Investigation of a Novel “Tablets in Capsule” Theophylline Formulation System for Modified Release

Abstract

In pharmaceutical research, new dosage forms that modify drug release are useful for circadian rhythm related diseases. The aim of this investigation is to examine the release behavior of multiple-unit modified-release formulations ('tablets in capsule') of theophylline. Mono-layered and three-layered minitablets, filled into capsules, were prepared using theophylline and dextran or pectin, as excipients. Their release behavior was compared with respect to powder filled capsules and the commercially available Theodur® 200 mg tablets. Dissolution tests were performed in three pH media (1.5, 7.4 and 6.0) in the presence and absence of the enzyme Pectinex® Ultra SP-L solution, which degrades polysaccharides. The results indicate that enteric-coated capsules showed no drug release, in the first two hours in the acidic media. Dextran produces a thicker gelled layer than pectin and therefore, dextran based 'tablets in capsules' systems are suitable as a model extended release formulation. The drug is released from 3-layered minitablets at a slower rate compared to matrix minitablets. The product, Pectinex® Ultra SP-L, was found to give more accurate dissolution results when used as an additive to the media, mimicking the large intestine/colon area especially when the formulations target this region.

A developed composite hard-gelatin capsules: delayed-release enteric properties

“…with acetaminophen as a medicinally active ingredient. The test procedure is immersing the capsules in the artificial stomach and intestines environments [ 16 , 17 ]. The use of these capsules creates a stable release rate from the stomach through the small intestine, and causes better drug performance and a higher release rate in the intestine.…”

New Dosage Forms for the Delayed Release of Mesalazine to the Colon

“…As already mentioned, the objective of the present work is to formulate new delivery systems of 5-ASA for colon targeted release based on the combination of time and bacterial degradation approaches, Many researchers have previously used enzymatic dispersions in dissolution tests in various concentrations; 86600PG/l [25], 44200PG/l [26], 61800PG/l [27,28], 45600 PG/l [29]. using capsules filled with tablets.…”

Modified release of furosemide from Eudragits® and poly(ethylene oxide)-based matrices and dry-coated tablets

“…We have previously reported on the development of modified release formulations containing active substances of diverse chemical structures and physicochemical properties (15)(16)(17)(18)(19)(20)(21). Aiming at optimal delivery of furosemide, in order to provide more effective therapy, devoid of high peak natriuretic and diuretic adverse effects, its modified release profile from matrix and compression coated tablets is presented herein.…”