Rifapentine, refampicin, rifabutin or rifamdin injection and its preparing method

A technology of rifapentine and rifampicin, which is applied in the direction of pharmaceutical formulations, medical preparations containing active ingredients, powder delivery, etc. It can solve the problems of poor directional controlled release, long time to peak blood drug concentration, and Long time and other issues, to achieve the effect of increasing the route of administration and drug efficacy, improving bioavailability, and facilitating storage and transportation

Inactive Publication Date: 2006-05-24
WUHAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although these drugs have strong penetrating power to human tissues and better absorption rate through oral administration, they must pass through the liver to reach the lungs, and the peak time is long, the effective drug concentration is low, and the directional controlled release effect is poor.
Due to the poor water solubility of rifapentine, rifampin, rifabutin and rifadine, the absorption of solid preparations is slow, and the time to peak blood drug concentration is long, the treatment cycle for refractory tuberculosis is between 6 months and 1 year. Its toxic and side effects and adverse effects caused by oral dosage are also very significant; and long-term use of this type of antibiotics, bacterial resistance also increases rapidly
[0004] About the preparation of rifampicin microemulsion Microencapsulation 1995; 12 (4) 401 reported a method, dissolving rifampicin in Span 85 was prepared into an oil droplet suspension, which was used for the sterilization experiment of Mycobacterium tuberculosis. This emulsion The dispersion is not good enough, the stability is poor, and it has not been used clinically so far
There are also reports in China that rifampicin is prepared into microcapsules by using degradable polymer material polylactic acid and attempts to develop their use. Due to the complexity of the preparation, the resulting particle size is too large and the distribution is uneven, so it is difficult to be used as an injection or perfusion solution. Clinical treatment for tuberculosis and other tuberculosis

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] 5 parts of rifapentine (one of rifampicin, rifabutin, and rifampin raw materials), 40 parts of organic co-solvent (replenish with water for injection or normal saline when not added), 5 parts of auxiliary drugs ( If the prescription is not added, supplement it with water for injection or normal saline), 0.05 parts of surfactant (if not added, supplement it with water for injection or normal saline), 0.0057 parts of sodium hydroxide, 0.1 part of alkaline antioxidant, normal saline (or water for injection) 49.85 parts, pH is 7.8~9.0.

[0031] Preparation method of aqueous injection: Accurately weigh the raw material drug, organic co-solvent, surfactant, auxiliary drug, alkaline antioxidant, physiological saline (or water for injection) according to the above formula, put them in the liquid preparation tank and dissolve them into a homogeneous phase first. , adding sodium hydroxide solution and stirring to adjust the pH value to 8.9, so that each component is fully dissolv...

Embodiment 2

[0038] *Sodium hydroxide is added in 0.005%~0.15% solution

[0039] According to the formula measurement, accurately weigh rifapentine (rifampicin, rifabutin or rifadin), cosolvent, polyethylene glycol, antioxidant, saline and place it in the liquid preparation tank, so that each component is fully Dissolve, add sodium hydroxide solution to adjust the pH value to 8.7, and generate a red transparent solution. Filtrate, fill, seal with nitrogen, and sterilize to prepare rifapentine injection.

Embodiment 3

[0041] Component

[0042] Measure and weigh rifapentine (rifampicin, rifabutin or rifampin), lauroyl diethanolamine, isoniazid, propylene glycol, sodium hydroxide, sodium formaldehyde sulfoxylate, and normal saline according to the formula. Stir in the liquid tank to fully dissolve, filter to obtain a transparent red solution, which is rifampicin compound drug injection. Divide into packages, fill with nitrogen and seal, and sterilize for use.

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PUM

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Abstract

The present invention relates to a kind of rifapentine, rifampicin, rifabutine or rifandin injection and its preparation method. It includes main medicine, medicinal organic cosolvent, alkaline antioxidant, injection water surfactant and sodium hydroxide. Its main medicine can be rifapentine, rifampicin, rifabutine or rifandin. Said invention also provides the concrete steps of its preparation method.

Description

technical field [0001] The present invention relates to rifapentine or rifampicin and a class of broad-spectrum killing Mycobacterium tuberculosis antibiotic drug injections and perfusions and their compound injections and perfusions new formulations and preparation methods thereof; specifically to rifapentine and rifampicin , rifabutin or rifadin single powder injection, water injection, compound drug powder injection, water injection and preparation method thereof. Background technique [0002] Rifapentine (Dickfell), rifampicin, rifabutin, and rifampin are a class of broad-spectrum antibiotics that kill Mycobacterium tuberculosis, and are widely used in the treatment of tuberculosis and other tuberculosis. Because this type of drug is almost insoluble in water, its application is greatly limited. So far, there is no injection for clinical treatment in China, and it can only be administered orally. [0003] At present, rifapentine and rifampicin powder capsules and tablet...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/496A61K9/08A61K9/14A61K45/06A61P31/06
Inventor 束家有全向阳束怡朱墨刘起军
Owner WUHAN UNIV
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