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Sodium aescinate micro-emulsification injection and preparation method thereof

A escin sodium and microemulsification technology, which is applied in the direction of anti-inflammatory agents, pharmaceutical formulas, emulsion delivery, etc., can solve the problems of low drug efficacy, effective concentration, low bioavailability, etc., and achieve the goal of reducing phlebitis Produce, reduce toxic and side effects, and have high bioavailability

Active Publication Date: 2012-11-28
TAIJI GROUP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the sodium aescinate tablet is convenient to take orally, the orally administered drug needs to be digested in the gastrointestinal tract first, and then enter the blood circulation to reach the disease site after distribution, diffusion, and absorption. Low, directly lead to low efficacy
Since the main adverse reactions of sodium aescinate are vascular irritation, phlebitis, and irritation of the urinary tract system, the current clinical application of sodium aescinate intravenous injection has been greatly affected.

Method used

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  • Sodium aescinate micro-emulsification injection and preparation method thereof
  • Sodium aescinate micro-emulsification injection and preparation method thereof
  • Sodium aescinate micro-emulsification injection and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1 7

[0040] Embodiment 1 Investigation of the oil-water partition coefficient of aescin sodium microemulsion injection

[0041] The n-octanol-water partition coefficient is the logarithm of the ratio of the concentrations of organic compounds in the n-octanol and water phases at equilibrium. Saturate n-octanol with double distilled water, acetic acid buffer at pH 4.0, phosphate buffer at pH 6.8, and phosphate buffer at pH 9.0, and use the above-treated water and buffer saturated with n-octanol. β-Aescin sodium was prepared, and the oil-water partition coefficient of 3.Oh after mixing was measured. The results are shown in Table 1.

[0042] Table 1. β-Aescin sodium oil-water partition coefficient

[0043]

[0044] The results showed that β-escin is weakly acidic, and β-escin sodium is weakly alkaline. -Aescin, showing a certain lipophilicity.

Embodiment 2 7

[0045] Embodiment 2 Investigation of the oil phase of aescin sodium microemulsion injection

[0046]The main instruments are: AL204-IC precision electronic balance (Mettler-Tomido Instruments), BP211D precision electronic balance (Sartorius AG), 85-2 constant temperature magnetic stirrer (Shanghai Sile Instrument Factory), JSM - Scanning Electron Microscope Model 5900LV (JEOL, Japan), Zetasizer Nano ZS90 Laser Particle Size Analyzer / Zeta Potentiometer (Malvern, UK). The main reagents are: aescin sodium (Wuxi Kaifu Pharmaceutical Co., Ltd.), soybean lecithin (SPC, Shanghai Taiwei Pharmaceutical Co., Ltd.), soybean oil (Tieling Beiya Medicinal Oil Co., Ltd.), medium chain triglyceride Acetate (Tieling Beiya Medicinal Oil Co., Ltd.) glycerol (Tieling Beiya Medicinal Oil Co., Ltd.), HS15 (BASF, Germany), Pluronic F-68 (BASF, Germany), etc. The rest of the reagents are of analytical grade.

[0047] Prescription screening of blank microemulsion

[0048] The key to preparing microe...

Embodiment 3

[0057] The screening of embodiment 3 emulsifier

[0058] The medium chain triglyceride screened out is used as the oil phase. Pluronic F-68, soybean lecithin, Pluronic F-68+ soybean lecithin (1:1), Pluronic F-68+HS15 (1:1), soybean lecithin+HS15 (1:1) For the emulsifier to be selected, take glycerol as the co-emulsifier, Km=2:1, accurately weigh the mixed surfactant and oil phase by mass ratio as 9:1, 8:2, 7:3, 6:4, 5 :5, 4:6, 3:7, 2:8, 1:9, and add distilled water dropwise at 25°C until transparent and clear microemulsion is formed. When the appearance is no longer clear, the critical addition is recorded. According to the mass percentage of oil, water and mixed surfactant at the critical point, draw a curve in the pseudo-ternary phase diagram to determine the O / W type microemulsion region. The experimental data are shown in Table 4-8.

[0059] Table 4 Screening of emulsifiers (Pluronic F-68)

[0060]

[0061] Table 5 Screening of emulsifiers (soy lecithin)

[0062] ...

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Abstract

The invention discloses a sodium aescinate micro-emulsion injection. The formula of the sodium aescinate micro-emulsion injection comprises sodium aescinate, an oil phase, a surfactant and a cosurfactant. Compared with the oral gavage, the sodium aescinate micro-emulsion injection for intravenous injection provided by the invention has the advantages that the bioavailability is high, the concentration of the injection in the liver can be increased obviously, the concentration of the injection in the kidney can be reduced, meanwhile, the irritation on the wall of the blood vessel is alleviated, and the generation times of phlebophlogosis can be reduced, so that the curative effect is improved, and the toxic and side effect is lowered.

Description

technical field [0001] The invention relates to a pharmaceutical preparation, in particular to a micro-emulsion injection of sodium aescin and a preparation method thereof. technical background [0002] Aescin is the main active ingredient extracted from the seeds of horse chestnut. The outer skin of the seeds and young branches can be used as medicine. It is widely used in Europe and belongs to the triterpenoid saponins. It is a white or off-white crystalline powder with a bitter and acrid taste, not stable enough in water, and easily soluble. It has anti-exudation, restores capillary permeability, eliminates edema, inhibits protein from passing through blood vessels into inflammatory areas, improves blood circulation, increases venous tension, promotes lymphatic return, corrects brain dysfunction, inhibits gastric emptying, and scavenges reactive oxygen species. Anti-tumor effects, etc. The current clinical dosage form of aescin sodium tablets is tablet, which is used fo...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/704A61K47/44A61K47/24A61K47/34A61K47/28A61P7/10A61P9/14A61P35/00A61P29/00A61K47/14
Inventor 白礼西覃瑶罗维早秦少容
Owner TAIJI GROUP
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