Posaconazole orally taken suspension and preparation method thereof

Abstract

The invention belongs to the technical field of medicines and specifically relates to a posaconazole orally taken suspension and a preparation method thereof. The preparation method is used for preparing a posaconazole orally taken suspension compound on the basis of a micro-crystallizing technology. The posaconazole orally taken suspension compound comprises the following components in parts by weight: 30-50 parts of posaconazole, 160-402 parts of additives, solvent and aqueous medium, wherein the solvent is one or more of glycerinum, ethanol in volume percentage of 95%, absolute ethyl alcohol, propylene glycol and polyethylene glycol 100 / 400. According to the invention, the posaconazole orally taken suspension is prepared through the micro-crystallizing technology; according to the method, the solubility difference of the drug in different solvents is utilized to quickly and uniformly separate out the main drug particles under low-temperature and strong stirring conditions, the grainsize of the main drug particles is small and the distribution is concentrated; and the required grain size is further achieved by adopting the micro-crystallizing technology, the processing steps aresimple, the processing time is shorter, the process is convenient and quick, no high-temperature operation exists in the whole process, the active ingredients are free from decomposing risk, the product impurities are few and the quality is effectively guaranteed.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a posaconazole oral suspension and a preparation method thereof. Background technique [0002] Posaconazole is a derivative of itraconazole, a new generation of triazole antifungal drugs. Chinese alias: 4-[4-[4-[4-[[(3R,5R)-5-(2,4-difluorophenyl)-5-(1,2,4-triazol-1-yl Methyl)oxolan-3-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-2-[(2S,3S)-2-hydroxypent-3-yl]-1 ,2,4-triazol-3-one, the structural formula is as follows. In vitro tests and clinical infection studies have shown that posaconazole has antibacterial activity against microorganisms such as Mycelia and Candida, and also has broad-spectrum antifungal activity against other fungal drug-resistant yeasts and molds. [0003] [0004] Fungal infection is a common disease that is harmful to human health and life-threatening. Invasive candidiasis is currently the most common invasive fungal disease clinically, and ...

AI Technical Summary

Problems solved by technology

Triazole antifungal drugs have stronger antibacterial activity and lower toxicity than amphotericin B and flucytosine, so they are widely used in clinical practice, but the first generation triazole drugs have narrow antibacterial spectrum, low bioavailability and limited Problems such as drug interaction and drug resistance can no longer meet the urgent clinical needs

[0007] However, the original research uses micro-jet technology to make the main drug initially suspended and then pass through narrow apertures and channels under high pressure. The collision and blasting in the process reduce the particle size of the main drug to a certain extent. The micro-jet equipment is expensive, especially for the equipment. It is the key accessories that require extremely high requirements. It is understood that there are few micro-fluidic equipment on the market at present, and the only few brands are almost all imported equipment, and the price is relatively high. Usually, the price ranges from 2 million to 5 million. There are very few equipment manufacturers, and the degree of industrialization is low

Moreover, this process still needs to go through multiple cycles, the process time is long, and each particle of the obtained main drug suspension has different degrees of collision and blasting, and the particle size has certain differences.

Furthermore, the main drug suspension will inevitably stick to the walls of the cavity, circulation pipeline, and transfer container during the micro-fluidic process, and it is difficult to clean and recover due to equipment modeling and other reasons. Compensation is made by means of high dosage of the main drug, and the amount of loss in each batch is different, resulting in a large fluctuation in the content of the finished product

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