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Oral pharmaceutical compositions in a solid dispersion comprising preferably posaconazole and HPMCAS

A solid composition, technology of posaconazole, applied in the field of oral pharmaceutical composition preferably containing posaconazole and HPMCAS in the form of solid dispersion, capable of solving problems such as hindering absorption

Inactive Publication Date: 2011-05-18
MERCK & CO INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, when posaconazole dissolved in gastric juice reaches the intestinal environment (usually acidic less than about pH 6.4), significant amounts of dissolved posaconazole precipitate, thereby hindering absorption in the intestine

Method used

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  • Oral pharmaceutical compositions in a solid dispersion comprising preferably posaconazole and HPMCAS
  • Oral pharmaceutical compositions in a solid dispersion comprising preferably posaconazole and HPMCAS
  • Oral pharmaceutical compositions in a solid dispersion comprising preferably posaconazole and HPMCAS

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0096] Example 1: Preparation of the extrusion composition of the present invention

Embodiment 1A

[0097] Example 1A - Extrusion Preparation at Small Pilot Plant Scale

[0098] By mixing 7.5 kg of HPMC-AS (M grade, Shin-Etsu AQOAT, as received from the manufacturer, with a particle size range of approximately 5 microns to 1 mm) and analyzed as Posaconazole free base-containing material in an amount corresponding to 2.5 kg of posaconazole free base (assay 25% active, total weight 10.0 kg of material, micronized, as received from the manufacturer, Schering-Plough corporation) Blended together, a blend of posaconazole free base and HPMC-AS polymer was prepared. The feeds are blended until a homogeneous blend is produced.

[0099] An aliquot of the blend prepared as above was passed through a Leistritz ZSE twin-screw extruder with a co-rotating screw 18 mm diameter, 450 mm long, until 10 kg of extrudate comprising the composition of the invention was produced . During the preparation of the extrudates, the blend was fed into the extruder through a KCL-KT20 gravity feeder e...

Embodiment 1B

[0102] Example 1B Extrusion Preparation of Large Pilot Plant Scale

[0103] By charging 15.0 kg of HPMC-AS (M grade, Shin-Etsu AQOAT, granulated, used as received) and posaconazole-containing amount analyzed to be equivalent to 5.0 kg of posaconazole free base in a drum blender From azole free base material (assay 25% active, total weight 20.0 kg micronized material, used as received from manufacturer), a blend of posaconazole free base and HPMC-AS polymer was prepared. The feeds are blended until a homogeneous blend is produced.

[0104] Extrudates were prepared from this blend using a Berstorff twin-screw extruder with a 25 mm diameter, 700 mm long co-rotating screw. The extruder was fed by a KCL-KT40 gravity feeder equipped with a 1:1 damper and twin paddle stirrer. The feeder was run at a speed sufficient to maintain an extrusion rate of 6.0 to 10.0 kg / hr at the exit of the extruder. The extruder screw was run at 140 RPM so that the residence time of the extruded mate...

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Abstract

The present application provides novel compositions comprising posaconazole and a polymer wherein the composition has a glass transition temperature temperature (Tg) of less than about 110 DEG C. The application also describes compositions comprising posaconazole and a polymer having a bulk density of greater than about 0.4 mg / mL. The application also describes compositions comprising posaconazole and a polymer which provide an exposure (AUCtf) of at least about 10,000 ng.hr / mL when administered to a patient in a fasted state. The application also describes a novel process for preparing these compositions.

Description

technical field [0001] The present application discloses novel solid compositions comprising posaconazole and pharmaceutical formulations comprising the same. Background technique [0002] Identification of any publication in this section or any part of this application is not an admission that such publication is prior art to the present invention. [0003] Posaconazole is an azole compound with antifungal properties. This compound and its synthesis are described, for example, in US Patent No. 5,703,079 (issued December 30, 1997) and related patent 5,661,151 (issued August 26, 1997), both to Saksena et al. A stable crystalline form of posaconazole and methods of preparing the crystalline form are described in US Patent No. 6,958,337 issued October 25, 2005 to Andrews et al. Pharmaceutical formulations comprising suspensions of this crystalline form (commercially available as Noxafil®) and their Preparation. [0004] Suspensions containing posaconazole in crystalline for...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/00
CPCA61K9/1652A61K31/496A61P31/10A61P7/00A61P3/10A61K9/14A61K47/38
Inventor L.Y.方D.哈里斯G.克里什娜A.E.小莫顿R.C.普雷斯蒂皮诺M.施泰因曼J.万H.A.瓦斯金
Owner MERCK & CO INC
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