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Atorvastatin calcium nano-lipid carrier and preparation method thereof

A technology of atorvastatin calcium and nano-lipid carrier, which can be used in pharmaceutical formulations, medical preparations with inactive ingredients, metabolic diseases, etc., can solve problems such as easy leakage and low encapsulation rate, and achieve low toxicity and improved Solubility, diameter reduction effect

Active Publication Date: 2014-04-02
RUNZE PHARMACEUTICAL (SUZHOU) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The problem with SLN is that a single lipid material tends to form more perfectly regular crystals, causing the encapsulated drug to efflux or crystallize out in the dispersed aqueous phase of the SLN
Therefore, NLC not only has the advantages of SLN, such as good biocompatibility and biodegradability, protecting sensitive drugs, improving the solubility of insoluble drugs, and improving the bioavailability of drugs, etc., but also overcomes the low encapsulation efficiency and easy leakage of SLN. insufficient

Method used

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  • Atorvastatin calcium nano-lipid carrier and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042]Dissolve 10mg of atorvastatin calcium, 30mg of glyceryl monostearate, 20mg of corn oil, and 150mg of soybean lecithin in 5ml of ethanol, heat in a water bath at 65°C until completely dissolved, and form an organic phase; another 250mg of poloxa Mel 188 was dissolved in 15ml of water, and heated in a water bath to 65°C to form the water phase; under 1000r / min magnetic stirring, the organic phase was added dropwise to the water phase with a No. 5ml to form colostrum; quickly disperse the colostrum into 25ml of ice water stirred at 1000r / min, continue to stir and solidify in the ice bath for 1.5h, and prepare the atorvastatin calcium nano-lipid carrier.

[0043] The prepared nano-lipid carrier is suitably diluted with distilled water, and the particle size and its distribution are measured. The particle size distribution is as follows: figure 1 As shown, the average particle diameter is 303.5nm, the PDI is 0.232, and the zeta potential is -13.84mV.

Embodiment 2

[0045] Dissolve 10mg of atorvastatin calcium, 20mg of glyceryl monostearate, 40mg of corn oil, and 140mg of soybean lecithin in 5ml of ethanol, heat in a water bath at 65°C until completely dissolved, and form an organic phase; another 100mg of poloxamer 188. Dissolve 100mg of Tween 80 in 15ml of water, heat in a water bath to 65°C to form the water phase; under magnetic stirring at 1000r / min, add the organic phase to the water phase drop by drop with a No. 7 needle, continue stirring, evaporate the organic phase and Concentrate the volume to 5ml to form colostrum; quickly disperse the colostrum into 25ml of ice water stirred at 1000r / min, continue to stir and solidify in the ice bath for 1.5h, and prepare the atorvastatin calcium nano-lipid carrier with an encapsulation efficiency of 82.1%.

Embodiment 3

[0050] Dissolve 5mg of atorvastatin calcium, 50mg of glyceryl monostearate, 20mg of corn oil, and 130mg of soybean lecithin in 5ml of ethanol, heat in a water bath at 65°C until completely dissolved, and form an organic phase; another 200mg of poloxamer Dissolve 188 in 15ml of water, heat in a water bath to 65°C to form the water phase; add the organic phase to the water phase drop by drop with a No. 7 needle under magnetic stirring at 1200r / min, continue stirring, evaporate the organic phase and concentrate the volume to 5ml , to form colostrum; quickly disperse the colostrum into 25ml of ice water stirred at 1000r / min, continue to stir and solidify under the ice bath for 1.5h, and prepare the atorvastatin calcium nano-lipid carrier.

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Abstract

The invention relates to an atorvastatin calcium nano-lipid carrier and a preparation method thereof. The atorvastatin calcium nano-lipid carrier comprises the following components: 1 wt% to 2 wt% of atorvastatin calcium, 12 wt% to 24 wt% of a lipid material, 10 wt% to 30 wt% of phospholipid and 30 wt% to 50 wt% of an emulsifier. The preparation method comprises the following steps: weighing the atorvastatin calcium, the lipid material and the phospholipid, ultrasonically dissolving in an organic solvent, heating to 60-75 DEG C in a water bath, and using an obtained product as an organic phase; dissolving the emulsifier in water, heating to 60-75 DEG C in the water bath, and using an obtained product as a water phase; dropwise adding the organic phase into the water phase stirred at the speed of 90-1,200 r / min, continuously stirring for fully volatilizing the organic solvent, and concentrating to form a primary emulsion; pouring the primary emulsion into ice water with the volume being 2-5 times that of the primary emulsion, and continuously stirring and solidifying in an ice bath to obtain the atorvastatin calcium nano-lipid carrier. The atorvastatin calcium nano-lipid carrier is internally degradable and high in encapsulation efficiency; after drugs are prepared into nano-lipid carriers, the stability, the water solubility and the bioavailability of the drugs can be improved.

Description

technical field [0001] The invention relates to an atorvastatin calcium nano lipid carrier and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Cardiovascular disease is one of the most common and serious diseases that endanger human health. It is estimated that by 2030, the number of patients with cardiovascular diseases in China will increase by 21.3 million, and the number of deaths from cardiovascular diseases will increase by 7.7 million. According to reports, although the blood lipid level and the prevalence of dyslipidemia in the Chinese population are lower than those in most western countries, they are still important risk factors that threaten the health of our people. Dyslipidemia is an important risk factor for atherosclerosis, coronary heart disease and ischemic stroke. [0003] Atorvastatin reduces blood cholesterol and lipoprotein levels by inhibiting HMG-CoA reductase and cholestero...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K31/40A61K47/46A61K47/22A61K47/14A61P3/06
Inventor 胡玮周志亮陈叶明孙川棣李先俊沈梦妮
Owner RUNZE PHARMACEUTICAL (SUZHOU) CO LTD
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