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

Formulation and Evaluation of Bioadhesive Buccal Drug Delivery of Tizanidine Hydrochloride Tablets

The study aim was concerned with formulation and evaluation of bioadhesive buccal drug delivery of tizanidine hydrochloride tablets, which is extensively metabolized by liver. The tablets were prepared by direct compression using bioadhesive polymers such as hydroxylpropyl methylcellulose K4M, sodium carboxymethyl cellulose alone, and a combination of these two polymers. In order to improve the permeation of drug, different permeation enhancers like beta-cyclodextrin (β-CD), hydroxylpropyl beta-cyclodextrin (HP-β-CD), and sodium deoxycholate (SDC) were added to the formulations. The β-CD and HP-β-CD were taken in 1:1 molar ratio to drug in formulations. Bioadhesion strength, ex vivo residence time, swelling, and in vitro dissolution studies and ex vivo permeation studies were performed. In vitro release of optimized bioadhesive buccal tablet was found to be non-Fickian. SDC was taken in 1%, 2%, and 3% w/w of the total tablet weight. Stability studies in natural saliva indicated that optimized formulation has good stability in human saliva. In vivo mucoadhesive behavior of optimized formulation was performed in five healthy male human volunteers and subjective parameters were evaluated