Current Issue : July - September Volume : 2013 Issue Number : 3 Articles : 6 Articles
Biowaivers are waivers of clinical bioequivalence studies which are often required for generic drugs or for small changes in drug products that evolve during drug development to ensure equivalence with dosage forms proven to be safe and effective. The application of the biowaivers thought has been prolonged to approval of certain APIs pertaining to BCS class 1 formulated in immediate release dosage form. Biowaivers typically save time and cost compared to clinical trials. Although typically mentioned, BCS-based biowaivers are still hardly used probably as a result of doubts on each, pharmaceutical firms and restrictive authorities. Substantial changes of biowaivers dossiers and specific valuations contribute to the impression that a standard understanding is lacking on a positive use of the BCS thought to support biowaivers. It is intended to reach an optimal and harmonized application of biowaivers among different regulatory authorities of The United States Food and Drug Administration (FDA), European Medicines Agency (EMEA) and Japanese Pharmaceuticals and Medical Devices Agency (PMDA), and World Health Organization (WHO). The article here summarizes and compares the possible differences and similarities between various regulatory bodies regarding BCS based biowaivers....
The property of nonsuperimposability of an object on its mirror image is called chirality. Enantiomers of a chiral compound with same molecular formula behave as a single entity in symmetric environment. Modern advances in chemical synthesis, chiral separation and analytical techniques enabled the drug manufacturers, pharmaceutical industries to make and market the single Enantiomeric drugs. The separate enantiomers of chiral racemate may exhibit different pharmacokinetic and pharmacodynamic profile due to the presence of asymmetric environment present in the body. Regulatory agencies are also encouraging pharmaceutical firms to launch single enantiomers instead of racemate. The old racemate has been reevaluated as potential single enantiomer products with the possibility for an improved therapeutic profile, this process is known as chiral switch, which provide market exclusivity period. The re-evaluation of individual enantiomer may or may not give the therapeutic profile and may associate with higher incidence of side effects. The present article addressed the basics of chirality, stereoselective pharmacokinetics and biological activity of single enantiomers, chiral switch and market trend of single enantiomers....
This study describes comparative disposition of long acting moxifloxacin in goats and sheep after intravenous administration in five animals. Long acting moxifloxacin solution (10 % moxifloxacin in solution with L- arginine, N-butyl alcohol and benzyl alcohol) was injected in jugular vein. Blood samples were collected from contra lateral jugular vein in test tubes containing 30-50 IU heparin (anticoagulant) periodically from 0.083 to 72 h of drug administration. Drug concentrations in plasma were determined using High Performance Liquid Chromatography (HPLC) with Fluorescence Detector. The mobile phase consisted of a mixture of buffer (10 gm of tetrabutyl ammonium hydrogen sulphate per liter-deionised water) and acetonitrile (80: 20). The buffer was 0.067 M of disodium hydrogen phosphate with pH of 7.5. The flow rate was 1 ml.min-1 at ambient temperature. The effluent was monitored at 296 nm excitation and 504 nm emissions wavelength. HPLC with Fluorescence Detector method for plasma moxifloxacin assay was standardized with specific modification for plasma of goats and sheep in present study. Long acting moxifloxacin the plasma concentration of 0.001±0.000 µg.ml-1 and 0.016±0.001 µg.ml-1 after single dose intravenous and was maintained for up to 72 h in goats and sheep, respectively....
The poor oral bioavailability of curcumin can be attenuated via topical application of nanocomposite thin polymeric film. Curcumin nanocomposite films composed of Eudragit RS 100 and Eudragit RL 100 were investigated for the higher topical bioavailability in inflammatory diseases. The nanocomposite films were developed by solvent evaporation method from polymeric nanodispersion, prepared by nanoprecipitation with homogenization and ultrasonic dispersion method. The permeability of curcumin from nanocomposite film was investigated across porcine ear epidermis in modified Franz diffusion cell. The anti-inflammatory properties of curcumin from the optimized film were evaluated by carrageenan induced rat paw edema method in wistar albino rats. The nanocomposite films showed good stability with uniform drug content in the range of 81 - 87 % w/w. The SEM and TEM data confirmed the deposition of spherical nanocurcumin in the size range of 78.8 – 97.3 nm. The skin permeability of curcumin was found to be more from the nanocomposite film, when compared to plain curcumin. The in vivo anti-inflammatory study in rat model showed that curcumin nanocomposite film reduced inflammation more effectively than the oral curcumin at the same dose. This study clearly indicates the superiority of curcumin nanocomposite film over plain curcumin in providing higher bioavailability with enhanced anti-inflammatory effect....
Pharmacokinetics of pefloxacin following single dose intravenous administration (10mg/kg) was investigated in healthy Ongole calves. The drug was assayed in serum by microbiological assay. Following intravenous administration, serum concentration-time curve was best fitted to two compartment open model. Therapeutic concentration of the drug was maintained in serum up to 10 hours. The drug was widely (Vd (area) 0.856±0.007 L/kg) and equally distributed between central and peripheral compartments as evinced by the fraction of the drug in the central compartment (0.500±0.003). Ongole calves exhibited an elimination half-life of 1.732±0.12 h and high values of area under curve (61.682±0.515 µg.h2/ml). The mean residence time was 2.112±0.012 h with total clearance of 0.342±0.001 L/kg/h. The concentration of the drug to exhibit the pharmacological effect was detectable up to 10 h....
Oromucosal delivery, especially that utilising the buccal and sublingual mucosa as the absorption site, is a promising drug delivery route which promotes rapid absorption and high bioavailability, with subseqent almost immediate onset of pharmacological effect. These advantages are the result of the highly vascularised oral mucosa through which drugs enter the systemic circulation directly, thus bypassing the gastrointestinal tract and the first pass effect in the liver. MFD tablet of piroxicam (PX) are subjected to in vivo pharmacokinetic evaluation to evaluate whether these systems improve oral bioavailability of the piroxicam. All the pharmacokinetic parameters of absorption, namely Ka, Cmax, Tmax, percent absorbed to various times and AUC indicated rapid absorption and higher bioavailability of piroxicam when administered as MFD Tablet. The absorption rate constant (Ka) was found to be increased compare with marketed formulation. Both Ka and AUC were markedly increased by MFD tablet. Thus, the results of pharmacokinetic studies indicated rapid and higher oral absorption of piroxicam when administered as MFD tablet....
Loading....