Selective LC determination of cabergoline in the bulk drug and in tablets: In vitro dissolution studies

Cabergoline (CAB) is an ergot alkaloid derivative with dopamine agonist activity. A novel, simple, and rapid stability-indicating high-performance liquid chromatographic (HPLC) method for assay of CAB in tablets has been developed and validated. Chromatography was performed on a 4.6 mm i.d. x 250 mm, 5 mu m particle, cyano column with acetonitrile-10 mM phosphoric acid, 35:65 (v/v), containing 0.04% triethylamine, as mobile phase, at a flow rate of 1.0 mL min(-1), and UV detection at 280 nm. Response was a linear function of concentration in the range 0.1-4 mu g mL(-1) (r(2) = 0.9999). The recovery of the method was good (99.45%) and RSD values for intra-day and inter-day precision were 0.24-0.88% and 0.66-1.19%, respectively. The method can be used for quality-control assay of CAB in tablets, for stability studies, and for in vitro dissolution studies

LC assay of eletriptan in tablets and in vitro dissolution studies

Eletriptan (ELT) is a new selective serotonin agonist approved for the treatment of acute migraine headaches. A simple and rapid liquid chromatographic method was developed and validated for the assay of ELT in tablets. Chromatography was carried out on a 250 mm x 4.6 mm C(18) column at 30 C. Acetonitrile-15 mM triethylamine solution (adjusted to pH 7.0 using concentrated o-phosphoric acid) (60:40, v/v) mixture was used as mobile phase at 1.0 mL min(-1) flow rate and UV detector was set at 225 nm. A linear response (r(2) = 0.9999) was observed in the range of 0.1-1.6 mu g mL(-1). The method showed good recoveries (100.08 %) and the RSD values for intra- and inter-day precision were 0.78-1.93 and 1.10-2.15%, respectively. The method can be used for quality control assays and in vitro dissolution studies of ELT in tablets

Preparation and characterisation of natamycin : gamma-cyclodextrin inclusion complex and its evaluation in vaginal mucoadhesive formulations

Novel formulations of vaginal bioadhesive tablets were prepared where the natamycin was complexed with gamma-cyclodextrin (NT-gamma CyD) to increase the solubility and stability of NT in aqueous solutions and reduce the side effects of the drug without decreasing antimycotic activity. Favourable interactions between the NT and gamma CyD and formation of the 1:1 inclusion complex were observed. The MIC(90) of both NT alone and NT-gamma CyD complexes were below 0.0313 microg mL(-1), suggesting that complexation with gamma CyD has effectively increased the antimycotic activity of NT, thus indicating the clinical usefulness of NT-gamma CyD complexes. The sustained drug release of NT was achieved to over 8 h periods by altering the polymer component of formulations which was responsible for differences in water absorption and erosion behaviour of the tablets. Bioadhesion studies have clearly indicated that enhancement of mucoadhesion was achieved by inclusion of Carbopol 934P and by tailoring the ratio of Carbopol 934P in the formulation, a high mucoadhesion to vaginal mucosa can be achieved. Hence, the formation of complex between NT and gamma CyD and effective combination with polymers attain a bioadhesive and sustained release formulation of NT suitable for vaginal delivery and the effective treatment of Candida infections

Preparation and characterisation of natamycin : gamma-cyclodextrin inclusion complex and its evaluation in vaginal mucoadhesive formulations

(c) 2008 Wiley-Liss, Inc. and the American Pharmacists AssociationNovel formulations of vaginal bioadhesive tablets were prepared where the natamycin was complexed with gamma-cyclodextrin (NT-gamma CyD) to increase the solubility and stability of NT in aqueous solutions and reduce the side effects of the drug without decreasing antimycotic activity. Favourable interactions between the NT and gamma CyD and formation of the 1:1 inclusion complex were observed. The MIC(90) of both NT alone and NT-gamma CyD complexes were below 0.0313 microg mL(-1), suggesting that complexation with gamma CyD has effectively increased the antimycotic activity of NT, thus indicating the clinical usefulness of NT-gamma CyD complexes. The sustained drug release of NT was achieved to over 8 h periods by altering the polymer component of formulations which was responsible for differences in water absorption and erosion behaviour of the tablets. Bioadhesion studies have clearly indicated that enhancement of mucoadhesion was achieved by inclusion of Carbopol 934P and by tailoring the ratio of Carbopol 934P in the formulation, a high mucoadhesion to vaginal mucosa can be achieved. Hence, the formation of complex between NT and gamma CyD and effective combination with polymers attain a bioadhesive and sustained release formulation of NT suitable for vaginal delivery and the effective treatment of Candida infections.Peer reviewe

Preparation, Characterization and Antiinflammatory Activity of Celecoxib-beta-Cyclodextrin Inclusion Complexes

The influence of beta-cyclodextrin on the in vitro dissolution rate, in vivo absorption and oral bioavailability of a poorly water soluble antiinflammatory agent, celecoxib was studied. For this purpose, celecoxib and beta-cyclodextrin complexes were prepared in 1: 1 and 1:2 molar ratios by the physical mixture, kneading and freeze-drying methods. The complexes were preliminary confirmed using differential scanning calorimetry, fourier transform-infrared spectroscopy and scanning electron microscopy. The solubility studies revealed a linear relationship between the increase in celecoxib solubility and the increase in beta-cyclodextrin concentration. The in vitro dissolution studies that were performed in phosphate buffer (pH 7.4) showed that celecoxib:beta-cyclodextrin (1:2) solid complexes prepared by freeze-drying method had highest celecoxib release compared to the other solid complexes, Pharmacological studies were performed with this complex in a carrageenan induced rat hind paw oedema model. Regarding to the inhibition of edema (%) and swelling (%) results, celecoxib:beta-cyclodextrin (1:2) binary mixture prepared by freeze-drying method showed significant improvement compared to pure drug

Bioadhesive sulfacetamide sodium microspheres: Evaluation of their effectiveness in the treatment of bacterial keratitis caused by Staphylococcus aureus and Pseudomonas aeruginosa in a rabbit model

The aim of this study was to prepare bioadhesive sulfacetamide sodium (SA) microspheres to increase their residence time on the Ocular Surface and to enhance their treatment efficacy on Ocular keratitis. Microspheres were fabricated by spray drying method using mixture of polymers such as pectin, polycarbophil and hydroxypropylmethyl Cellulose (HPMC) at different ratios. The particle size and distribution, morphological characteristics, thermal behavior, encapsulation efficiency, mucoadhesion and in vitro drug release studies on formulations have been investigated. After optimisation studies, SA-loaded polycarbophil microsphere formulation with polymer:drug ratio of 2:1 Was found to be the most Suitable for Ocular application and used in in vivo studies. In vivo studies were carried Out on New Zealand male rabbit eyes with keratitis caused by Pseudomonas aeruginosa and Staphylococcus aureus. Sterile microsphere Suspension in light mineral oil was applied to infected eyes twice a day. Plain SA Suspension Was used as a positive control, On 3rd and 6th days of the antimicrobial therapy, the eyes were examined in respect to clinical signs of infection (blepharitis, conjunctivitis, iritis, corneal oedema and corneal infiltrates) which are the main symptoms of bacterial keratitis and then cornea samples were counted microbiologically. The rabbit eyes treated with microspheres demonstrated significantly lower clinical scores than those treated with SA alone. A significant decrease in the number of viable bacteria in eyes treated with microspheres was observed in both infection models when compared to those treated with SA alone. In conclusion, in vitro and in vivo studies showed that SA-loaded microspheres were proven to be highly effective in the treatment of ocular keratitis. (C) 2009 Elsevier B.V. All rights reserved

Evaluation of risk factors for the development of bacteremia and complications in patients with brucellosis: Is it possible to predict the clinical course?

Introduction: Brucellosis is often confused with other diseases or accompanies the conditions it imitates. It causes treatment delays, failure, relapse, and complications. This study aimed to investigate bacteremia and complication predictors in Brucellosis patients. Early detection may help reduce relapse rates, length of hospital stay, and surgical intervention rates by providing appropriate treatment.Methodology: We examined 220 adult patients diagnosed with Brucellosis in our tertiary care hospital in the Black Sea Region between January 01, 2010, and January 01, 2022. Patients with and without bacteremia and complications were compared regarding demographic characteristics, clinical features, and laboratory parameters.Results: The mean age was 46.4 +/- 15.8 years (18-96 years), and 61% were male. Low back pain and absence of muscle pain were independent risk factors for predicting bacteremia (p = 0.049, p = 0.043, respectively). Weakness /fatigue, weight loss, and 1/320 Standard Tube Agglutination Test (STAT) or Brucella Coombs Gel Test (BCGT) titers were independent risk factors that reduced the risk of complications; in contrast, low back pain and splenomegaly were independent risk factors for development of complications. (p = 0.025, p = 0.007, p = 0.008, p = 0.003, p = 0.021 respectively). Thrombocytopenia was related to complications. When the platelet cut-off value was taken as 160,000/mu L in predicting complications, the sensitivity was 31.30%, and the specificity was 97.73% (p = 0.011).Conclusions: The risk of clinical progression and complications could be predicted with symptoms and signs such as myalgia, low back pain, weakness/fatigue, weight loss, splenomegaly, and easily accessible laboratory parameters such as serum STAT/BCGT titer and platelet level

Characterization of biodegradable chitosan microspheres containing vancomycin and treatment of experimental osteomyelitis caused by methicillin-resistant Staphylococcus aureus with prepared microspheres

The biodegradable chitosan microspheres containing vancomycin hydrochloride (VANCO) were prepared by spray drying method with different polymer:drug ratios ( 1: 1, 2:1, 3:1 and 4: 1). Thermal behaviour, particle size and distribution, morphological characteristics, drug content, encapsulation efficiency, in vitro release assessments of formulations have been carried out to obtain suitable formulation which shows sustained-release effect when implanted. Sterilized VANCO loaded microspheres were implanted to proximal tibia of rats with methicillin-resistant Staphylococcus aureus (MRSA) osteomyelitis. Intramuscular (IM) injection of VANCO for 21 days was applied to another group for comparison. After 3 weeks of treatment, bone samples were analysed with a microbiological assay