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Rifampicin and anethol trithione compound preparation

A technology of rifampicin, anise three, compound preparation, applied in the directions of pharmaceutical formulations, medical preparations containing active ingredients, antibacterial drugs, etc. Tuberculosis, the effect of good therapeutic effect

Inactive Publication Date: 2013-03-13
HAINAN WEI KANG PHARMA QIANSHAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, rifampicin is poorly soluble in water, and it is transported to the liver in the form of protein binding in the body, where it is acetylated in the liver and excreted with bile to intestinal metabolism

Method used

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  • Rifampicin and anethol trithione compound preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Weigh 150g of rifampicin and 1.25g of anethiol, 200g of carbomer, 10g of HPMC, 20g of stearyl alcohol, NaHCO 3 Pass through an 80-mesh sieve, and after fully mixing, add an appropriate amount of magnesium stearate as a lubricant, and after mixing evenly, directly compress into tablets by dry method, and the hardness is controlled at 3-4kg.

Embodiment 2

[0018] Weigh 150g of rifampicin, 2.5g of anetisone, raw material medicine and 250g of MCC (microcrystalline cellulose), respectively pulverize and pass through a 100-mesh sieve. Mix evenly with the method of equal incremental addition and pass through an 80-mesh sieve, add an appropriate amount of 2% HPMC solution to make a soft material, and extrude to form a ball. Take out the pellets, dry at 50°C for 3 hours, and sieve to obtain pellets with 18-24 mesh. The aperture of the sieve plate is 0.9mm, and the extrusion speed is 30r·min -1 , at 50r·min -1 High speed shearing 1min, 40r·min -1 Roll into a ball for 4 minutes. Take an appropriate amount of ethyl cellulose aqueous dispersion, dilute with water to prepare a coating solution with a solid content concentration of 12.5%, stir and mix evenly, and keep warm at 30°C for later use. Put the 18-24 mesh pellets in a micro-fluidized bed granulation coating dryer for fluidization preheating, coat with the prepared coating liquid...

Embodiment 3

[0020] Dissolve 100 g of Edragit® RS (a coating material) in 1000 mL of acetone, add 20 g of talc powder, 20 g of triethyl citrate, and an appropriate amount of simethicone, and stir overnight to obtain a coating solution. Weigh 150g of rifampicin and 2.5g of anethrizione, crush the raw materials to 100 mesh, mix them with lactose evenly, put them into the fluidized bed, adjust the inlet temperature to 35°C, and preheat for 5 minutes. Then adjust the boiling air volume to keep the material in the best fluidized state. Adjust the inlet temperature to 40 °C, the spray pressure to 150 kPa, and the spray rate to 5 mL min -1 , with a mass concentration of 1 g L -1 Pre-granulate 200mL of ethyl cellulose alcohol solution until the spraying is finished, stop spraying and continue drying for 10 minutes, take out the particles and sieve, take 80-120 mesh particles and put them into the fluidized bed for preheating for 5 minutes, increase according to the coating increase The weight is...

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Abstract

The invention provides a rifampicin anethol trithione compound preparation, and relates to the technical fields of medicine and medicine manufacturing. The compound preparation comprises the following components in percentage by weight: 0.1-99.9 percent of rifampicin and 99.9-0.1 percent of anethol trithione. The rifampicin and the anethol trithione have a good coordination function; and by the anethol trithione, the cell capability is improved, and liver injury caused by the rifampicin can be effectively treated by increasing choleresis. The rifampicin and the anethol trithione are compounded, so that a good treatment effect on tuberculosis patients is achieved, the adverse reaction of the rifampicin also can be reduced, and the liver injury caused by the rifampicin can be reduced.

Description

Technical field: [0001] The invention relates to the technical field of medicine and medicine manufacture, in particular to a compound preparation of rifampicin and anetisone. Background technique: [0002] Statistics from the World Health Organization (WHO) show that the incidence of tuberculosis has shown a sharp increase in the world in recent years, and the death rate ranks first among various infectious diseases. my country is one of the countries with a high incidence of tuberculosis in the world. [0003] Rifampin (RIF) is the first-line antituberculosis drug recommended by WHO. Rifampicin was invented in 1965, and the discovery of rifampicin brought another great leap forward in the treatment of tuberculosis. The sterilizing properties of rifampicin are: after it combines with the bacterial ribonucleic acid polymerase of Mycobacterium tuberculosis, it interferes with the synthesis of deoxyribonucleic acid and protein, thereby achieving the purpose of sterilization. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/496A61K31/385A61P31/06
Inventor 汪六一汪金灿吴函峰李彪
Owner HAINAN WEI KANG PHARMA QIANSHAN
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