Enhancement of Drugs Bioavailability by Floating Drug Delivery System – A Review

Gastric emptying is a complex process and one of the most important obstacles in the better absorption and enhances bioavailability of oral drug delivery system. In recent years various scientific and technological advancements have been made in the research and development of oral drug delivery systems to overcoming physiological adversities, such as short gastric residence times (GRT) and unpredictable gastric emptying time (GET). In order to avoid such adversities, efforts have been made to increase the retention time of the drug-delivery systems for more than 12 hour via floating drug delivery system. Floating delivery systems or hydro dynamically controlled systems are low density systems that have sufficient buoyancy to float over the gastric content and remain buoyant in the stomach. The recent development of these systems includes their physiological and formulation variables affecting the gastric retention and to design the single and multiple-unit floating systems and their formulation, evaluation aspects are covered in detail. This article aims at reviewing the numerous techniques that has been designed till date for optimizing floating drug delivery system (FDDS), and also summarize the evaluation of FDDS of tablet dosage forms

Buccal Drug Delivery: Past, Present and Future – A Review

The major hindrance for the absorption of a drug taken orally is extensive first pass metabolism or stability problems within the GI environment like instability in gastric pH and complexation with mucosal membrane. These obstacles can be overcome by altering the route of administration as parenteral, transdermal or trasmucosal. Among these trasmucosal has the advantage of ease of administration, patient compliance and are economic too. The mucosa of the buccal cavity is the most easily accessible transmuocosal site. Buccal transmucosal delivery helps to bypass first- pass metabolism by allowing direct access to the systemic circulation through the internal jugular vein. The buccal transmucosal route has been researched for a wide variety of drugs. Several methodologies have been considered so far, to design and manipulate the release properties towards the invention of buccal mucosal delivery systems. This article aims at reviewing the numerous techniques that has been designed till date for optimizing buccal transmucosal drug delivery.Keywords: complexation; parenteral; transdermal; trasmucosa

2-(2-Hydroxyphenyl)-4,5-dimethyl-1H-imidazol-3-ium acetate monohydrate

In the title compound, C11H13N2O+·C2H3O2 −·H2O, the dihedral angle between the benzene ring and the imidazole ring is 7.83 (6)°. In the crystal structure, N—H⋯O and O—H⋯O hydrogen bonds form a two-dimensional network. All the methyl H atoms are disorderd over two sites with equal occupancies

Enhancement of Drugs Bioavailability by Floating Drug Delivery System – A Review

Gastric emptying is a complex process and one of the most important obstacles in the better absorption and enhances bioavailability of oral drug delivery system. In recent years various scientific and technological advancements have been made in the research and development of oral drug delivery systems to overcoming physiological adversities, such as short gastric residence times (GRT) and unpredictable gastric emptying time (GET). In order to avoid such adversities, efforts have been made to increase the retention time of the drug-delivery systems for more than 12 hour via floating drug delivery system. Floating delivery systems or hydro dynamically controlled systems are low density systems that have sufficient buoyancy to float over the gastric content and remain buoyant in the stomach. The recent development of these systems includes their physiological and formulation variables affecting the gastric retention and to design the single and multiple-unit floating systems and their formulation, evaluation aspects are covered in detail. This article aims at reviewing the numerous techniques that has been designed till date for optimizing floating drug delivery system (FDDS), and also summarize the evaluation of FDDS of tablet dosage forms

Labeling of alprenolol with fluorescent aryl iodide as a reagent based on Mizoroki-Heck coupling reaction.

A novel fluorescent labeling method for alprenolol was developed based on Mizoroki-Heck coupling reaction. We designed and synthesized fluorescent aryl iodide, 4-(4,5-diphenyl-1H-imidazol-2-yl)iodobenzene (DIBI) as a labeling reagent. DIBI has a lophine skeleton carrying an iodide atom acting as fluorophore and reactive center, respectively. In order to evaluate the usefulness of DIBI, a high-performance liquid chromatography (HPLC) with fluorescence detection method was developed for the determination of alprenolol as a model compound of terminal double bond. The fluorescent labeling of alprenolol with DIBI was achieved in the presence of palladium acetate as a catalyst, and the labeled alprenolol was detected fluorometrically. In addition, it was found that the fluorescence of DIBI derivative increased and red shifted when compared with that of DIBI. Furthermore, the proposed method could be applied to determine the alprenolol concentration in rat plasma after administration of alprenolol without interferences from biological components. The detection limit (S/N=3) for alprenolol in rat plasma was 0.74 ng/mL (30 fmol on column)

Razvoj i karakterizacija mukoadhezivnih flastera salbutamol sulfata za jednosmjernu bukalnu isporuku

Buccal patches of salbutamol sulfate were prepared using five different water soluble polymers in various proportions and combinations using PEG-400/PG as plasticizers. A 32 full factorial design was used to design the experiments for each polymer combination. Patches were laminated on one side with a water impermeable backing layer for unidirectional drug release. The thickness of medicated patches ranged between 0.2 and 0.4 mm and showed an increase in mass whenever PEG-400 was used as plasticizer. The surface pH of all patches approached neutral. Eight formulations which had shown high folding endurance (> 300) were selected for evaluation. Patches prepared with PEG-400 showed a high swelling index. The residence time of the tested patches ranged between 105 and 130 min. Formulations A10, A32, B10 and B32 fitted the Higuchi model best, whereas formulations A19 and B19 showed super case II transport drug release. Stability studies indicated that there was no change in the chemical and physical characteristics during the test period of 6 months.U radu je opisana priprava flastera za bukalnu primjenu upotrebom različitih omjera pet vodotopljivih polimera i PEG-400/PG kao plastifikatora. Potpuni 32 faktorijalni dizajn upotrebljen je za dizajniranje eksperimenata za svaku kombinaciju polimera. Flasteri su postavljeni na jednu stranu usta s vodonepropusnom podlogom, koja omogućava jednosmjerno oslobađanje lijeka. Debljina flastera varirala je između 0,2 i 0,4 nm. Flasteri s PEG-400 bili su malo veće mase. pH na površini svih flastera bio je blizu neutralnog. Osam pripravaka vrlo otpornih na presavijanje (300) izabrano je za daljnju evaluaciju. Flasteri pripravljeni s PEG 400 imali su veliku sposobnost bubrenja. Flasteri su se zadržali na mjestu primjene između 105 i 130 min. Pripravci A10, A32, B10 i B32 najbolje su slijedili Higuchijev model, dok su pripravci A19 i B19 pokazivali anomalno oslobađanje koje ne slijedi Fickov zakon. Ispitivanje stabilnosti pokazalo je da ne postoje promjene u kemijskim i fizikalnim svojstvima pripravaka tijekom 6 mjeseci