Preparation and characterisation of lornoxicam solid dispersion systems using hot melt extrusion technique

Ritesh Fule,Tarique Meer,Purnima Amin,Dinesh Dhamecha,Shyam Ghadlinge 한국약제학회 2014 Journal of Pharmaceutical Investigation Vol.44 No.1

The aim of the research study was to investigatethe ability of Soluplus and surfactant individually aswell as in combination to improve the solubility, subsequentlythe dissolution profile of lornoxicam (LORX). Alaboratory size single screw rotating extruder with temperatureand speed control parameters employed during hotmelt extrusion (HME) processing of LORX along withpolymer-surfactant blends. Soluplus used as primarysolubilizing agent for preparing solid dispersion (SD). Along with Soluplus different concentrations of surfactantssuch as PEG 400, Lutrol F127, Lutrol F68 were usedto solve the permeability issues related to LORX. Encapsulationof LORX particles inside the molten matrix ofpolymer-excipient blend was confirmed by DSC, XRD andFT-IR. Drug excipient microscopic interaction was furtherconfirmed by scanning electron microscopy (SEM). Depending upon the ratio of the polymer and surfactantsused, the solubility of the hot melt extruded LORX wasimproved and found to be in the range 35–86 lg/ml (actualaqueous solubility of LORX was found to be 0.0083 lg/ml). Dissolution profile of the extruded SD was improvedand was found to be in the range of 98–104 % within20 min (actual dissolution profile of LORX was found tobe 8 % at the end of 1 h). SEM and Raman images suggestthe formation of amorphous dispersion systems. SD wassubjected to stability studies as per ICH guidelines andfound to be stable after 6 months when analyzed by HPLC. SD prepared from HME significantly improves the solubilityand dissolution profile of LORX—a BCS class IIdrug.

Solubility and dissolution rate enhancement of lumefantrine using hot melt extrusion technology with physicochemical characterisation

Ritesh Fule,Tariq Meer,Ajay Sav,Purnima Amin 한국약제학회 2013 Journal of Pharmaceutical Investigation Vol.43 No.4

The interest in hot-melt extrusion as a drug delivery technology for the production of solid dispersion is growing rapidly. Lumefantrine (LUMF) is an antimalarial drug that exhibits poor oral bioavailability, in consequence of its poor aqueous solubility. To improve its antimalarial activity, solid dispersion formulation using hot melt extrusion technology was prepared. Appropriate selection of polymers, favoured the production of amorphous LUMF-polymer solid dispersions. The physicochemical properties of solid dispersions were characterized using scanning electron microscope, Infrared spectroscopy,differential scanning calorimetry and X-ray diffraction. LUMF SD showed enhanced dissolution rate attributed to amorphosization of LUMF. The IC50 value of LUMF SD formulations was found to be (0.084–0.213 ng/mL) i.e. 220–101 times lower than the IC50 value of pure LUMF (18.2 ng/mL) and 45–18 times lower than the IC50 value of standard antimalarial drug, chloroquine (3.8 ng/mL). Molecular dynamic simulation approach was used to investigate drug-polymer molecular interaction using computational modelling Schrodinger software. LUMF SD powder makes the Coartem therapy more operative with value-added beneficial comeback.

The Chinese Version of the Work Control Scale for Nurses: Modifying the Translation and Psychometric Testing

Wen Fule,Wang Lin,Fang Zhiyin,Zhu Jinjin,Zhang Yaqing 한국간호과학회 2020 Asian Nursing Research Vol.14 No.2

Purpose: The aim of the study was to modify and test the psychometric properties of the Chinese version of the work control scale (C-WCS). Methods: The translated scale was administered to 840 nurses in Shanghai. Validity was assessed in terms of content validity and construct validity using exploratory factor analysis and confirmatory factor analysis. Internal consistency and testeretest reliability were estimated using Cronbach a and the intraclass correlation coefficient. Results: Psychometric analyses of the C-WCS indicate high reliability and good content and construct validity. Conclusion: The C-WCS has good psychometric properties and can be used as a valid tool for measuring work control among nurses in China. The C-WCS will help to further explore the correlations between perceived work control and organizational quality indicators such as nurses' satisfaction, job stress, wellbeing, or intention to stay. It can also be used in nursing outcome studies of work control strategies.

Endophytic Fungi from Dalbergia odorifera T. Chen Producing Naringenin Inhibit the Growth of Staphylococcus aureus by Interfering with Cell Membrane, DNA, and Protein

Yuan Gao,Yubin Ji,Wenlan Li,Fuling Wang,Fuling Wang,Xiaomeng Zhang,Zhihui Niu,Lulu Zhou,Lijun Yan 한국식품영양과학회 2021 Journal of medicinal food Vol.24 No.2

This study focused on the antibacterial effects of the endophytic fungi producing naringenin from Dalbergia odorifera T. Chen against Staphylococcus aureus. The antibacterial activity was measured by the inhibition diameters, minimum inhibitory concentration (MIC), and minimum bactericidal concentration (MBC). The time-killing curve was also used to evaluate its antibacterial efficacy. The results of antibacterial activity determinations showed that endophytic fungi secondary metabolites can inhibit the growth of five pathogenic bacteria (S. aureus, Escherichia coli, Salmonella enteritidis, Pseudomonas aeruginosa, and Bacillus subtilis) and the most sensitive strain was S. aureus that had the MIC and MBC values of 0.13 and 0.50 mg/mL, respectively. The membrane permeability study was measured by a DNA leakage assay and electrical conductivity assay. Furthermore, the whole-cell protein lysates and DNA fragmentation assay was evaluated. The morphology of S. aureus treated with the endophytic fungi products was observed by scanning electron microscopy (SEM). The probable antibacterial mechanism of endophytic fungi secondary metabolites was the increased membrane permeability that leads to leaks of nucleic acids and proteins. SEM results further confirmed that the extracts can interfere with the integrity of S. aureus cell membrane and further inhibit the growth of bacteria, resulting in the death of bacteria. This study provides a new perspective for the antibacterial functions of endophytic fungi secondary metabolites for biomedical applications.

Solubility modulation of bicalutamide using porous silica

Tarique Meer,Ritesh Fule,Deepak Khanna,Purnima Amin 한국약제학회 2013 Journal of Pharmaceutical Investigation Vol.43 No.4

Objective of the present study was to explore the potential of porous silica (AEROPERL 300 Pharma)in modulating dissolution kinetics of poorly water soluble drug bicalutamide (BCL). The drug release from the developed formulation was found to be significantly higher as compared to neat BCL. This improved release kinetics of BCL may be attributed to high surface area, improved wettability and decreased crystallinity. Solid state characterization of the developed formulation was carried out with respect to IR, XRPD, SEM, DSC and dissolution. The proposed system showed a significant capability for the solubility enhancement of BCL. The dissolution profile from BCL-AEROPERL 300 Pharma (AP) system was fitted into various drug release kinetics models, in order to understand the BCL release mechanism.

Optimization the extraction of anthocyanins from blueberry residue by dual-aqueous phase method and cell damage protection study

Yuan Gao,Yubin Ji,Fuling Wang,Wenlan Li,Xiaomeng Zhang,Zhihui Niu,Zhuo Wang 한국식품과학회 2021 Food Science and Biotechnology Vol.30 No.13

Blueberry residue is usually discarded as waste,but has a high anthocyanins content. The extraction methodof anthocyanins from blueberry residue with ultrasonicassisted dual-aqueous phase system was optimized. Interms of the principle of central group and design (CCD)experimental design, three-factor and five-level responsesurface analysis was adopted to optimize the extractionconditions with the extraction rate of anthocyanins. Theoptimum extraction rate of anthocyanin was12.372 ± 0.078 mg/g. Anthocyanin extract could protectthe pBR322 DNA oxidative damage induced by Fentonreagent, increase the superoxide dismutase(SOD) and glutathioneperoxidase (GSH-Px) enzyme activities, anddecrease the H2O2-induced cell apoptosis of human normalliver cell (LO2 cell). The study indicates that the extractionrate of anthocyanin was increased by optimized ultrasonicassisted dual-aqueous phase system. The anthocyaninextract could protect DNA and LO2 cell from oxidativedamage.

Approximate solutions to one-dimensional backward heat conduction problem using least squares support vector machines

곽도영,Ziku Wu,Fule Li 충청수학회 2016 충청수학회지 Vol.29 No.4

This article deals with one-dimension backward heat conduction problem (BHCP). A new approach based on least squares support vector machines (LS-SVM) is proposed for obtaining their approximate solutions. The approximate solution is presented in closed form by means of LS-SVM, whose parameters are adjusted to minimize an appropriate error function. The approximate solution consists of two parts. The first part is a known function that satisfies initial and boundary conditions. The other is a product of two terms. One term is known function which has zero boundary and initial conditions, another term is unknown which is related to kernel functions. This method has been successfully tested on practical examples and has yielded higher accuracy and stable solutions.

APPROXIMATE SOLUTIONS TO ONE-DIMENSIONAL BACKWARD HEAT CONDUCTION PROBLEM USING LEAST SQUARES SUPPORT VECTOR MACHINES

Wu, Ziku,Li, Fule,Kwak, Do Young Chungcheong Mathematical Society 2016 충청수학회지 Vol.29 No.4

This article deals with one-dimension backward heat conduction problem (BHCP). A new approach based on least squares support vector machines (LS-SVM) is proposed for obtaining their approximate solutions. The approximate solution is presented in closed form by means of LS-SVM, whose parameters are adjusted to minimize an appropriate error function. The approximate solution consists of two parts. The first part is a known function that satisfies initial and boundary conditions. The other is a product of two terms. One term is known function which has zero boundary and initial conditions, another term is unknown which is related to kernel functions. This method has been successfully tested on practical examples and has yielded higher accuracy and stable solutions.

Shear-strain induced structural relaxation of Cu Σ3 [110](112) symmetric tilt grain boundary: The role of foreign atoms and temperature

Li Yang,Xue Hongtao,Zhou Xin,Tang Fuling,Li Xiuyan,Ren Junqiang,Lu Xuefeng 한국물리학회 2021 Current Applied Physics Vol.28 No.-

Grain boundaries (GBs) relaxation is a promising and effective strategy to improving GB stability or stabilizing nanocrystalline metals. However, previous studies mainly focused on nanocrystalline pure metals and GB behaviors therein, without considering the role of foreign atoms such as impurity or alloying atoms in GB relaxation. In this work, the shear-strain induced structural relaxation of pure Cu Σ3 [110](112) symmetric tilt GBs (STGBs), and the effects of foreign elements (Fe and Ni) and temperature on the GB relaxation were investigated in detail by molecular dynamics method. The results show that shear strain can trigger the structural relaxation of pure, Fe- and Ni-containing Cu GBs by the emission of Shockley partial dislocations from Cu GBs. Both Fe and Ni have impediment effects on the shear-strain induced GB relaxation, though the content of Fe or Ni atom (0.00165 at.%) is quite low in the GB model. The temperature cannot trigger GB relaxation independently within the considered temperature range, but play a positive role in the shear-strain induced structural relaxations of pure, Fe- and Ni-containing Cu Σ3 [110](112) STGBs. Our work might gain new insights into the mechanically induced GB relaxation in nanocrystalline copper and could be beneficial for improving the stability of Cu GBs.

Microencapsulation using aqueous dispersion of lipid matrix by fluidized bed processing technique for stabilization of choline salt

Avinash B. Gangurde,Ritesh A. Fule,Sharadchandra D. Javeer,Rahul K. Patole,Jaywant N. Pawar,Purnima D. Amin 한국약제학회 2015 Journal of Pharmaceutical Investigation Vol.45 No.2

Choline bitartrate (CBT) is a water solubleessential nutrient belongs to vitamin-B family. It is moisturesensitive in nature and marketed formulation has stabilityrelated problems during storage which curtails itseffectiveness. Waxes such as hydrogenated soya bean oil(HSO) reported to be an excellent coating carrier to reducemoisture sensitivity or hygroscopic nature of drug candidates. However, literature dictates HSO applications hasbeen explored mostly using non-aqueous methods or hotmelt techniques of formulation development. In this work,microparticles of choline bitartrate with aqueous coatingdispersion of HSO as primary carrier was successfullydeveloped using fluidized bed coating technique. Aqueousdispersion of HSO was prepared using selected binder in ahomogenizer and formed aqueous dispersion was thensprayed through 0.8 mm gun in fluidized bed processor. The microparticles were evaluated for parameters like flowproperties, morphological characteristics, drug content,encapsulation efficiency and drug release behaviour. Thesolid state characterization of optimized microparticlebased formulation was done by differential scanning calorimetry,X-ray diffractometry, infrared spectroscopy andscanning electron microscopy. The results showed thatmicroencapsulation of choline bitartrate were successfullydone by aqueous wax coating dispersion without using anyorganic solvent or hot melt techniques. Discolouration,fishy odour and drug content variation was not observedafter 6 months stability studies. Choice of proper carrier todrug ratio and selective formulation technique are criticalparameters for dispensing CBT microparticle based formulationwhich might significantly enhance itseffectiveness.