Montmorillonite inlaid liposome preparation and preparation method thereof

The technology of montmorillonite lipid and montmorillonite is applied in the field of liposome preparation inlaid with montmorillonite and its preparation, and can solve the problem of reducing the toxic and side effects of drug bioavailability, low drug bioavailability and poor corneal permeability and other problems to achieve the effect of improving bioavailability, improving bioavailability and side effects, and slowing down the release rate

Inactive Publication Date: 2016-07-13
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0002]The traditional ocular drug delivery system, due to the special physiological barrier of the eyeball, the short residence time of the drug in front of the cornea, the rapid elimination of tears and the poor permeability of the cornea lead to the bioavailability of the drug Very low (<5%)
At the same time, it enters the blood through the conjunctiva and the nasolacrimal duct drains to the nasal mucosa / gastric mucosa and enters the systemic circulation, which reduces the bioavailability of the drug and even produces toxic side effects

Method used

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  • Montmorillonite inlaid liposome preparation and preparation method thereof
  • Montmorillonite inlaid liposome preparation and preparation method thereof
  • Montmorillonite inlaid liposome preparation and preparation method thereof

Examples

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preparation example Construction

[0027] A kind of preparation method of mosaic montmorillonite liposome preparation, with drug-loaded montmorillonite, phospholipid, cholesterol, antioxidant, octadecylamine as oil phase, ammonium sulfate solution as water phase, prepare liposome, drug-loaded The montmorillonite is loaded into the liposome, and then the liposome is incubated with the drug to obtain the montmorillonite-embedded liposome preparation.

[0028] A preparation method of mosaic montmorillonite liposome preparation, comprising the following steps:

[0029] 1) Adsorbing drugs with montmorillonite to prepare drug-loaded montmorillonite;

[0030] 2) Dissolve drug-loaded montmorillonite, phospholipids, cholesterol, octadecylamine, and antioxidants in an organic solvent to form an organic phase; use ammonium sulfate solution as the water phase;

[0031] 3) Heat the organic phase and the water phase to 40-80°C respectively, slowly inject the organic phase into the water phase under stirring conditions, and ...

Embodiment 1

[0053] (1) Place the montmorillonite in 5v / v% sulfuric acid, acidify it in a water bath at 70°C for 0.5h, wash it with double distilled water until neutral, treat it with ultrasonic to reduce the particle size, and obtain the acidified montmorillonite after drying, namely Acid-activated modified montmorillonite;

[0054] Prepare an aqueous solution of betaxolol hydrochloride (BH) with a concentration of 3 g / L, add acidified montmorillonite whose weight is 1 / 3 of the weight of BH, adjust the pH to 4, absorb in a water bath at 50 ° C for 6 h, and centrifuge and dry to obtain the loaded Medicinal montmorillonite (montmorillonite-betaxolol hydrochloride complex);

[0055] (2) Weigh 5 mg of drug-loaded montmorillonite, 150 mg of lecithin, 25 mg of cholesterol, 10 mg of octadecylamine and 3 mg of vitamin E and place them in a stoppered test tube, add an appropriate amount of absolute ethanol (so that the concentration of drug-loaded montmorillonite is 1~3mg / mL), after the cholester...

Embodiment 2

[0064] (1) Put the montmorillonite in 5v / v% sulfuric acid, acidify it in a water bath at 70°C for 0.5h, wash it with double distilled water until neutral, reduce the particle size by ultrasonic, and obtain the acidified montmorillonite after drying;

[0065] Prepare an aqueous solution of betaxolol hydrochloride (BH) with a concentration of 3g / L, add acidified montmorillonite with a weight of BH1 / 3, adjust the pH to 4, absorb in a water bath at 50°C for 6h, and centrifuge and dry to obtain the drug-loaded montmorillonite Tricholithiasis (montmorillonite-betaxolol hydrochloride complex);

[0066] (2) Weigh 15 mg of drug-loaded montmorillonite, 150 mg of lecithin, 25 mg of cholesterol, 10 mg of octadecylamine, and 5 mg of BHT (2,6-di-tert-butyl-4-methylphenol) into a stoppered test tube, Add an appropriate amount of absolute ethanol (so that the concentration of the drug-loaded montmorillonite is 1-3 mg / mL), after the cholesterol and stearylamine are dissolved, disperse the mont...

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Abstract

The invention discloses a montmorillonite inlaid liposome preparation and a preparation method thereof. According to the invention, montmorillonite is used as a drug carrier and is inlaid into the liposome so as to obtain a novel sustained drug release preparation montmorillonite inlaid liposome. The prepared liposome has good biological compatibility and sustained release performance, and can improve the bioavailability and side effect of drugs. Drugs can be released through ion-exchange action, the release rate of cationic type drugs is slowed down, and the side effects are reduced, thus being in favor of enhancing the drug bioavailability.

Description

technical field [0001] The invention relates to a liposome preparation embedded with montmorillonite and a preparation method thereof. Background technique [0002] In traditional ocular drug delivery systems, due to the special physiological barrier of the eyeball, the drug has a short retention time in front of the cornea, rapid tear removal and poor corneal permeability, resulting in very low bioavailability (<5%) of the drug. At the same time, it enters the blood through the conjunctiva and the nasolacrimal duct drains to the nasal mucosa / gastric mucosa and enters the systemic circulation, which reduces the bioavailability of the drug and even produces toxic and side effects. Therefore, colloid dosage forms are widely used in ocular drug delivery systems, including liposomes, nanoparticles, microemulsions, nanoemulsions, solid lipid nanoparticles, etc., which have the advantages of sustained release, controlled release, and reduced dosing frequency. [0003] Liposome...

Claims

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Application Information

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IPC IPC(8): A61K47/02A61K9/127
CPCA61K47/02A61K9/127
Inventor 潘育方侯冬枝陈燕忠胡晟黄燚田双艳
Owner GUANGDONG PHARMA UNIV
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