Farmakokinetika eprinomektina u ovaca nakon potkožne primjene.

The pharmacokinetics of eprinomectin was determined in lactating sheep following subcutaneous administration at a dose rate of 0.2 mg kg-1. The eprinomectin concentration in plasma was determined using High Performance Liquid Chromatography (HPLC) with a fluorescence detector. The kinetics of plasma concentrations were analysed using the non-compartment model. The maximum plasma concentration of 24.44 ng/mL occurred 2 days post-administration. Following subcutaneous administration of eprinomectin in sheep, the value of plasma elimination half-life, the area under the plasma concentration time curve (AUC) and mean residence time (MRT) were 388.52 ± 0.25 h. 4282.10 ng.h/mL and 374.50 h, respectively. The values of V (area), Vd(ss) and Cl(B) were 20.50 mL/kg, 13.70 mL/kg and 0.04 mL/h/kg, respectively. This study demonstrates that subcutaneous administration of eprinomectin led to higher bioavailability and longer mean residence time with a lower dose than a pour-on application, and that an injectable formulation may be applied in lactating sheep with zero withdrawal period.Farmakokinetika eprinomektina određivana je u ovaca u laktaciji nakon potkožne primjene u dozi od 0,2 mg/kg. Njegova koncentracija u plazmi utvrđena je visoko učinkovitom tekućinskom kromatografijom s fluorescentnim detektorom. Kinetika koncentracija u plazmi analizirana je na osnovi modela bez odjeljaka. Najveća koncentracija u plazmi od 24,44 ng/mL dokazana je dva dana nakon primjene. Poluživot eliminacije iz plazme iznosio je 388,52 ± 0,25 sati, površina ispod krivulje koncentracije u plazmi (AUC) 4282,10 ng/h/mL, a prosječno vrijeme zadržavanja iznosilo je 374,50 sati. Vrijednost prividnog volumena raspodjele, Vd(area), iznosila je 20,50 mL/kg, prosječni vidljivi volumen raspodjele, Vd(ss), 13,70 mL/kg, a ukupni klirens 0,04 mL/sat/kg. Istraživanje je pokazalo da potkožna primjena eprinomektina pruža veću bioraspoloživost, duže vrijeme zadržavanja s manjom dozom u odnosu na veliku te da se injekcijska formulacija može primijeniti u ovaca u laktaciji

Characteristics of Fatal Cases of Pandemic Influenza A (H1N1) from September 2009 to January 2010 in Saurashtra Region, India

Background: India reported first case of 2009 pandemic influenza A (H1N1) virus infection in May, 2009 and Saurashtra region in August, 2009. We describe the characteristics of fatal cases of 2009 influenza A (H1N1) infection reported in Saurashtra region. Methods: From September, 2009 to January, 2010, we observed 71 fatal cases that were infected with 2009 influenza A (H1N1) virus and admitted in different hospitals in Rajkot city. Real-time reverse-transcriptase-polymerase-chain-reaction (RT-PCR) testing was used to confirm infection; the clinico-epidemiological features were observed and documented. Results: Median age of the deceased (71) was 29 years, and 57.7% were females. Median time observed was 5 days from onset of illness to diagnosis of influenza A (H1N1), and 57.7% were referred from general practitioner (OR=0.42, CI=0.24-0.74). Median hospital stay reported was 3 days. All admitted patients received oseltamivir, but only 16.9% received it within 2 days of onset of illness. The most common symptoms were cough (97.2%), fever (93%), sore throat and shortness of breath. Co-morbid conditions were present in almost half of the patients who ultimately died, the most common of which was pregnancy (OR=0.15, CI=0.04-0.52). Radiological pneumonia was reported in 98% patients. Conclusion: Residing in urban area, delayed referral from general practitioner, presence of co-existing condition, especially pregnancy was responsible for mortality among influenza A (H1N1) infected positive

Development and characterization of controlled release mucoadhesive tablets of captopril to increase the residence time in the gastrointestinal tract

The present investigation concerns the development of mucoadhesive tablets of captopril which were designed to prolong the gastric residence time after oral administration. Matrix tablets of captopril were formulated using different mucoadhesive polymers such as guar gum, xanthan gum, hydroxyl propyl methyl cellulose (HPMC) K4M and K15M in various ratios. The tablets were evaluated for physical properties, content uniformity, swelling index, bioadhesive strength and in vitro drug release. Swelling was increased as the concentration and viscosity of HPMC increases. Tablets formulated using guar gum and xanthan gum alone were eroded faster and dissolved completely within 5-7 h, while tablet containing HPMC remain intact and provided slow release up to 11-12 h. It was evident from the study that the formulation F10 containing HPMC K15M and xanthan gum (1:1) exhibited maximum bioadhesive strength of 31.59 ± 0.05 gm and in vitro drug release was found to be 91.85 % at the end of 12 h with non-fickian diffusion mechanism. The stability studies of optimized batch showed that there was no change in bioadhesive strength and in vitro release when stored at different temperature condition for 90 days. It was concluded that formulation F10 shows the better bioadhesive strength and drug release.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Farmakokinetika eprinomektina u ovaca nakon potkožne primjene.

The pharmacokinetics of eprinomectin was determined in lactating sheep following subcutaneous administration at a dose rate of 0.2 mg kg-1. The eprinomectin concentration in plasma was determined using High Performance Liquid Chromatography (HPLC) with a fluorescence detector. The kinetics of plasma concentrations were analysed using the non-compartment model. The maximum plasma concentration of 24.44 ng/mL occurred 2 days post-administration. Following subcutaneous administration of eprinomectin in sheep, the value of plasma elimination half-life, the area under the plasma concentration time curve (AUC) and mean residence time (MRT) were 388.52 ± 0.25 h. 4282.10 ng.h/mL and 374.50 h, respectively. The values of V (area), Vd(ss) and Cl(B) were 20.50 mL/kg, 13.70 mL/kg and 0.04 mL/h/kg, respectively. This study demonstrates that subcutaneous administration of eprinomectin led to higher bioavailability and longer mean residence time with a lower dose than a pour-on application, and that an injectable formulation may be applied in lactating sheep with zero withdrawal period.Farmakokinetika eprinomektina određivana je u ovaca u laktaciji nakon potkožne primjene u dozi od 0,2 mg/kg. Njegova koncentracija u plazmi utvrđena je visoko učinkovitom tekućinskom kromatografijom s fluorescentnim detektorom. Kinetika koncentracija u plazmi analizirana je na osnovi modela bez odjeljaka. Najveća koncentracija u plazmi od 24,44 ng/mL dokazana je dva dana nakon primjene. Poluživot eliminacije iz plazme iznosio je 388,52 ± 0,25 sati, površina ispod krivulje koncentracije u plazmi (AUC) 4282,10 ng/h/mL, a prosječno vrijeme zadržavanja iznosilo je 374,50 sati. Vrijednost prividnog volumena raspodjele, Vd(area), iznosila je 20,50 mL/kg, prosječni vidljivi volumen raspodjele, Vd(ss), 13,70 mL/kg, a ukupni klirens 0,04 mL/sat/kg. Istraživanje je pokazalo da potkožna primjena eprinomektina pruža veću bioraspoloživost, duže vrijeme zadržavanja s manjom dozom u odnosu na veliku te da se injekcijska formulacija može primijeniti u ovaca u laktaciji

FORMULATION AND EVALUATION OF BILAYERED FLOATING TABLET OF DILTIAZEM DRUG

Aim of study was to develop bilayered floating drug delivery for treatment of hypertension by delivering loading and maintenance dose for fast achievement of peak plasma concentration and maintaining the same respectively. The prepared drug loaded bilayered floating tablets were evaluated for pre and post compression parameters. Stability study of the promising formulation was also performed. The tablets were prepared by direct compression method. The loading dose was delivered in the form of immediate release layer prepared by different super-disintegrations and maintenance dose was delivered through sustained release layer prepared by using polymers like HPMC K15M and Carbopol 934P. Both the immediate release layer and sustained release layers were separately optimized and then combined to optimize the bilayered floating tablets. No interactions were found between drug and excipients. Formulation containing crosscarmellose sodium shows immediate drug release. Formulation Containing HPMC K15M shows sustained release action and bilayered formulations FB7 shows releases up to 12 hours with good buoyancy and total floating time. All the Bilayered floating formulations buoyant up to 12 hrs. Bilayered floating tablets with release characteristics offer critical advantages such as, site specificity with improved absorption and efficacy. This technology can be inculcated to various medicaments which have stomach as the major site of absorption. Key words: Diltiazem, Bilayered floating tablet, sustain release table