Biorelevant dissolution testing to predict the plasma profile of lipophilic drugs after oral administration.

abstract：:The pharmacokinetics of cefixime, a new orally active cephalosporin, was studied after an intravenous dose of 50 mg/kg to four beagle dogs. Cefixime was shown to exhibit concentration dependent serum protein binding and saturable tubular reabsorption. The drug was excreted mainly in the urine, the net result of glomer...

journal_title：Pharmaceutical research

authors： Tonelli AP,Bialer M,Look ZM,Carson S,Yacobi A

更新日期：1986-06-01 00:00:00

abstract：PURPOSE:To compare the systemic delivery of deslorelin following intratracheal administration of different deslorelin formulations. The formulations included dry powders of deslorelin, large-porous deslorelin-poly(lactide-co-glycolide) (PLGA) particles, and small conventional deslorelin-PLGA particles. Also, solution f...

journal_title：Pharmaceutical research

authors： Koushik K,Dhanda DS,Cheruvu NP,Kompella UB

更新日期：2004-07-01 00:00:00

abstract：:Over the last few decades, intraperitoneal (IP) local drug delivery, providing high drug concentrations with prolonged retention in the peritoneal cavity, has opened a new horizon for the management of life-threatening peritoneal disorders, such as peritoneal carcinomatosis (PC). However, clinical translation of this ...

journal_title：Pharmaceutical research

authors： Alavi S,Haeri A,Mahlooji I,Dadashzadeh S

更新日期：2020-06-03 00:00:00

abstract：PURPOSE:To test the hypothesis of surface displacement as the underlying mechanism for IgG stabilization by polysorbates and HPβCD against surface-induced aggregation. METHODS:Adsorption/desorption-kinetics of IgG-polysorbate 80/-HPβCD were monitored. Maximum bubble pressure method was used for processes within second...

journal_title：Pharmaceutical research

authors： Serno T,Härtl E,Besheer A,Miller R,Winter G

更新日期：2013-01-01 00:00:00

abstract：:The topical antifungal Sch-39304 is a racemic compound comprised of two enantiomers, Sch-42427 and Sch-42426, only one of which (Sch-42427) is pharmacologically active. The pure enantiomers have a lower melting point and, therefore, a higher solubility than the racemic compound. Because of these differences in physico...

journal_title：Pharmaceutical research

authors： Wearley L,Antonacci B,Cacciapuoti A,Assenza S,Chaudry I,Eckhart C,Levine N,Loebenberg D,Norris C,Parmegiani R

更新日期：1993-01-01 00:00:00

abstract：PURPOSE:The aim of the present study was to design a new mucosal drug delivery system composed of liposomes dispersed within a bioadhesive hydrogel containing methyl-beta-cyclodextrin (Me(beta)CD) for controlled drug release. METHODS:A hydrophilic model molecule, inulin, was encapsulated within positively charged and ...

journal_title：Pharmaceutical research

authors： Boulmedarat L,Piel G,Bochot A,Lesieur S,Delattre L,Fattal E

更新日期：2005-06-01 00:00:00

abstract：PURPOSE:We investigated optimum formulation characteristics in the nasal absorption of salmon calcitonin (sCT) by incorporation of acylcarnitines. METHODS:Nasal sCT formulations were administered to anesthetized rats. Plasma calcium level was measured and pharmacological bioavailability (P.bioav) was calculated. RESU...

journal_title：Pharmaceutical research

authors： Kagatani S,Shinoda T,Fukui M,Ohmura T,Hasumi S,Sonobe T

更新日期：1996-05-01 00:00:00

abstract：:Recently a new in vivo approach in man, using a regional intestinal perfusion technique, has been developed. The perfusion tube consists of a multichannel tube with two inflatable balloons, which are placed 10 cm apart. The tube is introduced orally and the time required for insertion and positioning of the tube is ap...

journal_title：Pharmaceutical research

authors： Lennernäs H,Ahrenstedt O,Hällgren R,Knutson L,Ryde M,Paalzow LK

更新日期：1992-10-01 00:00:00

abstract：PURPOSE:Cationic liposomes are expected to be useful as nonviral vectors for gene delivery. Cationic liposomes showed cytotoxicity, and we proposed that the cytotoxicity is through apoptosis. In this study, we examined the effects of liposomal properties, such as liposomal charge, size, membrane fluidity, and PEG coati...

journal_title：Pharmaceutical research

authors： Takano S,Aramaki Y,Tsuchiya S

更新日期：2003-07-01 00:00:00

abstract：PURPOSE:Effects of polyvinylpyrrolidone (PVP) molecular weight on the solid-state intermolecular interactions among probucol/PVP/sodium dodecyl sulfate (SDS) ternary ground mixtures (GM) and the formation of nanoparticles were investigated by solid-state NMR spectroscopy. MATERIALS AND METHODS:Ternary GMs of probucol ...

journal_title：Pharmaceutical research

authors： Pongpeerapat A,Higashi K,Tozuka Y,Moribe K,Yamamoto K

更新日期：2006-11-01 00:00:00

abstract：PURPOSE:To show that atomic force microscopy (AFM) can be used to directly study the electrostatic charging and dissipation of single pharmaceutical particles. MATERIALS AND METHODS:Particles of lactose attached to AFM cantilevers were charged on a glass surface at a relative humidity (RH) of 0.1%. By recording force-...

journal_title：Pharmaceutical research

authors： Bunker MJ,Davies MC,James MB,Roberts CJ

更新日期：2007-06-01 00:00:00

abstract：:An alternative procedure for the simultaneous determination of trimethoprim and sulfamethoxazole in an intravenous pharmaceutical formulation is presented. Infrared spectra of 14 calibration and 6 validation samples were collected using Fourier transform-infrared/attenuated total reflectance (FT-IR/ATR). Partial least...

journal_title：Pharmaceutical research

authors： Hartauer KJ,Guillory JK

更新日期：1989-07-01 00:00:00

abstract：:The simultaneous diffusion and metabolism of the D- and L-isomers of the aminopeptidase substrate, leucine-p-nitroanilide (LPNA), were examined in vitro in the hamster cheek pouch. L-LPNA was completely hydrolyzed during diffusion across the cheek pouch, whereas D-LPNA crossed the cheek pouch intact. The metabolic bar...

journal_title：Pharmaceutical research

authors： Garren KW,Topp EM,Repta AJ

更新日期：1989-11-01 00:00:00

abstract：PURPOSE:To investigate the feasibility of using the Aerosol Solvent Extraction System (ASES) to produce fine powders of recombinant human deoxyribonuclease (rhDNase), lysozyme-lactose and rhDNase-lactose powders from aqueous based solutions. METHODS:The ASES technique using high pressure carbon dioxide modified with e...

journal_title：Pharmaceutical research

authors： Bustami RT,Chan HK,Sweeney T,Dehghani F,Foster NR

更新日期：2003-12-01 00:00:00

abstract：PURPOSE:To demonstrate a very effective and easy way of stabilization of amorphous indomethacin (IMC) by preparing binary mixtures with octaacetylmaltose (acMAL). In order to understand the origin of increased stability of amorphous system inter- and intramolecular interactions between IMC and acMAL were studied. METH...

journal_title：Pharmaceutical research

authors： Kaminska E,Adrjanowicz K,Zakowiecki D,Milanowski B,Tarnacka M,Hawelek L,Dulski M,Pilch J,Smolka W,Kaczmarczyk-Sedlak I,Kaminski K

更新日期：2014-10-01 00:00:00

abstract：PURPOSE:Cell-based permeability screens are widely used to identify drug-P-glycoprotein (PGP) interaction in vitro. However, their reliability in predicting the impact of PGP on human drug pharmacokinetics is poorly defined. The aim was to determine whether a quantitative relationship exists between PGP-mediated altera...

journal_title：Pharmaceutical research

authors： Collett A,Tanianis-Hughes J,Hallifax D,Warhurst G

更新日期：2004-05-01 00:00:00

abstract：PURPOSE:Good glycaemic control is essential to minimize the risk for diabetes-induced complications. Also, compliance is likely to be higher if the procedure is simple and painless. This study was designed to validate painless intradermal delivery via a patch-like microneedle array. MATERIALS AND METHODS:Diabetes was ...

journal_title：Pharmaceutical research

authors： Nordquist L,Roxhed N,Griss P,Stemme G

更新日期：2007-07-01 00:00:00

abstract：PURPOSE:Since the adoption of highly active antiretroviral therapy, HIV disease progression has slowed across the world; however, patients are often required to take multiple medications daily of poorly bioavailable drugs via the oral route, leading to gastrointestinal irritation. Recently, long acting antiretroviral i...

journal_title：Pharmaceutical research

authors： Collier MA,Gallovic MD,Bachelder EM,Sykes CD,Kashuba A,Ainslie KM

更新日期：2016-08-01 00:00:00

abstract：PURPOSE:In this study, we developed and evaluated a novel method to produce insulin-loaded hydrophilic microspheres allowing high encapsulation efficiency and the preservation of peptide stability during particle processing. The preparation method used the diffusion of water by an excess of solvent starting from a wate...

journal_title：Pharmaceutical research

authors： Trotta M,Chirio D,Cavalli R,Peira E

更新日期：2004-08-01 00:00:00

abstract：PURPOSE:To characterize the uptake mechanism of zidovudine (AZT), a nucleoside reverse transcriptase inhibitor, in syncytiotrophoblast cells using the TR-TBT 18d-1 cell line previously established by our group. MATERIALS AND METHODS:The effects of several transporter inhibitors on the initial and steady-state apical u...

journal_title：Pharmaceutical research

authors： Sai Y,Nishimura T,Shimpo S,Chishu T,Sato K,Kose N,Terasaki T,Mukai C,Kitagaki S,Miyakoshi N,Kang YS,Nakashima E

更新日期：2008-07-01 00:00:00

abstract：:We report the chemical and enzymatic hydrolysis of two hydrophobic prodrugs of ganciclovir (3 = dipropionate ester; 4 = diadamantoate ester). Both prodrugs undergo hydrolysis showing a pH dependence of kobs = kH+aH+ + ko + kHO-aHO- and a pH of maximum stability near pH 5. Only 4 exhibited a shelf life (t90) greater th...

journal_title：Pharmaceutical research

authors： Powell MF,Magill A,Chu N,Hama K,Mau CI,Foster L,Bergstrom R

更新日期：1991-11-01 00:00:00

abstract：PURPOSE:To investigate influence of inflammation on metabolism and pharmacokinetics (PK) of midazolam (MDZ) and construct a semi-physiologically based pharmacokinetic (PBPK) model to predict PK in mice with inflammatory disease. METHODS:Glucose-6-phosphate isomerase (GPI)-mediated inflammation was used as a preclinica...

journal_title：Pharmaceutical research

authors： Varkhede N,Patel N,Chang W,Ruterbories K,Forrest ML

更新日期：2018-06-21 00:00:00

abstract：PURPOSE:Carboxylesterases are important in the detoxification of drugs, pesticides and other xenobiotics. This study was to evaluate a series of substrates and inhibitors for characterizing these enzymes. METHODS:A series of novel aliphatic esters and thioesters were used in spectral assays to monitor human, murine an...

journal_title：Pharmaceutical research

authors： Huang TL,Shiotsuki T,Uematsu T,Borhan B,Li QX,Hammock BD

更新日期：1996-10-01 00:00:00

abstract：PURPOSE:Nonlinear conjugation metabolic rate of valproic acid (VPA) has been speculated previously from plasma elimination and liver concentration of VPA in guinea pigs. The purposes of the present study were to assess our speculation by direct measurement of VPA glucuronidation rate in vitro. METHODS:VPA at various c...

journal_title：Pharmaceutical research

authors： Yu HY,Shen YZ

更新日期：1996-08-01 00:00:00

abstract：PURPOSE:We reported that suramin produced chemosensitization at nontoxic doses. This benefit was lost at the approximately 10-fold higher, maximally tolerated doses (MTD). The aim of the current study was to identify in patients the chemosensitizing suramin dose that delivers 10-50 microM plasma concentrations over 48 ...

journal_title：Pharmaceutical research

authors： Chen D,Song SH,Wientjes MG,Yeh TK,Zhao L,Villalona-Calero M,Otterson GA,Jensen R,Grever M,Murgo AJ,Au JL

更新日期：2006-06-01 00:00:00

abstract：PURPOSE:The purpose of this study was to establish a useful methodology, possibly providing information on the stoichiometry of pharmaceutical drug salts obtained from salt screening by using a multiwell plate and a Raman microscope. METHODS:Tamoxifen salt screening was conducted with monobasic and polybasic acids on ...

journal_title：Pharmaceutical research

authors： Kojima T,Onoue S,Murase N,Katoh F,Mano T,Matsuda Y

更新日期：2006-04-01 00:00:00

abstract：PURPOSE:A series of studies was conducted to evaluate the preclinical pharmacokinetics of SB-239063 (trans-1-(4-hydroxycyclohexyl)-4-(4-fluorophenyl)-5-[(2-methoxy)pyrimidin-4-yl] imidazole), a potent and selective p38 MAP kinase inhibitor. METHODS:SB-239063 was administered both i.v. and p.o. in the rat, dog, cynomol...

journal_title：Pharmaceutical research

authors： Ward KW,Proksch JW,Azzarano LM,Salyers KL,McSurdy-Freed JE,Molnar TM,Levy MA,Smith BR

更新日期：2001-09-01 00:00:00

abstract：PURPOSE:Generation of valuable information about the biphasic geometrical configuration of porcine stratum corneum from Very Small Angle Neutron Scattering (VSANS) data and investigation of its effect on the corresponding effective diffusivity. METHODS:Spectra of porcine stratum corneum are mathematically transformed ...

journal_title：Pharmaceutical research

authors： Charalambopoulou GC,Karamertzanis P,Kikkinides ES,Stubos AK,Kanellopoulos NK,Papaioannou AT

更新日期：2000-09-01 00:00:00

abstract：PURPOSE:An ex vivo intact toe model was developed to assess two different applicator designs for iontophoretic delivery of terbinafine into the nail only or the nail and surrounding skin. METHODS:Iontophoretic permeation studies were carried out on intact cadaver toes using nail-only and nail/skin applicators with a c...

journal_title：Pharmaceutical research

authors： Nair AB,Kim HD,Davis SP,Etheredge R,Barsness M,Friden PM,Murthy SN

更新日期：2009-09-01 00:00:00

abstract：:The pharmacokinetics of and biologic response modification by recombinant human interferon-beta ser (rIFN-beta ser) were evaluated in 12 healthy male volunteers. Subjects received a single intravenous (iv) injection of 90 x 10(6) IU of rIFN-beta ser followed by a single or eight consecutive daily 90 x 10(6) IU subcuta...

journal_title：Pharmaceutical research

authors： Chiang J,Gloff CA,Yoshizawa CN,Williams GJ

更新日期：1993-04-01 00:00:00