Solid liposome nanoparticles of arenobufagin and preparation method thereof

A technology of solid lipid nanometers and toadstools, which is applied in the directions of liposome delivery, pharmaceutical formulations, and medical preparations containing active ingredients, to achieve the effects of high encapsulation efficiency, high drug loading, and low irritation.

Inactive Publication Date: 2007-04-25
SHANGHAI INST OF PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, since SLN technology is still in its infancy, further research is needed on how to improve drug encapsulation efficiency, drug loading, preparation stability, and safety.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～11

[0028] Embodiment 1~11 and comparative embodiment

[0029] The ingredients shown in Table 1 in each of the examples and comparative examples in the specified amount were prepared according to the following preparation method to prepare the venom SLN of the present invention.

[0030] 1) heating the toad venom extract, lipid material and fat-soluble emulsifier under the temperature conditions shown in Table 2 to make it into a melt;

[0031] 2) Take the water-soluble emulsifier and disperse it in 100ml water for injection to form a uniform water phase;

[0032] 3) Mixing and stirring (above 10,000 rpm) the melt obtained in step 1) and the aqueous phase obtained in step 2) under the temperature conditions shown in Table 2 for 1 minute to form uniform colostrum;

[0033] 4) The colostrum obtained in step 3) is transferred to a high-pressure homogenizer, homogenized under the conditions shown in Table 2, and rapidly cooled to room temperature to obtain 10-100nm solid lipid nanopa...

Embodiment 2

[0050] Test Example 2 Irritation Test

[0051] 1. Muscle stimulation test

[0052] Get more than 4 healthy rabbits with a body weight of 2kg, divide into 2 groups, and one group injects 1ml of Bufo solid lipid nanoparticle aqueous dispersion system of the present invention in embodiment 4 respectively in the quadriceps femoris of its left and right legs respectively , another group respectively injects 1ml of blank solid lipid nanoparticles of the control example in the quadriceps femoris of its left and right legs by aseptic operation method, and kills the animal 48 hours after the injection, dissects and takes out the quadriceps femoris, and cuts it vertically , observe the irritation reaction at the injection site and convert the corresponding reaction level. Then calculate the sum of the 4 quadriceps response levels. Muscle stimulation test observation result shows, two groups of 4 quadriceps femoris reaction grades summation all<10, the blank solid lipid nanoparticle th...

Embodiment 3

[0055] Test Example 3 Systemic Active Anaphylaxis

[0056] Get 6 healthy and harmless guinea pigs, body weight 200-250g, press aseptic operation, every other day every other day each intramuscularly injects 0.5ml of toad venom solid lipid nanoparticle aqueous dispersion system of the present invention that embodiment 4 makes, altogether 3 times, it is homogeneous Divide into two groups. On the 14th day after the first injection, one group was challenged by intravenous injection of 2ml samples, and observed whether the animals had allergic reaction symptoms such as nose scratching, erect hair, dyspnea, convulsions, shock and even death after injection. The second group was attacked and observed in the same way on the 21st day after the first injection. Both groups of guinea pigs had no obvious reaction.

[0057] Conclusion: Intravenous injection of SLN of the present invention does not produce allergic reaction to guinea pigs.

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Abstract

The invention discloses secretio bufonis solid liposome nano particles which comprise the following constituents (by weight portions): 0.01-1 part of toad venoms extract, grease material 0.2-20 parts, liposoluble emulsifying agent 0.2-15 parts, and water-soluble emulsifying agent 0.2-10 parts. The grease material is selected from stearinic acid, glycol tristearate and mountain-elm glyceride. The invention also discloses the process for preparation through fusion method and high pressure homogeneity. The secretio bufonis nano liposome has a grain size between 10-100nm and the advantages of high medicinal encapsulation efficiency, low medicinal percolation ratio and oxidation index, and better constancy.

Description

technical field [0001] The invention relates to a nano-preparation of toad venom, in particular to a nano-particle of toad venom solid lipid and a preparation method thereof. Background technique [0002] The active ingredients of toad venom mainly include bufolin, cinobufin base, lipobufogenin and other fat-soluble components. The existing Chansu injection is an aqueous preparation of Chansu extract, which has the functions of anti-tumor, anti-virus, and improving immune function. It has been widely used clinically in patients with middle and advanced tumors and chronic hepatitis B. However, in the course of clinical application, vascular irritating adverse reactions such as poor intravenous infusion, redness and swelling at the infusion site, and intravenous pain often occur. [0003] And solid lipid nanoparticle (SLN) is one of the nanocarriers that rises in the early nineties of the 20th century, and it adopts the lipid material such as fatty acid, fatty alcohol and pho...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K35/56A61K9/14A61K9/127A61P35/00A61P31/20A61P1/16A61P37/04A61K35/65
Inventor 奉建芳杨勇芦洁
Owner SHANGHAI INST OF PHARMA IND
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