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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

Supelco
Ambroxol hydrochloride, analytical standard
Ambroxol hydrochloride, European Pharmacopoeia (EP) Reference Standard
Supelco
Chloromethane solution, 200 μg/mL in methanol, analytical standard
Sigma-Aldrich
Hydrochloric acid, ACS reagent, 37%
Sigma-Aldrich
Acetone, histological grade, ≥99.5%
Sigma-Aldrich
Acetone, puriss. p.a., ACS reagent, reag. ISO, reag. Ph. Eur., ≥99.5% (GC)
USP
Acetone, United States Pharmacopeia (USP) Reference Standard
Sigma-Aldrich
Acetone, Laboratory Reagent, ≥99.5%
Sigma-Aldrich
Acetone, suitable for HPLC, ≥99.8%
Sigma-Aldrich
Acetone, ACS reagent, ≥99.5%
Sigma-Aldrich
Hydrogen chloride solution, 1.0 M in acetic acid
Sigma-Aldrich
Hydrogen chloride solution, 1.0 M in diethyl ether
Sigma-Aldrich
Acetone, puriss., meets analytical specification of Ph. Eur., BP, NF, ≥99% (GC)