Intranasal drug targeting of hypocretin-1 (orexin-A) to the central nervous system.

abstract：:The purpose of this work was to study the permeability of two relatively lipophilic sulfenamide prodrugs of linezolid (clogP 0.85), N-(phenylthio)linezolid (1, clogP 2.77) and N-[(2-ethoxycarbonyl)ethylthio]linezolid (2, clogP 1.43), across Caco-2 cell monolayers. Both prodrugs were found to convert to linezolid in th...

journal_title：Journal of pharmaceutical sciences

authors： Nti-Addae KW,Guarino VR,Dalwadi G,Stella VJ

更新日期：2012-09-01 00:00:00

abstract：:In recent years, controlled release coatings, comprised of drug-polymer composites, have been integrated with medical devices, improving device functionality and performance. However, relationships between material properties, manufacturing environment, composite (micro)structure, and subsequent release kinetics are n...

journal_title：Journal of pharmaceutical sciences

authors： Saylor DM,Kim CS,Patwardhan DV,Warren JA

更新日期：2009-01-01 00:00:00

abstract：:Quantitative determination of serum concentrations of carvedilol [(+/-)-1-(carbazol-4-yloxy)-3-[[2-(o-methoxyphenoxy)ethyl) amino]-2-propanol], a combined alpha- and beta-adrenergic receptor antagonist, was obtained using HPLC with spectrofluorometric detection. Carvedilol was extracted from alkalinized serum with eth...

journal_title：Journal of pharmaceutical sciences

authors： Varin F,Cubeddu LX,Powell JR

更新日期：1986-12-01 00:00:00

abstract：:We investigated the effects of excipients in solutions of keratinocyte growth factor 2 (KGF-2) on protein aggregation during agitation as well as on interfacial shear rheology at the air-water interface. Samples were incubated with or without agitation, and in the presence or absence of the excipients heparin, sucrose...

journal_title：Journal of pharmaceutical sciences

authors： Liu L,Qi W,Schwartz DK,Randolph TW,Carpenter JF

更新日期：2013-08-01 00:00:00

abstract：:The estimation of Michaelis-Menten pharmacokinetic parameters in patients with epilepsy receiving phenytoin continues to be a vexing problem. The various approximate methods suggested in the literature have serious shortcomings, primarily due to the role of the error term in the statistical model. In this report we pr...

journal_title：Journal of pharmaceutical sciences

authors： van Belle G,Leurgans S,Friel P,Guo SW,Yerby M

更新日期：1989-05-01 00:00:00

abstract：:Mechanical shock may cause cavitation in vials containing liquid formulations of therapeutic proteins and generate protein aggregates and other particulates. To test whether common formulation components such as protein molecules, air bubbles, or polysorbate 20 (PS20) micelles might nucleate cavitation, a high-speed v...

journal_title：Journal of pharmaceutical sciences

authors： Wu H,Chisholm CF,Puryear M,Movafaghi S,Smith SD,Pokhilchuk Y,Lengsfeld CS,Randolph TW

更新日期：2020-03-01 00:00:00

abstract：:This work reports the measurement of the partition rate of a model drug, ibuprofen (IBU), from aqueous solutions into octanol in the absence and presence of common pharmaceutical excipients including glucose, lactose, maltoheptaose, hydroxypropyl methylcellulose, polyvinylpyrrolidone, polyvinylpyrrolidone-vinyl acetat...

journal_title：Journal of pharmaceutical sciences

authors： Xu H,Wang W,Shi Y,Gao P

更新日期：2019-01-01 00:00:00

abstract：:Three aspirin derivatives, aspirin phenylalanine ethyl ester, aspirin phenylalanine amide, and aspirin phenyllactic ethyl ester, were investigated with respect to their hydrolysis by alpha-chymotrypsin. Of the three compounds, aspirin phenylalanine ethyl ester was the best substrate, with kcat = 25 sec-1 and Km = 1.3 ...

journal_title：Journal of pharmaceutical sciences

authors： Banerjee PK,Amidon GL

更新日期：1981-12-01 00:00:00

abstract：:Fifteen pyrimidine-related compounds were evaluated for their ability to inhibit enzymatic degradation of 5-fluoro-2'-deoxyuridine (FUdR). Acyclothymidine [5-methyl-1-(2'-hydroxyethoxymethyl)uracil] showed the highest inhibitory effect on the phosphorolytic degradation of FUdR in various tissue homogenates derived fro...

journal_title：Journal of pharmaceutical sciences

authors： Kawaguchi T,Saito M,Saneyoshi M

更新日期：1988-11-01 00:00:00

abstract：:Phenytoin (DPH) was delivered to the brain by a dihydropyridine in equilibrium pyridinium salt redox system, which was evaluated for anticonvulsant activity. Following iv injection of the lipophilic delivery system of DPH (2) to rats, concentrations of DPH were lower but sustained and, after 30 min, essentially the sa...

journal_title：Journal of pharmaceutical sciences

authors： Shek E,Murakami T,Nath C,Pop E,Bodor NS

更新日期：1989-10-01 00:00:00

abstract：:Insight into the stratum corneum (SC) permeation pathway for hydrophilic compounds is gained by comparing experimental measurements of permeability and lag time (tlag) with the predictions of a finite element (FE) model. A database of permeability and lag time measurements (n=27) of hydrophilic compounds was compiled ...

journal_title：Journal of pharmaceutical sciences

authors： Barbero AM,Frasch HF

更新日期：2006-10-01 00:00:00

abstract：:A physiological flow model was developed for the distribution of sulfathiazole residues in various tissues in swine. The approach was compartmental, in which the compartments and equilibrium constants had physiological meaning. Differential equations were developed, and appropriate parameter values and initial conditi...

journal_title：Journal of pharmaceutical sciences

authors： Duddy J,Hayden TL,Bourne DW,Fiske WD,Benedek IH,Stanley D,Gonzalez A,Heierman W

更新日期：1984-11-01 00:00:00

abstract：:A sucrose-lactose-starch granulation was used to study particulate motion and attrition in a fluid bed dryer. There is some classification of material in the dryer as drying proceeds; fine particles are dried faster and become less dense, and the less dry but denser large particles show some (although not great) accum...

journal_title：Journal of pharmaceutical sciences

authors： Zoglio MA,Streng WH,Carstensen JT

更新日期：1975-11-01 00:00:00

abstract：:A swellable matrix tablet is described which is partially coated with cellulose acetate (CA) to obtain a film having the shape of a cup, whose permeability to water and solutes was altered by mixing increasing amounts of poly(ethylene glycol) 400 (PEG). The drug-release mechanism from such systems was assessed by carr...

journal_title：Journal of pharmaceutical sciences

authors： Catellani PL,Colombo P,Peppas NA,Santi P,Bettini R

更新日期：1998-06-01 00:00:00

abstract：:A novel approach using a self-setting hydroxyapatite (HAP) cement as a skeletal drug-delivery system has been proposed to solve the problem of delivering drugs to skeletal tissue at sufficiently high local concentrations for desirable therapeutic effects. HAP cements loaded with antibiotics can be formed in situ and c...

journal_title：Journal of pharmaceutical sciences

authors： Yu D,Wong J,Matsuda Y,Fox JL,Higuchi WI,Otsuka M

更新日期：1992-06-01 00:00:00

abstract：:An electron-capture GLC method to measure nofedone in human serum was developed. A homolog of nofedone was added to the serum as an internal standard before the sample was alkalinized with pH 9.5 phosphate buffer and extracted with ethylene dichloride containing 0.5% isopentyl alcohol. This organic phase was extracted...

journal_title：Journal of pharmaceutical sciences

authors： Heusse D,Populaire P,Renard A,Pasquier P,Gregoire J

更新日期：1980-05-01 00:00:00

abstract：:A new parameter, the kinetic ratio, is suggested for estimating product potency during storage under ambient warehouse temperatures. Actual warehouse temperature data were integrated using Arrhenius kinetics, and the resulting potency errors, due both to the integration method and to temperature averaging, were evalua...

journal_title：Journal of pharmaceutical sciences

authors： Scher M

更新日期：1980-03-01 00:00:00

abstract：:Emerging 3D printing technologies offer an exciting opportunity to create customized 3D objects additively from a digital design file. 3D printing may be further leveraged for personalized medicine, clinical trial, and controlled release applications. A wide variety of 3D printing methods exists, and many studies focu...

journal_title：Journal of pharmaceutical sciences

authors： Chang SY,Li SW,Kowsari K,Shetty A,Sorrells L,Sen K,Nagapudi K,Chaudhuri B,Ma AWK

更新日期：2020-10-01 00:00:00

abstract：:A simultaneous GLC determination for methyl salicylate and menthol in a topical analgesic formulation is reported. n-Nonadecane is used as the internal standard. The method is rapid, accurate, precise, and selective in the presence of salicylic acid and ethyl salicylate. ...

journal_title：Journal of pharmaceutical sciences

authors： Sapio JP,Sethachutkul K,Moody JE

更新日期：1979-04-01 00:00:00

abstract：:Simultaneously Manufactured Nano-In-Micro (SIMANIM) particles for the pulmonary delivery of antibodies have been prepared by the spray-drying of a double-emulsion containing human IgG (as a model antibody), lactose, poly(lactide-co-glycolide) (PLGA) and dipalmitoylphosphatidylcholine (DPPC). The one-step drying proces...

journal_title：Journal of pharmaceutical sciences

authors： Kaye RS,Purewal TS,Alpar HO

更新日期：2009-11-01 00:00:00

abstract：:Model independent pharmacokinetic analysis of intravenous (iv) amphotericin B cochleates (CAMB), a new lipid-based drug delivery system, in mice (0.625 mg/kg) shows a two-phase disposition profile in blood [area under the curve of concentration versus time from time zero to infinity (AUC(0-infinity)) = 1.01 microg. h/...

journal_title：Journal of pharmaceutical sciences

authors： Segarra I,Movshin DA,Zarif L

更新日期：2002-08-01 00:00:00

abstract：:Crystallization of drugs in metastable, supersaturated adhesive polymeric matrices in transdermal drug delivery devices can be avoided by determination of the solubility of the drug in the adhesive polymer. A novel method is described to determine the solubility of the drug in polymeric matrices. Unlike existing metho...

journal_title：Journal of pharmaceutical sciences

authors： Jasti BR,Berner B,Zhou SL,Li X

更新日期：2004-08-01 00:00:00

abstract：:An immune response for a nasal ovalbumin (OVA) powder formulation with an applied nasal delivery platform technology, consisting of a powdery nasal carrier and a device, was evaluated in monkeys with similar upper respiratory tracts and immune systems to those of humans, in order to assess the applicability to a vacci...

journal_title：Journal of pharmaceutical sciences

authors： Torikai Y,Sasaki Y,Sasaki K,Kyuno A,Haruta S,Tanimoto A

更新日期：2020-12-03 00:00:00

abstract：:Various novel diesters of pilocarpic acid were synthesized and evaluated as prodrug forms for pilocarpine with the aim of improving the ocular delivery characteristics of the drug. The pilocarpic acid monoesters previously studied cyclized spontaneously to pilocarpine in aqueous solution and although they showed enhan...

journal_title：Journal of pharmaceutical sciences

authors： Bundgaard H,Falch E,Larsen C,Mosher GL,Mikkelson TJ

更新日期：1986-08-01 00:00:00

abstract：:The benzenesulfonate salt of an anti-methicillin-resistant Staphylococcus aureus carbapenem antibiotic studied is a crystalline, nonhygroscopic powder which is stable at room temperature, making it an ideal compound for long-term storage. However, the limited aqueous solubility of this salt prohibits parenteral admini...

journal_title：Journal of pharmaceutical sciences

authors： Antonucci V,Yen D,Kelly J,Crocker L,Dienemann E,Miller R,Almarrsson O

更新日期：2002-04-01 00:00:00

abstract：:A roadmap for the selection of a pharmaceutical salt form for a development candidate is presented. The free base of the candidate did not have sufficient chemical stability for development. The initially selected salt form turned out to be undevelopable because it was unstable during scale-up synthesis and storage. T...

journal_title：Journal of pharmaceutical sciences

authors： He Y,Orton E,Yang D

更新日期：2018-01-01 00:00:00

abstract：:The pharmacokinetic profiles of cimetropium bromide, after either intravenous injection of 10 mg or oral ingestion of 200 mg, were determined in eight healthy volunteers. After intravenous administration, the plasma levels and urinary excretion indicated that the drug is distributed and eliminated at a rapid rate (ter...

journal_title：Journal of pharmaceutical sciences

authors： Imbimbo BP,Daniotti S,Vidi A,Foschi D,Saporiti F,Ferrante L

更新日期：1986-07-01 00:00:00

abstract：:Effects of the commercial drug zanamivir (Relenza) covalently attached to poly-l-glutamine on the infectivity of influenza A viruses are examined using the plaque reduction assay and binding affinity to viral neuraminidase (NA). These multivalent drug conjugates exhibit (i) up to a 20,000-fold improvement in anti-infl...

journal_title：Journal of pharmaceutical sciences

authors： Weight AK,Haldar J,Alvarez de Cienfuegos L,Gubareva LV,Tumpey TM,Chen J,Klibanov AM

更新日期：2011-03-01 00:00:00

abstract：:Alginate microparticles incorporating hydrocortisone hemisuccinate were produced by aerosolization and homogenization methods to investigate their potential for colonic drug delivery. Microparticle stabilization was achieved by CaCl2 crosslinking solution (0.5 M and 1 M), and drug loading was accomplished by diffusion...

journal_title：Journal of pharmaceutical sciences

authors： Samak YO,El Massik M,Coombes AGA

更新日期：2017-01-01 00:00:00

abstract：:A colorimetric procedure for benzocaine and a number of its dosage forms was developed; it offers improvement in ease, speed, and sensitivity over the official method. The method is based on the formation of a red Schiff base between benzocaine and p-dimethylaminocinnamaldehyde in a nonaqueous acidic medium. At the ma...

journal_title：Journal of pharmaceutical sciences

authors： Tan HS,Bruemmer GA,Shelton D

更新日期：1977-07-01 00:00:00