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Palmatine nano particle preparations and preparation thereof

A technology of palmetine and nanoparticles, which is applied in the field of medicine, can solve the problems of long tablet disintegration time, low bioavailability, and prolonged disintegration speed, so as to improve bioavailability, prolong cycle time, and reduce drug administration effect of dosage

Inactive Publication Date: 2008-07-09
NORTHWEST A & F UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In these common dosage forms, the disintegration time of the tablet is long, the absorption is poor, the bioavailability is low, the amount of auxiliary materials is large, and the patient's compliance is poor; Especially in Europe, where the industry is developed, the medical excipients are more stringent; although the capsule preparation can improve the taste and reduce irritation, the disintegration speed is prolonged, which is not conducive to the rapid onset of the drug
Since gynecological inflammation is a chronic disease, if conventional dosage forms are used, the course of treatment will be longer, which will easily cause stomach discomfort, and there will be too long intervals between taking medicine at night to maintain effective blood drug levels, resulting in blind spots in treatment

Method used

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  • Palmatine nano particle preparations and preparation thereof
  • Palmatine nano particle preparations and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Accurately weigh 0.15 g of palmatine and add it to 20 mL of distilled water, heat and dissolve in a constant temperature water bath at 37°C to prepare liquid A. Accurately weigh 0.4 g of surfactant dextran D-70 and disperse it in 80 mL of distilled water to prepare liquid B. Adjust the pH of liquid A and liquid B to 2.0 with 0.1 mol / L hydrochloric acid, and slowly drop 0.1 g of monomeric propyl cyanoacrylate (ECA) into liquid B under constant temperature stirring conditions (25°C, 800 r / m). After stirring for 20 minutes, add liquid A gradually, stir on an electromagnetic stirrer for 7 hours, add additive NaCl 0.3 g, and continue stirring for 3 hours. Use 1mol / L sodium hydroxide solution to adjust the pH to 5.0, filter with a microporous membrane with a pore size of 0.45 μm, obtain a precipitate after low-temperature ultracentrifugation (4°C, 25000r / m, 150min), disperse and dilute the precipitate with distilled water, That is to obtain the palatine nanoparticle preparat...

Embodiment 2

[0038]Add 4 parts of palmatine raw materials to 100 parts of distilled water, heat it in a constant temperature water bath at 35°C to fully dissolve it to make solution A; add 4 parts of poloxamer F-68 to 350 parts of distilled water to make solution B ; Use 0.05mol / L hydrochloric acid to adjust the pH of liquid A and liquid B to 3.0 respectively, and slowly drop alkyl cyanoacrylate ACA into liquid B at 30°C under constant temperature and constant speed stirring within the range of 800r / m, After stirring for 20 minutes, add liquid A step by step; stir on a constant temperature and constant speed magnetic stirrer for 6 hours, then add additives, and continue stirring for 3 hours; Membrane suction filtration; under the condition of 4°C and 25,000r / m for 150min, the precipitate was obtained by low-temperature ultracentrifugation, and the precipitate was dispersed and diluted with distilled water to obtain a solution of palmatine nanoparticles.

Embodiment 3

[0040] Add 5 parts of palmatine crude drug to 150 parts of distilled water, heat it in a constant temperature water bath at 35°C to fully dissolve it to make liquid A; add 4 parts of Tween T-80 to 450 ℃ distilled water to make liquid B; liquid A Use 0.1mol / L hydrochloric acid to adjust the pH to 5.0 respectively, and slowly drop the alkyl cyanoacrylate ACA into the B liquid under the constant temperature and constant speed stirring condition in the range of 20°C to 0°C and 1000r / m, and stir After 30 minutes, add liquid A gradually; stir on a constant temperature and constant speed magnetic stirrer for 10 hours, then add additives, and continue stirring for 4 hours; Suction filtration; low-temperature ultracentrifugation at 25000 r / m for 150 min at 4°C to obtain a precipitate, and disperse and dilute the precipitate with distilled water to obtain a solution of palmatine nanoparticles.

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Abstract

The present invention discloses a palmatine nano-particle preparation which is that 3 to 5 portions of palmatine is added into the distilled water with proper quantity to be heated in water bath under constant temperature to be dissolved completely and confected as liquid A; 4 to 8 portions of surfactant is added into the rest distilled water to be confected as liquid B; the pH values of the liquid A and the liquid B are respectively adjusted to be acidic by hydrochloric acid; under the condition of stirring under constant temperature, 2 to 6 portions of alkyl cyanoacrylate (ACA) is dripped into the liquid B slowly to be stirred for minutes, the liquid A is added gradually to be stirred by an electromagnetic stirrer for a long time to be added with 3 to 9 portions of additive to be stirred for hours continuously; sodium hydroxide solution is used to adjust the pH value, and the reaction is finished; a microporous filtering film is used for filtering to obtain deposit after ultracentrifugation under low temperature, and the deposit is dispersed and diluted by the distilled water to obtain the palmatine nano-particle preparation which has low side effect, obvious curative effect and the functions of the slow-release and targeting.

Description

technical field [0001] The invention belongs to the field of medicine and relates to a novel preparation of palmetine, in particular to a preparation of palmetine nanoparticles and a preparation method thereof. Background technique [0002] Fibrauretin (Fibrauretin) is an alkaloid extracted from the dry stems of Phantasmus chinensis, and its effective chemical component is palmatine hydrochloride (C 21 h 22 NO 4 HCL), has multiple pharmacological effects such as broad-spectrum antibacterial, antiviral, significantly increasing leukocyte phagocytosis of bacteria, good anti-inflammation and enhancing body immunity. Due to the advantages of less toxic side effects and low drug resistance, this product has become a hot spot in the research and development of antibacterial and anti-inflammatory drugs in recent years. Treatment of conjunctivitis etc. [0003] Palmatine is odorless, has a very bitter taste, is slightly soluble in water, and is easily soluble in hot water; the a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4745A61K9/14A61K47/32A61K47/36A61P1/00A61P11/00A61P15/00A61P27/02A61P31/04A61P31/12
Inventor 欧阳五庆李云让
Owner NORTHWEST A & F UNIV
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