Berberine hydrochloride solid lipid nano preparation and preparation method thereof

A technology of solid lipid nanometer and berberine hydrochloride, which can be used in pharmaceutical formulations, medical preparations containing active ingredients, digestive system, etc., and can solve problems such as low bioavailability in vivo and difficulty in absorption.

Inactive Publication Date: 2013-03-06
THE FIRST AFFILIATED HOSPITAL OF XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The object of the present invention is to aim at the disadvantages of existing berberine solid lipid nano-preparations such as difficulty in absorbing and low bioavailability in vivo, and to provide a drug that is simple in method, low in production cost, easy to carry and transport, and suitable for any route of administration. Berberine Hydrochloride Solid Lipid Nano-Preparation

Method used

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  • Berberine hydrochloride solid lipid nano preparation and preparation method thereof
  • Berberine hydrochloride solid lipid nano preparation and preparation method thereof
  • Berberine hydrochloride solid lipid nano preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0037]

[0038] Weigh berberine hydrochloride and glyceryl monostearate according to the above prescription, add 10 mL of acetone, and heat to dissolve at 80°C; add 1 mL of ethanol to lecithin and dissolve it by ultrasound for 10 minutes; mix the above two solutions as the organic phase; Loxamer is dissolved in 20 mL of water as the water phase. Under stirring, the organic phase is injected into the 80 ℃ water phase with a needle, stirred at a constant temperature for 2 hours, the organic solvent is evaporated, the probe is ultrasonicated, naturally cooled, and filtered by a 0.45 μm microporous membrane. The berberine hydrochloride solid lipid nanoparticle suspension was obtained.

Embodiment 2

[0040]

[0041] Weigh berberine hydrochloride, tripalmitate glyceride, and lecithin according to the above prescription, add 10 mL of a 1:1 mixture of acetone and ethanol, and heat to dissolve at 80°C; mix the above two solutions as the organic phase ; Another poloxamer is dissolved in 20mL water as the water phase, the organic phase is injected into the 80 ℃ water phase with a needle under agitation, stirred at a constant temperature for 2 hours, the organic solvent is evaporated, the probe is ultrasonic, natural cooling, 0.45μm microporous filter Membrane filtration obtains the berberine hydrochloride solid lipid nanoparticle suspension.

Embodiment 3

[0043]

[0044] Weigh berberine hydrochloride, glyceryl monostearate, and lecithin according to the above prescription, add 10 mL of a 1:1 mixture of acetone and ethanol, and heat and dissolve at 80°C as the organic phase; take poloxamer in addition Dissolve in 20mL water as the water phase. Under stirring, inject the organic phase into the 80℃ water phase with a needle, stir at constant temperature for 2 hours, evaporate the organic solvent, ultrasonic probe, natural cooling, and filter with 0.45μm microporous membrane to obtain hydrochloric acid. Berberine solid lipid nanoparticle suspension.

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Abstract

The invention discloses a berberine hydrochloride solid lipid nano preparation and a preparation method thereof, relates to berberine hydrochloride, and provides the berberine hydrochloride solid lipid nano preparation which has the advantages of simple method, low production cost, convenience in carrying and transportation and suitability for any administration route and the preparation method thereof. The berberine hydrochloride solid lipid nano preparation comprises the following raw materials in percentage by mass: 1 percent of berberine hydrochloride, 5-15 percent of solid lipid, 5-15 percent of emulsifier and 1-3 percent of surfactant. The solid lipid and the emulsifier are added into an organic solvent; after the solid lipid is fully dissolved, the berberine hydrochloride is added and is dissolved to obtain an oil phase; the obtained oil phase is added into a water phase containing the surfactant and is stirred until the organic solvent is fully removed; the obtained material is subjected to ultrasonography, is cooled and then is filtered by using a micro-porous filter membrane to obtain berberine hydrochloride solid lipid nanoparticle suspension; and the obtained berberine hydrochloride solid lipid nanoparticle suspension is added into a free-dry protecting agent to be freeze-dried to obtain the berberine hydrochloride solid lipid nano preparation which is in the form of nanoparticle freeze-dried powder.

Description

Technical field [0001] The invention relates to a berberine hydrochloride, in particular to a berberine hydrochloride solid lipid nano preparation and a preparation method thereof. Background technique [0002] Berberine is a kind of quaternary amine isoquinoline alkaloid extracted from the rhizomes of Coptis ricinus and other plants. Its English name is Berberine, also known as berberine. It is mainly used clinically for intestinal infections and can also be widely used in various Kind of cardiovascular disease. Research results at home and abroad in recent years have shown that berberine has a definite effect on diabetes and is the hottest Chinese medicine monomer in the field of DB, but it has not been widely used in clinical practice. This is mainly because berberine is a quaternary ammonium alkaloid, which is easily absorbed by the mucin in the gastrointestinal tract and affects absorption. It is difficult to achieve an effective concentration for pharmacological effects. T...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K9/19A61K31/4375A61P1/00A61P31/00A61P9/00A61P3/10
Inventor 杨叔禹薛梅李学军
Owner THE FIRST AFFILIATED HOSPITAL OF XIAMEN UNIV
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