Solid preparation of fluconazole liposome and new application thereof

A technology of fluconazole lipid and solid preparation, applied in the field of liposome preparation, can solve the problems of low dissolution rate, poor stability and the like

Inactive Publication Date: 2010-05-12
HAINAN MEILAN SMITH KLINE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] An object of the present invention is to provide a liposomal solid preparation of fluconazole, specifically, through the combination of a certain amount of lecithin, cholesterol, antioxidant and active ingredient fluconazole, the film dispersion technology is used to make fluconazole Conazole liposome, and then mixed with certain excipients to make various solid preparations, which solved the problems of low dissolution rate and poor stability, and achieved satisfactory results

Method used

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  • Solid preparation of fluconazole liposome and new application thereof
  • Solid preparation of fluconazole liposome and new application thereof
  • Solid preparation of fluconazole liposome and new application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0072] The preparation of embodiment 1 fluconazole liposome

[0073] prescription:

[0074] Component Dosage

[0075] Fluconazole 25g

[0076] Soy Lecithin 55g

[0077] Cholesterol 32.5g

[0078] Ascorbyl Palmitate 2.5g

[0079] Preparation Process

[0080] (1) 25g fluconazole, 55g soybean lecithin, 32.5g cholesterol and 2.5g ascorbyl palmitate are dissolved in the mixed solvent of methanol, Virahol and acetone with a volume ratio of 2:1:2 in 600ml, mix homogeneously, Remove the mixed solvent under reduced pressure on a rotary thin film evaporator to obtain a phospholipid film;

[0081] (2) Add 450ml of citric acid-sodium citrate buffer solution with a pH value of 6.5, shake and stir for 20 minutes at a speed of 600r / min to completely hydrate the phospholipid membrane, and emulsify it at a high speed using a tissue masher for 20 minutes minutes, keep warm at 60°C, rotate at 12000r / min, and then filter with a 0.45 μm microporous membrane to obtain a liposome suspension; ...

Embodiment 2

[0083] The preparation of embodiment 2 fluconazole liposomes

[0084] prescription:

[0085] Component Dosage

[0086] Fluconazole 50g

[0087] Soy Lecithin 210g

[0088] Cholesterol 150g

[0089] Ascorbyl Palmitate 22.5g

[0090] Preparation Process

[0091] (1) 50g fluconazole, 210g soybean lecithin, 150g cholesterol and 22.5g ascorbyl palmitate are dissolved in the mixed solvent of ethanol, isopropanol and methanol in a volume ratio of 1:1:2 in 3400ml, mix well, and The mixed solvent was removed under reduced pressure on a rotary thin film evaporator to obtain a phospholipid film;

[0092] (2) Add 2000ml of phosphoric acid-sodium hydrogen phosphate buffer solution with a pH value of 5.5, shake, stir for 40 minutes, and rotate at a speed of 200r / min to completely hydrate the phospholipid film, and use a tissue masher for high-speed homogeneous emulsification for 10 minutes, Insulate at 50°C, rotate at 15000r / min, and then filter with a 0.45μm microporous membrane to o...

Embodiment 3

[0094] The preparation of embodiment 3 fluconazole liposomes

[0095] prescription:

[0096] Component Dosage

[0097] Fluconazole 100g

[0098] Soy Lecithin 600g

[0099] Cholesterol 450g

[0100] Ascorbyl Palmitate 80g

[0101] Preparation Process

[0102] (1) 100g fluconazole, 600g soybean lecithin, 450g cholesterol and 80g ascorbyl palmitate are dissolved in the mixed solvent of tert-butanol, acetone and methanol in a volume ratio of 3:2:2 in 7500ml, mix well, and The mixed solvent was removed under reduced pressure on a rotary thin film evaporator to obtain a phospholipid film;

[0103] (2) Add 3500ml of citric acid-sodium citrate buffer solution with a pH value of 7.5, shake, stir for 30 minutes, and rotate at 400r / min to completely hydrate the phospholipid film, and use a tissue masher for high-speed homogeneous emulsification for 15 minutes Minutes, keep warm at 60°C, rotate at 15000r / min, and then filter with a 0.45 μm microporous membrane to obtain a liposome ...

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Abstract

The invention provides a solid preparation of fluconazole liposome and a new application thereof. Specifically, the solid preparation of the fluconazole liposome is prepared by the fluconazole liposome and auxiliary materials. The invention discovers unexpectedly that when fluconazole and specific phospholipid and cholesterol are mixed in a certain matching ratio and combined with an antioxidant to prepare the liposome, and the problems about stability and dissolution rate of the solid preparation of the fluconazole liposome and the like are resolved. The liposome technique has high entrapment rate and good product quality and can be used for treating mucormycosis.

Description

technical field [0001] The invention relates to a liposome preparation, in particular to a liposome solid preparation of fluconazole, a preparation method thereof, and an application in treating mucormycosis. Background technique [0002] Mucor is a kind of fungus, which belongs to conditional pathogenic bacteria, widely exists in nature, especially in food and fruit. Distributed by air, dust and diet. Decreased immunity is a predisposing factor for disease, so patients with diabetes, leukemia, malnutrition, liver and kidney diseases, and long-term use of immunosuppressants and adrenal cortex hormones are prone to this disease. It enters the human body mainly through the mucocutaneous junction, respiratory tract, digestive tract, surgery or intubation and damaged skin. Fungi invade blood vessels, especially large and small arteries (rarely veins), causing thrombus and adjacent tissue ischemia, infarction, and necrosis, which can purify, but rarely show granulomatous change...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/4196A61K47/24A61K47/28A61P31/10
Inventor 杨明贵
Owner HAINAN MEILAN SMITH KLINE PHARMA
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