Characterization of cellulosic hot-melt extruded films containing lidocaine.

Hot-melt extrusion technology was used to produce thin films containing a model drug, lidocaine, and the cellulosic polymers hydroxypropyl cellulose (HPC) and hydroxypropyl methyl cellulose (HPMC). Two film formulations were extruded and compared, one containing only HPC and the other containing HPC:HPMC (80:20). Thermal analysis of the films using differential scanning calorimetry (DSC) suggested that the drug existed in the amorphous condition, which was confirmed by wide angle X-ray diffractometry. Sustained release of the drug was observed from both of the polymer matrices. Dissolution profiles suggested that HPMC retarded the drug release from HPC:HPMC (80:20) films. However, the mechanism of drug release from both of the films was predominantly diffusion of the drug through the polymer matrices. Incorporation of HPMC also increased both adhesive strength and work of adhesion as compared to the HPC-only films.     

Hepatoprotective Bile Acid Co-Drug of Isoniazid: Synthesis,Kinetics and Investigation of Antimycobacterial Potential

Pharmaceutical Chemistry Journal - The long-course treatment of tuberculosis with isoniazid (INH) leads to hazardous side effects on liver and poor patient compliance. To overcome these toxic...     

Constructing whole of population cohorts for health and social research using the New Zealand Integrated Data Infrastructure

Objectives: To construct and compare a 2013 New Zealand population derived from Statistics New Zealand’s Integrated Data Infrastructure (IDI) with the 2013 census population and a 2013 Health Service Utilisation population, and to ascertain the differences in cardiovascular disease prevalence estimates derived from the three cohorts. Methods: We constructed three national populations through multiple linked administrative data sources in the IDI and compared the three cohorts by age, gender, ethnicity, area‐level deprivation and District Health Board. We also estimated cardiovascular disease prevalence based on hospitalisations using each of the populations as denominators. Results: The IDI population was the largest and most informative cohort. The percentage differences between the IDI and the other two populations were largest for males and for those aged 15–34 years. The percentage differences between the IDI and Census cohorts were largest for people living in the most deprived areas. The ethnic distribution varied across the three cohorts. Using the IDI population as a reference, the Health Service Utilisation population generally overestimated cardiovascular disease prevalence, while the Census population generally underestimated it. Conclusions and implications: The New Zealand IDI population is the most comprehensive and appropriate national cohort for use in health and social research.     

G6PD deficiency in newborn infants

Five hundred consecutive newborns were screened for erythrocytic G6PD deficiency in cord blood. The overall incidence of G6PD deficiency was found to be 2.80 percent. The incidence of G6PD deficiency was higher among males (3.77%) compared to females (1.44%). The incidence of erythrocytic G6PD deficiency was higher in Muslims (16.67%) compared to Hindus (2.63%). No definite relationship of erythrocytic G6PD deficiency was observed with consanguinity. Fifty per cent mothers of G6PD deficient newborns were also found to be G6PD deficient. Among brothers and sisters of G6PD deficient children the incidence of G6PD deficiency was 50.00 and 9.10 per cent respectively. There was no significant difference in the incidence of hyperbilirubinemia between erythrocytic G6PD deficient and non deficient newborns.     

Socio-demographic co-relates of psychiatric disorders

Objective: To find out the magnitude of probable psychopathology in children and study association of psychopathology with demographic, developmental and social factors.Methods: Childhood Psychopathology Measurement Schedule (CPMS) was used to measure the magnitude of probable psychopathology in 620 children from an urban slum of Miraj (Maharashtra). A second schedule recorded demographic, developmental and social factors.Results: CPMS score >10 was observed in 102 children (16.5%). It was significantly higher in children aged 7–10 years, in males, belonging to lower socioeconomic status, large families, being first born, having low birth weight (LBW); body mass index (BMI) less than 18.5. Low maternal education and alcohol abuse in father also had significant association with CPMS score >10.Conclusion: Findings suggest a need to educate the community about psychological implications of LBW, large family size and overcrowding in children. Improving maternal education and controlling alcoholism could help in reducing childhood psychopathology.     

Water vapor sorption of hot-melt extruded hydroxypropyl cellulose films: effect on physico-mechanical properties, release characteristics, and stability

Hot-melt extrusion technology was used to prepare thin polymer films containing hydroxypropyl cellulose and clotrimazole (CT). Films containing hydroxypropyl celluloses of different molecular weight and the drug were investigated for moisture-sorption, mechanical properties, and release characteristics. Stability of the films was also studied at 25 degrees C/60% relative humidity (RH) and 40 degrees C/75% RH for up to 3 months. To study the moisture-sorption of the hot-melt extruded films, a rapid dynamic vapor sorption technique was used. Mechanical properties were evaluated using the Texture Analyzer. The molecular weight of the polymer had a significant effect on the mechanical and release characteristics of the films but did not influence the equilibrium moisture content in the films stored at RHs ranging from 0 to 90%. However, the time to reach equilibrium was longer for the higher molecular weight polymers. The drug release rate was dependent on the rate of erosion, which in turn depended on the molecular weight of the polymer. The films were stable at 25 degrees C/60% RH for up to 3 months with no significant degradation or recrystallization of CT. However, recrystallization of the drug was observed within the films stored in accelerated stability conditions at the end of 3 months in which only 92.9% (+/-1.9) CT remained.     

Reservoir Based Fentanyl Transdermal Drug Delivery Systems: Effect of Patch Age on Drug Release and Skin Permeation

Purpose  To understand and evaluate the stability and skin permeation profiles of fentanyl reservoir systems as a function of patch age. Methods  Drug release and skin permeation studies were performed using a modified USP apparatus 5 with a novel sample preparation technique. Results  The amount of fentanyl present in the EVA/adhesive layer (EAL) increased from about 17% of label claim (LC) at 5 months to 25% LC at 22 months. The increase in the drug concentration was mainly observed in the peripheral EAL. Simultaneously, the alcohol content of the patch decreased as a function of patch age. A significant effect of patch age on the drug content in the EAL and the drug release from the system was observed; however, skin permeation studies did not indicate an increase in drug delivery rate. Conclusions  Novel sample preparation technique with USP Apparatus 5 allowed determination of in vitro skin permeation rates for fentanyl transdermal patches with different designs. Permeation rates with cadaver skin as substrate were found not to change with patch age despite changing drug concentration in the EAL.     

Synthesis, kinetic studies and pharmacological evaluation of mutual azo prodrug of 5-aminosalicylic acid for colon-specific drug delivery in inflammatory bowel disease

Mutual azo prodrug of 5-aminosalicylic acid with l-tyrosine was synthesized by coupling l-tyrosine with salicylic acid, for targeted drug delivery to the inflamed gut tissue in inflammatory bowel disease. The structure was confirmed by elemental analysis, IR and NMR spectroscopy. In vitro kinetic studies in rat fecal matter showed 87.18% release of 5-aminosalicylic acid with a half-life of 140.28min, following first order kinetics. Therapeutic efficacy of the carrier system and the mitigating effect of the azo conjugate were evaluated in trinitrobenzenesulfonic acid-induced experimental colitis model. Myeloperoxidase activity was determined by the method of Krawisz et al. The synthesized prodrug was found to produce comparable mitigating effect as that of sulfasalazine on colitis in rats.