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Itraconazole emulsion for injection and its prepn

A technology of itraconazole and injection milk, which is applied in the field of medicine, can solve the problems of low bioavailability of oral capsules, aggravate adverse reactions and side effects, and complicated preparation process, so as to improve bioavailability and have lymphatic affinity sex, increase the effect of drug absorption

Inactive Publication Date: 2006-03-01
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the preparation process of the injection prepared by the cyclodextrin inclusion compound of itraconazole is complicated, and because it uses a large amount of hydroxypropyl beta cyclodextrin as a solubilizer, it not only aggravates the adverse reactions and side effects, but also It also increases the cost of the preparation; the low bioavailability of oral capsules limits its use in severe patients who are difficult to swallow (such as with mucositis) and with invasive infections, who need to reach the lowest steady-state drug trough concentration as soon as possible and need Use in Patients Maintaining High Blood Concentrations

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Mix 5 g of itraconazole and 150 g of hydroxypropyl-β-cyclodextrin, place in a mortar, heat until molten, and cool rapidly to obtain a solid complex of itraconazole.

[0032] The present invention contains following components in grams by weight in every 1000ml emulsion:

[0033] 3g of itraconazole solid compound, 10g of emulsifier, 60g of corn oil, 20g of isotonic regulator, and the rest is water. The emulsifier is egg yolk lecithin and poloxamer composition; the isotonic regulator is xylitol; the pH regulator is phosphoric acid.

[0034] Preparation method: disperse itraconazole solid complex and emulsifier in corn oil as the oil phase; dissolve the isotonic regulator in water for injection as the water phase; stir the two phases evenly and heat to about 60°C respectively; the water phase Slowly add it dropwise into the oil phase, stir while adding, continue to stir for 15 minutes after the addition, and then disperse and emulsify in a tissue masher to obtain colostru...

Embodiment 2

[0036] Mix 5 g of itraconazole and 40 g of poloxamer, place in a mortar, heat to melt, and cool rapidly to obtain a solid complex of itraconazole.

[0037] The present invention contains following components in grams by weight in every 1000ml emulsion:

[0038] 70g of itraconazole solid complex, 30g of emulsifier, 80g of castor oil, 50g of isotonic regulator, and the rest is water. The emulsifier is hydrogenated soybean lecithin and cholesterol composition; the isotonic regulator is glycerin; the pH regulator is glacial acetic acid.

[0039] Preparation method: the itraconazole solid complex is dispersed in castor oil as the oil phase; the emulsifier and isotonic regulator are dispersed in water for injection as the water phase; the two phases are stirred evenly and heated to about 80°C respectively; the oil phase Slowly add it dropwise into the water phase, stir while adding, continue to stir for 60 minutes after the addition, and then disperse and emulsify in a tissue mashe...

Embodiment 3

[0041] 40 g of itraconazole and 3 g of polyvinylpyrrolidone were dissolved in an appropriate amount of ethanol and chloroform, and then the solvent was evaporated under reduced pressure to obtain a solid complex of itraconazole.

[0042] The present invention contains following components in grams by weight in every 1000ml emulsion:

[0043] 25g of itraconazole solid compound, 45g of emulsifier, 150g of soybean oil, 70g of isotonic regulator, and the rest is water. The emulsifier soybean lecithin; the isotonic regulator is 1.2-propylene glycol; the pH regulator is sodium hydroxide.

[0044] Preparation method: heat the emulsifier with an appropriate amount of absolute ethanol to dissolve it, add itraconazole solid complex and peanut oil as the oil phase; dissolve the isotonic regulator in water for injection as the water phase; stir the two phases evenly and separate Heat to about 50°C; slowly drop the oil phase into the water phase, stir while adding, and continue stirring f...

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PUM

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Abstract

The present invention relates to medicine technology, and is one kind of Itraconazole emulsion for injection and its preparation process. Each 1000 ml of the Itraconazole emulsion for injection contains solid Itraconazole compound 2-80 g, vegetable oil for injection 50-300 g, emulsifier 5-50 g, and isosmotic regulator 15-100 g, except pH regulator and water. By means of emulsifying technology and with oil-water interface film in carrying medicine, the present invention solves the problem of dispersing water and oil insoluble Itraconazole. Compared with intravenous injection and oral liquid of Itraconazole, the present invention has less negative effect, less toxic side effect, high bioavailability, low preparation cost and taking convenience.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to an itraconazole injection emulsion and a preparation method thereof. Background technique [0002] Itraconazole (Itraconazole) is a second-generation triazole synthetic broad-spectrum antifungal drug, which has a good curative effect on the treatment of diseases caused by fungal infections. It has a broad antibacterial spectrum and good tolerance. The main metabolite, hydroxyitraconazole, also has high antifungal activity. [0003] However, itraconazole has very low solubility in water (less than 1 μg / ml), slightly soluble in ethanol, easily soluble in dichloromethane, and is a weakly basic compound (pKa=3.7), with an oil-water partition coefficient of 5.66 and lipophilicity. strong. It can be ionized in gastric juice only under low pH conditions. These physical and chemical properties greatly limit the development of its formulations. PCTWO85 / 02767 and US Patent 4,764,604 r...

Claims

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Application Information

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IPC IPC(8): A61K31/496A61K9/107A61P31/10
Inventor 王思玲苏德森孔蓓蓓
Owner SHENYANG PHARMA UNIVERSITY
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