Posaconazole orally taken suspension and preparation method thereof
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A posaconazole mouth, posaconazole technology, applied in the field of medicine, can solve the problems of product content fluctuation range, long process time, large main drug loss, etc., to achieve stable and qualified product content, simple process steps, and high quality Guaranteed effect
Inactive Publication Date: 2018-01-26
CHONGQING HUAPONT PHARMA
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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 b
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Embodiment 1
[0052] Example 1 is used to prepare the composition of posaconazole oral suspension by microcrystallization process
[0053] The composition for preparing posaconazole oral suspension by microcrystallization process is composed of the following components in parts by weight: posaconazole 35mg, polysorbate 80 8mg, simethicone 3mg, sodium benzoate 2mg , sodium citrate 0.6mg, citric acid 1.5mg, xanthan gum 3mg, fructose syrup 160mg, titanium dioxide 3mg, essence 4mg, glycerin 320mL and water medium.
Embodiment 2
[0054] Example 2 is used for the microcrystallization process to prepare the composition of posaconazole oral suspension
[0055] The composition used to prepare posaconazole oral suspension by microcrystallization process consists of the following components in parts by weight: posaconazole 45mg, polysorbate 80 10mg, simethicone 4mg, sodium benzoate 2mg , sodium citrate 0.6mg, citric acid 1.5mg, xanthan gum 4mg, fructose syrup 150mg, titanium dioxide 4mg, essence 3mg, glycerin 300mL and water medium.
Embodiment 3
[0056] Example 3 Composition for preparing posaconazole oral suspension by microcrystallization process
[0057] The composition for the preparation of posaconazole oral suspension by microcrystallization process consists of the following components in mg by weight: posaconazole 40mg, polysorbate 80 8mg, simethicone 3mg, sodium benzoate 2mg , sodium citrate 0.6mg, citric acid 1.5mg, xanthan gum 3mg, fructose syrup 340mg, titanium dioxide 4mg, essence 5mg, volume percentage is 200mL of 95% ethanol solution and water medium. Ethanol is filtered out during the process and is not carried into the finished product.
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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 ...
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