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Huperzine A solid lipid nano particle and preparation method thereof

A technology of solid lipid nanometer and huperzine A, which is used in pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc. granules, limiting the application of SLN pharmaceutical carriers, etc., to achieve the effects of increasing brain targeting, improving bioavailability, and high encapsulation efficiency

Active Publication Date: 2012-05-23
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the above-mentioned preparation methods all use organic solvents, and it is impossible to completely remove harmful organic solvents, thus limiting the application of SLN pharmaceutical carriers
At present, there is no report of huperzine A solid lipid nanoparticles in the preparation of high-pressure milk homogenization technology

Method used

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  • Huperzine A solid lipid nano particle and preparation method thereof
  • Huperzine A solid lipid nano particle and preparation method thereof
  • Huperzine A solid lipid nano particle and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0042] Prepare huperzine A solid lipid nanoparticles (the percentage in the prescription is the weight percentage that this component occupies in the whole prescription, and the following embodiments are identical):

[0043] Prescription: Huperzine A 30mg

[0044] Glyceryl monostearate 1.5g

[0045] Poloxamer 188 0.5g

[0046] Tween-80 0.5g

[0047] Distilled water 50mL

[0048] Preparation:

[0049] Step 1: Weigh Poloxamer 188 and Tween-80, add appropriate amount of distilled water and ultrasonically disperse until completely dissolved to form an aqueous phase; mix and melt huperzine A and glyceryl monostearate to form an oil phase;

[0050] Step 2: Heat the water phase and the oil phase in water baths to 65°C respectively. After the oil phase is completely dissolved into a clear hot body, add the water phase to the oil phase dropwise under constant temperature magnetic stirring conditions. The stirring speed is 1500rpm, and keep stirring at a cons...

Embodiment 2

[0054] Preparation of huperzine A solid lipid nanoparticles:

[0055] Prescription: Huperzine A 80mg

[0056] Glyceryl monostearate 2g

[0057] Poloxamer 188 1g

[0058] Egg yolk phospholipids 0.5g

[0059] Distilled water 50mL

[0060] Step 1: Weigh poloxamer 188 and egg yolk phospholipid, add appropriate amount of distilled water and ultrasonically disperse until completely dissolved to form an aqueous phase; mix and melt huperzine A and glyceryl monostearate to form an oil phase;

[0061] Step 2: Heat the water phase and the oil phase in a water bath to 85°C. After the oil phase is completely dissolved into a clear hot body, add the water phase to the oil phase dropwise under the condition of constant temperature magnetic stirring. The stirring speed is 800rpm, and the constant temperature is maintained. Stir for 30 minutes; then remove the water bath and continue to stir to room temperature, making it a milky white emulsion and forming colostrum...

Embodiment 3

[0065] Preparation of huperzine A solid lipid nanoparticles:

[0066] Prescription: Huperzine A 180mg

[0067] Glyceryl monostearate 3g

[0068] Poloxamer 188 1.5g

[0069] Tween-80 1.5g

[0070] Distilled water 50mL

[0071] Preparation:

[0072] Step 1: Weigh Poloxamer 188 and Tween-80, add appropriate amount of distilled water and ultrasonically disperse until completely dissolved to form an aqueous phase; mix and melt huperzine A and glyceryl monostearate to form an oil phase;

[0073] Step 2: Heat the water phase and the oil phase to 70°C in a water bath, and after the oil phase is completely dissolved into a clear hot body, add the water phase to the oil phase dropwise under the condition of constant temperature magnetic stirring, the stirring speed is 1000rpm, and the constant temperature is maintained Stir for 18 minutes; then remove the water bath and continue stirring to room temperature, making it a milky white emulsion and forming colos...

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Abstract

The invention relates to the field of pharmaceutical preparations, which discloses a huperzine A solid lipid nano particle and a preparation method thereof. The huperzine A solid lipid nano particle is prepared from the following components in weight percent: 0.05-1% of huperzine A, 3-10% of lipid material, 2-10% of emulsifying agent and the balance water. The preparation method adopts a high-pressure even emulsification method to coat the huperzine A into a solid lipid nano particle so as to prepare the huperzine A solid lipid nano particle. The particle diameter of the huperzine A solid lipid nano particle prepared by the invention is 10-100nm, the medicine envelopment rate and the medicine-carrying quantity are high, and the stability is good; simultaneously, the use of an addition agent and an organic solvent which are harmful to a human body is avoided; and the bioavailability is enhanced, the brain targeting property is increased, and the dose and the toxic or side effect are small.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a solid lipid nanoparticle of traditional Chinese medicine huperzine A and a preparation method thereof. Background technique [0002] Huperzine A (Huperzine A, C 15 h 18 N 2 O), is a new structural alkaloid isolated from Huperzaceae plant Huperzinus by Chinese medical researchers. The results of pharmacological studies show that Huperzine A is a highly efficient and reversible cholinesterase inhibitor. Cholinease (AChE) has a strong inhibitory effect. In 1993, the U.S. FDA approved it to go on the market. In 1996, my country approved it as a second-class new drug, which is used for the treatment and prevention of senile dementia and to improve the intellectual memory of young people. Clinical trials have confirmed that it can prevent the decomposition of ethyl choline in brain tissue, improve the efficiency of mental activity, and directly improve memory. It has t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K9/19A61K47/12A61K47/14A61K47/24A61K47/34A61K31/4748A61P25/28A61K47/10A61K47/26
Inventor 林华庆张蜀邓红李园陈桐楷余楚钦
Owner GUANGDONG PHARMA UNIV
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