IMPROVEMENT OF BIOAVAILABILITY OF CEFUROXIME AXETIL ORAL SUSPENSION BY INCLUSION COMPLEXATION METHOD

Objective: Cefuroxime axetil, a prodrug of Cefuroxime, is a poorly water soluble drug, thus it has got only limited solubility and dissolution rate in gastric fluids. Also, the bioavailability of Cefuroxime axetil oral suspension is only 40-45% when compared to the 60% bioavailability of tablets. The objective of this study was to develop an oral suspension of Cefuroxime axetil with improved oral bioavailability by inclusion complexation method using Hydroxypropyl beta cyclodextrin [HP-Beta-cylcodextrin]Methods: The complexation of Cefuroxime axetil and HP-Beta cyclodextrin was carried out at 1:1, 1:2, 1:2.5 and 1:3 ratios respectively. The prepared suspensions were evaluated for various parameters like pH, viscosity, re-dispersibility, pourability, and assay and in-vitro dissolution profile. A leading marketed product and the optimized formulation were evaluated for the pharmacokinetic parameters like Cmax, AUC0-t, AUC0-∞ and Tmax in healthy adult male rabbits.Results: Considering the in-vitro dissolution profile, formulation with 1:2.5 ratios of Cefuroxime axetil and HP-Beta cyclodextrin was selected as the optimized formulation. The Cmax of Optimized formulation and Marketed product were 148±1.26ng/ml and 126±1.52 ng/ml respectively, and the AUC0-t ofOptimized formulation and Marketed product were 989±16.42 ng. h/ml and 613±24.26 ng. h/ml respectively, which shows a significant improvement in the bioavailability of optimized formulationConclusion: From the results obtained it can be observed that there is a significant improvement in the bioavailability of optimized formulation compared to the marketed product. This demonstrates that the inclusion complexation method with HP-Beta cyclodextrin can significantly improve the oral bioavailability of Cefuroxime axetil.Keywords: Cefuroxime axetil, Bioavailability, Beta cyclodextrin, Inclusion complexatio

FORMULATION AND EVALUATION OF TASTE MASKED ORAL SUSPENSION OF CEFUROXIME AXETIL USING HYDROXYPROPYL-BETA-CYCLODEXTRIN

ABSTRACTObjective: Cefuroxime axetil is a prodrug of Cefuroxime, which is extremely bitter in taste, which reduces the patient compliance when taken asoral suspension especially in pediatric population. The objective of this study was to mask the bitter taste of Cefuroxime axetil using Hydroxy propylbetacyclodextrin [HP- Betacyclodextrin] by inclusion complexation method. Methods: The complexation of Cefuroxime axetil and HP- Betacyclodextrin was carried out at 1:1, 1:2, 1:2.5 and 1:3 ratios respectively. The preparedsuspension was evaluated for various parameters like pH, viscosity, redispersibility, pourability, assay and invitro dissolution profile. A comparativeevaluation of the taste masking was carried out for the developed formulations and marketed product. Results: All the formulations and the marketed product were meeting all the quality parameters. Formulations with 1:3 and 1:2.5 ratios showedbetter taste masking compared to the marketed product and the formulation with 1:2.5 ratio shown to have better invitro dissolution pattern. Conclusion: Considering the invitro dissolution profile and taste evaluation with marketed product, formulation with 1:2.5 ratio of Cefuroxime axetiland HP- Betacyclodextrin was selected as the optimum formulation.Keywords: Cefuroxime axetil, Taste masking, Betacyclodextrin, Inclusion complexation

QUALITY BY DESIGN BASED DEVELOPMENT OF ETRAVIRINE SELF MICRO EMULSIFYING DRUG DELIVERY SYSTEM

Objective: The main objective of the present research work was to develop systematically the Self Micro Emulsifying Drug Delivery system of BCS Class IV drug in a Quality by Design framework. Methods: The quality by design-based formulation development proceeds with defining the Quality Target Product Profile and Critical Quality Attributes of dosage form with appropriate justification for the same. The statistical Mixture design was used for the development of the formulation. The independent variables selected for the design were Oleic acid, Labrasol and PEG 6000, whereas droplet size (nm), emulsification time (sec), % drug loading and % drug release at 15 min were considered as the potential quality attributes of the Self Micro Emulsifying System. The eight different batches of Etravirine-Self Micro Emulsifying systems (ETV-SMEDDS) were prepared and checked for the Critical Quality Attributes. The simultaneous optimization of the formulation was done by the global desirability approach. Results: The characterization report obtained for all the different batches of formulation was analyzed statistically by fitting into regression models. The statistically significant models determined for droplet size (nm) (R2= 0.96 and p-0.1022), emulsification time (sec) (R2= 0.99 and p-0.0267), % drug loading (R2= 0.93 and p-0.1667) and % drug release at 15 min (R2= 0.96 and p-0.0911) and were statistically significant. The maximal global desirability value obtained was 0.9415 and the value indicates, the selected factors and responses have a good correlation and are significant enough for optimization and prediction of best formulation. Conclusion: The QbD approach utilized during the development of ETV-SMEEDS facilitated the identification of Critical Material Attributes and their significant impact on the Critical Quality Attributes of SMEDDS. The concept of building quality into product through the QbD application was utilized successfully in the formulation development

Results of Universal Prenatal Screening for Hepatitis C Infection in a Remote American Indian Primary Care Population

BACKGROUND: Although chronic liver disease remains a major area of health disparity for American Indian (AI) people, the epidemiology of hepatitis C virus (HCV) infection among AI people is poorly documented. Because of suspected high local prevalence, two remote AI clinics in the Northern Plains implemented universal prenatal HCV screening in 2005. When this screening program reported an unexpectedly high prenatal anti-HCV (anti-HCV antibody) positivity rate, we conducted a case-control study to determine risks for infection and opportunities for community intervention. MAIN FINDINGS: The clinics screened a total of 205 pregnant women (median age, 22 years). Of these 205 women, a total of 13 (6.3%; 95% confidence interval, 3.4–10.6) had anti-HCV confirmed. Of the anti-HCV-positive women, 10 (76.9%) were aged 15–24 years. We included 10 cases and 40 anti-HCV-negative prenatal controls in a case-control study. On multivariate analysis, only injection-drug use (IDU) remained associated with HCV seropositivity. CONCLUSIONS: Universal prenatal screening revealed a high prevalence of anti-HCV at these remote AI clinics. This population has not been previously described at being at elevated risk for HCV infection. In order to reduce health disparities, young, rural AI populations seeking prenatal care need to be included in interventions to reduce HCV transmission

Role of diffusion tensor imaging in early detection of cervical spondylotic myelopathy.

To (1) obtain microstructural parameters (Fractional Anisotropy: FA, Mean Diffusivity: MD) of the cervical spinal cord in patients suffering from cervical spondylotic myelopathy (CSM) using tractography, (2) to compare DTI parameters with the clinical assessment of these patients (3) and with information issued from conventional sequences. FA values were significantly correlated with some of the patients’ clinical scores. High signal intensity of the spinal cord on T2 was not correlated either with the DTI parameters or with the clinical assessment, suggesting that FA is more sensitive than T2 imaging

Primary Fibrinolysis in Acute Monocytic Leukemia

We present the case of a young man with acute monocytic leukemia (French-American-British classification:M5) and systemic hyperfibrinolysis with severe bleeding. Although fibrinolysis is usually mild and secorulary to disseminated intravascular coagulation, its role as a primary and dominant factor in rare cases of leukemia warrants that its presence be sought as a cause of abnormal bleeding. Decreased serum plasminogen and increased serum plasmin determined by synthetic substrate assay and a negative protamine paracoagulation test are crucial findings. Use of high-dose epsilon-aminocaproic acid was effective in treating this complication. A transient increase in fibrinolytic activity coincident with the early effect of antileukemic treatment suggested that plasminogen activator and/or fibrinolytic protease substances were released from leukemic cells. Fibrinolytic activity subsequently disappeared with reduction in the population of leukemic cells

Formation of Composite Surface during Friction Surfacing of Steel with Aluminium

Commercial pure aluminium was deposited on medium carbon steel using friction surfacing route. An aluminium rod was used as the consumable tool. Normal load and tool rotation speed were the variables. Under certain combinations of load and speed the deposition was continuous and uniform. The deposit consisted of Al embedded with fine particles of iron. The interface between substrate material and deposited material was smooth and relatively small. A mechanism is discussed for formation of a composite surface on the steel substrate

Efficient sensing of resorcinol using onion peel derived carbon and barium titanate nanocomposite

572-579A novel voltammetric sensor, Ag@BaTiO3/rCF/GCE has been designed based on silver nanoparticle (AgNPs), barium titanate (BaTiO3) and bio-inspired carbon derived from onion peel (OP) for the electrochemical determination of an organic pollutant, resorcinol (RS). The nanocomposite has been synthesized by ultrasonic irradiation of BaTiO3 decorated on reduced carbon flakes (rCF) on which the Ag nanoparticles (AgNPs) are stabilized. It has been characterized by spectroscopic and microscopic techniques and Impedence spectroscopy. Its electrochemical activity is studied by the surface modification of the glassy carbon electrode (GCE) through cyclic voltammetry (CV) and differential pulse voltammetry (DPV). The results show a considerable decrease in the Rct equal to 239Ω which confirms the surface modification of the electrode. The slope value 0.7814 confirms that the electrocatalytic oxidation of RS is a typical adsorption-controlled process. The linear concentration range of resorcinol detection varies from 6.66 to 131.67 μM with a LOD of 0.378 μM

Efficient sensing of resorcinol using onion peel derived carbon and barium titanate nanocomposite

A novel voltammetric sensor, Ag@BaTiO3/rCF/GCE has been designed based on silver nanoparticle (AgNPs), barium titanate (BaTiO3) and bio-inspired carbon derived from onion peel (OP) for the electrochemical determination of an organic pollutant, resorcinol (RS). The nanocomposite has been synthesized by ultrasonic irradiation of BaTiO3 decorated on reduced carbon flakes (rCF) on which the Ag nanoparticles (AgNPs) are stabilized. It has been characterized by spectroscopic and microscopic techniques and Impedence spectroscopy. Its electrochemical activity is studied by the surface modification of the glassy carbon electrode (GCE) through cyclic voltammetry (CV) and differential pulse voltammetry (DPV). The results show a considerable decrease in the Rct equal to 239Ω which confirms the surface modification of the electrode. The slope value 0.7814 confirms that the electrocatalytic oxidation of RS is a typical adsorption-controlled process. The linear concentration range of resorcinol detection varies from 6.66 to 131.67 μM with a LOD of 0.378 μM