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Total bufogenin nano cubic liquid crystal and preparation method thereof

A technology of nano-cubic liquid crystal and total bufanolactone, which can be used in pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc. Low, short half-life and other problems, to achieve the effect of improving bioavailability, improving solubility, and large drug loading

Inactive Publication Date: 2015-12-02
HEFEI HUAFANG PHARMA SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At the same time, total bufalide has low solubility in aqueous solution, short half-life in vivo, low bioavailability, and strong muscle irritation after injection. These characteristics extremely limit the clinical application of total bufalide

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Embodiment 1 Preparation of total bufolide nano-cubic liquid crystals

[0037] Precisely weigh 6mg of total bufolide and 26.1mg of glyceryl monooleate, dissolve in 5ml of absolute ethanol, and form an oil phase in a 60°C water bath; dissolve 3.9mg of poloxamer 407 in 39mL of water, and heat in a water bath same temperature. Slowly and uniformly inject the oil phase into the stirred water phase with a 1mL syringe, and continue to stir for 3h. After the organic solvent is completely volatilized, the primary emulsion is slowly poured into 75 mg of ice water (ice bath) under stirring conditions, and the stirring is continued for 2 hours to obtain total bufolide nanocubic liquid crystals.

[0038] Detection: the average particle diameter of total bufolide nanocubic liquid crystal nanoparticles is 108.4nm, and the encapsulation efficiency is 88.8%.

Embodiment 2

[0039] Example 2 Preparation of total bufolide nano-cubic liquid crystals

[0040] Precisely weigh 6mg of total bufolide and 26.1mg of phosphoglycerides, dissolve in 5ml of absolute ethanol, and form the oil phase in a 60°C water bath; dissolve 3.9mg of poloxamer 407 in 39mL of water, and heat the water bath to the same level as the oil phase temperature. Slowly and uniformly inject the oil phase into the stirred water phase with a 1mL syringe, and continue to stir for 3h. After the organic solvent is completely volatilized, the primary emulsion is slowly poured into 75 mg of ice water (ice bath) under stirring conditions, and the stirring is continued for 2 hours to obtain total bufolide nanocubic liquid crystals.

[0041] Detection: the average particle diameter of total bufolide nanocubic liquid crystal nanoparticles is 138.4nm, and the encapsulation efficiency is 82.5%.

Embodiment 3

[0042] Example 3 Preparation of total bufolide nano-cubic liquid crystals

[0043] Precisely weigh 6mg of total bufolide and 26.1mg of phosphatidylethanolamine, dissolve in 5ml of absolute ethanol, and form an oil phase in a 60°C water bath; dissolve 3.9mg of poloxamer 407 in 39mL of water, and heat in a water bath until it is the same as the oil phase temperature. Slowly and uniformly inject the oil phase into the stirred water phase with a 1mL syringe, and continue to stir for 3h. After the organic solvent is completely volatilized, the primary emulsion is slowly poured into 75 mg of ice water (ice bath) under stirring conditions, and the stirring is continued for 0.5 h to obtain total bufolide nanocubic liquid crystals.

[0044] Detection: the average particle size of total bufolide nanocubic liquid crystal nanoparticles is 135.5nm, and the encapsulation efficiency is 82.0%.

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Abstract

The invention discloses a total bufogenin nano cubic liquid crystal and a preparation method thereof. The total bufogenin nano cubic liquid crystal is composed of a lipid material, an emulsifying agent and purified water. The total bufogenin nano cubic liquid crystal provided by the invention is characterized in that amphipathic lipid with certain concentration spontaneously forms double layers of the lipid in water, and the double layers are assembled into a cubic liquid crystal form with thermodynamic stability. The total bufogenin nano cubic liquid crystal disclosed by the invention increases the medicine solubility, realizes the oral administration of lipid-soluble medicine total bufogenin, adjusts and controls the medicine release, improves the medicine bioavailability, effectively improves the tumor cell targeting property of total bufogenin, and reduces toxic or side effects.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to total bufolide nano-cubic liquid crystals and a preparation method thereof. More specifically, the total bufolide nano-cubic liquid crystals of the present invention increase the solubility of total bufolides and realize lipid The soluble drug total bufolide is orally administered to avoid the irritation of the injection to the body. Background technique [0002] Toad is the skin of Bafogararizaus, an animal of the Bufo family. The peeled skin is dried into dry toad skin. The white slurry secreted by the cheeks behind the ears and skin glands is toad venom. It is sweet and warm in nature, toxic, and has the function of detoxification swelling, relieve pain. As the main medicinal ingredient of toad, total bufolide has many functions such as strengthening the heart, boosting blood pressure, anti-shock, enhancing the body's immunity, and anti-tumor. Among them, it is widely...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/00A61K35/65A61K47/14A61K47/24A61K47/32A61P9/00A61P9/02A61P37/04A61P35/00A61K31/585
Inventor 张亮亮何勇吴宗好
Owner HEFEI HUAFANG PHARMA SCI & TECH
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