Sadašnjost i budućnost stentova za restenozu koji otpuštaju lijekove

Drug-eluting stents (DESs) prevail in the treatment of carotid artery diseases in the interventional cardiology world owing to their efficacy for significant reduction of restenosis. A current successful DES requires a polymer coating for drug delivery. Clinical trials examining several pharmaceutical agents have demonstrated marked reduction in restenosis following stenting. The development of DES is one of the major revolutions in the field of interventional cardiology. The ideal drug to prevent restenosis must have an anti-proliferative and anti-migratory effect on smooth muscle cells but, on the other hand, it must also enhance re-endothelialization in order to prevent late thrombosis. Additionally, it should effectively inhibit the anti-inflammatory response after balloon induced arterial injury. Although DES have significantly reduced the angiographic restenosis rate and have improved clinical outcomes, late thrombosis and restenosis remain an important subject of ongoing research.Stentovi koji otpuštaju lijekove (DESs) koriste se u kardiologiji za terapiju bolesti karotidnih arterija jer značajno smanjuju restenozu. Dobar DES ima polimerni sloj za isporuku lijekova. Klinički pokusi u kojima je ispitivano nekoliko agenasa pokazali su značajno smanjenje restenoze nakon ugradnje stenta. Razvoj DES-a jedno je od revolucionarnih otkrića u području interventne kardiologije. Idealni lijek za prevenciju restenoze mora imati antiproliferativni i antimigracijski učinak na stanice glatkih mišića, a s druge strane mora povećavati endotelizaciju kako bi se spriječila tromboza. Osim toga, treba učinkovito inhibirati protuupalni odgovor nakon ozljede arterije. Iako DES značajno smanjuje restenozu krvnih žila, kasna tromboza i restenoza ostaju i dalje problem i predmet brojnih istraživanja

ArticleEvaluation of Some Methods forPreparing Glipizide-β-Cyclodextrin Inclusion Complexes: Preparing glipizide-β-cyclodextrin inclusion complexes

Glipizide has been found to form inclusion complexes with β-cyclodextrin (β-CD) in solution and in solid state. The present study was undertaken to determine a suitable method for scaling up glipizide-β-CD inclusion complex formation and to evaluate the effect of some parameters on the efficiency of complexation. The solid inclusion complexes of glipizide and β-CD were prepared at a molar ratio of 1:1 and 1:2 by mixing, kneading, and co-precipitation methods both on small and large scales. The effect of parameters such as kneading time and temperature on complexation was also studied. Characterization was performed using infrared spectroscopy, X-ray diffractometry, and dissolution studies. In vitrorelease studies were carried out in phosphate buffer (pH 7.4). All the methods of preparation of complexes were found to be useful in increasing the solubility of glipizide except mixing method where the rise in solubility was not significant. Both kneading and co-precipitation methods in 1:2 molar ratios were found to be equally effective inimproving the solubility of glipizide. The formation of inclusion complexes was evident in these formulations as shown by IR and XRD studies. But when carried out on a large scale, co-precipitation method was found to be more tedious and time-consuming than kneading method. Moreover percent recovery of complexes in the kneading method was found to be 98.76% as compared to 92.05% in case of co-precipitation method. Drug content studies, IR spectroscopic studies, X-ray diffractometry studies andin vitrodissolution study data indicated that inclusion complexes prepared by kneading method in 1:2 molar ratios were suitable for improving the solubility of glipizide. The same formulation was prepared at large scale and optimum formulation conditions were established

FORMULATION OF FUROSEMIDE SOLID DISPERSION WITH MICRO CRYSTALLINE CELLULOSE FOR ACHIEVE RAPID DISSOLUTION

Furosemide, a weekly acidic, loop diuretic drug indicated for treatment of edema and hypertension having high permeability through stomach. It is practically insoluble in gastric fluid (0.006 mg/ mL) and having highly permeability through stomach but due to its solubility limitation it can’t enter into systemic circulation. It was logically decided to design experiment, so as to achieve the set objectives. Attempt was made to prepare solid dispersion of furosemide with Poly ethylene glycol (PEG) 6000 containing microcrystalline cellulose (MCC) as adsorbent which would dissolve completely in less than 30 minutes (target selected by considering minimum gastric empting time). Microcrystalline cellulose converted sticky dispersion in to free flow powder hence increase surface area which responsible for dissolution improvement. Factorial design was applied to optimize formulation. Amount of poly ethylene glycol 6000 and microcrystalline cellulose were selected as an Independent variable while angle of repose and T100% were selected as dependent variable. Attempts for dissolution rate of furosemide improve bioavailability and consequently dose reduction would possible