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Rotundine crystalline C-type solid substance and preparation method as well as application

A solid substance, rotundine technology, applied in the field of medicine, can solve problems such as poor absorption

Active Publication Date: 2014-12-17
INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the poor absorption of rotundine itself, rotundine hydrochloride tablets were developed to promote its absorption.

Method used

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  • Rotundine crystalline C-type solid substance and preparation method as well as application
  • Rotundine crystalline C-type solid substance and preparation method as well as application
  • Rotundine crystalline C-type solid substance and preparation method as well as application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0093] Preparation method 1 of crystalline rotundine sample:

[0094] The preparation method of the crystal type B rotundine sample uses the crystal type A solid sample as the preparation raw material, and adopts the method of physical and mechanical lattice destruction and molecular rearrangement to crystallize to obtain the crystal type B solid material.

[0095] Preparation method 2 of crystalline rotundine sample:

[0096] The preparation method of the crystalline type B rotundine sample comprises firstly using a tetrahydrofuran solvent to completely dissolve the rotundine sample at a normal temperature of 15-30° C., and then rapidly preparing the crystalline type B rotundine solid substance by using a cold spray method.

Embodiment 2

[0098] Crystalline C-type rotundine sample preparation method 1:

[0099] The preparation method of crystal C-type rotundine sample is to completely dissolve the rotundine sample with n-butanol solvent at room temperature of 15-30°C, and then use a rotary evaporator to quickly dissolve the solvent under vacuum at a temperature of 40°C. The obtained crystal C-type rotundine solid substance was prepared by distilling off.

[0100] Method 2 for the preparation of crystal C-type rotundine samples:

[0101] The preparation method of the crystalline type C rotundine sample is prepared by first dissolving the rotundine sample completely with a pyridine solvent at a normal temperature of 15-30°C, and then placing it under normal pressure at a temperature of 22°C to gradually volatilize the solvent. The crystalline type C rotundine solid substance.

Embodiment 3

[0103] The absorption characteristics and blood concentration characteristics of crystal B-type rotundine solid drug in rats:

[0104] Experimental animals: Wistar rats, male, body weight: 194.2±9.2g. purchased from the Institute of Experimental Animals, Chinese Academy of Medical Sciences.

[0105] Experimental method: Luotong fixed crystal type A, crystal type B. Prepare about 17mg / ml suspension with appropriate solution (physiological saline). Rats were reared under conventional feeding conditions, free to drink water, and after fasting for 12 hours, 200 mg / kg of drugs were given by intragastric administration. 0.083, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 24 (h) after administration. About 0.3-0.5ml of blood was collected from the orbit, and centrifuged at 5000rpm for 15min. Take 150 μl of plasma, add 1ml of ethyl acetate, vortex for 3 minutes, centrifuge at 13400 rpm for 5 minutes, take 800 μl of organic layer, and evaporate to dryness with nitrogen. The resi...

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Abstract

The invention discloses a novel crystal-type state of rotundine solid chemical matter, which is shown as the formula (I), a preparation method of the novel crystal-type sample, and superior clinical therapeutic action of the novel crystal-type matter of the rotundine as active components in the preparation and the development of various formulations and medicament compositions for preventing and treating pains caused by various reasons, including headache, cramp, labour pains, and the like, and diseases caused by pains, such as insomnia, arrhythmia, and the like. Compared with the traditional officinal crystal-type solid matter (Crystal A type), the two types of novel crystal-type solid matter of the rotundine have higher absorption and blood concentration. Different crystal-type matter can influence the absorption speed and the blood concentration in an organism as well as the bioavailability of the active components of the medicaments, and thereby influencing the preventive and therapeutic effect of the medicaments in clinical applications.

Description

technical field [0001] The invention relates to a crystal C type substance of rotundine, which belongs to the technical field of medicine. Background technique [0002] Rotundine, chemical name is 2,3,9,10-tetramethoxy-5,8,13,13a-tetrahydro-6H-dibenzo[a,g]thiazine, specific rotation is -290 °~-300°, the structural formula is as follows: [0003] [0004] Luotong was designated as the second part of the 2005 edition of "Chinese Pharmacopoeia" [1] The drug category is recorded. At present, the drug includes rotundine tablet (page 339), rotundine hydrochloride tablet (page 536), and rotundine sulfate injection (page 339). Because rotundine drug itself has the defect of poor absorption, so just developed rotundine hydrochloride tablet, to promote its absorption. [0005] An article about “(-)-Tetrahydropalmatine Monohydrate” published in Acta Crystallographica Section C, Volume 54, Issue 12, Page 1977, was retrieved from the literature [2] , which records the crystal stru...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61P9/06A61P29/00A61K31/4375C07D455/03A61P25/20
Inventor 杜冠华吕扬杨世颖强桂芬张恒艾应剑
Owner INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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