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Solid preparation of atorvastatin calcium liposome

A technology of atorvastatin calcium and solid preparations, which is applied in the field of medicine, can solve the problems of poor stability and bioavailability, and cannot effectively exert the pharmacological activity of atorvastatin, and achieve the protection of vascular endothelial cells and microvascular system, The effect of reducing myocardial infarction size and stabilizing drug loading

Inactive Publication Date: 2012-01-11
HAINAN MEIDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] CN101804029A discloses a kind of atorvastatin liposome, in order to overcome the dosage form existing in the prior art, adopt simple atorvastatin calcium crude drug without any modification to add the alkaline agent that pH is greater than 5 to make and this The stability and bioavailability of the preparation are poor, and the defects of the pharmacological activity of atorvastatin cannot be effectively brought into play. It is made into liposomes of atorvastatin or a pharmaceutical salt thereof, the liposomes obtained above and its None of atorvastatin calcium in fixed formulations overcomes crystalline form leading to bioavailability issues

Method used

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  • Solid preparation of atorvastatin calcium liposome
  • Solid preparation of atorvastatin calcium liposome
  • Solid preparation of atorvastatin calcium liposome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Example 1 Preparation of Atorvastatin Calcium Liposome

[0053] prescription:

[0054] Atorvastatin Calcium 100g

[0055] Soy Lecithin 133.3g

[0056] Dimyristoyl Phosphatidylethanolamine 66.7g

[0057] Cholesterol 40g

[0058] Octadecylamine 40g

[0059] Preparation Process:

[0060] (1) Dissolve 133.3g soybean lecithin, 66.7g dimyristoylphosphatidylethanolamine, 40g cholesterol and 40g octadecylamine in a mixed solvent of ethyl acetate and ethanol with a volume ratio of 3:2 in 2000ml, and place on a rotating film The organic solvent was removed under reduced pressure on the evaporator, and the phospholipid film was obtained;

[0061] (2) Add 800 ml of citric acid-sodium citrate buffer solution with 100 g of atorvastatin calcium and a pH value of 5.6 to fully hydrate the phospholipid film, mix the solution evenly, and heat it at 70° C. for 40 minutes with ultrasonic treatment;

[0062] (3) Spray-dry the solution obtained in the above step (2) to obtain atorva...

Embodiment 2

[0085] Example 2 Preparation of Atorvastatin Calcium Liposome

[0086] prescription:

[0087] Atorvastatin Calcium 100g

[0088] Soy Lecithin 333.3g

[0089] Dimyristoyl Phosphatidylethanolamine 166.7g

[0090] Cholesterol 150g

[0091] Octadecylamine 150g

[0092] Preparation Process:

[0093] (1) Dissolve 333.3g soybean lecithin and 166.7g dimyristoylphosphatidylethanolamine and 150g cholesterol and 150g octadecylamine in a mixed solvent of ethyl acetate and ethanol with a volume ratio of 3:2 in 6000ml, and place on a rotating film The organic solvent was removed under reduced pressure on the evaporator, and the phospholipid film was obtained;

[0094] (2) Add 3000 ml of citric acid-sodium citrate buffer solution with 100 g of atorvastatin calcium and a pH value of 5.6 to fully hydrate the phospholipid film, mix the solution evenly, and heat it at 50° C. for 60 minutes with ultrasonic treatment;

[0095] (3) Spray-dry the solution obtained in the above step (2) to...

Embodiment 3

[0103] Example 3 Preparation of Atorvastatin Calcium Liposome Particles

[0104] Shell (1000 bags):

[0105] Atorvastatin calcium liposome (calculated as atorvastatin calcium) 50g

[0106] Starch 150g

[0107] Sucrose 850g

[0108] Povidone K 30 10g

[0109] Orange flavor 30g

[0110] Preparation Process:

[0111] (1) pulverize the liposome containing 50g atorvastatin calcium, cross 80 mesh sieves, and set aside;

[0112] (2) take by weighing 150g starch, 850g sucrose cross 80 mesh sieves and mix, set aside;

[0113] (3) Mix the above raw and auxiliary materials evenly, then mix evenly with 30g orange essence, add 3% povidone K 30 330ml of 80% ethanol solution is used to make soft materials, passed through a 20-mesh sieve to granulate, dried at 60°C, granulated through a 18-mesh sieve, and set aside;

[0114] (4) Divide the dried granules to prepare atorvastatin calcium liposome granules.

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Abstract

The invention discloses a solid preparation of atorvastatin calcium liposome. The preparation is prepared from the atorvastatin calcium liposome and other pharmaceutically common auxiliary materials, wherein the atorvastatin liposome is prepared from the following components in parts by weight: 1 part of atorvastatin calcium, 2-5 parts of phospholipid and 0.8-3 parts of additive. The atorvastatinsolid preparation prepared from the liposome has the advantages that the dissolution rate is increased, the stability and bioavailability are greatly improved, the product quality of the preparation is improved and the toxic and side effect is reduced.

Description

technical field [0001] The present invention relates to an atorvastatin calcium liposome preparation, especially an amorphous atorvastatin calcium liposome preparation maintaining high bioavailability, and further relates to an atorvastatin calcium liposome solid preparation and its preparation method, which belongs to the field of medical technology. Background technique [0002] Cardiovascular disease is one of the most common and serious diseases that endanger human health. It has the characteristics of "high incidence, high disability rate, high mortality rate, high recurrence rate and many complications". At present, there are more than 270 million patients with cardiovascular and cerebrovascular diseases in my country. In recent years, domestic and foreign guidelines for the prevention and treatment of hypertension have indicated that the blood pressure of hypertensive patients should be actively and persistently lowered to below 140 / 90 mmHg (the best should be lowered...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K9/16A61K9/20A61K31/40A61K47/24A61K47/28A61P3/06A61P9/10
Inventor 廖爱国
Owner HAINAN MEIDA PHARMA
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