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Preparation method of amorphous fluvastatin sodium

A fluvastatin sodium and amorphous technology, which is applied in the field of preparation of amorphous fluvastatin sodium, can solve the problem of low yield and the like, and achieve the effects of high yield and simple process

Active Publication Date: 2008-10-29
ZHEJIANG LEPU PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] When above two kinds of methods prepare amorphous fluvastatin sodium, because fluvastatin sodium has larger solubility in methanol, THF, thereby yield is not high, and there is the mixed solvent that can produce azeotropy in the second kind of preparation method the separation problem

Method used

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  • Preparation method of amorphous fluvastatin sodium
  • Preparation method of amorphous fluvastatin sodium
  • Preparation method of amorphous fluvastatin sodium

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Put 20.0Kg of crystalline fluvastatin sodium into 500L stainless steel distillation kettle 1 with stirring and distillation tower 3 (diameter Φ300, equipped with 4 meters of BX wire mesh packing), add 300L of methanol saturated with n-hexane in advance, stir and heat up When it boils, the fluvastatin sodium crystals are completely dissolved. Open the valve of the high-position tank 2 for alkane, add n-hexane dropwise, and control the dropping rate at about 100L / hr. The azeotrope of alkane and methanol distilled from the top of the distillation tower is condensed in condenser 4, and the heating is adjusted to make the amount of methanol phase in the condensate about 100L / hr. In the stratifier 5, the methanol is separated continuously. The 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-hexane (68-69°C)...

Embodiment 2

[0027] Put 20.0Kg of crystalline fluvastatin sodium into the same device as in Example 1, add about 300L of methanol phase separated in the last batch of distillation, stir and raise the temperature to boiling, so that the fluvastatin sodium crystals are completely dissolved. Open the dripping valve, drip the mixture of about 250L of filtrate in Example 1 and supplementary 50L of n-hexane, and control the dripping rate at about 100L / hr. Perform azeotropic distillation, cooling, and filtration as in Example 1. , Drying operation, obtain amorphous fluvastatin sodium 20.0Kg.

Embodiment 3

[0029] Put 20.0Kg of crystalline fluvastatin sodium in the same device as in Example 1, add 300L of methanol saturated with cyclohexane in advance, control the temperature in the still to stop heating and drip when the temperature reaches about 80℃, and add The material was cooled to 15°C, and other operations were the same as in Example 1, and finally 19.8Kg of amorphous fluvastatin sodium was obtained.

[0030] The X-ray diffraction pattern of the amorphous fluvastatin sodium prepared in this example is shown in Figure 3, and it can be seen that the fluvastatin sodium has reached an amorphous shape.

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Abstract

The invention relates the preparing method of non-shaped fluorine-vastatin sodium. The current technology has many defects. The method comprises the following steps: preparing menthol dissolution liquid, dissolving fluorine-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, and particularly relates to a preparation method of amorphous fluvastatin sodium. Background technique: [0002] Fluvastatin sodium is a lipid-lowering drug, and its structural formula is as follows: [0003] [0004] Fluvastatin sodium can exist in a variety of crystal forms, and different crystal forms have different physical properties and bioavailability. It is generally believed that amorphous fluvastatin sodium has better solubility in the body, and therefore has better drug activity and bioavailability. Utilization. [0005] There have been two patent literature reports on the preparation method of amorphous fluvastatin sodium. [0006] The method reported in WO2006038219 is to dissolve fluvastatin sodium in methanol, concentrate in vacuo, filter the precipitated crystals, and dry to obtain amorphous fluvastatin sodium. [0007] The method reported in USP2005209259 is to dissolve fluvastatin sodium in...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D209/12A61K31/405A61P3/06
Inventor 陈正许陈志荣林洁王云德卢荣彬
Owner ZHEJIANG LEPU PHARMA CO LTD
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