Post Marketing Bioequivalence Study of Six Brands of Ciprofloxacin HCL in Egyptian Market and Evaluation as a Treatment of Human Periodontal Pockets

The availability of numerous brands of ciprofloxacin HCl in our drug market today places clinicians and pharmacists in a difficult situation of choice of a suitable brand or the possibility of alternative use. The aim of the present study was to evaluate physical standards of six brands of ciprofloxacin HCl tablets marketed in Egypt using in-vitro tests and then in vivo bioequivalence of best two brands of ciprofloxacin HCL, finally their evaluation in treatment of human periodontal pockets. The in-vitro dissolution study was carried out on six brands of ciprofloxacin HCl tablets using basket method according to US pharmacopoeia guidelines. Other general quality assessment tests like Weight variation, hardness, friability, drug content uniformity y and disintegration were also determined. Then brands of ciprofloxacin HCl were subjected to in-vivo efficacy studies in treatment of human periodontal pockets. Significant results were obtained with respect to both microbiological and clinical parameters. For evaluation of bioequivalence of best two brands of ciprofloxacin HCl, blood samples were taken, plasma concentration of ciprofloxacin HCl brands were determined by simple HPLC method. The pharmacokinetic parameters, Including peak plasma concentrations and time needed to reach the peak were obtained directly from plasma concentration–time profiles. The area under the curve was calculated using noncompartmental methods. Statistical analysis of in-vitro and in-vivo studies shows that ciprofloxacin brands are effective in treating periodontal pockets in order of ciprobay, cipromax, mifoxin, ciprocin, rancif and ciprofar. Statistical analysis of main parameters confirm the bioequivalence of the ciprofloxacin formulations in terms of pharmacokinetic characteristic, the results from this study demonstrate that Ciprobay and Cipromax are interchangeable in the clinical setting. Keywords: Bioequivalence, ciprofloxacin, periodontal pocket, Dissolutio

Proniosomes as Nano-Carrier for Transdermal Delivery of Atenolol Niosomal Gel

Available online on www.ijddt.com International Journal of Drug Delivery Technology 2017; 7(4); 283-297Objective of the study is to prepare Proniosomes that refers to a flexible vesicular carrier with the potential for drug administration through the transdermal route. Medthod: Proniosomes were prepared by the coacevation-phase separation technique The prepared formulations were evaluated for vesicle size, entrapment efficiency. The optimal poniosomes formula (A8) was prepared with different aqueous phase, incorporated in a gel base and studied for pH, viscosity, spredapility, stability, in vitro drug release and ex vivo permeation. Results: Niosomes formulations prepared with Span 40 and 60 have spherical and smaller Nano size. 25 mg atenolol loading has resulted 190.9 ± 15.033 nm sizes. EE% of the optimum formula prepared with distilled water was 62.11 to 92.38 .Rheological behavior showed combined shear thinning and thixotropic and gel was spreadable . Tested formulations were stable on cooling (4-8 oC) . In vitro drug release followed zero order kinetic, and gave sustained release. Release rate was significantly higher across cellulose membrane compared with rate skin. Amount of drug obtained after skin extraction was 92.6 ± 0.5% indicate enhanced permeation rate. Conclusion: All the proniosomal gel formulations were found through the acceptable range of vascular size and entrapment efficiency. Formulation A8 has been selected as an optimized therapeutic system of atenolol

Olmesartan Medoxomil-Loaded Self-Nanoemulsifying Drug Delivery Systems: Design, In-Vitro Characterization, and Pharmacokinetic Assessments in Rabbits Via LC-MS/MS

Olmesartan medoxomil (OLM) is a lipophilic (log P = 4.31) antihypertensive drug suffering from limited oral bioavailability in humans (26%) due to its low aqueous solubility, uncontrolled enzymatic conversion to the active metabolite (olmesartan; OL) and efflux by drug resistance pumps. Surmounting such limitations via incorporation of OLM into self-nanoemulsifying drug delivery systems (SNEDDS). Based on OLM-equilibrium solubility studies in various oils, surfactants and co-surfactants, Capmul® MCM, Tween® 20, Cremophor® EL and polyethylene glycol-400 (PEG) were combined in different ratios to plot ternary phase diagrams. OLM-loaded SENDDS were developed and evaluated for particle size, polydispersity index (PDI), zeta potential, self-emulsification time, morphology, drug released percentages after 5-min (Q5min%), 1-hour (Q1h%) and dissolution efficiency percentages (DE1h%). The OL pharmacokinetics from SNEDDS (F6) and Benicar® tablets were evaluated (LC-MS/MS) in rabbits. Spherical OLM-loaded SNEDDS were developed. The best-achieved SNEDDS (F6) showed short emulsification time (13 s), fine droplet size (60.00 nm), low PDI (0.25), negative zeta potential (-14.4 mV), promising dissolution parameters; Q5min% (29.78%), Q1h% (66.69%) and DE1h%(47.96%) and enhanced in vivo absorption characteristics; shorter Tmax, higher Cmax and larger AUC(0−48h; suggesting its potential for the enhancement of the oral absorption of practically insoluble drugs; like OLM

Preparation and Evaluation of Certain Hydrophilic Drug- Loaded Microspheres

Microencapsulation is a useful method for prolonging drug release from dosage forms and reducing adverse effects. Recently, dosage forms that can precisely control the release rates and target drugs to a specific body site have made an enormous impact in the formulation and development of novel drug delivery systems. Microspheres are defined as spherical polymeric particles. These microspheres constitute an important part of these drug delivery systems, by the virtue of their small and uniform size and efficient carrier characteristics. It would, therefore, be advantageous to have means for providing an intimate contact of the drug delivery system with the absorbing membranes. This preliminary study shows that optimum polymer concentration, crosslinker concentration and stirring speed are 3%, 7.5% and 400 rpm respectively, the optimum conditions to prepare microspheres by ionotropic gelation with high drug entrapment efficiency are: drug concentration 1.5% w/v, curing time 15 minutes and the concentration of another poly anionic polymer (sodium carboxymethyl cellulose) 0.3% w/v. In phosphate buffer (pH 7.4) the rapid swelling and erosion of the microspheres have greatly contributed in facilitating the drug release rate. Different mathematical models of drug release were obtained for the microspheres indicating that the drug release from the microspheres is controlled by first order kinetics