The MiniWiD-Coater. III. Effect of Application Temperature on the Dissolution Profile of Sustained-Release Theophylline Pellets Coated with Eudragit Rs 30 D

Theophylline pellets were coated with Eudragit RS 30 D in a miniature fluid-bed pan coater called MiniWiD developed recently. The dispersions were plasticized with varying amounts of triethyl citrate (TEC), dibutyl phthalate (DBP), and polyethylene glycol 6000 (PEG) and applied at different temperatures ranging from 25 to 45 °C. Theophylline release was tested by dissolution using the USP Apparatus 2 (paddle) in 0.1 N hydrochloric acid under sink conditions over 6 hours.

At a coating level of 4 % (0.7 mg/cm²) sustained-release profiles were obtained from dispersions plasticized with TEC or DBP. By reducing the amount of plasticizer from 20 to 10%, films with higher permeabilities were obtained. This effect was compensated by tempering the pellets at 50 deg;C for 24 hours. The coating temperature had little effect on the dissolution profiles of TEC-plasticized films and no effect on films with DBP.

Coatings plasticized with 20% PEG were applied at temperatures ranging from 25 to 45 °C. These films required a coating level of about 18 % (3.3 mg/cm²) to provide comparable sustained-release properties. In contrast to DBP and TEC, a strong influence of the coating temperature on the release rates was observed in which higher temperatures led to slower release rates. This behavior can be explained by the minimum film-forming temperature (MFT). Since PEG does not lower the MFT of Eudragit RS 30 D, the application of these films below the MFT of 45 °C is associated with a lower degree of film formation.     

Irrigation Modelling in the Context of Basin Water Resources

Management practices for irrigation schemes can often be improved by modelling the behaviour of a scheme and by evaluating its efficiency statistics. However, looking at an irrigation scheme without regard for other water uses within the river basin may not be effective. Efficiencies computed in this way are local and, since water may be used many times within the same basin, may not be realistic. Changes in water uses (e.g. irrigation, industrial, power production, urban water supply, navigation, environmental, recreational) will often have effects on other uses; and changes in irrigation schemes (management,structural, crop pattern) may affect other users within the basin. In addition, all water users will be affected by external changes such as changes in land cover or in climate. As demand for water increases, these links become more important until, at some stage, there is insufficient water for all users and hard choices must be made. Hydrological modelling is a tool that can be used to relate irrigation schemes to the other water uses within a river basin and can help in assessing real productivities and in evaluating alternative patterns of water usage. This paper discusses the techniques available to simulate irrigation schemes within overall basin water resources using, as an example, an intensively utilized basin in western Turkey.     

Measurement and prediction of pressure drop in two-phase flow

Experimental data for air–water two-phase co-current flow in two different pipe diameters were used to test the prediction of pressure drop by a number of existing theories and correlations. Several models are shown to be useful for prediction, particularly with the stratified regimes which have proved difficult to handle in the past. The model suggested by Olujic proved to be of particular value.     

Synthesis and characterisation of carboxylic acid and diphenylphosphine derivatives in the 1,3-diyne series: Spectral properties of polydiacetylene carboxylates

Symmetrically substituted 1,3-diynes containing hydroxyalkyl ( 1a-d ), bromoalkyl ( 1e-h ) (diphenylphosphinyl) ( 1i-k ) and carboxyalkyl ( 2a-d ) substituents have been prepared and characterised; the phosphine derivative ( 1k ) has been converted with alkyl iodides ( RI ; R = Me, Et) into bis(phosphonium) salts ( 1l and m ). During preparation of the diynedioic acid. ( 2a ), the non-centrosymmetrical diyne, HO₂CCH₂C?C—C?C(CH₂)₂OH ( 3 ), was also isolated. ⁶⁰Co γ-Irradiation of diacetylene monomers ( 2a – d ) and 10,12-tricosadiyn-1-oic acid gave the corresponding polydiacetylene derivatives ( 4a – d and 5 ), respectively. Rubidium salts of ( 4c ) and ( 4d ), a barium salt of ( 4c ), and a potassium salt of ( 5 ) were prepared and isolated; soluble potassium salts of the carboxylic acid polymers ( 4 ) were generated in aqueous solution. The effects of changes in pH on the UV/visible absorption spectra of aqueous solutions of selected carboxylic acid polydiacetylenes have been recorded, and are discussed.     

Electrical properties and positron annihilation study of (Ba<Subscript>1−<Emphasis Type="Italic">x</Emphasis></Subscript>Ho<Subscript><Emphasis Type="Italic">x</Emphasis></Subscript>)TiO<Subscript>3</Subscript> ceramics

DC resistivity, dielectric constant, dielectric loss and positron annihilation spectra of (Ba_1−x Ho _x )TiO₃ ceramics have been measured as a function of holmium concentration x. It has been found that the DC resistivity of (Ba_1−x Ho _x )TiO₃ is strongly dependent on the Ho content: it decreases three orders of magnitude and reaches a minimum at x = 0.4%. Doping with 0.6% holmium increases the permittivity of BaTiO₃ by approximately three times (from ∼1,300 to ∼4,000), with only a slight increase in the corresponding dielectric loss. The local electron density and defect concentration estimated using positron annihilation technique conforms well to the features found in the dielectric and resistivity measurements. The results have been discussed in terms of a mixed compensation model.     

Preliminary<Emphasis Type="Italic">in vitro</Emphasis> and<Emphasis Type="Italic">in vivo</Emphasis> characterizations of a sol-gel derived bioactive glass-ceramic system

This study investigates quantitatively and qualitatively the sol-gel derived bioactive glass-ceramic system (BGS)—apatite-wollastonite (AW) type granules in the size range of 0.5–1 mm, as an effective graft material for bone augmentation and restoration. Scanning electron micrographs (SEM) of the sintered granules revealed the rough material surface with micropores in the range 10–30 μm. X-ray diffraction (XRD) pattern of the granules revealed the presence of crystalline phases of the hydroxyapatite and wollastonite, and the functional groups of the silicate and phosphates were identified by Fourier transform infrared spectroscopy (FT-IR). Thein vitro cell culture studies with L929 mouse fibroblast cell line showed very few cells adhered on the BGS disc after 24 h. This could be due to the highly reactive surface of the disc concomitant with the crystallization but not due to the cytotoxicity of the material, since the cellular viability (MTT assay) with the material was 80‰ Cytotoxicity and cytocompatibility studies proved that the material was non-toxic and biocompatible. After 12 weeks of implantation of the BGS granules in the tibia bone of New Zealand white rabbits, the granules were found to be well osteointegrated, as observed in the radiographs. Angiogram with barium sulphate and Indian ink after 12 weeks showed the presence of microcapillaries in the vicinity of the implant site implicating high vascularity. Gross observation of the implant site did not show any inflammation or necrosis. SEM of the implanted site after 24 weeks revealed good osteointegration of the material with the newly formed bone and host bone. New bone was also observed within the material, which was degrading. Histological evaluation of the bone healing with the BGS granules in the tibial defect at all time intervals was without inflammation or fibrous tissue encapsulation. After 2 weeks the new bone was observed as a trabeculae network around the granules, and by 6 weeks the defect was completely closed with immature woven bone. By 12 weeks mature woven bone was observed, and new immature woven bone was seen within the cracks of the granules. After 24 weeks the defect was completely healed with lamellar bone and the size of the granules decreased. Histomorphometrically the area percentage of new bone formed was 67.77% after 12 weeks and 63.37% after 24 weeks. Less bone formation after 24 weeks was due to an increased implant surface area contributed by the material degradation and active bone remodeling. The osteostimulative and osteoconductive potential of the BGS granules was established by tetracycline labelling of the mineralizing areas by 2 and 6 weeks. This sol-gel derived BGS granules proved to be bioactive and resorbable which in turn encouraged active bone formation.     

Phosphorus Inputs to Lake Simcoe from 1990 to 2003: Declines in Tributary Loads and Observations on Lake Water Quality

Total phosphorus (TP) inputs to Lake Simcoe have led to hypolimnetic dissolved oxygen (DO) depletion and loss of cold water fish habitat. Since 1990, efforts have been made to reduce the total TP input to the lake below a defined target of 75 t/year, which was predicted to lead to reductions in spring TP concentration and improvements in end-of-summer hypolimnetic DO concentrations. The total TP load to the lake during the most recent period of record (1998/99-2003/04) ranged from 53 to 76 t/yr and averaged 67 t/yr, compared to an average of 114 t/yr estimated between 1990/91 and 1997/98 (range 85-157 t/yr). Reductions in TP loads from the catchment via tributary discharge (∼26 t) accounted for the majority of the decrease in total load between the two time periods. Total P concentrations decreased significantly in four out of six long-term monitored tributaries; however, concentrations in all six tributaries remain above the level recommended to avoid nuisance plant growth (30 μg/L). Although TP loads to the lake are currently below the target 75 t/yr, excessive growths of filamentous algae and macrophytes continue to be a problem in the nearshore zone. End-of-summer minimum hypolimnetic DO concentrations (average 4.3 mg/L, 1998/99-2003/04) remain substantially below the level (7 mg/L) that is considered protective of lake trout. Efforts to reduce TP loads to the lake therefore need to continue.     

Residual Stress Simulation of Injection Molding

In this study, distribution and history of residual stresses in plaque-like geometries are simulated based on linear thermoviscoelastic model, which helps to understand the mechanics and evolution of the residual stresses in the injection molding process. The numerical calculation of direction, combined with the specified boundary conditions. Results show that the stress variation across the thickness exhibits a high surface tensile value changing to a compressive peak value close to the surface, with the core region experiencing a parabolic tensile peak. Residual stress distribution throughout the thickness is almost same along the flowpath and the final residual stresses value near the gate is lower than the value near the end of flowpath.