Clonidine pamoate and preparation method thereof

A kind of technology of pamoate and pamoic acid, applied in the field of medicine

Active Publication Date: 2017-06-13
力赛生物医药科技(厦门)有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are no relevant reports on the preparation of clonidine and pamoic acid into salts, and the study of the crystal forms of their salts

Method used

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  • Clonidine pamoate and preparation method thereof
  • Clonidine pamoate and preparation method thereof
  • Clonidine pamoate and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0079] Example 1 Screening the preparation conditions of clonidine pamoate with different solvent systems and clonidine free base and pamoic acid molar ratio

[0080] Screen the preparation conditions of clonidine pamoate with different solvent systems and molar ratios of clonidine free base and pamoic acid, as shown in the table below.

[0081]

[0082]

[0083] As can be seen from the table above, the solvent used to prepare the clonidine pamoate and the molar ratio of clonidine free base and pamoic acid have a great influence on the preparation of clonidine pamoate, and many solvent systems form salts The crystal form of is a solvate and is relatively unstable. Clonidine free base and pamoic acid carry out feeding reaction at a molar ratio of 1:1, and the solvent is removed by suction filtration to obtain a solid, which is measured by XRD and HPLC, and the measurement results show that the solid is clonidine pamoate (2:1) The mixture of clonidine free base and pamoic...

Embodiment 2

[0084] Embodiment 2 Preparation of clonidine pamoate crystal form I

[0085] Add 10.0 mg of clonidine into 1 ml of DMSO, stir to obtain a clear solution, add 8.4 mg of pamoic acid, stir to dissolve at 25°C, continue stirring for 1 hour, slowly add 5 ml of water, and obtain a light yellow solid by suction filtration. Vacuum-dried at room temperature in a drying oven to obtain about 12.1 mg of light yellow crystals.

Embodiment 3

[0086] Embodiment 3 Preparation of clonidine pamoate crystal form I

[0087] Add 20mg of clonidine into 3ml of ethanol, stir to obtain a clear solution, add 8.4mg of pamoic acid, suspend and stir at 20°C for 2 hours, filter with suction to obtain a light yellow solid, place it in a drying oven and dry it under vacuum at room temperature to obtain About 10.5 mg of light yellow crystals.

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Abstract

The invention relates to clonidine pamoate and a preparation method thereof. The clonidine pamoate is formed by clonidine and pamoate in a solvent in a molar ratio of 2:1. The clonidine pamoate provided by the invention exists in three crystal forms, the solubility of each crystal form is lower, the solubility in water is about 0.02mg/ml and is equivalent to one hundredth of the solubility of clonidine (2.19mg/ml) and one thousandth of the solubility of clonidine hydrochloride (79.4mg/ml), the slow-release effect can be achieved without a complex preparation technology and is very stable, and crystal transformation does not occur under hot and humid and strong light conditions and under an accelerated test condition; and a production process is simple, and granularity can be easily controlled, so that the clonidine pamoate is applicable to enlarged production. The clonidine pamoate is applicable to being made into a long-acting slow-release preparation, can reduce mediation frequency, improves the medication compliance of a patient, can enable blood drug concentration to be balanced, avoids a peak valley phenomenon and reduces adverse reactions during medication.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to pamoate of clonidine and a preparation method thereof. Background technique [0002] Clonidine, the chemical name is: 2,6-dichloro-N-(2-imidazolin-2-yl)aniline, the molecular weight is 230.1, the melting point is 131°C, and the Pka is 8.05. Its structural formula is as follows: [0003] [0004] It is a selective central α2-receptor agonist, which can reduce peripheral sympathetic nerve activity and present a strong antihypertensive effect. In addition to being widely used in the treatment of various high blood pressure, it can also be used to prevent and treat migraine, glaucoma, attention deficit and hyperactivity disorder in children and adolescents, etc. [0005] Clonidine is a weak organic base and there are various counterions for preparing salts of the base using inorganic and organic acids. For the formation of salts of basic drugs, the most commonly use...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D233/50
CPCC07B2200/13C07D233/50
Inventor 朱海健许凉凉揭从能蔡林辉顾自强
Owner 力赛生物医药科技(厦门)有限公司
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