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

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

TOXICITY RISK ASSESSMENT OF SOME NOVEL QUINOXALINES

ABSTRACT Ten novel quinoxalines were synthesised and evaluated for antitubercular activities. They showed excellent antitubercular activities. In continuation of our research we then predicited the toxicity parameters like mutagenicity, tumerogenicity, skin irritancy, reproductive effects and teratogenicity. They were predicted using software programmes Osiris and insilicofirst. All the ten compounds were predicted as non toxic against these evaluated toxicities. So they are found to be safe. Some of the important physicochemical parameters like Clog P, Molecular weight, Drug likeness were also predicted

Crystal structure of 4-amino-1-(4-methylbenzyl)pyridinium bromide

The title molecular salt, C13H15N2+·Br−, crystallized with two independent ion pairs (A and B) in the asymmetric unit. In the cations, the planes of the pyridine and benzene rings are inclined to one another by 79.32 (8) and 82.30 (10)° in ion pairs A and B, respectively. In the crystal, the anions and cations are connected by N—H...Br hydrogen bonds, forming a centrosymmetric tetramer-like unit enclosing an R84(16) ring motif. These units are linked via C—H...Br hydrogen bonds, forming a three-dimensional network

2-(2-Methylphenyl)-4,5-diphenyl-1H-imidazole

In the title molecule, $C_{22}H_{18}N{2}$, all bond lengths and angles are normal. Intermolecular N—H...N hydrogen bonds with an N...N distance of $2.933(2)A{^o}$, link the molecules into chains running along the c axis. Thecrystal packing is further stabilized by van der Waals forces