Atorvastatin calcium and phospholipid compound and preparation method thereof

A technology of atorvastatin calcium phospholipid and atorvastatin calcium, which is applied in the field of pharmacy and can solve complex problems (including the process of preparing tablet core, isolation coat coating process, adhesive coating process, laser drilling process and intestinal Dissolving and coating process, high energy consumption, reducing drug degradation and other problems, to achieve excellent transmembrane transport properties, good reproducibility, and promote the effect of in vivo absorption

Inactive Publication Date: 2017-05-24
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Patent CN105434391A discloses an enteric-coated tablet containing atorvastatin calcium, which aims to reduce the degradation of the drug in gastric juice. According to the results, although the preparation has improved bioavailability, it inevitably has complex preparation processes (including preparation Tablet core process, isolation coat coating process, adhesive coating process, laser drilling process and enteric coating process, etc.), high energy consumption and other defects
Other inventions related to oral preparations of atorvastatin calcium have been prepared from the perspective of improving drug dispersibility, soft capsules (CN100450471C), dripping pills (CN1939286A), dry suspensions (CN101637452B), and fast-disintegrating tablets (CN100411612C ), etc., but there is no report about improving the solubility and permeability of atorvastatin calcium from the level of drug molecules

Method used

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  • Atorvastatin calcium and phospholipid compound and preparation method thereof
  • Atorvastatin calcium and phospholipid compound and preparation method thereof
  • Atorvastatin calcium and phospholipid compound and preparation method thereof

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preparation example Construction

[0042] The preparation method and characterization of the atorvastatin calcium phospholipid complex of the present invention comprise the following steps:

[0043](1) Prepare atorvastatin calcium with the molar ratios of atorvastatin calcium and phospholipids being 0 / 5, 1 / 4, 2 / 3, 2.5 / 2.5, 3 / 2, 4 / 1, 5 / 0 respectively Phospholipid complexes and physical mixtures and keep the drug concentration constant at 0.005mol / L. Measure the absorbance value A of atorvastatin calcium phospholipid complex and atorvastatin calcium at a wavelength of 244nm, and calculate the difference △A between the two, and plot △A against the molar ratio, and the corresponding one with the largest change in △A The mol ratio is the drug-lipid complex ratio of atorvastatin calcium-phospholipid complex.

[0044] (2) Weigh an appropriate amount of atorvastatin calcium and phospholipids in corresponding molar ratios, stir in a series of aprotic solvents at 20°C to 90°C for 0.1 to 8 hours, then carry out rotary ev...

Embodiment 1

[0051] This embodiment provides a kind of atorvastatin calcium phospholipid complex, the molar ratio that comprises atorvastatin calcium and natural soybean lecithin is 1: 1, and the total molar number of atorvastatin calcium and natural soybean lecithin is 0.005mol / L, about 0.0025mol of atorvastatin calcium and 0.0025mol of natural soybean lecithin in 1L of acetone solution, stirred at 50°C for 3 hours, then rotary evaporated at 40°C until there was no organic solvent smell, and Vacuum drying at 40°C for 24 hours to obtain the atorvastatin calcium phospholipid complex. Store at 4°C after sealing. In this embodiment, the concentration of atorvastatin calcium is 2.89 mg / ml, the concentration of phospholipid is 1.88 mg / ml, and the concentration of reactants is 4.77 mg / ml.

Embodiment 2

[0053] This embodiment provides a kind of atorvastatin calcium phospholipid complex, the molar ratio that comprises atorvastatin calcium and phosphatidylethanolamine is 1: 1, and the total molar number of atorvastatin calcium and phosphatidylethanolamine is 0.005mol / L, about 0.0025mol of atorvastatin calcium and 0.0025mol of phosphatidylethanolamine in 1L of acetone solution, stirred at 30°C for 3 hours, then rotary evaporated at 40°C until there was no organic solvent smell, and in Vacuum drying at 40° C. for 20 hours to obtain the atorvastatin calcium phospholipid complex. Store at 4°C after sealing. In this embodiment, the concentration of atorvastatin calcium is 2.89 mg / ml, the concentration of phospholipid is 1.88 mg / ml, and the concentration of reactants is 4.77 mg / ml.

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Abstract

The invention discloses an atorvastatin calcium and phospholipid compound. The atorvastatin calcium and phospholipid compound is prepared from atorvastatin calcium and phospholipid, wherein the mol ratio of the atorvastatin calcium to the phospholipid is (1-4) to (4-1); the concentration of reactants is 0.1mg/ml-10mg/ml; and the phospholipid is selected from at least one of natural soybean phospholipid, natural lecithin or artificially synthetic phosphatidylcholine, phosphatidylglycerol, phosphatidylethanolamine, phosphatidylserine and phosphatidic acid. According to the atorvastatin calcium and phospholipid compound and a preparation method, disclosed by the invention, structural features of insoluble drugs are improved from a molecular level, so that the aims of improving the permeability and increasing the oral bioavailability are realized.

Description

technical field [0001] The invention relates to the technical field of pharmacy, in particular to an atorvastatin calcium phospholipid complex and a preparation method thereof. Background technique [0002] Atorvastatin calcium (Atorvastatin calcium, ATC) is a statin drug widely used in clinical practice. It is a selective and competitive inhibitor of HMG-CoA reductase. Synthesis to reduce the concentration of cholesterol in plasma and lipoprotein in serum, and increase the uptake and catabolism of LDL by increasing the low-density lipoprotein (LDL) receptor on the surface of liver cells, and reduce the production of LDL. The commercially available preparation of atorvastatin calcium is produced and sold by Pfizer Pharmaceutical Company of the United States, and the dosage form is a common tablet. [0003] Atorvastatin calcium is a poorly soluble drug, and its solubility has a typical pH dependence. It can be dissolved in slightly acidic aqueous solution. When the pH value ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/54A61K31/40A61P3/06
CPCA61K31/40
Inventor 秦凌浩牛亚伟董晓婷赵嘉兰王悦敏
Owner GUANGDONG PHARMA UNIV
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