PHD theses : Pharmacy
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Item PRE-CLINICAL STUDIES ON CIPROFLOXACIN EFFERVESCENT TABLETS(Al Neelain University, 2017) Ahmed Mohammed Ahmed Mohammed MsaadIntroduction Enhancement of physicochemical properties of tablets with, and studied their characters in vivo is the duty of pharmaceutical efforts. The effervescent tablets are palatable dosage forms since they are easy to swallow, have the ability to mask the bitter taste for many drugs and, may increase therapeutic and clinical effect. Objectives The study aimed to formulate ciprofloxacin HCl, a main drug for GIT and UTI infections, as effervescent tablets, and Compare the pharmaceutical properties of these effervescent tablets with those of a reference marketed ciprofloxacin hydrochloride tablets for in vitro, in vivo correlation. Methodology The study was done at the Departments of Pharmaceutics, Pharmacology and, Pharmaceutical Chemistry, College of Pharmacy Taif University. The reference tablets were selected from Bayer, its origin of the patency. The drug was formulated as an effervescent tablet, by two methods (direct compression and wet granulation). The bitter taste was masked by saccharine as sweeting agent, furthermore the effervescent effect of citric acid, tartaric acid and, sodium bicarbonate lead to improve the taste of the drug. Also the Guar gum is used, as binding agent, lead to hide the taste. The vanillin, which was used as flavoring agent also enhances the palatability. The physico-chemical and stability study experiments were done according to monographs and microbiological sensitivity test was also carried out on both, reference and, test tablets. Furthermore, bioavailability study was done in rabbits and estimating the concentrations in plasma, by HPLC according to restricted protocol. In vitro and in vivo correlation was made. Results and Discussion The effervescent tablets passed all the fundamental tests in the monograph and has been found stable upon different conditions, both for reference and effervescent tablet, the dissolution test, microbiological sensitivity test were carried out against (Escherichia coli, Salmonella typhi, Salmonella para typhi and Staphylococcus aureus).The pharmacokinetic parameters of ciprofloxacin were determined, following oral administration of a single dose of 20mg/kg body weight for Ciprobay as reference and a new formulation of effervescent ciprofloxacin as test product in 20 normal healthy male rabbits. High performance liquid chromatographic method was employed for estimation of ciprofloxacin in plasma samples. A significant (P≤ 0.05) increase in drug plasma concentration was recorded at 0.5, 1, 3. 4, 8, 12 hours sampling time, and highly significant (P≤ 0.01) increase of drug concentrations was observed at 1.5 hour for test formula due to highly dissolution rate of effervescent base at that time, except at 24 hour because of clearance of the drug from the body. A highly significant (P≤ 0.01) the increase percent of wet granulation effervescent tablets for absorption half-life (50%), distribution rate constant (34.95%) area under the curve AUC0-α (38%) and peak plasma concentration (Cmax) (42.30%) were recorded for effervescent tablets rather than reference tablets by using SAS (Statistical Analysis System). Distribution time, elimination time, and Tmax decreased (P≤ 0.05)significantly for effervescent tablets because whenever there is an increase in Cmax, Tmax decreases. Mean Residence Time and lag time were significantly (P≤ 0.05) higher in rabbits, which take the effervescent formula. The results reflect that enhancement in dissolution rate by effervescent base with sustained release for using guar gum in new formula might increase bioavailability. It was concluded that the effervescent ciprofloxacin, might improve bioavailability, might increase patient compliance, and might decrease microorganisms resistant which might be solution of microbial resistance to ciprofloxacin.