Hydrolysis and protein binding of melphalan.

abstract：:Carboxy group-terminated synthetic polymers--branched poly(ethylene glycol), poly(acryloylmorpholine), and poly(vinylpyrrolidone)--were made amphiphilic by derivatization with phosphatidyl ethanolamine via the terminal carboxy group and then incorporated into lecithin-cholesterol liposomes prepared by the detergent di...

journal_title：Journal of pharmaceutical sciences

authors： Torchilin VP,Trubetskoy VS,Whiteman KR,Caliceti P,Ferruti P,Veronese FM

更新日期：1995-09-01 00:00:00

abstract：:Antisense phosphorodiamidate Morpholino oligomers (PMO) are resistant to degradation by cellular hydrolases, DNases, RNases, and phosphodiesterases, but remain sensitive to prolonged exposure to low pH. The present studies evaluate the oral fractional bioavailability, stability, and efficacy of two distinct PMO sequen...

journal_title：Journal of pharmaceutical sciences

authors： Arora V,Knapp DC,Reddy MT,Weller DD,Iversen PL

更新日期：2002-04-01 00:00:00

abstract：:Various complex mechanisms and their multifactorial pathways decisively provoke low-grade local and systemic inflammation in β-cells of pancreatic islets and peripheral tissues to induce β-cells' dysfunction and apoptosis, insulin resistance, and ultimately, overt type 2 diabetes mellitus (T2DM). Conventional antidiab...

journal_title：Journal of pharmaceutical sciences

authors： Akash MS,Shen Q,Rehman K,Chen S

更新日期：2012-05-01 00:00:00

abstract：:Regional permeability coefficients of 19 drugs with different physicochemical properties were determined using excised segments from three regions of rat intestine: jejunum, ileum, and colon. The results are discussed in relation to the characteristics of the drug, i.e., MW (range 113-1071 Da), pKa, log D (octanol/wat...

journal_title：Journal of pharmaceutical sciences

authors： Ungell AL,Nylander S,Bergstrand S,Sjöberg A,Lennernäs H

更新日期：1998-03-01 00:00:00

abstract：:Metronidazole and four derivatives were studied in vitro to investigate the differences in the extent of their binding to plasma proteins. Modification at the terminal portion of the alkyl side chain resulted in wide differences in the extent of binding. Molecular orbital calculations were performed by the CNDO and MI...

journal_title：Journal of pharmaceutical sciences

authors： Sanvordeker DR,Chien YW,Lin TK,Lambert HJ

更新日期：1975-11-01 00:00:00

abstract：:Oral Almotriptan maleate (ALM) is used in the treatment of migraine; however, due to its extreme aqueous solubility, shows poor penetration and lesser concentration in the brain thus requiring frequent oral dosing. Being flexible and lipophilic in nature, nanostructured lipid carriers (NLCs) represent a promising tool...

journal_title：Journal of pharmaceutical sciences

authors： Salem LH,El-Feky GS,Fahmy RH,El Gazayerly ON,Abdelbary A

更新日期：2020-07-01 00:00:00

abstract：:A method to determine drugs having a carbothionamido group using an ammonia gas-sensing electrode is described. To obtain analytical accuracy, the effect of factors that influence the potential is also discussed. Ethionamide or prothionamide was refluxed with 20% HCl to give ammonium chloride, hydrogen sulfide, and a ...

journal_title：Journal of pharmaceutical sciences

authors： Tagami S,Maeda H

更新日期：1983-09-01 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：:Cyclosporin A (CyA) interacts with lipid membranes. Binding reaction and membrane location of CyA and analogs were examined with 2H-NMR, high-sensitivity isothermal titration calorimetry (ITC), and CD spectroscopy. Effects of CyA and charged analogs on the phosphocholine head group and on the membrane interior were in...

journal_title：Journal of pharmaceutical sciences

authors： Schote U,Ganz P,Fahr A,Seelig J

更新日期：2002-03-01 00:00:00

abstract：:The axial and radial tensile strengths were compared to the hardness of compressed tablets containing various concentrations of lubricants. Since radial tensile strength measurement considers the thickness of a tablet, and only tensile stress and axial tensile strength express the strength in the direction in which ca...

journal_title：Journal of pharmaceutical sciences

authors： Jarosz PJ,Parrott EL

更新日期：1982-06-01 00:00:00

abstract：:Chitosan microspheres were evaluated for sustained-release of recombinant human interleukin-2 (rIL-2) in this study. In addition, the effects of different formulation factors, such as chitosan and protein concentrations, the volume of sodium sulfate solution, addition technique of rIL-2, and presence of glutaraldehyde...

journal_title：Journal of pharmaceutical sciences

authors： Ozbaş-Turan S,Akbuğa J,Aral C

更新日期：2002-05-01 00:00:00

abstract：:The blood-brain barrier (BBB) limits the distribution of systemically administered therapeutics to the central nervous system (CNS). Intranasal delivery is a noninvasive method that targets drugs to the brain and spinal cord along olfactory and trigeminal neural pathways, bypassing the BBB and minimizing systemic expo...

journal_title：Journal of pharmaceutical sciences

authors： Dhuria SV,Hanson LR,Frey WH 2nd

更新日期：2009-07-01 00:00:00

abstract：:Oxycodone is an opioid analgesic that is administered orally or parenterally. The time-course of opioid action is a function of the systemic kinetics of the opioid, and the rate and extent of its entry into the brain and central nervous system. The latter is incompletely understood for oxycodone. Therefore, the cerebr...

journal_title：Journal of pharmaceutical sciences

authors： Villesen HH,Foster DJ,Upton RN,Somogyi AA,Martinez A,Grant C

更新日期：2006-08-01 00:00:00

abstract：:The application of raster image correlation spectroscopy (RICS) as a tool for the characterisation of protein diffusion was assessed using a model protein, bovine serum albumin (BSA), as a function of formulation and denaturing conditions. RICS results were also validated against dynamic light scattering and fluoresce...

journal_title：Journal of pharmaceutical sciences

authors： Hamrang Z,Pluen A,Zindy E,Clarke D

更新日期：2012-06-01 00:00:00

abstract：:Unlike most organic compounds, both digoxin and digitoxin melted over a wide temperature range, with the widest range being 88 and 33 degrees for both compounds, respectively. Furthermore, the melting ranges varied markedly among several untriturated powders obtained from commercial sources and after recrystallization...

journal_title：Journal of pharmaceutical sciences

authors： Chiou WL,Kyle LE

更新日期：1979-10-01 00:00:00

abstract：:The expression of carboxylesterase (CES) and the transdermal movement of an ester prodrug were studied in rat skin. Ethyl-fexofenadine (ethyl-FXD) was used as a model lipophilic prodrug that is slowly hydrolyzed to its parent drug, FXD (MW 502). Among the CES1 and CES2 isozymes, Hydrolase A is predominant in rat skin ...

journal_title：Journal of pharmaceutical sciences

authors： Imai T,Ariyoshi S,Ohura K,Sawada T,Nakada Y

更新日期：2016-02-01 00:00:00

abstract：:The peptide hormone calcitonin (CT) is a potent drug for the therapy of different bone diseases. Salmon CT (sCT) is reported to be more active than human CT (hCT). Human CT, but not sCT, has a strong tendency to aggregate and fibrillate in aqueous solutions. Recent investigations of the fibrillation mechanisms contrib...

journal_title：Journal of pharmaceutical sciences

authors： Cudd A,Arvinte T,Das RE,Chinni C,MacIntyre I

更新日期：1995-06-01 00:00:00

abstract：:A method for the simultaneous determination of etoricoxib and its carbon-13 analog ((13)C(6)-etoricoxib) from human plasma has been developed and used to support bioavailability studies. Plasma samples (0.5 mL) were extracted by using a 3M Empore 96-well plate (C(8)) and the resulting extracts were analyzed by using a...

journal_title：Journal of pharmaceutical sciences

authors： Rose MJ,Agrawal N,Woolf EJ,Matuszewski BK

更新日期：2002-02-01 00:00:00

abstract：:A stability-indicating reversed-phase high-performance liquid chromatographic method using a refractive index detector is described for the determination of propylene carbonate in pharmaceutical formulations. Good precision and accuracy of the method was demonstrated using an aqueous formulation. This method is also a...

journal_title：Journal of pharmaceutical sciences

authors： Cheng H,Gadde RR

更新日期：1985-06-01 00:00:00

abstract：:Biopharmaceuticals represent an important and growing class of medicines. Immunogenic responses to biopharmaceuticals in patients can sometimes result in reduced safety and efficacy. Although multiple factors are known to influence immunogenicity, our understanding of the complex underlying mechanisms remains imperfec...

journal_title：Journal of pharmaceutical sciences

authors： Bee JS,Goletz TJ,Ragheb JA

更新日期：2012-10-01 00:00:00

abstract：:DB844 (CPD-594-12), N-methoxy-6-{5-[4-(N-methoxyamidino)phenyl]-furan-2-yl}-nicotinamidine, is an oral prodrug that has shown promising efficacy in both mouse and monkey models of second stage human African trypanosomiasis. However, gastrointestinal (GI) toxicity was observed with high doses in a vervet monkey safety ...

journal_title：Journal of pharmaceutical sciences

authors： Ju W,Yang S,Ansede JH,Stephens CE,Bridges AS,Voyksner RD,Ismail MA,Boykin DW,Tidwell RR,Hall JE,Wang MZ

更新日期：2014-01-01 00:00:00

abstract：:A high-performance liquid chromatographic method has been developed for the simultaneous determination of azobenzene and hydrazobenzene in phenylbutazone and sulfinpyrazone raw materials and formulations. The drug raw material or formulation is shaken with 1N NaOH and n-hexane and centrifuged. The n-hexane layer is in...

journal_title：Journal of pharmaceutical sciences

authors： Matsui F,Lovering EG,Curran NM,Watson JR

更新日期：1983-10-01 00:00:00

abstract：:The purpose of this study was to understand the combined effect of two polymers showing drug-polymer interactions on amorphous stabilization and dissolution enhancement of indomethacin (IND) in amorphous ternary solid dispersions. The mechanism responsible for the enhanced stability and dissolution of IND in amorphous...

journal_title：Journal of pharmaceutical sciences

authors： Prasad D,Chauhan H,Atef E

更新日期：2014-11-01 00:00:00

abstract：:Transdermal delivery of fentanyl from various adhesive matrix formulations to achieve a steady-state skin flux was investigated. For this purpose, various pressure-sensitive adhesives selected from the three chemical classes of polymers (polyisobutylene (PIB), acrylate, and silicone adhesives) were characterized with ...

journal_title：Journal of pharmaceutical sciences

authors： Roy SD,Gutierrez M,Flynn GL,Cleary GW

更新日期：1996-05-01 00:00:00

abstract：:Subcutaneous injection allows for self-administration of monoclonal antibodies using prefilled syringes, autoinjectors, and on-body injector devices. However, subcutaneous injections are typically limited to 1 mL due to concerns of injection pain from volume, viscosity, and formulation characteristics. Back pressure c...

journal_title：Journal of pharmaceutical sciences

authors： Doughty DV,Clawson CZ,Lambert W,Subramony JA

更新日期：2016-07-01 00:00:00

abstract：:The relationship between the concentration of a drug and its pharmacologic effect is of central interest in pharmacodynamics. Various compartmental and noncompartmental methods have been proposed for elucidating this relationship when the plasma drug concentration and effects are both measured. Although the relationsh...

journal_title：Journal of pharmaceutical sciences

authors： Modi NB,Veng-Pedersen P

更新日期：1994-03-01 00:00:00

abstract：:One manifestation of cystic fibrosis (CF) is the presence of a viscid mucus secretion in the lungs. The clearance of this mucus is significantly slower than in "normals" due to uncoordinated beating of the cilia and the increased viscosity of the mucus. In these studies, the permeabilities of p-aminosalicylic acid, is...

journal_title：Journal of pharmaceutical sciences

authors： Bhat PG,Flanagan DR,Donovan MD

更新日期：1996-06-01 00:00:00

abstract：:The application of drug ion-selective electrodes as sensors for the direct determination of the released drug in a continuous-flow analyzer for automated dissolution studies is described. Flow-through electrodes, selective to chlorpromazine, amitriptyline, propantheline, cimetidine, and ranitidine, have been construct...

journal_title：Journal of pharmaceutical sciences

authors： Mitsana-Papazoglou A,Christopoulos TK,Diamandis EP,Koupparis MA

更新日期：1987-09-01 00:00:00

abstract：:The solubility equation of Yalkowsky was used to estimate the aqueous solubility of 33 barbiturates in the temperature range of 5 to 45 degrees C. The equation was extended by adding a term which accounts for the effect of pH on the solubility of the drug. The extended equation is successful in estimating the aqueous ...

journal_title：Journal of pharmaceutical sciences

authors： Pinal R,Yalkowsky SH

更新日期：1987-01-01 00:00:00

abstract：:Two high-performance liquid chromatographic (HPLC) assay procedures were developed for the determination of salicylamide and its metabolites in serum, urine, and saliva. One method involves reverse-phase ion-pair chromatography and UV detection, and is used to determine salicylamide, salicylamide glucuronide, and sali...

journal_title：Journal of pharmaceutical sciences

authors： Morris ME,Levy G

更新日期：1983-06-01 00:00:00