Stability-Indicating HPTLC Assay for Leuprolide Acetate

JPC – Journal of Planar Chromatography – Modern TLC - A new stability-indicating HPTLC assay has been established for leuprolide acetate. Silica gel 60F254 was used as stationary phase....     

A Comment on Change of Nusselt Number Sign in a Channel Flow Filled by a Fluid-Saturated Porous Medium with Constant Heat Flux Boundary Conditions

The aim of this Letter is to show that, the Nusselt number sign might be changed without changing of heat transfer direction at the wall of channels, even for flows without viscous dissipation.     

Erratum: Investigation of drug release and 1H‐NMR analysis of the in situ forming systems based on poly(lactide‐co‐glycolide)

This paper was published online on 10 October 2008 (DOI: 10.1002/pat.1279 ) and appears in the January 2009 issue (Vol. 20, No. 1, pp. 48‐57). The following changes should be recognized: The second corresponding author should be changed to M. Rafiena. ** Correspondence to: M. Rafienia, Medical Physics and Medical Engineering Department, Isfahan University of Medical Sciences (IUMS), P.O. Box 81744‐176, Isfahan, Iran. E‐mail: m_rafienia@med.mui.ac.ir     

In situ forming PLGA implant for 90 days controlled release of leuprolide acetate for treatment of prostate cancer

In prostate cancer, hormone therapy via leuprolide acetate drug (LUP) is used to lower the level of testosterone down to castration level to effectively control the development of prostate cancer. The objective of this study was to evaluate the effective parameters in degradation and controlled release of an injectable in situ formed polymeric implant, loaded with leuprolide acetate, in order to achieve an optimum formulation for sustained drug release for 90 days with minimum burst release. The main problem associating with such implants is their high burst release. Designing an injectable implant with sustained and minimum burst release has thus become an attractive challenge in drug delivery field. Effects of type of poly(lactic‐co‐glycolic acid) 75:25 copolymers (RG752, RG756) and addition of nano‐hydroxyapatite (HA) particles on degradation rates of the implants and release profiles were examined in vitro and in vivo in a rabbit animal model. Results showed that implants containing polymers with higher molecular weights had significantly lower weight loss and molecular weight reduction. Adding nanoparticles of hydroxyapatite into poly(lactic‐co‐glycolic acid) implants caused further reduction in degradation rates, leading to a more sustained drug release in vivo, with reduced burst release. Different conventional kinetic models were applied to drug release and degradation data. The degradation data fit well to the first‐order degradation model. Higuchi model was the best kinetic release model fitted to the experimental in vitro release data. This study led to an optimum formulation (RG756:RG752 3:1 + 5% HA) with sustained leuprolide release and testosterone suppression over a 90‐day period with significant decrease of burst release phase (50%, p < 0.001) compared with the conventional Eligard formulation. The histopathology test showed that the formulated implant had no effects of toxicity or tissue necrosis in organs of the animal model. Copyright © 2017 John Wiley & Sons, Ltd.     

Microcalorimetric investigation of water vapor adsorption on silica gel

In this study, the activities of four ginsenosides Rc, Re, Rd, and Rf on splenic lymphocytes growth were studied by microcalorimetry. Some qualitative and quantitative information, such as the metabolic power–time curves, growth rate constant k, maximum heat-output power of the exponential phase P _max and the corresponding appearance peak time t _max, total heat output Q _t, and promotion rate R _p of splenic lymphocytes growth affected by the four ginsenosides were calculated. In accordance with thermo-kinetic model, the corresponding quantitative relationships of k, P _max, t _max, Q _t, R _p, and c were established, . Also, the median effective concentration (EC₅₀) was obtained by quantitative analysis. Based on both the quantitative quantity–activity relationships (QQAR) and EC₅₀, the sequence of promotion activity was Rc > Re > Rd > Rf. The analysis of structure–activity relationships showed that the number, type, and position of sugar moieties on the gonane steroid nucleus had important influences on the promotion activity of Rc, Re, Rd, and Rf on splenic lymphocytes growth. Microcalorimetry can be used as a useful tool for determining the activity and studying the quantity–activity relationship of drugs on cell.     

Computation of conjugate natural convection heat transfer from a rectangular fin on a partially heated horizontal base

In this study, a numerical investigation has been carried out to reveal the mechanism of fluid flow and heat transfer from a vertical rectangular fin attached to a partially heated horizontal base. The problem is a conjugate conduction-convection heat transfer problem with open boundaries. The governing equations for the problem are the conservation of mass, momentum and energy equations for the fluid and the heat conduction equation for the fin. The control volume technique based on the SIMPLEC algorithm with a nonstaggerred grid arrangement is employed to solve the governing equations. The effect of the heated base, on the mechanism of the fluid flow and heat transfer, is numerically investigated. Temperature distribution and flow patterns around the fin are plotted to support the discussion. Results are obtained for air at laminar and steady flow. Received on 15 May 1997     

Comparison of Uniform and Non-uniform Pressure Approaches Used to Analyze an Adsorption Process in a Closed Type Adsorbent Bed

Heat and mass transfer in an annular adsorbent bed filled with silica gel particles is numerically analyzed by uniform and non-uniform pressure approaches. The study is performed for silica gel–water pair, particle radius from 0.025 to 1 mm and two bed radii of 10 and 40 mm. For uniform pressure approach, the energy equation for the bed and the mass transfer equation for the particle are solved. For non-uniform pressure approach, the continuity and Darcy equations due to the motion of water vapor in the bed are added, and four coupled partial differential equations are solved. The changes of the adsorbate concentration, pressure, and temperature in the bed throughout the adsorption process for both approaches are obtained and compared. The obtained results showed that the particle size plays an important role on the validity of uniform pressure approach. Due to the interparticle mass transfer resistance, there is a considerable difference between the results of the uniform pressure and non-uniform pressure approaches for the beds with small size of particles such as $r_\mathrm{{p}} =$ 0.025 mm.     

The effect of solvent composition on vancomycin hydrochloride and free base vancomycin release from in situ forming implants

In situ forming drug delivery systems that are formed by solvent‐induced phase inversion have attracted extensive attention in sustained delivery of peptides and proteins. Based on the findings of our previous studies, N‐methyl‐2‐pyrrolidone (NMP) and acetone are two solvents that could improve the release profile of vancomycin from in situ forming systems based on poly(D,L‐lactide‐co‐glycolic acid). In this study, the effect of different compositions of these solvents on the release profile of hydrochloride and free base forms of vancomycin was investigated. To this end, several formulations with vancomycin (either hydrochloride or free base form) and different proportions of NMP and acetone were prepared. The cumulative drug release at specified time was determined and tested against conventional kinetic models. The surface and cross‐sectional morphology of implants were investigated by SEM. The experimental results showed that as solvent composition changed, the amount of vancomycin release during the first 12 h changed, too. The use of free base vancomycin resulted in an extended vancomycin release profile with less initial burst release. The formulation containing free base vancomycin and mixed solvents of acetone and NMP in 2:1 ratio released 70% of loaded drug in 6 weeks with near zero‐order kinetic. The best kinetic model to fit the in vitro release profiles was found to be Peppas–Sahlin model. Copyright © 2016 John Wiley & Sons, Ltd.     

Fully Developed Forced Convection Heat Transfer in a Porous Channel with Asymmetric Heat Flux Boundary Conditions

An analytical study is performed on steady, laminar, and fully developed forced convection heat transfer in a parallel plate channel with asymmetric uniform heat flux boundary conditions. The channel is filled with a saturated porous medium, and the lower and upper walls are subjected to different uniform heat fluxes. The dimensionless form of the Darcy–Brinkman momentum equation is solved to determine the dimensionless velocity profile, while the dimensionless energy equation is solved to obtain temperature profile for a hydrodynamically and thermally fully developed flow in the channel. Nusselt numbers for the lower and upper walls and an overall Nusselt number are defined. Analytical expressions for determination of the Nusselt numbers and critical heat flux ratio, at which singularities are observed for individual Nusselt numbers, are obtained. Based on the values of critical heat flux ratio and Darcy number, a diagram is provided to determine the direction of heat transfer between the lower or upper walls while the fluid is flowing in the channel.     

The effect of additives on naltrexone hydrochloride release and solvent removal rate from an injectable in situ forming PLGA implant

Biodegradable in situ forming drug delivery systems for naltrexone release are promising for post‐treatment of drug addicts. The effect of two different additives, glycerol and ethyl heptanoate, on the naltrexone hydrochloride release and solvent removal from a poly(DL ‐lactide‐co‐glycolide) (PLGA) injectable implant is presented in this article. The experimental results showed that the in vitro initial release of the drug was decreased in the presence of these additives. Ethyl heptanoate was, however, more effective than glycerol and increasing the amount of additives in PLGA solution up to 5% (w/w) resulted in a decrease of initial naltrexone release rate up to 50%. The morphological evaluation of implants using scanning electron microscopy indicated that the additives generated a less porous structure together with a finger‐like to sponge‐like transition. The solvent removal profiles of injectable implants, which can be well described by thermogravimetric and morphological analysis, were in good agreement with drug release profiles. Copyright © 2006 John Wiley & Sons, Ltd.