Fluvastatin preparation without stabilizing agents

A fluvastatin and stabilizer technology, applied in the field of biopharmaceuticals, can solve the problems of low solubility, high hygroscopicity, and low light stability

Inactive Publication Date: 2011-09-21
SHANGHAI TIANLONG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Fluvastatin has the characteristics of good taste, high hygroscopicity, low solubility in acidic medium, low stability to heat, humidity and light, unstable in acidic aqueous medium, etc.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Granule prescription

[0021] Fluvastatin Sodium 84g

[0022] Poloxamer 188 20g

[0023] PEG6000 60g

[0024] Preparation: Weigh fluvastatin sodium, poloxamer and PEG6000 according to the prescription amount, pulverize fluvastatin sodium through an 80-mesh sieve for later use; pulverize the poloxamer and PEG6000 through a 40-mesh sieve, heat in a water bath at 80-90°C Melt, slowly add fluvastatin sodium, stir until the drug powder completely disappears, put the molten drug-containing liquid in a freezer at 4°C for 24 hours, pulverize to obtain fluvastatin sodium particles.

[0025] tablet prescription

[0026] Fluvastatin sodium granules (equivalent to fluvastatin sodium 84g)

[0027] Microcrystalline Cellulose 145g

[0028] Hydroxyethyl Cellulose 50g

[0029] Magnesium Stearate 4g

[0030] Preparation: Mix the granules with other materials in the prescription evenly, add magnesium stearate, and compress into tablets.

Embodiment 2

[0032] Granule prescription

[0033] Fluvastatin Sodium 84g

[0034] Mannitol 80g

[0035] Preparation: Weigh fluvastatin sodium and mannitol according to the prescription amount, pulverize fluvastatin sodium through an 80-mesh sieve, dissolve in mannitol ethanol solution, freeze and spray to obtain fluvastatin sodium granules.

[0036] tablet prescription

[0037] Fluvastatin sodium granules (equivalent to fluvastatin sodium 84g)

[0038] Microcrystalline Cellulose 145g

[0039] Sodium carboxymethyl starch 50g

[0040] Magnesium Stearate 4g

[0041] Preparation: Mix the granules with other materials in the prescription evenly, add magnesium stearate, and compress into tablets.

Embodiment 3

[0043] Granule prescription

[0044] Fluvastatin Sodium 84g

[0045] PVP k30 60g

[0046] PVPP xl 20g

[0047] Preparation: Take fluvastatin sodium, PVP k30 and PVPPxl according to the prescription amount, pulverize fluvastatin sodium through an 80 mesh sieve, dissolve in the acetone: ethanol (1:2) solution of PVP k30 and PVPPxl, freeze and spray to obtain Fluvastatin Sodium Granules.

[0048] tablet prescription

[0049] Fluvastatin sodium granules (equivalent to fluvastatin sodium 84g)

[0050] Microcrystalline Cellulose 145g

[0051] Low-substituted hypromellose 30g

[0052]Magnesium Stearate 4g

[0053] Preparation: Mix the granules with other materials in the prescription evenly, add magnesium stearate, and compress into tablets.

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PUM

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Abstract

The invention provides a fluvastatin preparation without stabilizing agents. The fluvastatin preparation is characterized in that the fluvastatin preparation does not contain alkalizers for elevating the pH value of the preparation; fluvastatin is dispersed on pharmaceutically applicable polymer carriers to achieve the aim of stabilization; and the polymer carriers are selected from one or more of polyethylene glycols, polyvidones, surfactants containing polyoxyethylene groups, water-soluble cellulose derivatives, organic acids, saccharides and alcohols. The preparation can be prepared by a freeze drying method.

Description

technical field [0001] The invention belongs to the field of biopharmaceuticals, and in particular relates to a stabilizer-free fluvastatin preparation, the specific preparation form of which is tablet or capsule. The invention also relates to its preparation method. Background technique [0002] Statins, namely HMG-CoA reductase inhibitors, are currently used, including lovastatin, fluvastatin, rosuvastatin, pravastatin, atorvastatin and simvastatin. Fluvastatin has the characteristics of good taste, high hygroscopicity, low solubility in acidic medium, low stability to heat, humidity and light, and instability in acidic aqueous medium. When preparing fluvastatin formulations, it is necessary to avoid direct exposure of fluvastatin to the air, for example by using film coating, and it is also necessary to take stabilizing measures to improve the stability of the formulation. Fluvastatin is generally suitably formulated in an alkaline medium such that the pH of the aqueous...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/405A61K47/30A61K47/32A61K47/34A61K47/38A61K47/26A61P3/06
Inventor 宋波
Owner SHANGHAI TIANLONG PHARMA
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