External colchicine composition

Abstract

The invention relates to an external colchicine composition. The external colchicine composition at least comprises colchicine and a cosolvent, wherein the cosolvent is polyhydric alcohol. According to the invention, the administration route of colchicine is changed, and a new colchicine dosage form is formed, so that the colchicine can be put into clinical use in the new dosage form.

Description

[0001] This case is a divisional application with the application number 2016109824148, the application date is November 8, 2016, the application type is invention patent, and the application name is colchicine composition for external use and its preparation method. technical field

[0002] The invention belongs to the field of medicine, in particular to the field of medicine for treating gouty arthritis. Specifically, the present invention relates to a colchicine topical composition for preventing or treating gouty arthritis, especially a colchicine liniment, and a preparation method thereof. Background technique

[0003] Gout is a disease caused by the disorder of purine metabolism in the body. It is mainly manifested as hyperuricemia. Urate crystallizes in joints, kidneys and connective tissues, which can cause local inflammation of joints and infiltration of granulocytes, leading to gout attacks. The incidence of gout is increasing year by year worldwide. In my country...

Examples

Embodiment 1

[0031] Embodiment one, the prescription research of colchicine liniment

[0032] 1 Instruments and reagents

[0033] 1.1 Instrument

[0034] Agilont1260 high performance liquid chromatograph (Agilent company) includes G131K quaternary gradient pump, G13298 injector, G1316A column thermostat, G1315DDAD detector, workstation: ChemstationforLC3Dsystes. VV-1800 UV-Vis Spectrophotometer (Shimadzu, Japan); KS-2500 Ultrasonic Instrument (Ningbo Kesheng Instrument Factory); pH211A Acidity Meter (Italy HANNA); BP211D 1 / 100,000 Precision Electronic Balance ( Germany Sartorius); ZORBAXC18 chromatographic column (150mm × 4.60mm, 5μm, Agilent Company); YB-3 clarity detector (Tianjin University Precision Instrument Factory); DHG-9140A electric heating constant temperature blast drying oven (Shanghai-Heng Technology Co., Ltd Company); SDC-II high-purity water device (Institute of Health Equipment, Academy of Military Medical Sciences); SHZ-D (III) circulating water vacuum pump (Gongyi Ying...

Embodiment 2

[0098] Embodiment 2, the anti-inflammatory effect of colchicine liniment on gout model animals

[0099] 1. Materials and methods

[0100] 1.1 Drugs and reagents Colchicine liniment (prescription 4 in Table 1-1, also 2.5.1 prescription i in Example 1, colchicine content is 0.2w / v%), colchicine (Yunnan Kunming Pharmaceutical Co., Ltd. Company pharmaceutical factory, content 99.79%), sodium urate (provided by Sigma company), prostaglandin E2 (PGE2) radioimmunoassay kit (provided by Beijing East Asia Institute of Immunology Technology), tumor necrosis factor-α (TNF-α) kit ( Institute of Military Medical Sciences).

[0101] 1.2 Experimental animals SD rats, male, clean grade, weighing 200-250g, were provided by the Experimental Animal Center of the Academy of Military Medical Sciences, and were tested after 3 days of normal feeding in the laboratory.

[0102] 1.3 Method

[0103] 1.3.1 Establishment of acute gouty arthritis model according to CODERRE classic method (Coderre TJ, W...

Embodiment 3

[0124] Example 3: Research on irritation and sensitization of colchicine liniment to skin

[0125] Toxicology research is a key link in drug research and development, which determines whether the drug can enter the clinic and whether the drug is safe to use. Chemical drug irritation and allergy refer to chemical drug preparations administered through eyes, ears, nose, oral cavity, respiratory tract, joint cavity, skin, rectum, vagina, vein, artery, muscle, subcutaneous, paravenous and intrathecal, etc. Drugs, local toxicity (such as irritation and allergy, etc.) and / or systemic toxicity (such as anaphylaxis and hemolysis, etc.) produced by the drug. It is an integral part of the preclinical safety evaluation.

[0126]The colchicine liniment of the present invention is a novel dosage form of colchicine. The invention of this dosage form is based on the fact that the effective therapeutic dose under the oral dose of the colchicine tablet is close to the systemic poisoning dose,...

[0001] This case is a divisional application with the application number 2016109824148, the application date is November 8, 2016, the application type is invention patent, and the application name is colchicine composition for external use and its preparation method. technical field

[0002] The invention belongs to the field of medicine, in particular to the field of medicine for treating gouty arthritis. Specifically, the present invention relates to a colchicine topical composition for preventing or treating gouty arthritis, especially a colchicine liniment, and a preparation method thereof. Background technique

[0003] Gout is a disease caused by the disorder of purine metabolism in the body. It is mainly manifested as hyperuricemia. Urate crystallizes in joints, kidneys and connective tissues, which can cause local inflammation of joints and infiltration of granulocytes, leading to gout attacks. The incidence of gout is increasing year by year worldwide. In my country...

Examples

Embodiment 1

[0031] Embodiment one, the prescription research of colchicine liniment

[0032] 1 Instruments and reagents

[0033] 1.1 Instrument

[0034] Agilont1260 high performance liquid chromatograph (Agilent company) includes G131K quaternary gradient pump, G13298 injector, G1316A column thermostat, G1315DDAD detector, workstation: ChemstationforLC3Dsystes. VV-1800 UV-Vis Spectrophotometer (Shimadzu, Japan); KS-2500 Ultrasonic Instrument (Ningbo Kesheng Instrument Factory); pH211A Acidity Meter (Italy HANNA); BP211D 1 / 100,000 Precision Electronic Balance ( Germany Sartorius); ZORBAXC18 chromatographic column (150mm × 4.60mm, 5μm, Agilent Company); YB-3 clarity detector (Tianjin University Precision Instrument Factory); DHG-9140A electric heating constant temperature blast drying oven (Shanghai-Heng Technology Co., Ltd Company); SDC-II high-purity water device (Institute of Health Equipment, Academy of Military Medical Sciences); SHZ-D (III) circulating water vacuum pump (Gongyi Ying...

Embodiment 2

[0098] Embodiment 2, the anti-inflammatory effect of colchicine liniment on gout model animals

[0099] 1. Materials and methods

[0100] 1.1 Drugs and reagents Colchicine liniment (prescription 4 in Table 1-1, also 2.5.1 prescription i in Example 1, colchicine content is 0.2w / v%), colchicine (Yunnan Kunming Pharmaceutical Co., Ltd. Company pharmaceutical factory, content 99.79%), sodium urate (provided by Sigma company), prostaglandin E2 (PGE2) radioimmunoassay kit (provided by Beijing East Asia Institute of Immunology Technology), tumor necrosis factor-α (TNF-α) kit ( Institute of Military Medical Sciences).

[0101] 1.2 Experimental animals SD rats, male, clean grade, weighing 200-250g, were provided by the Experimental Animal Center of the Academy of Military Medical Sciences, and were tested after 3 days of normal feeding in the laboratory.

[0102] 1.3 Method

[0103] 1.3.1 Establishment of acute gouty arthritis model according to CODERRE classic method (Coderre TJ, W...

Embodiment 3

[0124] Example 3: Research on irritation and sensitization of colchicine liniment to skin

[0125] Toxicology research is a key link in drug research and development, which determines whether the drug can enter the clinic and whether the drug is safe to use. Chemical drug irritation and allergy refer to chemical drug preparations administered through eyes, ears, nose, oral cavity, respiratory tract, joint cavity, skin, rectum, vagina, vein, artery, muscle, subcutaneous, paravenous and intrathecal, etc. Drugs, local toxicity (such as irritation and allergy, etc.) and / or systemic toxicity (such as anaphylaxis and hemolysis, etc.) produced by the drug. It is an integral part of the preclinical safety evaluation.

[0126]The colchicine liniment of the present invention is a novel dosage form of colchicine. The invention of this dosage form is based on the fact that the effective therapeutic dose under the oral dose of the colchicine tablet is close to the systemic poisoning dose,...

Images