Surgery for urinary incontinence

Burch colposuspension remains the most effective surgical procedure for stress urinary incontinence with a continence rate, which shows better longevity than other methods of treatment. Sling procedures have a comparable continence rate to colposuspension and there appears to be little reduction in continence over time. It is expected that the tension-free vaginal tape will eventually supersede the open Burch colposuspension as the preferred method of primary incontinence surgery principally because it is a minimal-access procedure and medium-term data suggest similar effectiveness to colposuspension. Initial reports on the trans-obturator tape, which minimises bladder and vascular trauma, are encouraging but longer term results remain uncertain. Although the injectable agents have a lower success rate than other procedures, they may still have a role when other procedures have failed due to their low morbidity. Anterior colporrhaphy and needle suspension procedures should no longer be offered as treatments for stress urinary incontinence.The surgical options for detrusor activity should be considered when pharmacological options have been exhausted. Appropriate patient selection is crucial when choosing which surgical option would be most suitable, especially as many of these procedures carry with them a significant risk of morbidity. Some surgical options are becoming less invasive and modern developments, such as intravesical botulinum toxin injection may in future become a first line treatment option for detrusor overactivity.     

Novel biocidal polymers based on branched and linear poly(hydroxystyrene)

New biocidal polymers based on branched as well as linear poly(p-hydroxystyrene) were synthesized. Biocidal polymers were synthesized in two steps by creation of active centers via chloroacetylation of linear and branched poly(p-hydroxystyrene) using chloroacetyl chloride. The second step involves the immobilization of onium salts onto the chloroacetylated polymers. All the prepared polymers were characterized using elemental microanalysis, FT-IR, ¹H NMR spectra, and TGA. Antimicrobial activity of the prepared polymers was tested against various pathogenic microorganisms. The antimicrobial activity was found to be affected by the active group and the tested microorganism. The phosphonium salts showed higher activity than ammonium salts.     

Thermal studies on paper treated with flame‐retardant

Sodium silicate and sodium borate were tested as flame retardants on two types of paper sheet (100% rice straw pulp paper with a high silica content while the other consisted of 100% wood pulp paper). After addition of inorganic flame retardant salts (sodium silicate and sodium borate) on to the two samples of paper, the thermal behaviour of the treated paper sheets revealed differences in the course of the differential thermal analysis curves. The thermal analysis studies were carried out under an oxidizing atmosphere using differential thermal (DTA) and thermogravimetric (TGA) analysis. The flame retardants used in this study reduced the amount of volatile products formed during decomposition of the paper and increased the weight loss due to formation of char for the treated papers. The thermal degradation of paper can be considered as a first order degradation. Two stages of thermal degradation were kinetically differentiated, namely, a volatilization stage and a decarbonization stage. The activation energy for these two stages were calculated. The addition of flame‐retarding salts decreased the activation energy for both stages. Sodium silicate salt showed more reduction of activation energy than sodium borate, especially for the rice straw paper. Copyright © 1999 John Wiley & Sons, Ltd.     

Identification of Novel Circulating miRNAs in Patients with Acute Ischemic Stroke

Ischemic strokes are associated with significant morbidity and mortality, but currently there are no reliable prognostic or diagnostic blood biomarkers. MicroRNAs (miRNAs) regulate various molecular pathways and may be used as biomarkers. Using RNA-Seq, we conducted comprehensive circulating miRNA profiling in patients with ischemic stroke compared with healthy controls. Samples were collected within 24 h of clinical diagnosis. Stringent analysis criteria of discovery (46 cases and 95 controls) and validation (47 cases and 96 controls) cohorts led to the identification of 10 differentially regulated miRNAs, including 5 novel miRNAs, with potential diagnostic significance. Hsa-miR-451a was the most significantly upregulated miRNA (FC; 4.8, FDR; 3.78 × 10⁻⁸⁵), while downregulated miRNAs included hsa-miR-574-5p and hsa-miR-142-3p, among others. Importantly, we computed a multivariate classifier based on the identified miRNA panel to differentiate between ischemic stroke patients and healthy controls, which showed remarkably high sensitivity (0.94) and specificity (0.99). The area under the ROC curve was 0.97 and it is superior to other current available biomarkers. Moreover, in samples collected one month following stroke, we found sustained upregulation of hsa-miR-451a and downregulation of another 5 miRNAs. Lastly, we report 3 miRNAs that were significantly associated with poor clinical outcomes of stroke, as defined by the modified Rankin scores. The clinical translation of the identified miRNA panel may be explored further.     

Living polymerization

Summary Isoprene was polymerized using very low concentration of n-Butyllithium in bulk and in different hydrocarbon and polar solvents. The concentration of n-Bu-lithium was kept constant to correlate the influence of solvent on the stereoregularity of the resulting polyisoprene.     

Continuous potentiometric monitoring of viagra (sildenafil) in pharmaceutical preparations using novel membrane sensors

Two potentiometric sensors responsive to sildenafil citrate (SC) drug (the active component of viagra) are described, characterized, compared and used for drug assessment. The sensors are based on the use of the ion-association complexes of (SC) cation with tungstophosphate (TP) and reineckate (Re) anions as electroactive materials in plasticized poly(vinyl chloride) membranes. The sensors demonstrate fast near-Nernstian response for SC over the concentration ranges 1.0×10⁻²–7.9×10⁻⁷ and 1.0×10⁻²–1.0×10⁻⁶ M with detection limits of 0.53 and 0.67 μg ml⁻¹ over pH 3–6 for TP and Re based membrane sensors, respectively. The sensors display good selectivity for SC drug over many nitrogeneous compounds, some inorganic cations and excipients and diluents commonly used in drug formulations. Validation of the assay methods with both sensors by measuring the lower detection limit, range, accuracy, precision, repeatability and between-day-variability reveals good performance characteristics confirming applicability for continuous determination of SC in pharmaceutical formulations and in spiked human serum. A membrane incorporating SC–TP complex in a tubular flow detector is used in a two channel flow injection set up for continuous monitoring of the drug at a frequency of 25–30 samples h⁻¹. The results obtained with drugs containing 50–100 mg SC tablet⁻¹ show a mean standard deviation of ±2% of the nominal which agree fairly well with data obtained by spectrophotometry.     

Preparation and evaluation of enteric coated tablets of hot-melt extruded lansoprazole

Abstract

The objective of this work was to use hot-melt extrusion (HME) technology to improve the physiochemical properties of lansoprazole (LNS) to prepare stable enteric coated LNS tablets. For the extrusion process, we chose Kollidon^® 12?PF (K12) polymeric matrix. Lutrol^® F 68 was selected as the plasticizer and magnesium oxide (MgO) as the alkalizer. With or without the alkalizer, LNS at 10% drug load was extruded with K12 and F68. LNS changed to the amorphous phase and showed better release compared to that of the pure crystalline drug. Inclusion of MgO improved LNS extrudability and release and resulted in over 80% drug release in the buffer stage. Hot-melt extruded LNS was physically and chemically stable after 12 months of storage. Both formulations were studied for compatibility with Eudragit^® L100-55. The optimized formulation was compressed into a tablet followed by coating process utilizing a pan coater using L100-55 as an enteric coating polymer. In a two-step dissolution study, the release profile of the enteric coated LNS tablets in the acidic stage was less than 10% of the LNS, while that in the buffer stage was more than 80%. Drug content analysis revealed the LNS content to be 97%, indicating the chemical stability of the enteric coated tablet after storage for six months. HME, which has not been previously used for LNS, is a valuable technique to reduce processing time in the manufacture of enteric coated formulations of an acid-sensitive active pharmaceutical ingredient as compared to the existing methods.     

Brain-targeted intranasal zaleplon solid dispersion in hydrophilic carrier system; 23 full-factorial design and in vivo determination of GABA neurotransmitter

Intranasal zaleplon solid dispersion was formulated to enhance the solubility, bioavailability and deliver an effective therapy. Zaleplon belongs to Class II drugs, and undergoes extensive first-pass metabolism after oral absorption exhibiting 30% bioavailability. A 2³ full-factorial design was chosen for the investigation of solid dispersion formulations. The effects of different variables include drug to carrier ratio (1:1 and 1:2), carrier type (polyethylene glycol 4000 and poloxamer 407), and preparation method (solvent evaporation and freeze drying) on different dissolution parameters were studied. The dependent variables determined from the in vitro characterization and their constraints were set as follows: minimum mean dissolution time, maximum dissolution efficiency and maximum percentage release. Numerical optimization was performed according to the constraints set based on the utilization of desirability functions. Differential scanning calorimetry, infrared spectroscopy, X-ray diffraction and scanning electron microscopy were performed. Ex vivo estimation of nasal cytotoxicity and assessment of the γ-aminobutyric acid level in plasma and brain 1?h after nasal SD administration in rabbits compared to the oral market product were conducted. The selected ZP-SD, with a desirability 0.9, composed of poloxamer 407 at drug to carrier ratio 1:2 successfully enhanced the bioavailability showing 44% increase in GABA concentration than the marketed tablets.     

Synthesis, characterization polymerization and antibacterial properties of novel thiophene substituted acrylamide

Ethyl 2-acrylamido-4,5,6,7-tetrahydrobenzo [b] thiophene-3-carboxylate (ETTCA) has been synthesized and its structure has been elucidated by elemental analysis and spectral tools. Free radical polymerization of (ETTCA) has been conducted in several solvents using azobisisobutyronitrile (AIBN) as an initiator. The kinetic parameters of polymerization of the ETTCA were investigated, and it was found that the polymerization reaction follows the conventional free radical scheme. The overall activation energy of polymerization ΔE was determined (ΔE = 45.11 kJ mol⁻¹). The copolymerization of ETTCA with three conventional monomers was carried out in dioxane at 65 °C. The monomer reactivity ratios for the copolymerization of ETTCA with methyl methacrylate (MMA), vinyl acetate (VA) and vinyl ether (VE) were calculated. Thermal stability of the ETTCA polymer and its copolymers were investigated by thermogravimetric analysis. It has been found that the prepared polymer (PETTCA) and its copolymers with VA have moderate biological activity and highly dependent on the copolymer composition.     

Corrosion Inhibition Efficiency,Electrochemical and Quantum Chemical Studies of Some New Nonionic Surfactants for Carbon Steel in Acidic Media

In this work, three types of nonionic surfactant as corrosion inhibitors were synthesized. The chemical structure of the prepared inhibitors was confirmed using FT‐IR and ¹H‐NMR spectroscopy. The surface tension and thermodynamic properties of these inhibitors were investigated. The corrosion inhibition efficiency of these surfactants was investigated on a carbon steel surface in 1 M HCl solution by weight loss and electrochemical measurements. Untreated and treated steel surfaces were characterized by scanning electron microscopy. Results show that the inhibition efficiency of the prepared inhibitors increases with increasing the ethylene oxide units. Also, the potentiodynamic polarization curves indicated that the investigated inhibitors behave as a mixed type inhibitor. Adsorption of these surfactants on the carbon steel surface was found to obey Langmuir's adsorption isotherm. The computed quantum chemical properties viz., electron affinity (EA), highest occupied molecular orbital (E_HOMO), the lowest unoccupied molecular orbital (E_LUMO), energy gap ΔE = E_HOMO ? E_LUMO, dipole moment (μ), polarizability and total energy (E_T) show good correlation with experimental inhibition efficiency.