0.125 mg / mL, and the solubility of...

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Abstract

The invention provides a memantine pamoate crystal and a preparation method and application thereof. The memantine pamoate crystal is in a crystal form IV, and an X-ray powder diffraction pattern expressed by 2[theta] has characteristic peaks at 7.38 + / -0.2 degrees, 9.92 + / -0.2 degrees, 10.68 + / -0.2 degrees, 11.74 + / -0.2 degrees, 13.28 + / -0.2 degrees and 19.58 + / -0.2 degrees; and the memantine pamoate crystal has the advantages of reducing the solubility of memantine and further realizing sustained and controlled release.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical crystallization, and relates to a memantine pamoate crystal, a preparation method and application thereof. Background technique [0002] Memantine hydrochloride (memantine hydrochloride) chemical name is 3,5-dimethyl-1-amino-adamantane hydrochloride (3,5-Dimethyl-1-aminoadamantane hydrochloride), also known as 3,5-dimethyl tri Cyclo[3.3.1.1.(3.7)]decane-1-amine hydrochloride (3,5-Dimethyltricyclo(3.3.1.1(3,7))decan-1-amine hydrochloride). Its molecular formula is C 12 h 21 N·HCl, its chemical structural formula is: [0003] [0004] Memantine hydrochloride is the only NMDA receptor antagonist marketed for the treatment of Alzheimer's disease, and the only drug used to treat moderate to severe disease. It is a low-to-moderate affinity, non-competitive, strong voltage-dependent N-methyl-D-aspartate receptor antagonists, which can block glutamate-induced N-methyl-D-aspartate receptor ov...

Claims

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Application Information

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IPC IPC(8): C07C211/38C07C65/11C07C51/41C07C51/43C07C209/68C07C209/84A61K31/13A61K31/205A61P25/28
CPCC07C211/38C07C65/11A61P25/28C07B2200/13C07C2603/74
Inventor 龚俊波匡雯婕吴送姑林霞杨子毅候宝红杨奕张聪
Owner TIANJIN UNIV
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