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Bionic lovastatin nano-structured lipid carrier and preparation method thereof

A nano-lipid carrier, lovastatin technology, used in microcapsules, emulsion delivery, nanocapsules, etc., can solve the problems of low drug loading, hemolysis, poor water solubility, etc., to improve poor oral absorption and reduce toxicity. The effect of reducing side effects and toxic side effects

Inactive Publication Date: 2013-02-20
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, lovastatin has poor water solubility (LogP=4.5), oral absorption rate is only 31%, decreases by 30% on an empty stomach, and bioavailability is less than 5%.
In addition, after taking lovastatin, adverse reactions such as abdominal pain, constipation, flatulence, liver toxicity and rhabdomyolysis may occur
These have brought a lot of inconvenience for prophylactic medication and most patients with chronic diseases, so developing a lovastatin preparation with long-acting sustained release, low toxicity and side effects, and high bioavailability will have broad development prospects, thereby providing lovastatin Provide more choices in the formulation of sustained and controlled release preparations
[0006] After 2000, a new generation of nano-structured lipid carriers (NLC) appeared on the basis of solid lipid nanoparticles (SLN), that is, a certain proportion of liquid oil or liquid lipid Mixed with solid lipids, it overcomes the shortcomings of solid lipid nanoparticles such as low drug loading, easy drug precipitation, and poor physical stability.
[0007] Certain lipid materials used in the preparation of traditional nanolipid carriers may be toxic to macrophages, and bile salts, poloxamers, and some other ionic or nonionic surfactants are often used as Emulsifier, may cause irritation, hemolysis or other allergic reactions

Method used

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  • Bionic lovastatin nano-structured lipid carrier and preparation method thereof
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  • Bionic lovastatin nano-structured lipid carrier and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1: Preparation of biomimetic lovastatin nano-lipid carrier

[0023] prescription:

[0024]

[0025] Preparation process: Weigh the prescribed amount of lovastatin, soybean lecithin, arachidonic acid, cholesterol oleate, triolein, and cholesterol, dissolve in ethanol, and evaporate under reduced pressure to obtain a dry lipid film. Add hydration medium and hydrate in a constant temperature water bath at 30°C for one hour, ultrasonically disperse the hot colostrum, then perform probe ultrasonication (300W, 200s), then filter and sterilize with a 0.22μm microporous membrane, put it in a sterile bottle and seal it for storage.

[0026] The prepared lovastatin nano-lipid carrier has a particle size of 128.3nm, a polydispersity index (PI) of 0.246, an encapsulation efficiency of 91.62%, a drug loading capacity of 3.4%, and a Zeta potential of -34.2mV. release curve as figure 1 shown.

Embodiment 2

[0027] Embodiment 2: Preparation of biomimetic lovastatin nano-lipid carrier

[0028] prescription:

[0029]

[0030] Preparation process: Weigh the prescribed amount of lovastatin, egg yolk lecithin, arachidonic acid, cholesterol oleate, triolein, and cholesterol, dissolve in chloroform, and dry lipid film by rotary evaporation under reduced pressure. Add hydration medium and hydrate in a constant temperature water bath at 25°C for one hour, ultrasonically disperse the hot colostrum, then perform probe ultrasonication (300W, 200s), then filter and sterilize with a 0.22μm microporous membrane, put it in a sterile bottle and seal it for storage.

[0031] The prepared lovastatin nano-lipid carrier has a particle size of 135.5nm, a polydispersity index (PI) of 0.253, an encapsulation efficiency of 91.34%, a drug loading capacity of 3.1%, and a Zeta potential of -32.6mV. release curve as figure 1 shown.

Embodiment 3

[0032] Embodiment 3: Preparation of biomimetic lovastatin nano-lipid carrier

[0033] prescription:

[0034]

[0035]

[0036] Preparation process: Weigh the prescribed amount of lovastatin, dioleoyl lecithin, arachidonic acid, cholesterol oleate, triolein, and cholesterol, dissolve in dichloromethane, and dry lipid by rotary evaporation under reduced pressure film. Add hydration medium and hydrate in a constant temperature water bath at 40°C for one hour, ultrasonically disperse the hot colostrum, then perform probe ultrasonication (300W, 200s), then filter and sterilize with a 0.22μm microporous membrane, put it in a sterile bottle and seal it for storage.

[0037] The prepared lovastatin nano-lipid carrier has a particle size of 123.2nm, a polydispersity index (PI) of 0.227, an encapsulation efficiency of 92.51%, a drug loading capacity of 2.8%, and a Zeta potential of -37.4mV. release curve as figure 2 shown.

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Abstract

The invention relates to the field of pharmaceutical preparation, and in particular relates to a bionic lovastatin nano-structured lipid carrier and a preparation method thereof. The method is characterized in that endogenic lipid material is adopted so as to encapsulate medicines in the carrier, so that injection for intravenous injection can be produced. The prepared nano-structured lipid carrier has good biocompatibility and is biodegradable, and toxic and side effects are reduced; the bionic lovastatin nano-structured lipid carrier has small grain size, high dispersity, good stability and can long-lastingly and slowly release medicines; and lovastatin medicines and the bioactive lipid carrier can be combined together so as to achieve a collaborative treatment function, and the curative effect of the medicine in treating cardiovascular disease is increased.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a biomimetic nano lipid carrier containing lovastatin and a preparation method thereof. Background technique [0002] Lovastatin is a blood lipid-lowering drug of the statin class. In addition to acting on liver cells and inhibiting endogenous cholesterol synthesis, it can also improve endothelial function, inhibit the proliferation and migration of vascular smooth muscle cells, induce smooth muscle cell apoptosis, Anti-inflammatory, improve plaque stability and other effects. In 1987, the US FDA approved it as the first statin drug to regulate blood lipids. Lovastatin currently used clinically is mainly oral preparations, mainly tablets and capsules, and micropills, dripping pills, and sustained-release tablets have also been developed in China. [0003] The structural formula of lovastatin is as follows, [0004] [0005] However, lovastatin has poor water solub...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K9/107A61K31/366A61P3/06A61P9/00
Inventor 刘建平王济
Owner CHINA PHARM UNIV
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