Pharmaceutical formulation

A technology of pharmaceutical activity and medicine, applied in the field of preparation of solid dispersion, can solve the problems of lowering glass transition temperature of amorphous material, crystallization and physical instability, etc.

Inactive Publication Date: 2006-03-15
NOVARTIS AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Also, additives such as plasticizers lower the glass transition temperature of the amorphous, thereby promoting crystallization and physical instability

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0077] Solid dispersions prepared from melt extrudates containing 30% TKA731 and PVPK-30 (ISP Technologies, Wayne, NJ) showed a single glass transition by differential scanning calorimetry, indicating that solid solutions formed by this method were compatible with Dispersions prepared by the solvent method were similar. The extrudate had a glass transition temperature of 137.20°C and an onset temperature of 130.0°C, which was very similar to the dispersion prepared by the solvent method, which had a glass transition temperature of 139.9°C , the initial temperature is 131.9°C.

[0078] The glass transition temperature of PVPK-30 was determined to be 175°C by DSC. Attempts were made to first liquefy PVPK-30 by heating to about 175°C and above, and observation of samples by optical microscopy demonstrated that it did not liquefy even when heated up to 240°C. Additionally, the polymer changed from white to orange / brown, indicating degradation.

[0079] The glass transition temp...

Embodiment 2

[0090] Solid dispersions were prepared from melt extrudates containing 30% TKA731 and PVPK-30 (ISP Technologies, Wayne, NJ), which additionally contained sorbitol at a concentration of 5% or 10% by weight (EM Industries, Darmstadt, Germany ) or without additional sorbitol (control). A single glass transition was shown by differential scanning calorimetry, suggesting that solid solutions formed by this method were similar to dispersions prepared by the solvent method.

[0091] The plasticizing effect of sorbitol (EM Industries, Darmstadt, Germany) on the drug / polymer mixture was shown by no degradation at a processing temperature of 170 °C (see Table 3)

[0092] table 3:

[0093] Amorphous drug

polymer content

Plasticizer Concentration

Processing temperature (℃) 2

X-ray analysis

HPLC analysis

Drug loading

(PVPK-30)

Tg=175℃

(sorbitol)

20％

70％

10％ 1

170

amorphous

no degradati...

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Abstract

The present invention provides processes for making and forms of solid dispersions of pharmaceutical active ingredients.

Description

technical field [0001] The present invention provides methods and forms for the preparation of solid dispersions of pharmaceutically active ingredients. Background technique [0002] Substances selected for drug development based on their in vitro pharmaceutical activity include active substances that may have solubility or dissolution issues in aqueous media and in vivo. Drug discovery The solubility of a compound in aqueous media often determines whether the compound will ultimately be useful as a drug. Relatively insoluble compounds exhibiting promising pharmaceutical activity, such as those with a solubility in water of less than 200 μg / ml, such as 100 μg / ml, pose a great challenge to the development of pharmaceuticals, especially oral dosage forms. [0003] Several factors can lead to insufficient dissolution of a pharmaceutically active substance including, for example, hydrophobic functional groups on the outside of the active substance molecule, the non-ionizable na...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/20
CPCA61K9/145A61K9/1635A61K9/2095A61K9/1694A61K9/146A61K9/2027A61K9/2018A61P3/06A61P9/00A61P25/02A61P37/06A61P43/00
Inventor R·A·阿布什梅茨-齐亚德赫J·科瓦尔斯基S·L·克里尔L·J·帕蒂尔本Z·王
Owner NOVARTIS AG
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