EFFECT OF PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR-ALPHA-AGONISTS ON DIABETES-INDUCED ACUTE KIDNEY INJURY: ROLE OF OXIDATIVE STRESS AND HYPERLIPIDEMIA

Objective: The present study investigated the possible effect of fenofibrate and gemfibrozil peroxisome proliferator-activated receptor-alpha agonist in diabetes-induced acute kidney injury (AKI) in rats.Methods: Rats were administered streptozotocin (STZ) (50 mg/kg, i.p., single dose) to induce experimental diabetes mellitus. The development of diabetic AKI was assessed biochemically and histologically. In addition, the diabetes-induced lipid profile and renal oxidative stress were assessed. The single dose of STZ produced diabetes, which induced renal oxidative stress, altered the lipid profile and subsequently produced kidney injuryAKI in 7 weeks by increasing serum creatinine, blood urea nitrogen (BUN), proteinuria, and glomerular damage. Treatment with fenofibrate and gemfibrozil (30 mg/kg p.o, 7 weeks) normalized the altered lipid profile by decreasing serum cholesterol, triglycerides, and increasing serum high-density lipoprotein in diabetic rats. Lisinopril (1 mg/kg, p.o., 7 weeks, reference compound) prevents lipid alteration and development of diabetic AKI.Result: Fenofibrate and gemfibrozil, besides hyperglycemia, significantly prevented the development of diabetic AKI by reducing (serum and tissue) oxidative stress, hyperlipidemia, serum BUN, creatinine, and urinary protein. Further, fenofibrate, but not gemfibrozil, considerably reduced renal structural and functional abnormalities in diabetic rats. The fenofibrate was more effective in attenuating the diabetes-induced AKI and renal oxidative stress as compared to treatment with and gemfibrozil.Conclusion: The fenofibrate and gemfibrozil treatment markedly prevented the diabetes-induced AKI. In comparison, the fenofibrate is found to be a superior approach to attenuate the diabetic AKI than gemfibrozil

Evaluation of physico-mechanical properties of carvedilol-cyclodextrin agglomerates obtained by emulsion solvent diffusion method

Spherical crystallization (SC) is a promising alternative for improiving micromeritic properties and dissolution rate of active pharmaceutical ingredients. In the present work spherical agglomerates of carvedilol (CAR) were prepared by emulsion solvent diffusion (ESD) method using acetone, water and dichloromethane as good solvent, poor solvent and bridging liquid, respectively. Agglomerates were prepared by using β-cyclodextrin and hydroxy propyl-β-cyclodextrin as a hydrophilic polymers. The agglomerates were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM) and were evaluated for flowability, solubility and drug release. CAR agglomerates exhibited significantly improved micromeritic properties, solubility as well as dissolution behaviors in comparison with pure CAR crystals. Differential scanning calorimetric and powder X-ray diffraction studies confirm that formulation process altered the crystalline nature of carvedilol.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Spherically agglomerated solid dispersions of valsartan to improve solubility, dissolution rate and micromeritic properties

The objective of the present work was to enhance the solubility and dissolution rate of valsartan (VAL) a poorly water soluble antihypertensive, by spherically agglomerated solid dispersions using methanol, water and dichloromethane as good solvent, poor solvent and bridging liquid, respectively. The hydrophilic polymers like polyvinyl pyrrolidone, Hydroxypropyl β-cyclodextrin, Hydroxypropyl methylcellulose were used in agglomeration process. The pure drug (VAL) and its agglomerates with different polymers were characterize by differential scanning calorimetry (DSC), X-ray diffraction (XRD), IR spectroscopic studies and scanning electron microscopy (SEM). The DSC results indicated that decrease in melting enthalpy related to disorder in the crystalline content. XRD studies also showed changes in crystallanity, IR spectroscopy revealed that there were no chemical changes in the recrystallized agglomerates. The spherically agglomerated solid dispersions with different polymers exhibited marked increase in solubility, dissolution rate and micromeritic properties (bulk density, flow property, compactability) compared with VAL. The SEM studies showed that the agglomerates posseeses a good spherical shape.Keywords: Valsartan; Spherical agglomeration; Solid dispersion; Solubility; Dissolution rate; Micromeritic properties

Evaluation of physico-mechanical properties of carvedilol-cyclodextrin agglomerates obtained by emulsion solvent diffusion method

Spherical crystallization (SC) is a promising alternative for improiving micromeritic properties and dissolution rate of active pharmaceutical ingredients. In the present work spherical agglomerates of carvedilol (CAR) were prepared by emulsion solvent diffusion (ESD) method using acetone, water and dichloromethane as good solvent, poor solvent and bridging liquid, respectively. Agglomerates were prepared by using β-cyclodextrin and hydroxy propyl-β-cyclodextrin as a hydrophilic polymers. The agglomerates were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM) and were evaluated for flowability, solubility and drug release. CAR agglomerates exhibited significantly improved micromeritic properties, solubility as well as dissolution behaviors in comparison with pure CAR crystals. Differential scanning calorimetric and powder X-ray diffraction studies confirm that formulation process altered the crystalline nature of carvedilol.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Spherically agglomerated solid dispersions of valsartan to improve solubility, dissolution rate and micromeritic properties

The objective of the present work was to enhance the solubility and dissolution rate of valsartan (VAL) a poorly water soluble antihypertensive, by spherically agglomerated solid dispersions using methanol, water and dichloromethane as good solvent, poor solvent and bridging liquid, respectively. The hydrophilic polymers like polyvinyl pyrrolidone, Hydroxypropyl β-cyclodextrin, Hydroxypropyl methylcellulose were used in agglomeration process. The pure drug (VAL) and its agglomerates with different polymers were characterize by differential scanning calorimetry (DSC), X-ray diffraction (XRD), IR spectroscopic studies and scanning electron microscopy (SEM). The DSC results indicated that decrease in melting enthalpy related to disorder in the crystalline content. XRD studies also showed changes in crystallanity, IR spectroscopy revealed that there were no chemical changes in the recrystallized agglomerates. The spherically agglomerated solid dispersions with different polymers exhibited marked increase in solubility, dissolution rate and micromeritic properties (bulk density, flow property, compactability) compared with VAL. The SEM studies showed that the agglomerates posseeses a good spherical shape.Keywords: Valsartan; Spherical agglomeration; Solid dispersion; Solubility; Dissolution rate; Micromeritic properties

Evaluation of physico-mechanical properties of carvedilol-cyclodextrin agglomerates obtained by emulsion solvent diffusion method

Spherical crystallization (SC) is a promising alternative for improiving micromeritic properties and dissolution rate of active pharmaceutical ingredients. In the present work spherical agglomerates of carvedilol (CAR) were prepared by emulsion solvent diffusion (ESD) method using acetone, water and dichloromethane as good solvent, poor solvent and bridging liquid, respectively. Agglomerates were prepared by using β-cyclodextrin and hydroxy propyl-β-cyclodextrin as a hydrophilic polymers. The agglomerates were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM) and were evaluated for flowability, solubility and drug release. CAR agglomerates exhibited significantly improved micromeritic properties, solubility as well as dissolution behaviors in comparison with pure CAR crystals. Differential scanning calorimetric and powder X-ray diffraction studies confirm that formulation process altered the crystalline nature of carvedilol.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Deer antlers- Traditional use and future perspectives

245-251Antlers are bony skeletal protuberances of the skull, and consist mainly of the protein collagen and the mineral calcium hydroxyapatite. Antlers occur in most species of the deer family (Cervidae) and are grown and shed annually, typically only by males. Traditional medical reports and clinical observations show that antler is biologically active to cure various diseases. To make antler products acceptable as nutraceuticals and functional foods, chemical and biological properties of velvet antlers have to be clearly determined. Antlers are made of chemical components consisting of sugars, fatty acids, amino acids, and nucleotides as essential molecules, which become macromolecules such as polysaccharides, lipids, proteins and nucleic acids, respectively. For their physicochemical properties, each of these macromolecules is responsible for not only antler growth and development, but also biomedical and nutraceuticals uses of antlers. Therefore, understanding chemical and molecular characteristics of antlers is crucially important to elucidate the clinical and medicinal efficacies of antlers. Hence, the review highlights information about various species of deer, its farming, antler preparation, antler composition, its traditional uses and scientific substantiation to it, dose and its future scope

Development and Evaluation of Oral Controlled Release Chlorpheniramine-Ion Exchange Resinate Suspension

An oral controlled release suspension of chlorpheniramine maleate was prepared using ion-exchange resin technology. A strong cation exchange resin Indion 244 was utilized for the sorption of the drug and the drug resinates was evaluated for various physical and chemical parameters. The drug-resinate complex was microencapsulated with a polymer Eudragit RS 100 to further retard the release characteristics. Both the drug-resinate complex and microencapsulated drug resinate were suspended in a palatable aqueous suspension base and were evaluated for controlled release characteristic. Stability study indicated that elevated temperature did not alter the sustained release nature of the dosage form indicating that polymer membrane surrounding the core material remained intact throughout the storage period