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LOW VISCOSITY HPMC WITH IMPROVED EXTRUSION PERFORMANCE

IP.com Disclosure Number: IPCOM000249777D
Publication Date: 2017-Apr-03
Document File: 1 page(s) / 101K

Publishing Venue

The IP.com Prior Art Database

Abstract

Highly substituted hydroxypropyl methylcelluloses (HPMCs) which have a DS(methoxyl) of 1.0 - 2.7 and an MS(hydroxypropoxyl) of 0.4 - 1.3 can be extruded at a broad processing window of 90 - 190°C. The HPMC can be blended with a drug before extrusion. The blend can be extruded to produce a solid dispersion of the drug in HPMC to improve the bioavailability of the drug.

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LOW VISCOSITY HPMC WITH IMPROVED EXTRUSION PERFORMANCE

Highly substituted hydroxypropyl methylcelluloses (HPMCs) which have a

DS(methoxyl) of 1.0 - 2.7 and an MS(hydroxypropoxyl) of 0.4 - 1.3 can be extruded at a

broad processing window of 90 - 190°C. The HPMC can be blended with a drug before

extrusion. The blend can be extruded to produce a solid dispersion of the drug in HPMC to

improve the bioavailability of the drug.

The viscosity of the HPMC can be 2.4 to 200,000 mPas, measured as a 2 weight-%

solution in water at 20 °C. When a low viscosity HPMC is used for extrusion, e.g. a HPMC of

a viscosity of 2.4 to 200 mPas, partial depolymerization of a HPMC of higher viscosity is

conducted. Partial depolymerization processes are known, e.g. by treatment with gaseous

HCl. When the partially depolymerized HPMC is thoroughly washed after HCl treatment, the

subsequent extrusion is facilitated.

Example

HPMC was partially depolymerized with gaseous HCl. The partially depolymerized

HPMC having a DS(methoxyl) of 2.22, an MS(hydroxypropoxyl) of 1.21 and a viscosity of

44 mPas, measured as a 2 weight-% solution in water at 20 °C, was added to 1.7 L of boiling

water and treated with high-shear (Ultra-Turrax, 5000 rpm) for 45 sec. Afterwards the wet

cake was separated with a warm (pre-heated at 55°C) G1 frit. This step was 3x repeated until

no chloride ions were detectable. Then the material was dried at 40°C overnight.

A capillary rheometer (Malvern RH10, Malvern Instruments) ha...