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A kind of homogenine hydrobromide compound and preparation thereof

A technology of clathrin hydrobromide and compound, which is applied in the field of medicine, can solve the problems of insignificant change of pH of solution, unstable and falling under strong light irradiation, and achieves good stability, safe and reliable clinical application, and improved stability. Effect

Active Publication Date: 2016-05-04
SHANDONG LUOXIN PHARMA GRP CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] It has been found by research that the raw material of homogenin hydrobromide is stable to humidity or heat, and is more sensitive to light. Its degradation rate constant is about 2 times that of the constant temperature accelerated test, and the pH of the solution does not change significantly; the drug content and its aqueous solution of the lyophilized powder decrease significantly when irradiated by strong light
Both uricine hydrobromide injection and freeze-dried powder are unstable to strong light irradiation

Method used

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  • A kind of homogenine hydrobromide compound and preparation thereof
  • A kind of homogenine hydrobromide compound and preparation thereof
  • A kind of homogenine hydrobromide compound and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] 1. Grind the crude homogenin hydrobromide, pass it through a 200-mesh sieve, and then add it to anhydrous methanol at 45°C to prepare a saturated solution of homogenin hydrobromide;

[0049]2. While stirring, add water: dimethyl sulfoxide: ethyl acetate mixed solution with a volume ratio of 3:1:1, and lower the temperature to 10°C at the same time; the stirring speed is 360 rpm; the weight of the mixed solvent is the weight of the methanol solution 8 times of , the adding speed is 20 ml / min;

[0050] 3. After adding the mixed solution, let it stand still, and continue to cool down to 2°C at a cooling rate of 1.5°C / hour; grow the crystal for 4 hours, wash, and dry to obtain homogenin hydrobromide dihydrate.

[0051] The compound crystal is detected by high-performance liquid chromatography, and the purity is 99.97%, and the yield is 94.7%; the X-ray powder diffraction pattern obtained by using Cu-Kα ray measurement is as follows: figure 1 As shown, the thermogravimetric...

Embodiment 2

[0053] 1. Grind the crude homogenin hydrobromide, pass through a 300-mesh sieve, and then add it to anhydrous methanol at 40°C to prepare a saturated solution of homogenin hydrobromide;

[0054] 2. While stirring, add water: dimethyl sulfoxide: ethyl acetate mixed solution with a volume ratio of 2:1:2, and lower the temperature to 20°C at the same time; the stirring speed is 720 rpm; the weight of the mixed solvent is the weight of the methanol solution 12 times of , the adding speed is 40 ml / min;

[0055] 3. After adding the mixed solution, let it stand still, and continue to cool down to 4°C at a cooling rate of 1.5-3°C / hour; grow crystals for 3 hours, wash, and dry to obtain homogenin hydrobromide dihydrate.

[0056] The compound crystal is detected by high-performance liquid chromatography, and the purity is 99.97%, and the yield is 95.1%; the X-ray powder diffraction pattern obtained by using Cu-Kα ray measurement is as follows: figure 1 As shown, the thermogravimetric a...

Embodiment 3

[0058] 1. Grind the crude homogenin hydrobromide, pass through a 300-mesh sieve, and then add it to anhydrous methanol at 42°C to prepare a saturated solution of homogenin hydrobromide;

[0059] 2. While stirring, add water: dimethyl sulfoxide: ethyl acetate mixed solution with a volume ratio of 3:1:3, and lower the temperature to 15°C at the same time; the stirring speed is 480 rpm; the weight of the mixed solvent is the weight of the methanol solution 10 times of , the adding speed is 30 ml / min;

[0060] 3. After adding the mixed solution, let it stand still, continue to cool down to 2°C, and the cooling rate is 2°C / hour; grow crystals for 4 hours, wash, and dry to obtain homouginin hydrobromide dihydrate.

[0061] The compound crystal is detected by high-performance liquid chromatography, and the purity is 99.97%, and the yield is 94.3%; the X-ray powder diffraction pattern obtained by using Cu-Kα ray measurement is as follows: figure 1 As shown, the thermogravimetric anal...

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Abstract

The invention belongs to the field of medicine, and particularly relates to a lappaconite hydrobromide compound and a preparation thereof. The lappaconite hydrobromide compound provided by the invention is lappaconite hydrobromide dihydrate, and the lappaconite hydrobromide dihydrate is measured by using a Cu-K alpha ray to obtain an X-ray powder diffraction pattern (as shown in Figure 1). The invention also discloses a pharmaceutical composition containing the lappaconite hydrobromide dihydrate, and the dosage form of the pharmaceutical composition is an aseptic powder injection, a freeze-dried powder injection or a water injection. The lappaconite hydrobromide dihydrate prepared by the invention is good in stability, especially, the stability under a light condition is improved, and the bioavailability is greatly improved, and the lappaconite hydrobromide dihydrate is more suitable for clinical application.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a homogenine hydrobromide compound and its preparation. Background technique [0002] Urine hydrobromide (C 32 h 44 N 2 o 8 .HBr.H 2 O) is the hydrobromide monohydrate of rabaaconitine extracted from the root of the ranunculaceae plant Aconitum aconitum. It is the first non-addictive central nervous system analgesic drug in China. Moderate analgesics as prescribed in the Guiding Principles of Analgesic Therapy. Its analgesic strength is 7 times that of aminopyrine, and its analgesic effect is equivalent to that of pethidine. It has no teratogenic and mutagenic effects, and has local anesthesia, cooling and antipyretic and significant anti-inflammatory and detumescent effects. Clinically, it is mainly used to treat moderate and above pain caused by various reasons. Its molecular structural formula is: [0003] [0004] At present, some literatures and patents have been published...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D221/22A61K31/439A61P25/04
CPCC07D221/22
Inventor 朱玉青徐淑周徐太平陈维彩
Owner SHANDONG LUOXIN PHARMA GRP CO LTD
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