A kind of trientine hydrochloride compound

一种盐酸曲恩、化合物的技术，应用在盐酸曲恩汀化合物领域，能够解决药物晶型报道等问题

Active Publication Date: 2019-06-21
KAIMOSI MEDICAL TECH(SHANGHAI) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Compared with the earlier penicillamine, trientine hydrochloride has few side effects, and there are no reports of allergic reactions to the drug
[0007] The chemical name of trientine hydrochloride is triethylenetetramine dihydrochloride, and there is no report on the crystal form of the drug yet

Method used

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  • A kind of trientine hydrochloride compound
  • A kind of trientine hydrochloride compound
  • A kind of trientine hydrochloride compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065] Trientine hydrochloride of the present invention is prepared according to the following steps:

[0066] Weigh 50.0g of trientine, add 25.0mL of water and stir, add dropwise hydrochloric acid to adjust the pH value to 8.0, add 50mL of ethanol, stir and crystallize at room temperature, take the precipitate, and dry it at 80°C to obtain trientine hydrochloride compound The white powder of the crystalline form I, the yield is 80%.

[0067] The detection method of crystal of the present invention comprises:

[0068] 1. X powder diffraction test

[0069] 1) Sample treatment: directly weigh the sample for X-ray diffraction test.

[0070] 2) Test instrument: X'Pert Pro MPD Philips X-ray powder diffractometer (radiation source CuKα, graphite monochromator, measuring range: 5-50°2θ).

[0071] 3) Test conditions: CuKα radiation, graphite monochromator, tube pressure 40KV, tube current 35mA, 2θ scanning range 5-50°, scanning speed 9° / min, step size 0.03°. Slit conditions: the e...

Embodiment 2

[0078] Trientine hydrochloride of the present invention is prepared according to the following steps:

[0079] Weigh 50.0g of trientine, add 25.0mL of water and stir, add dropwise hydrochloric acid to adjust the pH value to 7.5, add 250mL of methanol, stir and crystallize at room temperature, take the precipitate, and dry it at 80°C to obtain trientine hydrochloride compound The white powder of the crystal form I, the yield is 78%.

[0080] Detect the crystal form I of the trientine hydrochloride compound obtained according to the method described in Example 1, and record its powder X-ray diffraction as shown in Figure 4 .

Embodiment 3

[0082] Trientine hydrochloride of the present invention is prepared according to the following steps:

[0083] Weigh 50.0g of trientine, add 100.0mL of water and stir, add dropwise hydrochloric acid to adjust the pH value to 9.5, add 500.0mL of ethanol, stand at 0°C for crystallization, take the precipitate, and dry at 60°C to obtain koji hydrochloride The white powder of crystal form I of Entine compound has a yield of 75%.

[0084] Detect the crystal form I of the trientine hydrochloride compound obtained according to the method described in Example 1, and record its powder X-ray diffraction as shown in Figure 5 .

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Abstract

The invention discloses a trientine hydrochloride compound, which is characterized by being in a crystal form. The invention further discloses a preparation method and application of the compound, and a medical combination of the compound. The crystal form of the trientine hydrochloride compound has characteristics of good stability, low hygroscopicity, high purity, and low impurity content.

Description

[0001] This application is a divisional application of China's invention patent application No. 201410787042.4. The filing date of this application is December 17, 2014, and the title of the invention is a trientine hydrochloride compound. technical field [0002] The invention provides a trientine hydrochloride compound, specifically crystal form I and crystal form II of the trientine hydrochloride compound, and belongs to the field of medicines. Background technique [0003] Hepatolenticular degeneration, also known as Wilson's disease, is an autosomal recessive disorder of copper metabolism caused by mutations in the ATP 7B gene. Clinically, the disease has liver type, brain type, mixed type and asymptomatic type. Renal impairment and corneal pigment rings. [0004] The worldwide prevalence of hepatolenticular degeneration is 3 / 100,000, of which gene carriers account for 1 / 90. The treatment plan for this type of disease follows the principles of early diagnosis and earl...

Claims

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Application Information

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Patent Type & AuthorityPatents(China)
IPC IPC(8): C07C209/68C07C209/82C07C209/86C07C211/14
CPCC07B2200/13C07C209/68C07C209/82C07C209/86C07C211/14
Inventor宿磊傅霖刘志鸿陈刚李文婕
OwnerKAIMOSI MEDICAL TECH(SHANGHAI) CO LTD