Monolithic LC method applied to fesoterodine fumarate low dose extended-release tablets:Dissolution and release kinetics

A dissolution test for fesoterodine low dose extended-release tablets using liquid chromatographic（LC） method equipped with a C18 monolithic column was developed and validated. LC system was operated isocratically at controlled temperature（40 1C） using a mobile phase of acetonitrile：methanol：0.03 M ammonium acetate（p H 3.8）（30：15：55, v/v/v）, run at a flow rate of 1.5 m L/min and detected at 208 nm. The best dissolution conditions for this formulation were achieved using a USP apparatus 2（paddle） at 100 rpm and 900 m L of phosphate buffer at p H 6.8 as the dissolution medium.Validation parameters such as the specificity, linearity, accuracy, precision, and robustness were evaluated according to international guidelines, giving results within the acceptable range. The kinetic parameters of drug release were also investigated using model-dependent methods and the dissolution profiles were best described by the Higuchi model. The validated dissolution test can be applied for quality control of this formulation.

Effects of polyamines on the early development of cystocarps,spore release,survival,and germination rate of Gracilariopsis lemaneiformis

Three polyamines(PAs)(spermidine(Spd),spermine(Spm),and putrescine(Put))were used as growth regulators to the marine macroalgae Gracilariopsis lemaneiformis and to female gametophyte and reproductive tissues(cystocarps were constructed),which led to early maturation of cystocarps and spore release.Laboratory cultivation revealed that exogenous PA application accelerated the development of cystocarps,and the mean sporeling growth rate was 20%–50%/d during the initial week of cultivation.The spore count(SC),survival rate(SR),and germination rate(GR)of G.lemaneiformis showed different responses to PA(10-6 mol/L and 10-3 mol/L)treatments under different temperatures(18,26,and 34℃),light intensities(30,60,and 90μmol photons/(m^(2)·s)),salinities(25,30,and 35),and nutrient levels(25꞉2.5,50꞉5.0,and 75꞉7.5μmol/L NH4Cl꞉K2HPO4),and the optimal conditions were 26℃,light intensity of 60μmol/(m^(2)·s),salinity of 35,and nutrient level of 50꞉5.0μmol/L NH4Cl꞉K2HPO4.Under the optimum conditions,the SC per cystocarp increased by 82.38%,and the spore SR and GR increased by 33.07%and 46.44%,respectively.Each experiment lasted for 7 days,with the highest SC on Day 4 and plateauing on Day 7.The results indicate that PAs could promote the early maturation,spore release,survival,and germination of G.lemaneiformis under laboratory conditions.

Effect of CaO/SiO_(2) Slag Mass Ratio on Dissolution Rate of Alumina-based Refractory Ceramics

The dissolution of alumina-based refractory ceramics in CaO-Al2O3-SiO_(2)slag melts was performed based on the in-situ observation system of an ultra-high-temperature laser confocal microscope,and the effect of the CaO/SiO_(2)slag mass ratio(C/S ratio)on the dissolution rate of alumina-based refractory ceramics was investigated.The results indicate that the dissolution rate increases with an increase of the C/S ratio and is mainly controlled by diffusion.During the early stage of dissolution,for all C/S ratios,the dissolution process conforms to the classical invariant interface approximation model.During the later stage of dissolution,when the C/S ratio is≥6,the dissolution process is significantly different from the model above because of the formation of a thick interfacial layer,which can be explained by dissolution kinetics.

Silymarin-laden PVP-PEG polymeric composite for enhanced aqueous solubility and dissolution rate: Preparation and in vitro characterization

The aim of this work was to develop, optimize and characterize a silymarin-laden polyvinylpyrrolidone(PVP)-polyethylene glycol(PEG) polymeric composite to resolve low aqueous solubility and dissolution rate problem of the drug. A number of silymarin-laden polymeric formulations were fabricated with different quantities of PVP K-30 and PEG 6000 by the solvent-evaporation method. The effect of PVP K-30 and PEG 6000 on the aqueous solubility and dissolution rate was investigated. The optimized formulation and its constituents were characterized using powder X-ray diffraction(PXRD), differential scanning calorimetry(DSC), scanning electron microscopy(SEM) and Fourier transform infrared spectroscopy(FTIR) techniques. Both the PEG 6000 and PVP K-30 positively affected the aqueous solubility and dissolution rate of the drug. In particular, a formulation consisting of silymarin, PVP K-30 and PEG 6000(0.25/1.5/1.5, w/w/w) furnished the highest solubility(24.3972.95 mg/mL) and an excellent dissolution profile( $100% in 40 min). The solubility enhancement with this formulation was $ 1150-fold as compared to plain silymarin powder. Moreover, all the constituents existed in the amorphous state in this silymarin-laden PVP-PEG polymeric composite. Accordingly, this formulation might be a promising tool to administer silymarin with an enhanced effect via the oral route.

Criterion of local energy release rate of gob instability in deep mines considering unloading stress path

The stress path characteristics of surrounding rock in the formation of gob were analyzed and the unloading was solved. Taking Chengchao Iron Mine as the engineering background, the model for analyzing the instability of deep gob was established based on the mechanism of stress relief in deep mining.The energy evolution law was analyzed by introducing the local energy release rate index(LERR), and the energy criterion of the instability of surrounding rock was established based on the cusp catastrophe theory. The results show that the evolution equation of the local energy release of the surrounding rock is a quartic function with one unknown and the release rate increases gradually during the mining process.The calculation results show that the gob is stable. The LERR per unit volume of the bottom structure is relatively smaller which means that the stability is better. The LERR distribution showed that there was main energy release in the horizontal direction and energy concentration in the vertical direction which meets the characteristics of deep mining. In summary, this model could effectively calculate the stability of surrounding rock in the formation of gob. The LERR could reflect the dynamic process of energy release,transfer and dissipation and that provided an important reference for the study of the stability of deep mined out area.

Dissolution rate determination of alumina in molten cryolite-based aluminum electrolyte

Determination of dissolution rate of alumina is one of the classical problems in aluminum electrolysis. A novel method which can measure the dissolution rate of alumina was presented. Effect of factors on dissolution rate of alumina was studied intuitively and roundly using transparent quartz electrobath and image analysis techniques. Images about dissolution process of alumina were taken at an interval of fixed time from transparent quartz electrobath of double rooms. Gabor wavelet transforms were used for extracting and describing the texture features of each image. After subsampling several times, the dissolution rate of alumina was computed using these texture features in local neighborhood of samples. Regression equation of the dissolution rate of alumina was obtained using these dissolution rates. Experiments show that the regression equation of the dissolution rate of alumina is y=-0.000 5x^3＋0.024 0x^2-0.287 3x＋ 1.276 7 for Na3AIF6-AIF3-Al2O3-CaF2-LiF- MgF2 system at 920 ℃.

Release rate kinetics of corrosion inhibitor loaded halloysite nanotube-based anticorrosion coatings on magnesium alloy AZ91D

Halloysite nanotubes were used as nanocontainers to hold corrosion inhibitors such as Ce^(3+)-Zr^(4+),2-mercaptobenzothiazole and 8-hydroxyquinoline in their lumen.An acid assisted etching of the nanotubes was carried out with a view to increase the lumen diameter and thereby,increase the amount of loading of the corrosion inhibitor.The morphology of as-received and etched halloysite nanotubes was ob-served using TEM analysis.The loading of corrosion inhibitors was confirmed using SEM-EDS and BET analysis.Polymeric microcapsules were used as capping agents for the ends of the loaded HNTs following which,they were dispersed into a hybrid sol-gel silica matrix.Dip coating method was used to generate coatings on AZ91D substrates followed by heat treatment at 130℃ for 1 h.The release rate kinetics of corrosion inhibitors from as-received and etched nanotubes was investigated in buffer solutions of 3.5 wt%NaCl at different pH.The release mechanism of corrosion inhibitors from the HNT lumen was validated using various semi-empirical models.Coatings were also evaluated for their corrosion protection ability using electrochemical techniques after exposure to 3.5 wt%NaCl solution for 120 h.Coatings generated using Ce^(3+)-Zr^(4+)loaded into as-received halloysite nanotubes have shown more effective corrosion protection when compared to other corrosion inhibitors after 120 h exposure to the corrosive medium.

Effect of Complexation with Hydroxylpropyl-β-Cyclodextrin on Solubility, Dissolution Rate and Chemical Stability of Prostaglandin E1

Aim To study the effect of complexation with hydroxylpropyl-β-cyclodextrin(HP-β-CD) on the solubility, dissolution rate and chemical stability of prostaglandin E_1 (PGE_1) ,thereby providing a basis for preparing a stable solid or aqueous preparation of PGE_1 formulatedwith HP-β-CD. Methods The effect of HP-β-CD on the solubility of PGE_1 was studied by phasesolubility method. The formation of inclusion complexes of PGE_1 with HP-β-CD in the aqueoussolution was confirmed by UV spectra, circular dichroism spectroscopy, and that in the solid stateby IR spectra and X-ray diffractome-try. An solid inclusion complex of PGE_1 with HP-β-CD wasprepared by lyophilization. The dissolution rate and stability of the inclusion complex weredetermined and compared with those of PGE_1 alone. Meanwhile, the stability of PGE_1 aqueoussolutions in the presence of HP-β-CD was studied under different pH conditions. Results Thesolubility of PGE_1 increased linearly with increasing HP-β-CD concentration in various pH bufferedsolutions, showing typical A_L-type phase solubility diagrams. The stability and dissolution rateof the solid inclusion complex of PGE_1 were significantly increased, compared with those of purePGE_1 . The stability of PGE_1 in HP-β-CD solutions was also obviously improved under acidic andbasic conditions, but the stabilizing effect was absent under neutral conditions. Conclusions Thesolubility,dissolution rate and chemical stability of PGE_1 are markedly improved by complexationwith HP-β-CD: It is quite possible to prepare a stable PGE_1 inclusion complex-containing soliddosage forms, but almost impossible to obtain a stable aqueous preparation of PGE_1 formulated withHP-β-CD.

Acoustic emission characteristics and stress release rate of coal samples in different dynamic destruction time

Considering the importance of the prediction of rock burst disasters, and in order to grasp the law of acoustic emission(AE) of coal samples in different dynamic destruction time, the SH-II AE monitoring system was adopted to monitor the failure process of coal samples. The study of the change rule of the AE numbers, energy, ‘b' value and spectrum in the micro crack propagation process of the coal samples shows that as dynamic damage time went by, AE presented high-energy counts and the accumulated counts increased during the compression phase. The AE energy and cumulative counts increased during the elastic stage. The AE blank area increased gradually and the blank lines were more and more obvious in the molding stage. The AE counts and energy showed a trend of decrease in the residual damage phase.AE ‘b' values gradually became sparse, and the large scale cracks percentage compared with micro cracks decreased and the degree of damage decreased. The AE frequency spectrum peak went from the residual damage phase to the molding phase, and finally it was nearly stable, besides the bandwidth of the main frequency is gradually narrowed. Also, the frequency peak changed from single peak frequency to bi-peak frequency and to the single peak frequency. Uniaxial compressive strength is more sensitive than the elastic modulus to dynamic damage time.

The energy release rate for hygrothermal coupling elastic materials

In the fracture problems of hydrophilic elastic materials under coupling effects of heat conduction, moisture diffusion and mechanical deformation, the conventional J-integral is no longer path independent. The value of J is unequal to the energy release rate in hygrothermal coupling cases. In the present paper, we derived a general form of the energy release rate for hygrothermal fracture problems of the hydrophilic elastic materials on the basis of energy balance equation in cracked areas. By introducing the constitutive relations and the essential equations of irreversible thermodynamics, a specific expression of the energy release rate was obtained, and the expression can be reformmulated as path independent integrals, which is equivalent to the energy release rate of the fracture body. The path independence of the integrals is then verified numerically.

MSNCs and MgO-MSNCs as drug delivery systems to control the adsorption kinetics and release rate of indometacin

Mesoporous silica cocoon materials(MSNCs) and MgO doped mesoporous silica cocoons(MgO-MSNCs) with the cocoon-like hierarchical morphology and different alkalinities were synthesized as carriers for acidic drugs. Indomethacin(IMC) was selected as a model drug and loaded into carriers. All materials and the drug-loaded samples were characterized by nitrogen adsorption, FTIR spectroscopy, transmission electron microscopy(TEM), powder X-Ray diffraction(XRD) and differential scanning calorimetry(DSC). The effect of the Mg/Si molar ratio on the kinetics and equilibrium of IMC adsorption on MgO-MSNCs was thoroughly examined, and it was found that the increase in the Mg/Si molar ratio resulted in an increasing IMC adsorption rate due to the increased affinity between alkaline MgO-MSNCs and weak acid IMC. The adsorption kinetics fitted a pseudo second-order model well. The Freundlich isotherm showed a better fit, indicating that the coverage of IMC on the surface of MgO-MSNCs was heterogeneous. The maximum adsorption capacity of adsorbent was calculated by the Langmuir isotherm equation. The Temkin equation provided further support that the IMC adsorption on MgO-MSNCs was dominated by a chemisorption process. MgO-MSNCs also have the advantage of allowing an adjustment of the drug release rate of weak acid drug. The cytotoxicity assay indicated good biocompatibility of MgO-MSNCs. Our research on MgO-MSNCs carriers demonstrated their potential therapeutic benefit for safe and effective management of IMC adsorption and in vitro release.

Analysis of energy release rate for composite delaminated cylindrical shells subjected to axial compression

In this paper, the postbuckling governing equations and the analytical expression of the energy release rates associated with delamination growth in a compression-loaded cylindrical shell are derived by using the variational principle of moving boundary and the Griffith fracture criterion. The finite difference method is used to generate the postbuckling solutions of the delaminated cylindrical shells, and with these solutions, the values of the energy release rates are determined. In simulational examples, the effects of a wide range of parameters, such as delamination sizes and depths, boundary conditions, geometrical parameters, material properties and laminate stacking sequences on the energy release rates of axisymmetrical laminated cylindrical shells are intensively discussed.

Effect of Membrane Thickness on Core Release Rate of Microcapsule

Membrane thickness of microcapsule is measured by op-tical microscope duplex focusing,the core release rate iscalculated by theoretical formula,and the effect of mem-brane thickness on release rate is revealed.As a result,with changes of formaldehyde dosage,complex coacerva-tion times,core dosage,agitation speed and emulsifica-tion time,membrane thickness and apparent diffusioncoefficient are of great importance on core release rate,but membrane thickness is dominant.

RESEARCH FOR THE STRAIN ENERGY RELEASE RATE OF COMPLEX CRACKS BY USING POINT-BY-POINT CLOSED EXTRAPOLATION APPROACH

A new extrapolation approach was proposed to calculate the strain energy release rates of complex cracks. The point_by_point closed method was used to calculate the closed energy, thus the disadvantage of self_inconsistency in some published papers can be avoided. The disadvantage is that the closed energy is repeatedly calculated: when closed nodal number along radial direction is more than two, the displacement of nodes behind the crack tip that is multiplied by nodal forces, the closed energy has been calculated and the crack surfaces have been closed, and that closed energy of middle point is calculated repeatedly. A DCB (double cantilever beam) specimen was calculated and compared with other theoretical results, it is shown that a better coincidence is obtained. In addition the same results are also obtained for compact tension specimen, three point bend specimen and single edge cracked specimen. In comparison with theoretical results,the error can be limited within 1 per cent. This method can be extended to analyze the fracture of composite laminates with various delamination cracks.

ANALYSIS OF ENERGY RELEASE RATE FOR CRACKED LAMINATES

An interface crack analysis is presented for further understanding the characteristics of the crack-tip field. The conditions under which the energy release rate components would exist are emphasized and the relations between energy release rate components and the stress intensity factors are given. Combining with the results of chasical plate theory analysis. a closed-form solution for stress intensity factors in terms of external loading as well as some geometric and material parameters for fairly general composite laminates is derived Then. an analytical solution for energy release rate components is deduced. In order to get energy release rate components under general loading condition. a mode mix parameter, Ω, must be determined separately. A methodology for determining Ω is discussed. Finally. several different kinds of laminates are examined and the results obtained could be used in engineering applications.

Comparing post-release survival and habitat use by captive-bred Cabot's Tragopan(Tragopan caboti) in an experimental test of soft-release reintroduction strategies

Background: Restoring a viable population by reintroduction is the ultimate goal of a large number of ex situ conservation projects for endangered animals. However, many reintroductions fail to establish a population in the wild, partly because released animals cannot acclimate to the native environment of the release site, resulting in very low survival rates. Acclimation training is a technique to resolve this problem, although it does not have positive results in all species. We tested whether acclimation training and soft-release could improve the reintroduction success for captive-bred Cabot's Tragopan(Tragopan caboti), an endangered pheasant in southern China.Methods: Reintroduction of captive-bred Cabot's Tragopan was carried out in the Taoyuandong National Nature Reserve, China from 2010 to 2011. We built a soft-release enclosure for acclimation training in the typical montane habitat of this pheasant. Nine birds were acclimated to the environment of this release site in this cage for more than 50 days before release("trained birds"), while 11 birds remained only in the cage for 3 days prior to release("untrained birds"). Released birds were tagged with a collar radio-transmitter.Results: Post-release monitoring revealed that the survival rate of trained birds was higher than that of untrained birds after 50 days(trained: 85.7%; untrained: 20.0%). Cox regression analysis showed that there was a significant difference in the mortality rates between the trained and untrained birds. In addition, a survey of the habitat of the experimental and the control groups showed significant differences in habitat selection between the groups.Conclusion: Our study suggests that pre-release acclimatization training is an important factor that can lead to improved survival and habitat selection of captive-bred reintroduced tragopans.

Energy Release Rates for Interface Cracks in Multilayered Structures

This paper examines the evolution of the interfacial deflection energy release rates in multilayered structures under four-point bending.The J-integral and the extended finite element method(XFEM)are adopted to investigate the evolution of the interfacial deflection energy release rates of composite structures.Numerical results not only verify the accuracy of analytical solutions for the steady-state interfacial deflection energy release rate,but also provide the evolutionary history of the interfacial deflection energy release rate under different crack lengths.In addition,non-dimensional parametric analyses are performed to discuss the effects of normalized ratios of the crack length,the elastic modulus,and the thickness on the interfacial deflection energy release rate.The results demonstrate that the elastic modulus ratio and thickness ratio have a distinct influence on the interfacial deflection energy release rate for multilayered beams.Furthermore,an unstable interfacial crack tends to occur for elastic multilayer beams with higher elastic modulus on the upper sub-beam under bending moments.The unstable interfacial fracture shows a decreasing interfacial deflection energy release rate with an increasing interfacial crack length.

Energy Release Rate Measurement of Welded Bamboo Joints

Double cantilever beam tests were used to measure the energy release rates of linear vibrational welded moso bamboo joints.The influence of the length of the preserved cracks,the different combinations of the inner and outer bamboo surfaces and the moisture content is studied herein.The experimental compliance method,which is based on linear elastic fracture mechanics and has been shown to be an ideal method,was used to analyze data with the power equation.The results show that the preserved initial crack length does not have a significant effect on the final measured energy release rate,while the moso bamboo combination does affect the properties dramatically.The welded moso bamboo joints with inner-inner surfaces have the highest energy release rate of 122 J/m^2.The average energy release of the outer-outer combination was only 102 J/m^2.The expansion of the cracks also became easier when the moisture content of the welded joints was 18.5%compared to 4.5% and 10.1%.So the moisture resistance of the welded joints should be duly improved.

Mechanism study on the effect of different surfactants on dissolution rate of recrystallized prednisolone in various concentrations

The effects of re-crystallization of prednisolone as a poorly water-soluble drug in aqueous surfactant solutions on its dissolution rate were investigated. A significant enhancement was observed for crystal dissolution rate in hydrophilic surfactants such as tween 80 and sodium lauryl sulfate （SLS）. Differential scanning calorimetry （DSC） and Fourier transform infrared spectroscopy （FT-IR） indicated the existence of both form Ⅰ and Ⅱ ofprednisolone in SLS treated crystals. The FT-IR results also showed that, only form Ⅱ could be detected in prednisolone crystals without surfactant and prednisolone form Ⅲ was produced in tween 80 treated crystals. These results were also confirmed by X-ray （XRD） diffraction and scanning electron microscopy （SEM）. In general, the results indicated that the presence of hydrophilic surfactants could generate forms Ⅱ and Ⅲ of the crystals. These forms would give rlse to the increase of prednisolone＇s dissolution rate owing to their physicochemical instability and more hydrophilic property in comparison with stable polymorph of form Ⅰ.

ON CRACK-TIP STRAIA ENERGY RELEASE RATE IN NON-PRINCIPAL DIRECTIONS OF ELASTICITY FOR SIMPLE LAYER PLATE OF COMPOSITE MATERIALS

In this paper,the fracture problem in non-principal directions of elasticity for a simple layer plate of linear-elastic orthotropic composite materials is studied.The formulae of transformation between characteristic roots,coefficients of elastic compliances in non-principal directions of elasticity and corresponding parameters in principal directions of elasticity are derived.Then,the computing formulae of strain energy release rate under skew-symmetric loading in terms of engineering parameters for principal directions of elasticity are obtained by substituting crack-tip stresses and displacements into the basic formula of the strain energy release rate.