Transdermal delivery ointment containing colchicine, and preparation method thereof

A technology for colchicine and ointment, applied in the field of preparation of the ointment, can solve the problems of slow onset of oral dosage forms, discomfort, obvious side effects, etc. fast effect

Active Publication Date: 2013-08-21
SHANGHAI INST OF PLANNED PARENTHOOD RES +4
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Because colchicine is a highly toxic drug, most of the commercially available colchicine dosage forms are oral dosage forms, and the oral dosage forms take effect slowly and bring obvious side effects, which are common in the digestive system. For example, colchicine may appear after oral administration. Nausea, vomiting, abdominal discomfort, loss of appetite, diarrhea, etc., and some even give up taking medicine because of this

Method used

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  • Transdermal delivery ointment containing colchicine, and preparation method thereof
  • Transdermal delivery ointment containing colchicine, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Water Phase Formulation:

[0028] Colchicine

medical sterile water

Glycerin

Sodium dodecyl sulfate

25mg

5mL

0.5g

0.3g

[0029] Oil Phase Formula:

[0030] stearic acid

Glyceryl monostearate

liquid paraffin

vaseline

Azone

4g

2g

0.75g

0.5g

0.5mL

[0031] Liquid silicone rubber: 1g

[0032] Weigh the water phase, oil phase and liquid silicone rubber respectively according to the formula, fully heat and dissolve the three respectively at 80°C, and then slowly add the water phase to the oil phase under the stirring condition of a rotation speed of 300 rpm to obtain a mixture solution, and then add liquid silicone rubber into the above mixed solution, reduce the stirring speed to 100 rpm, stop heating, and cool to obtain.

Embodiment 2

[0034] Water Phase Formulation:

[0035] Colchicine

[0036] Oil Phase Formula:

[0037] Glyceryl monostearate

[0038] Operation steps: Weigh the water phase and oil phase respectively according to the formula, fully heat and dissolve the two respectively at 60°C, and then slowly add the water phase to the oil phase under stirring at a speed of 400 rpm to obtain a mixed solution , the stirring speed was reduced to 80 rev / min, the heating was stopped, cooled, and it was ready.

Embodiment 3

[0040] Water Phase Formulation:

[0041] Colchicine

medical sterile water

Glycerin

Poloxamer

15mg

7mL

1.5g

0.4g

[0042] Oil Phase Formula:

[0043] Glyceryl monostearate

stearic acid

vaseline

vegetable oil

Azone

3g

1.5g

0.6g

2g

0.45mL

[0044] Liquid silicone rubber: 2g

[0045] Operation steps: Weigh the water phase, oil phase and liquid silicone rubber according to the formula, fully heat and dissolve the three respectively at 70°C, and then slowly add the water phase to the oil phase under stirring at a speed of 300 rpm , to obtain a mixed solution, then add liquid silicone rubber to the above mixed solution, reduce the stirring speed to 50 rpm, stop heating, and cool to obtain.

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PUM

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Abstract

The invention provides a transdermal delivery ointment. The transdermal delivery ointment comprises 0.05-10wt% of colchicine, 5-45wt% of medical sterile water, 5-30wt% of a water-soluble excipient, 10-60wt% of an oil-soluble excipient, and 0.1-10wt% of a transdermal enhancer, wherein the sum of the percentages of the above components is 100wt%. The invention also relates to a preparation method of the transdermal delivery ointment. The transdermal delivery ointment can be directly used against foci, and can avoid the generation of side effects of colchicine.

Description

technical field [0001] The invention relates to a transdermal ointment containing colchicine, and also relates to a preparation method of the ointment. Background technique [0002] Colchicine (colchicine), also known as colchicine. Pure colchicine is in the form of yellow needle-like crystals with a melting point of 157°C. Soluble in water, ethanol and chloroform. Bitter, poisonous. Colchicine can control local joint pain, swelling and inflammatory response by inhibiting the production of interleukin-6 by local cells. The pharmacological effect of colchicine on the symptoms of gout is mainly through reducing the activity and phagocytosis of white blood cells and reducing the formation of lactic acid, thereby reducing the deposition of uric acid crystals, reducing the inflammatory response of patients with gout inflammation, and thus playing an analgesic effect. However, colchicine is mainly used for acute gout, and has basically no effect on general pain, inflammation a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K9/48A61K31/165A61K47/44A61P19/06
Inventor 邵海浩李元春陈建兴袁维姝
Owner SHANGHAI INST OF PLANNED PARENTHOOD RES
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