Formulation and Comparative Bioavailability of 2 Ciprofloxacin Sustained Release Tablets

Abstract

The aim of this study is to formulate and evaluate the quality of ciprofloxacin (CAS number: 85721-33-1) sustained release tablet (Ciprocare®XR) 1 000 mg ciprofloxacin (test formulation) by comparing its pharmacokinetic parameters with Cipro®XR sustained release tablet (reference formulation). For this purpose ciprofloxacin SR tablets were developed using the 2-layer method. To assess the quality of the produced sustained release tablets a randomized, 2-way, crossover, bioequivalence study was performed in 24 healthy, male volunteers. The selected Middle Eastern volunteers were divided into 2 groups of 12 subjects. One group was treated with the reference formulation and the other one with the test formulation, with a cross-over after a drug washout period of 7 days. Blood samples were collected at fixed time intervals and Ciprofloxacin concentrations were determined by a validated HPLC assay method. The pharmacokinetic parameters AUC0-48, AUC0-∞, Cmax, Tmax, Ke and T1/2 were determined for both sustained release tablets and were compared statistically to evaluate the bioequivalence between the 2 formulations of ciprofloxacin, using the statistical model recommended by the FDA. The analysis of variance (ANOVA) did not show any significant difference between the 2 formulations and 90% confidence intervals (CI) fell within the acceptable range for bioequivalence. According to the obtained results it was concluded that the test and reference formulations are bioequivalent, since they exhibit comparable pharmacokinetic parameters.

Cellulose and Xylan Based Prodrug of Diclofenac Sodium: Synthesis, Physicochemical Characterization and In Vitro Release

“…Thus, the successful drug delivery to colon via GIT requires protection of a drug from being released in the stomach and small intestine. Consequently scientists have developed various approaches such as (a) enteric coating with Sureteic [1]; (b) tablet preparation with guar gum, Ethyl cellulose and Acrycoat L100 [2]; (c) encapsulation with guar gum [3], copolymer of methoxy polyethylene glycol and poly (D, L-lactide) [4] and interpenetrating network (IPN) beads of sodium carboxymethyl cellulose (SCMC) and sodium carboxymethyl xanthan (SCMX) [5]; (d) pH-sensitive hydrogel preparation with synthetic polymer, poly (vinyl alcohol) [6], or microbially triggered natural polymers such as guar gum with poly (acrylic acid), attapulgite (APT), and sodium alginate (GG-g-PAA=APT= SA) [7], dietary fiber psyllium with acrylamide (AAm)-acrylic acid (AAc) [8], and chitosan with polyvinyl pyrrolidone crosslinking via glyoxal [9] to protect drugs from acidic environment of stomach. All of these discussed approaches showed improved drug encapsulation efficiency along with enhanced drug release in cecal medium induced with enzymes causing degradation of the biodegradable polymer.…”