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Acehytisine freeze-drying emulsion and reparation method thereof

A technology of Guanfu A and freeze-dried emulsion, which is applied in the field of Guanfu A freeze-dried emulsion and its preparation, to achieve the effects of prolonging circulation time, reducing drug dosage and high pharmacological activity

Inactive Publication Date: 2011-06-22
刘静涵 +3
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no report on the freeze-dried emulsion of Guanfu A at home and abroad, and there is no influence of the particle size of the emulsion prepared under the prescription process involved in the present invention on the kinetic behavior of Guanfu A in vivo

Method used

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  • Acehytisine freeze-drying emulsion and reparation method thereof
  • Acehytisine freeze-drying emulsion and reparation method thereof
  • Acehytisine freeze-drying emulsion and reparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Dissolve 0.05 part of Guanfu A in 0.8 part of soybean oil for injection as the oil phase; 0.2 part of soybean lecithin, 0.001 part of vitamin C, 0.125 part of glycerin and 0.25 part of mannitol are dissolved in water for injection; add the oil phase to water In the phase, after high-speed dispersion at 8,000 rpm, the first-stage valve is 1,000 bar, and the second-stage valve is 150 bar high-pressure homogenization to obtain a uniformly dispersed emulsion; after filtration sterilization, pre-freeze at -20°C for 8 hours, and then heat up at a rate of 0.5°C / min Freeze-dried for 12 hours to obtain. After reconstitution into a liquid emulsion, the particle size is between 300-400nm.

Embodiment 2

[0047] Dissolve 0.07 part of Guanfu A in 1 part of medium-chain fatty acid for injection as the oil phase; 0.12 part of soybean lecithin, 0.2 part of poloxamer F-68, 0.005 part of L-cysteine ​​and 0.5 part of glucose In water for injection; add the oil phase to the water phase and disperse at a high speed of 10,000 rpm, and then homogenize at a high pressure of 1500 bar with the first stage valve and 300 bar with the second stage valve to obtain a uniformly dispersed emulsion; after filter sterilization, pre-freeze at -40°C for 12 hours Afterwards, freeze-dry at a rate of 0.3°C / min for 24 hours to obtain the product. After reconstitution into a liquid emulsion, the particle size is between 300-400nm.

Embodiment 3

[0049] Dissolve 0.1 part of Guanfu A in a mixed oil of 0.5 part of soybean oil for injection and 0.5 part of medium-chain fatty acid as the oil phase; 0.1 part of lecithin, 0.15 part of poloxamer F-68, 0.01 part of anhydrous sodium sulfite , 0.12 parts of glycerin and 0.3 parts of sorbitol are dissolved in water for injection; after the oil phase is added to the water phase to disperse at a high speed of 9000 rpm, the first-stage valve is 1300 bar, and the second-stage valve is 200 bar high-pressure homogenization to obtain a uniformly dispersed emulsion; After sterilizing, pre-freeze at -30°C for 10 hours, then freeze-dry at a rate of 0.15°C / min for 20 hours to obtain the product. After reconstitution into liquid emulsion, the particle diameter is between 300-400nm.

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Abstract

The invention discloses an acehytisine freeze-drying emulsion and a reparation method thereof. The acehytisine freeze-drying emulsion uses the acehytisine as the active component, comprises oil for injection, emulsifier, additive and freeze-drying protective agent generally used in pharmacy and is dispersed into the emulsifier combination solution having a grain diameter ranging from 300 to 400nmafter being added with water for injection. Compared with the acehytisine hydrochloride parenteral solution, the invention can realize 1.36 times of AUC and 1.59 times of MRT with half dosage and hasequivalent pesticide effect for resisting arrhythmia.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a freeze-dried emulsion of Guanfu A and a preparation method thereof. Background technique [0002] Guanfu A (Guan-Fu Base A, GFA) is a tertiary amine diterpene alkaloid extracted from Aconitumcoreanum (levl.) Rapaics tuber root Guanbaizhong of Ranunculaceae. Preclinical pharmacological studies have shown that Guan-Fu Fujiasu injection can resist ventricular tachycardia and ventricular fibrillation induced by high calcium, coronary artery ligation and aconitine nitrate. Guanfujia hydrochloride is the reaction of insoluble Guanfujia free base with hydrochloric acid to form a salt. Although the water solubility of Guanfu A can be greatly increased after salt formation, the pharmacological activity of the drug decreases, the dosage is large (the current clinical dosage is 140 mg), and the half-life in the human body is very short (T 1 / 2π 2.6±1.2ml / min), the me...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/439A61K47/44A61P9/06
Inventor 熊非杨春华刘静涵刘沙汪豪顾宁朱家壁
Owner 刘静涵
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