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Merck

Gastro retention using polymer cocoons.

Artificial cells, nanomedicine, and biotechnology (2014-08-01)
Julien Arnold, David Hunkeler
ABSTRACT

A gastro-retentive capsule has been prepared which is retained in the stomach for a period of 24h, providing a vehicle for the controlled delivery to the upper intestines. These "gastro cocoons" can resist passage through the sphincter of the stomach, and can retain a high drug payload (30%). They are made from oppositely charged polyelectrolytes and can swell to twice their initial volume. They are strong and also can resist 550 N of compressive force. They are based on filled pharmaceutical capsules which are visible to X-rays. Using ambroxol hydrochloride as a model drug linear, zero-order, release curves were obtained.

MATERIALS
Product Number
Brand
Product Description

Ambroxol hydrochloride, European Pharmacopoeia (EP) Reference Standard
Supelco
Ambroxol hydrochloride, analytical standard
Sigma-Aldrich
Acetone, ACS reagent, ≥99.5%
Sigma-Aldrich
Hydrochloric acid, ACS reagent, 37%
Supelco
Acetone, analytical standard
Supelco
Hydrochloric acid solution, volumetric, 0.1 M HCl (0.1N), endotoxin free
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Hydrochloric acid, 36.5-38.0%, BioReagent, for molecular biology
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Acetone, suitable for HPLC, ≥99.9%
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Acetone, ≥99%, meets FCC analytical specifications
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Hydrochloric acid solution, 32 wt. % in H2O, FCC
USP
Acetone, United States Pharmacopeia (USP) Reference Standard
Supelco
Acetone, Pharmaceutical Secondary Standard; Certified Reference Material
Sigma-Aldrich
Acetone, suitable for HPLC, ≥99.8%
Sigma-Aldrich
Acetone, suitable for HPLC, ≥99.9%
Sigma-Aldrich
Acetone, HPLC Plus, for HPLC, GC, and residue analysis, ≥99.9%