Controlled entry of orally administereddrugs: physiological considerations

Hofmann, Alan F.; Pressman, Jeffrey; Code, Charles F.; Witztum, Kathryn F.

doi:10.3109/03639048309046314

Cited by 48 publications

(18 citation statements)

References 56 publications

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“…The bulk density and tapped density for all formulations was found in the range of 0.283333±0.005774 to 0.53±0.01 g/cm 3 and 0.323333±0.015275 to 0.683333±0.005774 g/cm 3 . …”

Section: Bulk Density and Tapped Densitymentioning

confidence: 90%

“…[1] However the oral route of administration that be suffers mutually unquestionable limitations one as short residence time of the dosage comprise in the gastrointestinal tract, unpredictable gastric emptying, degradation of the drug what is coming to one to intensively reactive nature of gastrointestinal contents and existence of an absorption window in the gastric and upper small intestine for several drugs. [2], [3] Several approaches are currently used to retain the dosage in the stomach. These boost bioadhesive system [8] , swelling and expanding systems [11], [12] , floating systems [5], [6] and other delayed gastric emptying devices.…”

Section: Introductionmentioning

confidence: 99%

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FORMULATION & IN VITRO EVALUATION OF GASTRORETENTIVE FLOATING DRUG DELIVERY SYSTEM OF MEBHYDROLIN NAPADISYLATE

Hossain¹

2017

WJPR

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Gastro retentive drug delivery systems (GRDDS) are the systems which are retained in the stomach for a longer period of time and thereby, improve the bioavailability of drugs. The objective of this study was to formulate gastro retentive floating matrix tablet of Mebhydrolin Napadisylate using different ratios of HPMC K4M & HPMC K100LV. The sodium bi carbonate and citric acid was used in combination as gas generating agent. The tablets were prepared by wet granulation method and evaluated for the pre and post compression parameters such as angle of repose, tapped density, bulk density, Carr's Index, Hausner's ratio, hardness, friability, weight variation, thickness, swelling index, In vitro buoyancy studies and In vitro drug release studies. The tablets containing Mebhydrolin Napadisylate released 61.6 to 87.6% of drug at the end of 10 hrs by In vitro release study. Formulation F3 containing HPMC K4M and HPMC K100LV at a ratio of 1:1 found to be the best formulation in terms of drug release and In vitro buoyancy time. The drug release followed the Higuchi model controlled mechanism of tablet Mebhydrolin Napadisylate. FTIR spectrums obtained suggest that there was no significant chemical interaction between the polymers and drug.

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“…The bulk density and tapped density for all formulations was found in the range of 0.283333±0.005774 to 0.53±0.01 g/cm 3 and 0.323333±0.015275 to 0.683333±0.005774 g/cm 3 . …”

Section: Bulk Density and Tapped Densitymentioning

confidence: 90%

Section: Introductionmentioning

confidence: 99%

FORMULATION & IN VITRO EVALUATION OF GASTRORETENTIVE FLOATING DRUG DELIVERY SYSTEM OF MEBHYDROLIN NAPADISYLATE

Hossain¹

2017

WJPR

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“…Oral controlled-release formulations are usually designed to limit gastric acid destruction and deliver drugs to the more distal portions of the gastrointestinal tract to enhance bioavailability. 11 To achieve delivery of chloroquine to these regions, we envisaged entrapping the drug in pectin hydrogel beads. Pectin (polygalacturonic acid) has been previously used for specific delivery to the colon.…”

Section: Introductionmentioning

confidence: 99%

An Investigation into the Suitability of Amidated Pectin Hydrogel Beads as a Delivery Matrix for Chloroquine

Munjeri

Hodza

Osim

et al. 1998

Journal of Pharmaceutical Sciences

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The aim of the present study was to delay the release of chloroquine to distal parts of the gastrointestinal tract by using a multiparticulate hydrogel formulation. Amidated pectin chloroquine beads (PC) with varying pectin-to-chloroquine ratios (PC) w/w loadings of 4:1, 2:1, and 1:1 in the dried beads were prepared by the gelation of drug-loaded pectin solutions in the presence of calcium. In vitro release studies of chloroquine from pectin-chloroquine hydrogel beads and chloroquine diphosphate powder were carried out in simulated gastric and intestinal fluids. The total release of the entrapped chloroquine from the hydrogel beads was achieved between 4 and 7 h in simulated intestinal fluid, but total release was not achieved in simulated gastric fluid. However, total release from chloroquine diphosphate powder was achieved by 1.5 and 2 h in gastric and intestinal fluids, respectively. The plasma pharmacokinetics of chloroquine from pectin hydrogel beads and chloroquine diphosphate solution following single or repeated dosing were compared in male Sprague-Dawley rats over a period of 60 h. Oral administration of the hyrogel beads to rats produced maximum plasma concentrations by 7 h, but highest plasma concentrations following chloroquine solution administration were observed by 2 h. The dissolution data and appearance of significant plasma concentrations of chloroquine 2 to 4 h after oral administration suggests release in duodenum, jejunum, or ileum.

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“…Two theories have been postulated to explain the retention of particles on the stomach mucosa. First, large indigestible solids such as a capsule may be cleared from the stomach to the small intestine by the migrating myoelectric complex (MMC) (25). The capsule was retained in the stomach until it was emptied by waves of MMC, but MMC may not be strong enough to move the whole capsule to the small intestine.…”

Section: In Vivo Studiesmentioning

confidence: 99%

The Impact of Vehicles on the Mucoadhesive Properties of Orally Administrated Nanoparticles: a Case Study with Chitosan-4-Thiobutylamidine Conjugate

et al. 2010

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Abstract. The aim of this study was to evaluate the impact of various vehicles on mucoadhesive properties of thiolated chitosan nanoparticles both in vitro and in vivo. Nanoparticles (NPs) were prepared by in situ gelation technique followed by labeling with fluorescein diacetate. Comparative studies on mucoadhesion were done with these thiolated chitosan NPs and unmodified chitosan NPs (control). The obtained nanoparticles displayed a mean diameter of 164.2±6.9 nm and a zeta potential of 21.5±5 mV. In an in vitro adhesion study, unhydrated thiolated NPs adhered strongly to freshly excised porcine small intestine, which was more than threefold increase compared to the control. In contrast, in the presence of various vehicles (PEG 300, miglyol 840, PEG 6000, cremophor EL, and caprylic triglyceride), the mucoadhesive properties of thiolated NPs were comparatively weak. Thiolated NPs suspended in caprylic triglyceride, for example, had a percent mucoadhesion of 22.50±5.35% on the mucosa. Furthermore, results from in vivo mucoadhesion studies revealed that the dry form of nanoparticles exhibits the strongest mucoadhesion, followed by nanoparticles suspended in PEG 300, miglyol, and 100 mM phosphate buffer, in that order. Three hours after administration, the gastrointestinal residence time of the dry form of thiolated NPs was up to 3.6-fold prolonged. These findings should contribute to the design of highly effective oral mucoadhesive nanoparticulate drug delivery systems.

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Controlled entry of orally administereddrugs: physiological considerations

Cited by 48 publications

References 56 publications

FORMULATION & IN VITRO EVALUATION OF GASTRORETENTIVE FLOATING DRUG DELIVERY SYSTEM OF MEBHYDROLIN NAPADISYLATE

FORMULATION & IN VITRO EVALUATION OF GASTRORETENTIVE FLOATING DRUG DELIVERY SYSTEM OF MEBHYDROLIN NAPADISYLATE

An Investigation into the Suitability of Amidated Pectin Hydrogel Beads as a Delivery Matrix for Chloroquine

The Impact of Vehicles on the Mucoadhesive Properties of Orally Administrated Nanoparticles: a Case Study with Chitosan-4-Thiobutylamidine Conjugate

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