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1.
Drug Dev Ind Pharm ; 45(8): 1258-1264, 2019 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-30995878

RESUMEN

Gemfibrozil (GEM) is cholesterol-lowering agent which is being proposed as poorly water soluble drug (PWSD). Temperature based solubility values of GEM are not yet available in literature or any pharmacopoeia/monograph. Hence, the present studies were carried out to determine the solubility of PWSD GEM (as mole fraction) in various pharmaceutically used solvents such as water (H2O), methanol (MeOH), ethanol (EtOH), isopropanol (IPA), 1-butanol (1-BuOH), 2-butanol (2-BuOH), ethylene glycol (EG), propylene glycol (PG), polyethylene glycol-400 (PEG-400), ethyl acetate (EA), dimethyl sulfoxide (DMSO) and Transcutol® (THP) at the temperatures ranging from T = 298.2 K-318.2 K under atmospheric pressure P = 0.1 MPa. Equilibrium/experimental solubilities of GEM were recorded by applying a saturation shake flask methodology and regressed using 'van't Hoff and Apelblat models'. Hansen solubility parameters for GEM and various pharmaceutically used solvents were estimated using HSPiP software. The solid states of GEM (both in pure and equilibrated states) were studied by 'Differential Scanning Calorimetry' which confirmed no transformation of GEM after equilibrium. Experimental solubilities of GEM in mole fraction were observed maximum in THP (1.81 × 10-1) followed by DMSO, PEG-400, EA, 1-BuOH, 2-BuOH, IPA, EtOH, PG, MeOH, EG and H2O (3.24 × 10-6) at T = 318.2 K and similar tendencies were also recorded at T = 298.2 K, T = 303.2 K, T = 308.2 K and T = 313.2 K. 'Apparent thermodynamic analysis' on experimental solubilities furnished 'endothermic and entropy-driven dissolution' of GEM in each pharmaceutically used solvent.


Asunto(s)
Gemfibrozilo/química , Solubilidad/efectos de los fármacos , Solventes/química , 2-Propanol/química , Acetatos/química , Glicoles de Etileno/química , Metanol/química , Polietilenglicoles/química , Temperatura , Termodinámica , Agua/química
2.
Bioresour Technol ; 201: 304-11, 2016 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-26687490

RESUMEN

In this research, organic solvent composed of hexane and methanol was used for lipid extraction from dry and wet biomass of Chlorella vulgaris. The results indicated that lipid and fatty acid extraction yield was decreased by increasing the moisture content of biomass. However, the maximum extraction efficiency was attained by applying equivolume mixture of hexane and methanol for both dry and wet biomass. Thermodynamic modeling was employed to estimate the effect of hexane/methanol ratio and moisture content on fatty acid extraction yield. Hansen solubility parameter was used in adjusting the interaction parameters of the model, which led to decrease the number of tuning parameters from 6 to 2. The results indicated that the model can accurately estimate the fatty acid recovery with average absolute deviation percentage (AAD%) of 13.90% and 15.00% for the two cases of using 6 and 2 adjustable parameters, respectively.


Asunto(s)
Chlorella vulgaris/metabolismo , Hexanos/química , Humedad , Lípidos/aislamiento & purificación , Metanol/química , Modelos Teóricos , Solventes/química , Biomasa , Ácidos Grasos/aislamiento & purificación , Liofilización , Termodinámica
3.
Pharm Biol ; 50(4): 458-67, 2012 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-22129224

RESUMEN

CONTEXT: Halophila spp. is a strong medicine against malaria and skin diseases and is found to be very effective in early stages of leprosy. Seagrasses are nutraceutical in nature and therefore of importance as food supplements. OBJECTIVE: The antibacterial, antioxidant, and anti-inflammatory activities of Halophila ovalis R. Br. Hooke (Hydrocharitaceae) methanol extract were investigated and the chemical constituents of purified fractions were analyzed. MATERIALS AND METHODS: Plant materials were collected from Pondicherry coastal line, and antimicrobial screening of crude extract, and purified fractions was carried out by the disc diffusion method and the minimum inhibitory concentration (MICs) of the purified fractions and reference antibiotics were determined by microdilution method. Antioxidant and anti-inflammatory activities were investigated in vitro. Chemical constituents of purified fractions V and VI were analyzed by gas chromatography-mass spectrometry (GC-MS), and the phytochemicals were quantitatively determined. RESULTS: Methanol extract inhibited the growth of Bacillus cereus at a minimum inhibitory concentration of 50 µg/mL and other Gram-negative pathogens at 75 µg/ml, except Vibrio vulnificus. Reducing power and total antioxidant level increased with increasing extract concentration. H. ovalis exhibited strong scavenging activity on 2,2-diphenyl-1-picrylhydrazyl (DPPH) and superoxide radicals at IC(50) of 0.13 and 0.65 mg/mL, respectively. Methanol extract of H. ovalis showed noticeable anti-inflammatory activity at IC(50) of 78.72 µg/mL. The GC-MS analysis of H. ovalis revealed the presence of triacylglycerols as major components in purified fractions. Quantitative analysis of phytochemicals revealed that phenols are rich in seagrass H. ovalis. DISCUSSION AND CONCLUSION: These findings demonstrated that the methanol extract of H. ovalis exhibited appreciable antibacterial, noticeable antioxidant, and anti-inflammatory activities, and thus could be use as a potential source for natural health products.


Asunto(s)
Antiinflamatorios/farmacología , Antioxidantes/farmacología , Hydrocharitaceae , Extractos Vegetales/farmacología , Antibacterianos/farmacología , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Bacterias/efectos de los fármacos , Bacterias/crecimiento & desarrollo , Compuestos de Bifenilo/química , Proliferación Celular/efectos de los fármacos , Células Cultivadas , Pruebas Antimicrobianas de Difusión por Disco , Relación Dosis-Respuesta a Droga , Cromatografía de Gases y Espectrometría de Masas , Humanos , Hydrocharitaceae/química , Leucocitos Mononucleares/efectos de los fármacos , Leucocitos Mononucleares/inmunología , Metanol/química , Pruebas de Sensibilidad Microbiana , Picratos/química , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Plantas Medicinales , Solventes/química , Superóxidos/química
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