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Suspension containing andrographolide solid lipid nanoparticles as well as preparation method and application of suspension

A technology of solid lipid nano and andrographolide, which is applied to medical preparations containing active ingredients, liquid delivery, pharmaceutical formulations, etc. It can solve problems affecting drug absorption and efficacy, lack of targeting, and application limitations. , to achieve the effect of improving bioavailability, meeting treatment needs, and improving curative effect

Active Publication Date: 2012-10-10
HENAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In vivo and in vitro studies have found that isoandrographolide has anti-inflammatory and anti-tumor activities, but its water solubility is poor, which affects the drug absorption and efficacy of its preparations after administration
In addition, common preparations are used for tumor treatment, which lacks targeting, so its application is limited

Method used

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  • Suspension containing andrographolide solid lipid nanoparticles as well as preparation method and application of suspension
  • Suspension containing andrographolide solid lipid nanoparticles as well as preparation method and application of suspension
  • Suspension containing andrographolide solid lipid nanoparticles as well as preparation method and application of suspension

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Take 600 mg of glyceryl monostearate and heat and melt in a water bath at 70° C., then add 100 mg of isoandrographolide to the above molten liquid and mix well. Dissolve 200mg of soybean lecithin in 20ml of purified water, and heat to 70°C in a water bath. Under the condition that the stirring speed is 4000r / min, the above-mentioned glycerol monostearate and isoandrographolide melt is added to the aqueous soybean lecithin solution to form a colostrum suspension. Then use a high-pressure milk homogenizer to homogenize for 5 times (homogeneous pressure 60-80MP), that is.

[0037] The particle diameter of isoandrographolide solid lipid nanoparticles in the resulting suspension is 247.1 nm (see figure 1 ), the zeta potential is -39.7 mV (see figure 2 ), the encapsulation efficiency was 92.9%.

Embodiment 2

[0039] Take 600 mg of glyceryl monostearate and heat and melt in a water bath at 70° C., then add 50 mg of isoandrographolide to the above melt and mix evenly. Take 400mg of soybean lecithin and dissolve in 20ml of purified water, and heat to 70°C in a water bath. Under the condition that the stirring speed is 4000r / min, the above-mentioned glycerol monostearate and isoandrographolide melt is added to the aqueous soybean lecithin solution to form a colostrum suspension. Then use a high-pressure milk homogenizer to homogenize for 5 times (homogeneous pressure 70-80MP), that is.

[0040] The particle size of isoandrographolide solid lipid nanoparticles in the obtained suspension was 221.1 nm, the Zeta potential was -36.7 mV, and the encapsulation efficiency was 92.5%.

Embodiment 3

[0042]Take 600mg of glyceryl behenate and heat it in a water bath at 75°C to melt, then add 100mg of isoandrographolide to the above melt and mix evenly. Dissolve 300mg of poloxamer 188 in 20ml of purified water, and heat to 75°C in a water bath. Under the condition that the stirring speed is 5000r / min, the above-mentioned glycerol monostearate and poloxamer 188 melt are added to the poloxamer 188 aqueous solution to form a colostrum suspension. Then use a high-pressure milk homogenizer to homogenize for 5 times (homogeneous pressure 60-80 MP), that is to say.

[0043] The particle diameter of isoandrographolide solid lipid nanoparticles in the obtained suspension was 181.2 nm, the Zeta potential was -32.9 mV, and the encapsulation efficiency was 90.7%.

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Abstract

The invention relates to suspension containing andrographolide solid lipid nanoparticles as well as a preparation method and an application of the suspension, wherein the andrographolide solid lipid nanoparticles are dispersed in emulsion formed by purified water and emulsifying agents and consists of andrographolide and lipid materials, the weight ratio of the andrographolide to the lipid materials to the emulsifying agents is (1-15): (35-70):(20-50), and the consumption of the purified water is metered according to the principle that 1ml of purified water is added into 5 to 20mg of emulsifying agents. The suspension has the advantages that the andrographolide is covered and sealed in lipid inner cores of the solid lipid nanoparticles, the in-vivo absorption of the medicine is improved, the bioavailability is improved, meanwhile, and the slow release performance and the targeting performance are realized, so the toxic or side effect is reduced, and the anti-tumor curative effect is improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a suspension containing isoandrographolide solid lipid nanoparticles and a preparation method and application thereof. Background technique [0002] Andrographolide (AND) is a diterpene lactone compound extracted from Andrographis paniculata (Burm. f.) Nees, a plant of the Acanthaceae family. It is one of the main active ingredients of Andrographis paniculata (Burm. f.) Nees. Traditional medical research has found that andrographolide has antibacterial, antipyretic, cough and asthma effects, and is mainly used clinically to treat infectious diseases such as upper respiratory tract inflammation and bacillary dysentery with few side effects. In recent years, with the in-depth study of the pharmacological effects of andrographolide and its derivatives in modern medicine, it has been found that it has anti-tumor effects. Isoandrographolide is a derivative of andrographolid...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/365A61P35/00
Inventor 张瑜韩光杜钢军张生杰焦温文华素
Owner HENAN UNIVERSITY
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