An in vitro/in vivo correlation for the disintegration and onset of drug release from enteric-coated pellets.

abstract：:Despite substantial research carried out over the last decades, it remains difficult to understand the wide range of pharmacological effects of dopaminergic agents. The dopaminergic system is involved in several neurological disorders, such as Parkinson's disease and schizophrenia. This complex system features multipl...

journal_title：Pharmaceutical research

authors： van den Brink WJ,Palic S,Köhler I,de Lange ECM

更新日期：2018-02-15 00:00:00

abstract：:The effect of the penetration enhancers Azone, oleic acid, 1-dodecanol, dodecyl N,N-dimethylaminoacetate (DDAA), and dodecyl N,N-dimethylaminoisopropionate (DDAIP) on epithelial membrane lipids was examined using human buccal cell membranes as a model for epithelial lipid bilayer. Buccal epithelial cells (BEC) were la...

journal_title：Pharmaceutical research

authors： Turunen TM,Urtti A,Paronen P,Audus KL,Rytting JH

更新日期：1994-02-01 00:00:00

abstract：:Chemoembolization using microspheres of 100- to 200-microns is a useful way to treat primary and secondary hepatic tumors. In a search for a better embolic material, we described in detail the preparation and characterization of a poly(benzyl l-glutamate) (PBLG) microspheres containing cisplatin (CDDP). We determined ...

journal_title：Pharmaceutical research

authors： Li C,Yang DJ,Nikiforow S,Tansey W,Kuang LR,Wright KC,Wallace S

更新日期：1994-12-01 00:00:00

abstract：PURPOSE:The work aims at investigating the correlation of water sorption potential with different measures of molecular mobility in an annealed amorphous model compound (trehalose). METHODS:Amorphous trehalose, prepared by freeze-drying, was annealed at 100°C (17°C < T (g)) for up to 120 h. Global mo...

journal_title：Pharmaceutical research

authors： Bhardwaj SP,Suryanarayanan R

更新日期：2013-03-01 00:00:00

abstract：PURPOSE:There is evidence that cholesterol affects the ATPase and transport functions of P-glycoprotein (P-gp). To study the influence of cholesterol on P-gp in a well defined lipid environment, we reconstituted P-gp in egg phosphatidylcholine (PhC) and PhC/cholesterol proteoliposomes with negligible residual amounts o...

journal_title：Pharmaceutical research

authors： Bucher K,Belli S,Wunderli-Allenspach H,Krämer SD

更新日期：2007-11-01 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:Our previous studies indicated that drug leaked from discoidal reconstituted high density lipoprotein (d-rHDL) during the remodeling behaviors induced by lecithin cholesterol acyl transferase (LCAT) abundant in circulation, thus decreasing the drug amount delivered into the target. In this study, arachidonic ac...

journal_title：Pharmaceutical research

authors： He H,Liu L,Bai H,Wang J,Zhang Y,Zhang W,Zhang M,Wu Z,Liu J

更新日期：2014-07-01 00:00:00

abstract：PURPOSE:A pattern fitting procedure using X-ray powder diffraction patterns was applied to study the crystallization kinetics of amorphous griseofulvin. From the optimized parameters obtained by pattern fitting, a change in the quantity and quality of griseofulvin crystals with crystallization was also investigated. M...

journal_title：Pharmaceutical research

authors： Yamamura S,Takahira R,Momose Y

更新日期：2007-05-01 00:00:00

abstract：PURPOSE:To develop resource-sparing in silico approaches that aim to reduce experimental effort and material required by developability assessments (DA) of monoclonal antibody (mAb) drug candidates. METHODS:A battery of standardized biophysical experiments was performed on high concentration formulations of 16 drug pr...

journal_title：Pharmaceutical research

authors： Tomar DS,Singh SK,Li L,Broulidakis MP,Kumar S

更新日期：2018-08-20 00:00:00

abstract：PURPOSE:Proteasome inhibition induces endoplasmic reticulum (ER) stress and compensatory autophagy to relieve ER stress. Disturbance of intracellular calcium homeostasis can lead to ER stress and alter the autophagy process. It has been suggested that inhibition of the proteasome disrupts intracellular calcium homeosta...

journal_title：Pharmaceutical research

authors： Williams JA,Hou Y,Ni HM,Ding WX

更新日期：2013-09-01 00:00:00

abstract：UNLABELLED:PURPOSE; The aim of this study was to investigate asparagine (Asn) deamidation and aspartate (Asp) isomerization and to measure the content of isoaspartate (isoAsp) in recombinant human interleukin-11 (rhIL-11). METHODS:The rhIL-11 control and heat stressed samples were characterized with trypsin and endopr...

journal_title：Pharmaceutical research

authors： Zhang W,Czupryn JM,Boyle PT Jr,Amari J

更新日期：2002-08-01 00:00:00

abstract：PURPOSE:To study the role of unsaturated fatty acid ester substituents in the autoxidation of polysorbate 80 using quantitative kinetics. METHODS:Oxidation kinetics were monitored at 40 degrees C in aqueous solution by tracking head space oxygen consumption using a fiber optic oxygen sensor with phase shift fluorescen...

journal_title：Pharmaceutical research

authors： Yao J,Dokuru DK,Noestheden M,Park SS,Kerwin BA,Jona J,Ostovic D,Reid DL

更新日期：2009-10-01 00:00:00

abstract：PURPOSE:Supramolecular Biovectors (SMBV) consist of cross-linked cationic nanoparticles surrounded by a lipid membrane. The purpose was to study the structure of the lipid membrane and to characterise its interaction with the nanoparticles in order to differentiate SMBV from other polymer/lipid associations. METHODS:T...

journal_title：Pharmaceutical research

authors： De Miguel I,Imbertie L,Rieumajou V,Major M,Kravtzoff R,Betbeder D

更新日期：2000-07-01 00:00:00

abstract：:A series of multilamellar liposome dispersions was prepared from lipids of soy phosphatidylcholine or hydrogenated soy phosphatidylcholine containing from 0 to 30 mol% of either cholesterol, stearylamine, or dipalmitoyl phosphatidylglycerol. The liposome dispersions were aerosolized with a Collison nebulizer for 80 mi...

journal_title：Pharmaceutical research

authors： Niven RW,Schreier H

更新日期：1990-11-01 00:00:00

abstract：PURPOSE:Lapatinib, a small molecule EGFR/HER2 inhibitor, partially inhibits the outgrowth of HER2+ brain metastases in preclinical models and in a subset of CNS lesions in clinical trials of HER2+ breast cancer. We investigated the ability of lapatinib to reach therapeutic concentrations in the CNS following (14)C-lapa...

journal_title：Pharmaceutical research

authors： Taskar KS,Rudraraju V,Mittapalli RK,Samala R,Thorsheim HR,Lockman J,Gril B,Hua E,Palmieri D,Polli JW,Castellino S,Rubin SD,Lockman PR,Steeg PS,Smith QR

更新日期：2012-03-01 00:00:00

abstract：PURPOSE:Induction of cell-mediated immune (CMI) responses is crucial for vaccine-mediated protection against difficult vaccine targets, e.g., Chlamydia trachomatis (Ct). Adjuvants are included in subunit vaccines to potentiate immune responses, but many marketed adjuvants stimulate predominantly humoral immune response...

journal_title：Pharmaceutical research

authors： Schmidt ST,Neustrup MA,Harloff-Helleberg S,Korsholm KS,Rades T,Andersen P,Christensen D,Foged C

更新日期：2017-08-01 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：:The area function method for assessing zero-order (ko) drug absorption rates was compared to four other methods under conditions where variation occurs in the plasma concentration data and in the elimination rate constant (kel or k10) for one- or two-compartment models. For deviant kel values of a one-compartment mode...

journal_title：Pharmaceutical research

authors： Cheng HY,Jusko WJ

更新日期：1990-01-01 00:00:00

abstract：:Enoximone and piroximone are cardiotonic agents for use in patients with congestive heart failure. Electroanalytical studies revealed that the dihydroimidazolone functionality was oxidizable and that this property can be analytically useful. The compounds undergo a two-electron, irreversible oxidation in neutral to ac...

journal_title：Pharmaceutical research

authors： Housmyer CL,Lewis RL Jr

更新日期：1991-07-01 00:00:00

abstract：PURPOSE:This study focuses on the formulation optimization, in vitro and in vivo performance of differently sized nano-crystalline liquid suspensions and spray-dried powders of a poorly soluble BCS class II compound i.e. Danazol. METHODS:A DoE approach was utilized to optimize stabilizer concentration and formulate da...

journal_title：Pharmaceutical research

authors： Kumar S,Jog R,Shen J,Zolnik B,Sadrieh N,Burgess DJ

更新日期：2015-05-01 00:00:00

abstract：PURPOSE:The investigation was aimed at developing micellar nanocarriers for nose-to-brain delivery of zolmitriptan with the objective to investigate the pathway involved in the drug transport. METHODS:The micellar nanocarrier was successfully formulated and characterized for particle size and shape by multi-angle dyna...

journal_title：Pharmaceutical research

authors： Jain R,Nabar S,Dandekar P,Patravale V

更新日期：2010-04-01 00:00:00

abstract：:Transdermal drug delivery of ionized drugs can be enhanced by iontophoresis. Drug in the ionic form, contained in some reservoir, can be "phoresed" through the skin with a small current across two electrodes, one above the reservoir and one at a distal skin location. Positive ions can be introduced from the positive p...

journal_title：Pharmaceutical research

authors： Tyle P

更新日期：1986-12-01 00:00:00

abstract：:The transient dynamic swelling and dissolution behavior during the release of a growth hormone releasing peptide, [D-Trp2-D-Phe5]GHRP, from erodible, non-cross-linked poly(methyl methacrylate-co-methacrylic acid) (PMMA/MAA) beads has been investigated at pH 7.4 as a function of buffer concentration. Although the swell...

journal_title：Pharmaceutical research

authors： Lee PI

更新日期：1993-07-01 00:00:00

abstract：PURPOSE:The aim of the present study was to improve the dry powder inhalation behavior of steroid KSR-592 with lactose by altering the crystal shape and the particle size of the drug for use in a newly designed inhalation device, Jethaler. METHOD:The shape of the crystals was changed by polymorphic transformation of o...

journal_title：Pharmaceutical research

authors： Ikegami K,Kawashima Y,Takeuchi H,Yamamoto H,Isshiki N,Momose D,Ouchi K

更新日期：2002-10-01 00:00:00

abstract：:The transport of thyrotropin releasing hormone (TRH) in rabbit buccal mucosa in vitro has been investigated with respect to (a) rate and type of metabolism of TRH on mucosal and serosal sides of buccal mucosa, (b) mechanism of TRH transport including charge effect on its permeability, and (c) pathway and rate-limiting...

journal_title：Pharmaceutical research

authors： Dowty ME,Knuth KE,Irons BK,Robinson JR

更新日期：1992-09-01 00:00:00

abstract：PURPOSE:The aim of this study was to investigate the depth-dependent intradermal immunogenicity of inactivated polio vaccine (IPV) delivered by depth-controlled microinjections via hollow microneedles (HMN) and to investigate antibody response enhancing effects of IPV immunization adjuvanted with CpG oligodeoxynucleoti...

journal_title：Pharmaceutical research

authors： Schipper P,van der Maaden K,Romeijn S,Oomens C,Kersten G,Jiskoot W,Bouwstra J

更新日期：2016-09-01 00:00:00

abstract：PURPOSE:To examine the presence of multiplicity for the biliary excretion of xenobiotic conjugates, we studied the disposition of glycyrrhizin (GR), which has glucuronide within its molecular structure and has the ability to inhibit the biliary excretion of liquiritigenin (LG) glucuronides. METHODS:GR was administered...

journal_title：Pharmaceutical research

authors： Shimamura H,Suzuki H,Tagaya O,Horie T,Sugiyama Y

更新日期：1996-12-01 00:00:00

abstract：PURPOSE:The purpose of this study was to obtain an in vitro/in vivo correlation for the sustained release of a protein from poly(ethylene glycol) terephthalate (PEGT)/poly(butylene terephthalate) (PBT) microspheres. METHODS:Radiolabeled lysozyme was encapsulated in PEGT/PBT microspheres via a water-in-oil-in-water emu...

journal_title：Pharmaceutical research

authors： van Dijkhuizen-Radersma R,Wright SJ,Taylor LM,John BA,de Groot K,Bezemer JM

更新日期：2004-03-01 00:00:00

abstract：PURPOSE:A mechanism-based PK-PD model was developed to predict the time course of dopamine D(2) receptor occupancy (D(2)RO) in rat striatum following administration of olanzapine, an atypical antipsychotic drug. METHODS:A population approach was utilized to quantify both the pharmacokinetics and pharmacodynamics of ol...

journal_title：Pharmaceutical research

authors： Johnson M,Kozielska M,Pilla Reddy V,Vermeulen A,Li C,Grimwood S,de Greef R,Groothuis GM,Danhof M,Proost JH

更新日期：2011-10-01 00:00:00

abstract：PURPOSE:To investigate cellular uptake pathways of novel anionic siRNA-lipoplexes as a function of formulation composition. METHODS:Anionic formulations with anionic lipid/Ca(2+)/siRNA ratio of 1.3/2.5/1 (AF1) and 1.3/0.3/1 (AF2) were utilized. Uptake mechanisms were investigated using uptake inhibition and co-localiz...

journal_title：Pharmaceutical research

authors： Kapoor M,Burgess DJ

更新日期：2013-04-01 00:00:00