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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 formulations, emulsion delivery, etc., can solve the problems of low drug efficacy, low bioavailability, and effective concentration, and achieve the goal of reducing phlebitis Production, high bioavailability, and the effect of reducing toxic and side effects

Active Publication Date: 2015-03-18
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
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Effect test

Embodiment 1 7

[0040] The investigation of the oil-water partition coefficient of embodiment 1 sodium aescinate microemulsion injection

[0041] The n-octanol-water partition coefficient is the logarithm value of the ratio of the concentration of organic compounds in the n-octanol phase and the water phase at equilibrium. Saturate n-octanol with double distilled water, pH4.0 acetate buffer, pH6.8 phosphate buffer, pH9.0 phosphate buffer, and use the above-mentioned n-octanol-saturated water and buffer Prepare β-escin sodium, and measure the oil-water partition coefficient 3.Oh after mixing respectively. The results are shown in Table 1.

[0042] Table 1. Oil-water partition coefficient of β-escin sodium

[0043]

[0044] The results show that β-escin is weakly acidic, β-escin sodium is weakly alkaline, and β-escin sodium has strong hydrophilicity under neutral and alkaline conditions, and is free under acidic conditions to β - Aescin, showing a certain lipophilicity.

Embodiment 2 7

[0045] The investigation of embodiment 2 sodium aescinate microemulsion injection oil phase

[0046]The main instruments are: AL204-IC precision electronic balance (Mettler-Tomido Instrument Co.), BP211D precision electronic balance (Sartorius AG), 85-2 constant temperature magnetic stirrer (Shanghai Sile Instrument Factory), JSM -5900LV scanning electron microscope (JEOL, Japan), Zetasizer Nano ZS90 laser particle size analyzer / Zeta potential meter (Malvern, UK). The main reagents are: sodium aescinate (Wuxi Kaifu Pharmaceutical Co., Ltd.), soybean lecithin (SPC, Shanghai Taiwei Pharmaceutical Co., Ltd.), soybean oil (Tieling Beiya Pharmaceutical Oil Co., Ltd.), medium chain triglycerides Ester (Tieling Beiya Medicinal Oil Co., Ltd.), glycerin (Tieling Beiya Medicinal Oil Co., Ltd.), HS15 (Germany BASF), Pluronic F-68 (Germany BASF), etc., and other reagents are of analytical grade.

[0047] Prescription Screening of Blank Microemulsion

[0048] The key to preparing microem...

Embodiment 3

[0057] The screening of embodiment 3 emulsifiers

[0058] The screened medium-chain triglyceride is used as the oil phase. Respectively with Pluronic F-68, soybean lecithin, Pluronic F-68 + soybean lecithin (1:1), Pluronic F-68 + HS15 (1:1), soybean lecithin + HS15 (1:1) As the emulsifier to be selected, glycerin is used as the co-emulsifier, Km=2:1, and the mass ratio of the mixed surfactant and oil phase is 9:1, 8:2, 7:3, 6:4, 5 :5, 4:6, 3:7, 2:8, 1:9 mixed, and distilled water was added dropwise at 25°C until a transparent and clear microemulsion was formed. When the appearance is no longer clear, record the critical addition. According to the mass percentage of oil, water and mixed surfactant at the critical point, the curve is drawn in the pseudo ternary phase diagram to determine the O / W microemulsion area. 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 (so...

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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 sodium aescinate microemulsion injection and a preparation method thereof. technical background [0002] Aescin is the main active ingredient extracted from the seeds of Horse Chestnut. The skin of its seeds and young branches can be used as medicine. It is widely used in Europe and belongs to triterpenoid saponins. It is white or off-white crystalline powder, bitter and pungent, not stable enough in water and easily soluble. Anti-exudation, restore capillary permeability, reduce edema, inhibit protein from entering the inflammatory area through blood vessels, improve blood circulation, increase venous tone, promote lymphatic return, correct brain dysfunction, inhibit gastric emptying, remove active oxygen and anti-tumor effects. Sodium aescinate tablets are currently in the form of tablets in clinical use, which are used for swelling caused by cerebral edema, trauma or surgery...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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