TGA studies of metoclopramide complexes of cobalt(II) in the solid state

A new series of cobalt(II) complexes with metoclopramide (MCP) ligand have been prepared. The prepared Co(II)-MCP complexes were characterized for various analytical techniques. Conductivity and elemental analysis of complexes have been measured. The thermal stability and degradation kinetics have been measured using thermogravimetric analyser. Kinetic parameter was obtained for each stage of thermal degradation for Co(II)-MCP complexes using Horowitz-Metzger, Coats-Redfern and Broido's methods. The activation energy (Ea) of the complexes for the thermal degradation process lie in the range 31-168, 23-161 and 33-170 kJ mol-1 for Horowitz-Metzger, Coats-Redfern and Broido's methods, respectively. © 2003 Elsevier B.V. All rights reserved

ZIPRASIDONE HYDROCHLORIDE LOADED NANOSTRUCTURED LIPID CARRIERS (NLCS) FOR INTRANASAL DELIVERY: OPTIMIZATION AND IN VIVO STUDIES

Objective: The present study was an attempt to systemically deliver the most desirable schizophrenia drug, ziprasidone hydrochloride (ZRS) via the intranasal route using nanostructured lipid carrier (NLC) approach. Methods: The desired ZRS loaded NLCs were developed using central composite statistical design and the developed formulation was monitored for improving ZRS bioavailability and their brain targeting efficacy. Results: Pharmacokinetic studies revealed a 10 fold increase (ZRS blood-brain ratio) for NLCs administered through nasal route (in comparison to intravenous route). Similarly, the concentration of ZRS (in the brain) delivered via nasal route exhibits 4 fold increment at all-time points. Conclusion: Therefore, the obtained results suggest a potential nose to brain transport of loaded ZRS by effective bypassing of the Blood-Brain Barrier (BBB)

IMPROVEMENT AND ESTIMATION OF ORALLY DISINTEGRATING TABLETS CONTAINING PILOCARPINE 2-HYDROXY PROPYL β-CYCLODEXTRIN INCLUSION COMPLEX BY RESPONSE SURFACE METHODOLOGY

Objective: The study aimed to develop and evaluate an orally disintegrating tablet that contains pilocarpine and 2-hydroxy propyl β-cyclodextrin as an inclusion complex that is prepared by lyophilization used for treatment for dry mouth. Pilocarpine is utilized to treat dry mouth disorder. The inclusion complex lowers the taste of pilocarpine through the oral mucosa by the use of 2-hydroxy propyl β-cyclodextrin. Methods: The in vitro release from the insertion complex is also been studied. The parameters like differential scanning calorimetry (DSC), Fourier transformer infrared spectroscopy (FTIR), X-ray diffraction (XRD), and morphological study have been evaluated. The design of an experiment is carried out based on the concentration of croscarmellose sodium (CCS) and microcrystalline cellulose (MCC). Evaluation of the prepared orally disintegrating tablets have been carried out by different test methods like weight variation, thickness, drug content, disintegration, and in vitro dissolution study. Results: Orally disintegrating tablets are studied by utilizing the immediate pressure technique. Pilocarpine indicates the anhydrous crystalline medication, displaying sharp endothermic top at 120.2 °C, bend of 2-HPβCD demonstrates an exceptionally wide endothermal wonder among 55-100 °C for DSC. In pilocarpine spectra, characteristic band of aromatic C-H stretch at 3277 cm-1, C=C stretching at 1608 cm-1, C-N stretching at 1445 cm-1 and methoxy (CH3-O-) stretch at 2921 cm-1 was observed. The investigation shows that tablet hardness of 4.3N, breaking downtime of 12 sec and mean disintegration time is 1.562 min. Conclusion: The different diluents and super disintegrating have been applied for the quick elevation of dry mouth that helps us for patient compliance

Glycaemic variation in insulin treated diabetic patients with end stage renal disease on maintenance haemodialysis and its effect on cardiac electrical activity

M.D.ThesisDiabetic kidney disease remains the single most common cause of renal failure in UK, accounting for 26.9% of patients needing renal replacement therapy (UK renal registry, 2016). Mortality rates on RRT are worse for the diabetes population compared to the non-diabetic population. Diabetic patients on maintenance haemodialysis experience huge variation in their glycaemia, which is not well understood to guide appropriate therapy. ESRD patients are at higher risk of sudden cardiac death and arrhythmia is suspected to be a major cause. However there is no established guideline in detecting at risk patients for preventative therapy. We aimed to study the glycaemic variation in patients with ESRD on maintenance HD using continuous glucose monitoring for longer periods in order to help understand the variation in relation to dialysis and associated change in cardiac electrical conductivity simultaneously to explore any relation with glycaemia. In a pilot study we studied glucose variation and cardiac electrical activity using CGM and Holter monitor respectively during 37 weeks in 15 diabetic patients and 5 weeks in 5 nondiabetic subjects. Diabetic subjects had a significant variation in their glycaemia through the week. There was a significant drop in the interstitial glucose level during HD, followed by a rise in the post-HD period (preHD vs HD vs postHD: 11.4±5.1 vs 8.4±3.6 vs 11.5 ± 4.6mmol/l). There was a significant change in QTc interval from start to end of HD in this population (468 ± 42 vs 481 ± 36 vs 495 ± 49). Short but frequent episodes of arrhythmia were noted throughout the week. All diabetic patients who were prone for arrhythmias had abnormal QTc. Non-diabetic patients also experienced significant variation in IG levels and were noted to have IG in both the hypo and hyperglycaemic range. CGM helps in understanding the glycaemic variation in this population and real time recording would help in reducing the episodes of hypoglycaemia and hyperglycaemia. There is no relation between glycaemic variation or hypoglycaemia and change in QTc interval or cardiac dysrhythmias, which remain common in this population. Asymptomatic dysrhythmic episodes put these patients at risk of sudden cardiac death. The data suggest that baseline ECG and/or periodic Holter monitoring should be used in clinical care

SILVER NANOPARTICLES AND COCONUT OIL INCORPORATED BIOPOLYMER BASED ELECTROSPUN NANOFIBERS FOR WOUND DRESSING

Objective: The main aim of this study was to develop and evaluate the nanofiber loaded with coconut oil and silver nanoparticles (Ag NPs) for the treatment of wound healing by the electrospun method. Methods: The nanofibers have been created using the reduced form of silver nanoparticles and coconut oil along with Eudragit L-100 by the electrospun method. The presence of coconut oil and chemical interaction was determined by the FTIR method. XRD was made to evaluate the crystalline nature of AgNPs and Eudragit L-100. TEM was carried out to show the presence of AgNPs on the surface of nanofibers and SEM represents the diameter of the fiber. The antibacterial activity of nanofibers was carried out using a disk diffusion assay. Results: The diameter of the fibers was diminished by the excess of AgNPs in the fibers, while it increases by the coconut oil concentration, enhancing the nanofiber's hydrophilicity. FTIR spectroscopy was found in the range of coconut oil at 3553 cm-1for O-H stretch, 1365 cm-1, and 1240 cm-1 for the C-O stretch of ester groups. The diffraction peaks at 2θ of 38.5°, 44.6°, and 64.7°, in the XRD spectra of nanofiber, changed with silver NP affirming the total decrease of Ag salt. The bactericidal activity has been carried out between Escherichia coli and Staphylococcus aureus showing zones of inhibition of 20.0±0.2 mm and 14.8±0.4 mm, exhibiting excellent bactericidal characteristics for wound healing. Conclusion: The formulated nanofibers were obtained to offer protection against external agents and help in the regeneration of new tissue

Optical, structural and thermal properties of hybrid PVA/CaAl2ZrO6 nanocomposite films

This report focuses on fabrication, characterization, and fundamental optical, structural and thermal properties of PVA/calcium aluminum doped zirconate (CaAl2ZrO6) nanocomposites (NCs) films. The PVA-NCs with different amounts viz., 2, 4, 6 and 8 wt% of calcium aluminum zirconate (CaAl2ZrO6) have been fabricated using solvent casting technique. The NC films structural and morphology have been investigated by X-ray diffraction, FTIR and scanning electron microscopy. TEM result indicates that the size of nanoparticles (NPs) lies in the range 10-23nm.. Thermal studies have been evaluated by differential scanning calorimetry (DSC). The optical properties of NCs has been investigated by UV-vis spectroscopy, where the optical study reveals an increased refractive index from 1.22 to 2.23 at a wave length of 300 nm, where as the band gap energy (E-g) is reduced from 5.01 to 3.32 eV for PVA to PVA/8wt% CaAl2ZrO6, respectively. The dielectric studies, optical conductivity measurements and Urbach energy analysis also supports the dopant dependent optical property, tuning of PVA/CaAl2ZrO6 NC films to enable effective material property engineering to suit specified application requirements

Encapsulation of Lornoxicam into spermaceti microspheres and comparative bioavailability study

In this study, Lornoxicam (LX) loaded spermaceti (SC) microspheres were prepared using meltable emulsified dispersion cooling induced solidification technique and the bioavailability of the marketed product (Flexispaz® capsule-reference-product A) was compared with the optimized formulation (lornoxicam loaded spermaceti microspheres–test–product B). Morphological studies of wax microspheres were evaluated using scanning electron microscopy (SEM). The SEM images showed the spherical shape of wax microspheres and more than 97% of the isolated microspheres were in the size range 309-317 μm. Differential scanning calorimetry (DSC), Fourier transforms infrared (FTIR) spectroscopy and stability studies showed that the drug after encapsulation with SC microspheres was stable and compatible. A single dose, randomized, complete cross over study of LX (8mg) microspheres were carried out on 10 healthy male and female Albino sheep’s under fasting conditions. Plasma LX concentrations and other pharmacokinetic parameters obtained were statistically analyzed. Based on this study, it can be concluded that drug loaded LX microspheres and Flexispaz® capsule are bioequivalent in term of the rate and extent of absorption.Key words: Lornoxicam; Wax microspheres; Release kinetics; Bioavailability; Bioequivalence

FORMULATION AND EVALUATION OF SOLID SELF MICRO EMULSIFYING DISPERSIBLE TABLET OF PIROXICAM

Objective: The aim of this study was to formulate the solid self-micro emulsifying dispersible tablets for promoting the dissolution of Piroxicam. Methods: Solubility study test was performed to know the solubility of various oil phase, surfactants, cosurfactants. Self-emulsifying grading test was done by visual grading system. Ternary phase diagrams and droplet size analysis test were performed to screen and optimize the Piroxicam-self microemulsifying drug delivery system (SMEDS). Then microcrystalline cellulose (KG802) was added as a suitable adsorbent and dispersible tablet were prepared by wet granulation compression method. Results: The final composition of Piroxicam-SMEDS was oil phase (oleic acid, 23%), surfactant (Cremophor R H-40,61%), co-surfactant (PEG-400,16%) based on the result of solubility test, self-emulsifying grading test, droplet size analysis and ternary phase diagrams. Microcrystalline cellulose (KG802) was selected based on dissolution study (98.35%) and added to liquid Piroxicam-Smeds formulation to form dispersible tablets. The in vitro dissolution study showed 98.02 % of drug release from Piroxicam-SMEDS tablets. Conclusion: Piroxicam–Self microemulsifying dispersible tablets have increased the solubility and bioavailability of the Piroxicam to a greater extent. SMEDS formulation can help the solubility of poorly water-soluble drugs