Mzi. Khan, RECENT TRENDS AND PROGRESS IN SUSTAINED OR CONTROLLED ORAL DELIVERY OF SOME WATER-SOLUBLE DRUGS - MORPHINE SALTS, DILTIAZEM AND CAPTOPRIL, Drug development and industrial pharmacy, 21(9), 1995, pp. 1037-1070
The development of oral controlled release systems has been a challeng
e to formulation scientists due to their inability to restrain and loc
alise the system at targeted areas of the gastrointestinal (GI) tract.
Controlled/sustained release preparations using alternative routes ha
ve been formulated but the oral route still remains the most desirable
. For obvious reason, water soluble drugs are more difficult to delive
r orally in sustained or controlled release manner than lipophilic dru
gs. Attempts have been made to regulate the release process by incorpo
rating hydrophobic fillers within the system or by coating the drug wi
th poorly soluble, swollen or non-swollen polymers or other substances
. Others used the so called 'hydrodynamically balanced systems' which
float in the gastric fluid at the stomach thereby increase the residen
ce time for the device in the GI tract. A new approach has been the us
e of mucoadhesive systems to increase the residence time of the device
within the GI tract. This review focuses on the progress made in the
design of controlled/sustained release delivery systems for some water
soluble drugs. Highly/freely water soluble diltiazem, captopril and m
orphine salts have been selected as model drugs due to the leading rol
e they play in their respective field of therapy and their widespread
use in treating chronic patients. Particular emphasis is given to deli
very systems designed to achieve their once a day dose treatment.