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Preparation method of amorphous atorvastatin calcium

An atorvastatin calcium and amorphous technology, which is applied in the field of preparation of amorphous atorvastatin calcium, can solve the problems of high toxicity of acetonitrile and difficulty in meeting the requirements of residual solvents, etc., and achieve the effect of high yield and simple process

Active Publication Date: 2008-07-30
ZHEJIANG LEPU PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method seems relatively simple, but acetonitrile is highly toxic and difficult to meet the requirements of residual solvents

Method used

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  • Preparation method of amorphous atorvastatin calcium
  • Preparation method of amorphous atorvastatin calcium
  • Preparation method of amorphous atorvastatin calcium

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Put 20.0Kg of crystalline atorvastatin calcium into a 500L stainless steel still 1 with stirring and distillation tower 3 (diameter Φ300, equipped with 4m BX wire mesh packing), add 300L of methanol saturated with n-hexane in advance, stir and heat up Bring to a boil to completely dissolve the crystals of atorvastatin calcium. Open the alkane high tank 2 valve, add n-hexane dropwise, and control the drop rate at about 100L / hr. The azeotrope of alkane and methanol evaporated from the top of the distillation tower is condensed in the condenser 4, and the heating is adjusted so that the amount of the methanol phase in the condensate is about 100L / hr, and the stratification is carried out in the stratifier 5, and the methanol is continuously separated phase is placed in the methanol phase storage tank 6, and the upper n-hexane phase is all refluxed to the top of the distillation tower. After about 3 hours, when the temperature in the kettle rose to the boiling point of n-h...

Embodiment 2

[0034] In the device identical with embodiment 1, drop into 20.0Kg crystalline atorvastatin calcium, add about 300L of the methanol phase that separates when last batch of distillation, stir and be warmed up to boiling, make atorvastatin calcium crystal dissolve completely. Open the dripping valve, drip the mixed solution formed by about 250L of the filtrate in Example 1 and the added 50L n-hexane, the rate of addition is controlled at about 100L / hr, and carry out azeotropic distillation, cooling, and filtration the same as in Example 1 , dry operation, obtain amorphous atorvastatin calcium 19.9Kg.

Embodiment 3

[0036] In the same device as in Example 1, 20.0Kg of crystalline atorvastatin calcium was dropped into, and 300L of methanol saturated with cyclohexane was added in advance, and when the temperature in the still was controlled to reach about 80°C, heating and dripping were stopped, and the mixture was stirred under stirring. The material was cooled to 15° C., and other operations were the same as in Example 1, and finally 19.7 Kg of amorphous atorvastatin calcium was obtained.

[0037] The X-ray diffraction pattern of the amorphous atorvastatin calcium prepared according to this embodiment is shown in Figure 3, it can be seen that the atorvastatin calcium has reached the amorphous state.

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Abstract

The invention relates the preparing method of non-shaped aphtha-vastatin calcium. The current technology has many defects. The method comprises the following steps: preparing menthol dissolution liquid, dissolving aphtha-vastatin calcium in the liquid, distilling and getting the menthol dissolution liquid which can be recovered. The invention has the advantages of simple technology and high productivity.

Description

technical field [0001] The invention belongs to the field of pharmacy, in particular to a preparation method of amorphous atorvastatin calcium. Background technique: [0002] Atorvastatin calcium is a lipid-lowering drug, and its structure is as follows: [0003] [0004] Atorvastatin calcium can exist in a variety of crystal forms, and different crystal forms have different physical properties and bioavailability. It is generally believed that amorphous atorvastatin calcium has better solubility in organisms, and thus has better drug activity and bioavailability. Utilization. [0005] There are many patent literature reports on the preparation method of amorphous atorvastatin calcium. According to the different methods adopted, there are roughly the following categories: [0006] (1) Concentration method [0007] The preparation of amorphous atorvastatin calcium by concentration method usually involves dissolving crystalline atorvastatin calcium in solvents such as a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D207/335A61K31/40A61P3/06
Inventor 陈志荣陈正许沈荣兵王云德林洁
Owner ZHEJIANG LEPU PHARMA CO LTD