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Praziquantel crystal A substance, its preparation method and its applications in medicines and healthcare products

A technology of praziquantel and substance, applied in the field of medicine, can solve the problems such as patents or literature reports of other crystal forms of praziquantel are not found

Inactive Publication Date: 2012-11-21
INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0017] After searching domestic and foreign patents and literature, no other crystal form patents or literature reports related to praziquantel were found

Method used

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  • Praziquantel crystal A substance, its preparation method and its applications in medicines and healthcare products
  • Praziquantel crystal A substance, its preparation method and its applications in medicines and healthcare products
  • Praziquantel crystal A substance, its preparation method and its applications in medicines and healthcare products

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] The preparation method of praziquantel crystal type A sample:

[0054] The preparation method of praziquantel crystal type A sample is characterized in that 110 mg of praziquantel sample is completely dissolved at a temperature of 20°C using 20ml of chloroform as a solvent, and the solvent is removed under a vacuum pressure condition of 40°C to prepare praziquantel crystal type samples.

[0055] The powder X-ray diffraction pattern of gained praziquantel crystal form sample is as attached figure 1 shown

[0056] The infrared absorption spectrum figure of gained praziquantel crystal form sample is as attached figure 2 shown

[0057] The DSC collection of illustrative plates of gained praziquantel crystal form sample is as attached image 3 shown

[0058] The results of the above spectrum data show that the crystal form of the crystal obtained in this example is praziquantel crystal type A.

Embodiment 2

[0060] The preparation method of praziquantel crystal type A sample:

[0061] The preparation method of praziquantel crystal type A sample is as follows: firstly, 150 mg of praziquantel sample is completely dissolved at 20°C by adding 10ml of methanol to 20ml of water solvent at room temperature, and then the solvent is removed under vacuum at 40°C to obtain A sample of praziquantel crystal form.

[0062] The powder X-ray diffraction pattern of gained praziquantel crystal form sample is as attached figure 1 shown

[0063] The infrared absorption spectrum figure of gained praziquantel crystal form sample is as attached figure 2 shown

[0064] The DSC collection of illustrative plates of gained praziquantel crystal form sample is as attached image 3 shown

[0065] The results of the above spectrum data show that the crystal form of the crystal obtained in this example is praziquantel crystal type A.

[0066] The problem that needs to be explained: Since there are many ki...

Embodiment 3

[0068] Absorption characteristics and blood concentration characteristics of praziquantel crystal type A samples in rats:

[0069] Wistar rats with a body weight of 205±10g were reared under conventional feeding conditions, free to drink water, and after fasting for 12 hours, 200 mg / kg of praziquantel crystal type A was administered intragastrically, at 0.083, 0.25, and 0.5 before and after administration. , 1, 1.5, 1, 2, 2.5, 3, 4, 6, and 8 hours, about 0.5 ml of blood was collected from the orbit, and centrifuged at 4,000 rpm for 15 minutes to prepare plasma. Take 100μl of plasma, add 1ml of ethyl acetate, vortex for 3min, centrifuge at 13,400rpm for 15min, absorb the upper layer of ethyl acetate, dry it with nitrogen, then dissolve it in 100μl of methanol, inject 20μl for HPLC detection. HPLC detection system: Aligent 1100 high performance liquid chromatography system, chromatographic column: Aligent TC-C18, (150×4.6mm, 5μm), mobile phase: methanol: water = 67:33, injection...

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Abstract

The invention discloses a praziquantel crystal A substance with the structure represented by formula (I), a preparation method of a praziquantel crystal A sample, products prepared through treating the praziquantel crystal A substance as an active component, and applications of the praziquantel crystal A in the disease control and the healthcare, wherein the products comprise medicines and healthcare products.

Description

technical field [0001] The present invention relates to a crystal type A substance state of praziquantel, a method for preparing a sample of praziquantel crystal type A, a product using praziquantel crystal type A substance as an active ingredient, and an application of praziquantel crystal type A, belonging to field of medical technology. Background technique [0002] Praziquantel, English name is Praziquantel, and molecular structure is as shown in formula (I) [0003] [0004] In Chinese patent CN1414847 (publication number), it is recorded that Hong Xingtai, Li Chengjin, Gao Yuangui, and Zhu Tingzhe invented "slow-release anti-helminth composition containing praziquantel" [1] , which relates to a slow-release anti-helminth composition containing praziquantel and a preparation method. [0005] In the Chinese patent CN1452489 (publication number), it is recorded that "praziquantel compound for treating diseases caused by Sarcocystis, Neospora, Toxoplasma and Isospora"...

Claims

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Application Information

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IPC IPC(8): C07D471/04A61K31/4985A61P33/14A23L1/29A23L33/00
Inventor 吕扬杜冠华陈芊茜田硕杜立达
Owner INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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