Notes

Coarse Don involving High-Carbon Low-Alloyed Austenite Steel: Microhardness, Microstructure and X-ray Traits involving Put on Area.
© 2018 Published by Elsevier B.V. on behalf of Shenyang Pharmaceutical University.The aim of this study was to optimize a tablet formulation of dutasteride that is bioequivalent to a commercially available soft gelatin capsule (Avodart®). The effect of cyclodextrin on enhancing the aqueous solubility of dutasteride was investigated, after which the formulation was further optimized with solubilizing polymer and surfactant. Among the cyclodextrins tested, the highest solubility was observed when dutasteride was complexed with γ-cyclodextrin. Moreover, the addition of polyvinylpyrrolidone and Gelucire/TPGS further enhanced the solubility of dutasteride. Differential scanning calorimetry (DSC) and powder X-ray diffraction (pXRD) studies demonstrated that dutasteride existed in the amorphous form in the complex. Optimized dutasteride complexes were selected after a pharmacokinetic study in rats, and film-coated tablets were prepared by the direct compression method. In vitro dissolution profiles for the tablets of dutasteride complexes were similar to those of the reference. Moreover, pharmacokinetic parameters including the Cmax and AUC values after oral administration in beagle dogs were not significantly different from those of the reference with a relative bioavailability of 92.4%. These results suggest the feasibility of developing a tablet formulation of dutasteride using cyclodextrin complex in addition to a solubilizing polymer and surfactant. © 2018 Shenyang Pharmaceutical University. Pifithrin-μ inhibitor Published by Elsevier B.V.In this study, we show that the percutaneous absorption and brain distribution of tetramethylpyrazine (TMP) is enhanced when combined with borneol (BN) in a microemulsion-based transdermal therapeutic system (ME-TTS). The formulation of the TMP and BN microemulsion (TEM-BN-ME) was optimized in skin permeation studies in vitro following a uniform experimental design. Male Sprague-Dawley rats were used for the in vivo pharmacokinetic and tissue distribution studies of TMP-BN-ME-TTS. In the pharmacokinetic study, the TMP-BN-ME-TTS treated rats had significantly higher (P less then 0.05) C max and AUC of TMP than the TMP-ME-TTS treated rats, indicating that BN improves the rate and extent of TMP percutaneous absorption. In the tissue distribution study, the AUC of TMP in brain was significantly higher in the TMP-BN-ME-TTS group (P less then 0.05), indicating that BN facilitates the distribution of TMP in brain. In summary, BN enhanced the percutaneous absorption and brain distribution of TMP in a microemulsion-based transdermal therapeutic system. © 2018 Shenyang Pharmaceutical University. Published by Elsevier B.V.The current study was to understand how process variables of high shear wet granulations affect physical properties of granules and tablets. The knowledge gained was intended to be used for Quality-by-Design based process design and optimization. The variables were selected based on the risk assessment as impeller speed, liquid addition rate, and wet massing time. Formulation compositions were kept constant to minimize their influence on granules properties. Multiple linear regression models were built providing understanding of the impact of each variable on granule hardness, Carr's index, tablet tensile strength, surface mean diameter of granules, and compression behavior. The experimental results showed that the impact of impeller speed was more dominant compared to wet massing time and water addition rate. The results also revealed that quality of granules and tablets could be optimized by adjusting specific process variables (impeller speed 1193 rpm, water spray rate 3.7 ml/min, and wet massing time 2.84 min). Overall desirability was 0.84 suggesting that the response values were closer to the target one. The SEM image of granules showed that spherical and smooth granules produced at higher impeller speed, whereas rough and irregular shape granules at lower speed. Moreover, multivariate data analysis demonstrated that impeller speed and massing time had strong correlation with the granule and tablet properties. In overall, the combined experimental design and principal component analysis approach allowed to better understand the correlation between process variables and granules and tablet attributes. © 2018 Shenyang Pharmaceutical University. Published by Elsevier B.V.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. © 2018 Shenyang Pharmaceutical University. Published by Elsevier B.V.Although active constituents extracted from plants show robust in vitro pharmacological effects, low in vivo absorption greatly limits the widespread application of these compounds. A strategy of using phyto-phospholipid complexes represents a promising approach to increase the oral bioavailability of active constituents, which is consist of ''label-friendly" phospholipids and active constituents. Hydrogen bond interactions between active constituents and phospholipids enable phospholipid complexes as an integral part. This review provides an update on four important issues related to phyto-phospholipid complexes active constituents, phospholipids, solvents, and stoichiometric ratios. We also discuss recent progress in research on the preparation, characterization, structural verification, and increased bioavailability of phyto-phospholipid complexes. © 2018 Published by Elsevier B.V. on behalf of Shenyang Pharmaceutical University.Cellulose derivatives have gained immense popularity as stabilizers for amorphous solid dispersion owing to their diverse physicochemical properties. More than 20 amorphous solid dispersion-based products that have been approved for marketing consist of cellulose derivatives as stabilizers, thus highlighting their importance in generation of amorphous solid dispersions. These polymers offer numerous advantages like drug solubilization, crystallization inhibition and improvement in release patterns of drugs. Exploring their potential and exploiting their chemistry and pH responsive behaviour have led to the synthesis of new derivatives that has broadened the scope of the use of cellulose derivatives in amorphous formulation development. The present review aims to provide an overview of different mechanisms by which these cellulose derivatives inhibit the crystallization of drugs in the solid state and from supersaturated solution. A summary of different categories of cellulose derivatives along with the newly explored polymers has been provided. A special segment on strengths, weaknesses, opportunities, and threats (SWOT) analysis and critical quality attributes (CQAs) which affect the performance of the cellulose based amorphous solid dispersion will aid the researchers in identifying the major challenges in the development of cellulose based solid dispersion and serve as a guide for further formulation development. © 2018 Shenyang Pharmaceutical University. Published by Elsevier B.V.Thrombus formed in blood vessel is a progressive process, which would lead to life-threatening thrombotic diseases such as ischemic stroke. Unlike other diseases, the recognition of thrombus is usually in the late stage where blood vessels are largely blocked. So acute thrombotic diseases have a narrow therapeutic window, and remain leading causes of morbidity and mortality, whereas current thrombolysis therapy has limited therapeutic effects and bleeding complications. Thrombolytic agents in unwanted sites would cause hemorrhage due to the activation of plasminogen. Moreover, untargeted thrombolysis therapy require large amounts of thrombolytic agents, which in return would enhance hemorrhage risk. To improve the efficiency while minimizing the adverse effects of traditional thrombolysis therapy, novel drug delivery systems have been investigated. Various targeting strategies including ultrasound and magnetic field directed targeting, and specific binding, have been designed to deliver thrombolytic drugs to the thrombotic sites. These strategies demonstrate promising results in reducing bleeding risk as well as allowing less dosage of thrombolytic drugs with lowered clot lysis time. In this review, we discuss recent progress on targeted delivery of thrombolytics, and summarize treatment advantages and shortcomings, potentially helping to further promote the development of targeted thrombolysis. © 2019 Shenyang Pharmaceutical University. Published by Elsevier B.V.The object of the study was to develop a quick and reproducible accelerated in vitro release method to predict and deduce the function of the real time (37 °C) release for long acting PLGA microspheres. The method could be described in several steps. First, the release of the microspheres were studied using the sample and separate method at 37 °C with normal orbital shaking and elevated temperatures with magnetic stirring to further accelerate the release. Second, the most similar profile at elevated temperatures with the real time release was chosen with the help of the n value in the fitted Korsmeyer-Peppas Function. Third, the Weibull function and conversion ratio were used to deduce the function of real time release according to the chosen profile at elevated temperatures. The key point in this study was to provide a quick and precise method to predict the real time release for long acting progesterone PLGA microspheres. So the elevated temperatures coupled with magnetic stirring were used to accelerate the release further, and when there have many similar release profiles with the real time release at elevated temperatures, releasing time at elevated temperatures and the R2 of the final deduced function will be used to help choosing the most similar release profile with the real time release. Four different types of progesterone PLGA microspheres were used to verify the method, and all the deduced function correlated well with the real time releases, for R 2  = 0.9912, 0.9781, 0.9918 and 0.9972, respectively. © 2018 Shenyang Pharmaceutical University. Published by Elsevier B.V.
My Website: https://www.selleckchem.com/products/pifithrin-u.html