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Itraconazole dispersible tablets and preparation method thereof
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A technology of itraconazole and dispersible tablets, applied in the field of itraconazole dispersible tablets and its preparation
Active Publication Date: 2013-08-07
HARBIN SANLIAN PHARMA CO LTD
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[0008] Patent ZL200910305827.2 discloses an itraconazole composition and its preparation method. The composition is composed of itraconazole, starch, mannitol, sucrose, and stevioside. The preparation process is simple, and the pharmaceutical excipients used are safe, Does not contain organic solvents that are harmful to the human body, has low cost and good stability, but it takes more than 100 minutes for the dissolution rate to reach more than 85%, and the dissolution rate needs to be improved
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Embodiment 1
[0023] Accurately weigh the following ingredients:
[0024] Itraconazole 100g (Shandong Shouguang Fukang Pharmaceutical Co., Ltd.), hydroxypropyl methylcellulose 100g (Anhui Shanhe Pharmaceutical Excipients Company), crospovidone (purchased from BASF) 100g, dichloromethane 1000g (Tianjin Fuchen Chemical Reagent Factory). Mix the raw materials evenly, control the solution temperature to 40°C, and let itraconazole and other solids be dissolved in liquid dichloromethane.
[0025] Accurately weigh the following ingredients:
[0026] Cyclodextrin 100g, sodium lauryl sulfate 10g, polyethylene glycol 400010g, absolute ethanol 300g. Mix the raw materials evenly, control the solution temperature to 40°C, and let the solids such as cyclodextrin dissolve in the liquid ethanol.
[0027] Mix the above two solutions evenly until itraconazole is completely dissolved, and then dry it with a spray dryer, the temperature at the inlet of the dryer is 170°C, and the temperature at the outlet i...
Embodiment 2 to 9
[0030] Examples 2 to 9, as shown in Table 1: the operation steps are the same as in Example 1, except that the addition amount of each component is different. In addition, for the process conditions in the preparation method of the present invention (such as the dissolution temperature of each step described in the foregoing summary of the invention, the temperature of the inlet and outlet of the drier, the temperature of the inlet and outlet of the granulator, the selection type of the granulator, etc.), it can be based on the addition of Simple adjustments to the amounts of components or actual operating conditions have basically no effect on the properties of the obtained itraconazole dispersible tablets.
[0031] The selection and weight ratio of each component in the preparation method of itraconazole dispersible tablet of the present invention is the preferred range value obtained by the inventor through consulting a large number of documents and numerous tests, that is, ...
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Abstract
The invention relates to itraconazole dispersible tablets with improved dissolubility and a preparation method thereof. The method comprises the following steps of: mixing itraconazole, hydroxypropyl methyl cellulose, crosslinking povidone and dichloromethane in a weight ratio of 1:(1-5):(1-5):(10-20) uniformly, dissolving fully, and controlling the temperature to be between 40 and 80 DEG C; mixing cyclodextrin, lauryl sodium sulfate, polyethyleneglycol 4000 and ethanol in a weight ratio of 1:(0.1-1):(0.1-2):(3-6) uniformly, dissolving fully, and controlling the temperature to be between 40 and 60 DEG C; mixing the mixture uniformly until the itraconazole is dissolved completely, drying, and granulating to obtain itraconazole composite powder; and mixing the composite powder and pharmaceutic adjuvants uniformly, and tabletting to obtain the itraconazole dispersible tablets. The itraconazole dispersible tablets are high in water solubility, easy to disperse and high in dissolution, andthe problems of low water solubility and low bioavailability of the itraconazole are solved.
Description
technical field [0001] The invention relates to itraconazole, in particular to an itraconazole dispersible tablet with improved solubility and a preparation method thereof. Background technique [0002] Itraconazole is a triazole antifungal drug that is insoluble in water. It has antifungal effects on deep fungi and superficial fungi. It is widely used because of its strong activity, broad antibacterial spectrum and high cure rate. Its structural formula is as follows: [0003] [0004] Studies have shown that itraconazole has poor water solubility, and it is difficult to disperse tablets. The dissolution process is a difficult point in the work of itraconazole dispersible tablets. Due to its low water solubility (below 1 μg / ml), there is a problem of very low bioavailability when administered orally. [0005] In order to increase the water solubility of itraconazole to improve its bioavailability, patent ZL98806999.7 discloses an amorphous form of itraconazole particle...
Claims
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