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Norisoboldine self-microemulsion preparation and preparing method thereof

A technology of norisoboldine and milk preparations, which is applied in the fields of pharmaceutical formula, emulsion delivery, and medical preparations of non-effective ingredients, etc., can solve the problems of low bioavailability of norisoboldine, and achieve improvement Bioavailability, overcoming easy metabolism, and improving the effect of oral absorption

Inactive Publication Date: 2015-11-25
FUJIAN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The object of the present invention is to provide a kind of noriboldine self-microemulsion preparation and preparation method thereof for the problem of low bioavailability of noriboldine

Method used

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  • Norisoboldine self-microemulsion preparation and preparing method thereof
  • Norisoboldine self-microemulsion preparation and preparing method thereof
  • Norisoboldine self-microemulsion preparation and preparing method thereof

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Embodiment 1

[0022] laboratory apparatus

[0023] U.S. WatersAlliance high performance liquid chromatography; Waters2998PAD detector; ultra-high performance liquid chromatography mass spectrometry (Waters, U.S.); nanoparticle size and potential analyzer (Microtrac, U.S.); HH-4 digital constant temperature water bath (Guohua Electric Appliance Co., Ltd.); constant temperature magnetic stirrer (Guohua Electric Co., Ltd.); VDRTEX-5 vortex mixer (Qilin Bell Instrument Company, Haimen City); small desktop centrifuge (Eppendorf, Germany); micropipette gun ( Germany Eppendorf company) and so on.

[0024] Experimental material

[0025] Norisoboldine (provided by Shanghai Traditional Chinese Medicine Standardization Research Center, with a purity greater than 98%); tributyrin (Aladdin, USA); polyoxyethylene castor oil (EL-40, Aladdin, USA); absolute ethanol (Shanghai Ziqin Chemical Co., Ltd.); Triton (Amresco, USA); acetonitrile, formic acid, methanol (chromatographically pure, Merck, Germany), o...

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Abstract

The invention belongs to the field of medicament preparing and particularly relates to norisoboldine self-microemulsion preparation and a preparing method thereof. The method includes: adding norisoboldine into anhydrous ethanol, adding tributyrin and emulsifier EL-40 after 37-DEG C ultrasonic dissolving saturation, and well mixing in a vortex manner to prepare the norisoboldine self-microemulsion preparation, wherein the volume fraction of the tributyrin in the self-microemulsion preparation is 22.5%; the volume ratio of the emulsifier to the anhydrous ethanol is 3:1. The norisoboldine self-microemulsion preparation prepared by the method is clear and transparent liquid and stable in property and forms O / W type light blue microemulsion when meeting water, the self-emulsifying rate of the norisoboldine self-microemulsion preparation is 28.3s, the particle size of the norisoboldine self-microemulsion preparation is 14.73 nanometers, the Zeta potential of the norisoboldine self-microemulsion preparation is 0.7mV, and the drug loading capacity of the norisoboldine self-microemulsion preparation is 14.8676mg / mL.

Description

technical field [0001] The invention belongs to the field of preparation of medicaments, and in particular relates to a norisoboldine self-microemulsion preparation and a preparation method thereof. Background technique [0002] black medicine Lindera aggregate (Sims) Kosterm. is a plant of the genus Piper in the family Lauraceae, and norisoboldine is isolated from its dry tuber, with a content of up to 1%. Animal experiments have shown that noribordine can significantly reduce the severity of arthritis in mice (CIA), protect joint damage, reduce the content of anti-collagen antibodies in serum, etc., with clear pharmacological effects and low toxic and side effects. Because noribordine itself is slightly soluble in water, its rapid metabolism in vivo, low blood concentration and bioavailability greatly limit its clinical application. In order to solve these problems, it is possible to increase the blood drug concentration by changing the dosage form, reduce the metabolic ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/473A61K47/44A61K47/14A61K47/10A61P19/02
Inventor 陈建忠侴桂新李彧
Owner FUJIAN UNIV OF TRADITIONAL CHINESE MEDICINE
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