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Characterization of the uptake of rocuronium and digoxin in human hepatocytes: carrier specificity and comparison with in vivo data cheap glimepiride 1 mg online diabetes insipidus tijdens zwangerschap. Stereoselective inhibition by the diastereomers quinidine and quinine of uptake of cardiac glycosides into isolated rat hepatocytes cheap glimepiride 4mg online diabetes insipidus management guidelines pdf. Role of P-glycoprotein in renal tubular secretion of digoxin in the isolated perfused rat kidney cheap 2 mg glimepiride amex brewers yeast and diabetes in dogs. Inhibition of P-glycoprotein-mediated drug transport: a unifying mechanism to explain the interaction between digoxin and quinidine [see comments]. Role of P-glycoprotein as a secretory mechanism in quinidine absorption from rat small intestine. Contribution of oatp (organic anion- transporting polypeptide) family transporters to the hepatic uptake of fexofenadine in humans. Inhibition of oat3-mediated renal uptake as a mechanism for drug-drug interaction between fexofenadine and probenecid. P-glycoprotein plays a major role in the efflux of fexofenadine in the small intestine and blood-brain barrier, but only a limited role in its biliary excretion. Lack of dose-dependent effects of itraco- nazole on the pharmacokinetic interaction with fexofenadine. The effect of short- and long-term administration of verapamil on the disposition of cytochrome P450 3A and P-glycoprotein substrates. Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. Effect of grapefruit juice volume on the reduction of fexofenadine bioavailability: possible role of organic anion transporting poly- peptides. Evaluation of peppermint oil and ascorbyl palmitate as inhibitors of cytochrome P4503A4 activity in vitro and in vivo. Grapefruit juice reduces the oral bioavail- ability of fexofenadine but not desloratadine. Increase in cerivastatin systemic exposure after single and multiple dosing in cyclosporine-treated kidney transplant recipients. Inhibition of transporter-mediated hepatic uptake as a mechanism for drug-drug interaction between cerivastatin and cyclosporin A. Effects of organic anion transporting polypeptide 1B1 haplotype on pharmacokinetics of pravastatin, valsartan, and temocapril. Polymorphic organic anion transporting polypeptide 1B1 is a major determinant of repaglinide pharmacokinetics. Multiple interactions of cimetidine and pro- benecid with valaciclovir and its metabolite acyclovir. Effects of probenecid on the pharma- cokinetics and elimination of acyclovir in humans. Pharmacokinetics of intravenously admin- istered cefmetazole and cefoxitin and effects of probenecid on cefmetazole elimi- nation. Pharmacokinetic interactions of cefprozil with food, propantheline, metoclopramide, and probenecid in healthy volunteers. Comparison of dose doubling with pro- benecid for sustaining serum cefuroxime levels. Clinical pharmacokinetics of cidofovir in human immunodeficiency virus-infected patients. Effect of probenecid on the distribution and elimination of ciprofloxacin in humans. The inhibitory effect of probenecid on renal excretion of famotidine in young, healthy volunteers. Different effects of three transporting inhibitors, verapamil, cimetidine, and probenecid, on fexofenadine pharmacoki- netics. The anti-influenza drug oseltamivir exhibits low potential to induce pharmacokinetic drug interactions via renal secretion-correlation of in vivo and in vitro studies. Fluorescence-based assay for the interaction of small molecules with the human renal organic anion transporter 1. Cytotoxicity of antiviral nucleotides adefovir and cidofovir is induced by the expression of human renal organic anion transporter 1. A physiologically based kidney model for the renal clearance of ranitidine and the interaction with cimetidine and probenecid in the dog. Drug inhibition of penicillin tubular secretion: concordance between in vitro and clinical findings. Effect of penicillin on the renal tubular secretion of methotrexate in the monkey. Characterization of methotrexate transport and its drug interactions with human organic anion transporters. Quantitative evaluation of the drug-drug interactions between methotrexate and nonsteroidal anti-inflammatory drugs in the renal uptake process based on the contribution of organic anion transporters and reduced folate carrier. Structural specificity of mucosal-cell transport and metabo- lism of peptide drugs: implication for oral peptide drug delivery. Cephalosporins: determination of intrinsic membrane absorption parameters in the rat intestine in situ. Positively cooperative sites for drug transport by P-glycoprotein with distinct drug specificities. In vivo evaluation of P-glycoprotein function at the blood-brain barrier in nonhuman primates using [11C]verapamil. Protein distribution diet restores motor function in patients with dopa-resistant ‘‘off’’ period. Characterization of the large neutral amino acid transport system of bovine brain microvessel endothelial cell monolayers. Facilitated transport of melphalan at the rat blood-brain barrier by the large neutral amino acid carrier system. Genipin enhances Mrp2 (Abcc2)-mediated bile formation and organic anion transport in rat liver. Role of nuclear receptors in the adaptive response to bile acids and cholestasis: pathogenetic and therapeutic considerations. Phenobarbital confers its diverse effects by activating the orphan nuclear receptor car. The quantitative prediction of in vivo enzyme- induction caused by drug exposure from in vitro information on human hepatocytes. Induction of P-glycoprotein by rifampin increases intestinal secretion of talinolol in human beings: a new type of drug/drug interaction. Differential regulation of sinusoidal and canalicular hepatic drug transporter expression by xenobiotics activating drug- sensing receptors in primary human hepatocytes. Regulation of mouse organic anion-transporting polypeptides (Oatps) in liver by prototypical microsomal enzyme inducers that acti- vate distinct transcription factor pathways.
Anhydrous solvent-based suspension: waterproof but not smudge- proof and difﬁcult to remove buy generic glimepiride online diabetes mellitus type 2 nursing interventions. Water-in-oil emulsion: waterproof but not smudge-proof and can be removed with soap and water cheap glimepiride 1mg visa diabetes type 2 overweight. Oil-in-water emulsion: ‘‘water-based’’ if the ﬁlm is sufﬁciently ﬂexi- ble purchase 2 mg glimepiride with visa diabetes mellitus definition cdc, can be ﬂake-proof and smudge-proof. Additional ﬁlm former: solution polyacrylate (improves ﬂake resistance); emulsion polyacrylate; polyurethane; polyvinyl acetate; rosin derivatives; di- methiconol; proteins: wheat, soy, corn, keratin, oat, silk. Manufacturing: procedure is general oil-in-water emulsiﬁcation procedure except that iron oxides are ﬁrst wet and milled in the water phase prior to emulsi- ﬁcation and ﬁnal product goes through a colloid mill, roller mill, or homogenizer. Solvent-Based Hard, high melting point waxes; rosin derivative (optional); wetting agent; pig- ment; suspending agent (organoclay); volatile solvent (to achieve wax solubil- ity)—petroleum distillate; cyclomethicone. Preservatives: parabens; Plasticizer: lanolin or derivative, liquid fatty alcohol. Additives: emulsion polymer (optional); preservative: formaldehyde donor (not for use in Japan). Anhydrous Mascara Ingredients Solvents—branched chain hydrocarbons and petroleum distillates, isopara- fﬁnic hydrocarbons, and volatile silicones. Waxes—beeswax and its derivatives, candelilla, carnauba, parafﬁn, poly- ethylene, microcrystalline, castor, synthetic, ceresin, and ozokerite. Resins (could be introduced, but do not have to be)—include aromatic/ aliphatic, hydrogenated aromatics, polyterpene, synthetic, rosin, acrylics, and silicones. Gellants—clays (stearalkonium hectorite, quaternium-18 bentonite, quater- nium-18 hectorite), metal soaps (Al, Zn stearates). Brush/rod/wiper: works complementarily with each other to deliver re- quired product attributes. For a thickening mascara, the following are required: larger diameter rod; larger diameter wiper; larger brush with signiﬁcant spacing between the bristles. For a deﬁning mascara, the following are suggested: smaller diameter rod; smaller diameter wiper; brush with minimal spacing between the bristles. Brush materials, ﬁber diameter, brush shape, ﬁber shape, ﬁber length, wire diameter, and the number of turns in the wire all affect performance. Decorative Products 301 Creme Eyeshadows Generally, cream eye shadows are another form of eye shadow not as popular as the pressed form. They are similar to cream eye shadows but contain high melting point waxes to make them moldable. Waxes: similar to those utilized in the anhydrous waterproof mascaras although at lower concentrations. For enhanced textural properties, higher solids loading, improved application and coverage, use surface treated raw materials whose coatings are neither tempera- ture nor solvent sensitive. Balance the absorption of ﬁllers to main similar tex- tures throughout the shade range. Eyeliners Eyeliners frame the eye while adding shape or changes the shape of the eye. They give the illusion of a larger or smaller eye bringing out the color contrast between the iris and white of the eye. Cake eyeliner was popular in the past and was a wettable pressed cake applied with a wet brush. Pencils Pencils are used in general for coloring the eyebrows and eyelids, although they are now popular as lipsticks, lip liner, and blushers depending on the hardness of the pencil and the color composition. Chemists’ responsibility is to evaluate the ﬁnished product, rather than cre- ate one. Evaluation includes shade, texture, sharpenability, wear, application, sta- bility (freeze-thaw and at 40–45°C) and penetration. Lipsticks Lipsticks add color to the face for a healthier look, shape and sometimes condi- tions the lips. Ingredients in a Classical Lipstick Emollients: castor oil, esters, lanolin/lanolin oil, oily alcohols (octyl dode- canol), organically modiﬁed silicones (phenyltrimethicone and alkyl di- methicones), meadowfoam seed oil, jojoba oil and esters and triglycer- ides Waxes: candelilla, carnauba, beeswax and derivatives, microcrystalline, ozokerite/ceresein, alkyl silicone, castor, polyethylene, lanolin, parafﬁn, synthetic and ester Wax modiﬁers (plasticizers): work in conjunction with the waxes to im- prove texture, application and stability include cetyl acetate and ace- tylated lanolin, oleyl alcohol, synthetic lanolin, acetylated lanolin alcohol and petroleum (white and yellow) Colorants widely used—D&C’s (Red #6 and Ba Lake, Red #7 and Ca Lake, Red #21 and Al Lake- (stains), Red #27 and A1 Lake- (stains), 304 Schlossman Red #33 and Al Lake, Red #30, Red #36, Yellow #10). Grind phase is added to complete emollient phase and waxes, heated and mixed until uniform (approx. Pearls and ﬁllers are added to above phases and mixed with shear (if necessary) until homogeneous. Maintain a temperature just above the initial set point of the waxes and ﬁll as appropriate. Ingredients for Volatile Lipstick The proper balance of solvents and emollients prevent transfer and allow lipstick not to become too dry on the lips (15). They should be waterproof, glossy, adherent, dry quickly and be resistant to chipping and abrasion. The main constituents include a ﬁlm former, modifying resin, plasti- cizer, and solvents. Additionally, pigments, suspending agents and ultraviolet absorbers are usually included. Nitrocellulose is derived from cellulose, a polymer made of several anhy- droglucose units connected by ether linkages. Nitrocellulose by itself will produce a hard brittle ﬁlm so it is necessary to modify it with resins and plasti- cizers to provide ﬂexibility and gloss. The most commonly used modifying resin is para foluene sulfonamide formaldehyde resin, which is contained at 5–10% levels. This resin provides gloss, adhesion, and increases the hardness of the nitrocellulose ﬁlm. The formaldehyde resin has caused allergies with a small number of consumers so that other modiﬁers such as sucrose benzoate, polyester 306 Schlossman resin and toluene sulfonamide epoxy resin have been used in its place with varying results. Plasticizers used include camphor, glyceryl diesters (16), di- butyl phthalate, citrate esters and castor oil. Other resins such as polyurethanes and acrylics have been used as auxiliary resins. Variations of plasticizers and resins will change the viscosity, dry time, and gloss of the lacquer. Colorants include titanium dioxide, iron oxides, most organics, and pearlescent pigments. In order to reduce settling of the heavier pigments, treatment such as silicone (17) and oxidized polyethylene (18) have been utilized. Modiﬁed clays derived from bentonite and/or hectorite are used to suspend the pigments and make the nail enamel thixotropic and brushable. Solvents that constitute approximately 70% of nail lacquers include n-butyl acetate, ethyl acetate, and toluene. Cream shades may be shear or full coverage with titanium dioxide as the chief pigment. Pearlescent nail polish usually contains bismuth oxychloride and/or titanium dioxide coated micas and may even contain guanine-natural ﬁsh scales. The manufacturing of nail lacquer is usually carried out by specialty manufacturing ﬁrms that are familiar with the hazards of working with nitrocellulose and solvents. The manufacture consists of two separate operations: (1) manufacture and compounding of the lacquer base; and (2) the coloring and color matching of shades.