Comparison of the hanson microette and the Van Kel apparatus for in vitro release testing of topical semisolid formulations.

abstract：PURPOSE:Herein we report the discovery of a group of derivatized alpha-amino acids that increase the oral bioavailability of sodium cromolyn. METHODS:We prepared three N-acylated alpha-amino acids and used these compounds to demonstrate the oral delivery of cromolyn in an in vivo rat model. In vitro experiments, inclu...

journal_title：Pharmaceutical research

authors： Leone-Bay A,Leipold H,Sarubbi D,Variano B,Rivera T,Baughman RA

更新日期：1996-02-01 00:00:00

abstract：:Published permeability coefficient (Kp) data for the transport of a large group of compounds through mammalian epidermis were analyzed by a simple model based upon permeant size [molecular volume (MV) or molecular weight (MW)] and octanol/water partition coefficient (Koct). The analysis presented is a facile means to ...

journal_title：Pharmaceutical research

authors： Potts RO,Guy RH

更新日期：1992-05-01 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：PURPOSE:To address the problem of precipitation of a poorly soluble drug during dissolution of highly soluble cocrystals by preparing granules intimately mixed with a water-soluble polymer. METHODS:Effectiveness of polymers as precipitation inhibitors during the dissolution of carbamazepine-nicotinamide (CBZ-NCT) cocr...

journal_title：Pharmaceutical research

authors： Yamashita H,Sun CC

更新日期：2019-04-23 00:00:00

abstract：PURPOSE:To investigate the effect of γ-irradiation of poly(lactic-co-glycolic acid) (PLGA)/Al(OH)₃/0 or 5 wt% diethyl phthalate (DEP) microspheres for active self-healing encapsulation of vaccine antigens. METHODS:Microspheres were irradiated with ⁶⁰Co at 2.5 and 1.8 MRad and 0.37 and 0.20 MRad/h. Encapsulation of tet...

journal_title：Pharmaceutical research

authors： Desai KG,Kadous S,Schwendeman SP

更新日期：2013-07-01 00:00:00

abstract：PURPOSE:To evaluate organic anion transporter-mediated drug-drug interaction (DDI) potential for individual active components of Danshen (Salvia miltiorrhiza) vs. combinations using in vitro and in silico approaches. METHODS:Inhibition profiles for single Danshen components and combinations were generated in stably-ex...

journal_title：Pharmaceutical research

authors： Wang L,Venitz J,Sweet DH

更新日期：2014-12-01 00:00:00

abstract：:An open, randomized, six-way crossover study was conducted in 12 healthy males to assess pharmacokinetics and bioinversion of ibuprofen enantiomers. The mean plasma terminal half-life (t1/2) of R(-)ibuprofen was 1.74 hr when intravenously infused as a racemic mixture and was 1.84 hr when intravenously infused alone. T...

journal_title：Pharmaceutical research

authors： Cheng H,Rogers JD,Demetriades JL,Holland SD,Seibold JR,Depuy E

更新日期：1994-06-01 00:00:00

abstract：PURPOSE:The objective of the current study was to investigate whether blood-brain barrier (BBB) permeability studies in vitro could be accelerated by running several compounds together in the same experiment. METHODS:To address this question, we compared the transport of six compounds run separately with the results o...

journal_title：Pharmaceutical research

authors： Berezowski V,Landry C,Lundquist S,Dehouck L,Cecchelli R,Dehouck MP,Fenart L

更新日期：2004-05-01 00:00:00

abstract：PURPOSE:To examine the transport characteristics of the multidrug resistance-associated protein (MRP) substrate fluorescein across the isolated rat small intestinal segments. METHODS:The transport of fluorescein was studied in side-by-side diffusion chambers under short-circuited conditions at physiological pH. RESUL...

journal_title：Pharmaceutical research

authors： Legen I,Kristl A

更新日期：2004-04-01 00:00:00

abstract：:A two-step analytic procedure to determine the rate and extent of metabolite production following administration of the parent compound is described. The procedure provides the rate and extent of metabolite production as a function of time by application of the general model independent approach of deconvolution. The ...

journal_title：Pharmaceutical research

authors： Karol MD,Goodrich S

更新日期：1988-06-01 00:00:00

abstract：:A rapid quantitative, enantioselective HPLC method for the analysis of the four stereoisomers, (+) and (-) erythro and (+) and (-) threo forms, of mefloquine has been developed using a Chiralpak Ad analytical column containing amylose tris-3,5-dimethylphenyl carbonate coated on silica gel and hexane/ethanol/diethylami...

journal_title：Pharmaceutical research

authors： Qiu Y,Kitamura S,Guillory JK

更新日期：1992-12-01 00:00:00

abstract：PURPOSE:Paclitaxel is active and widely used to treat multiple types of solid tumors. The commercially available paclitaxel formulation uses Cremophor/ethanol (C/E) as the solubilizers. Other formulations including nanoparticles have been introduced. This study evaluated the effects of nanoparticle formulation of pacli...

journal_title：Pharmaceutical research

authors： Yeh TK,Lu Z,Wientjes MG,Au JL

更新日期：2005-06-01 00:00:00

abstract：PURPOSE:Monocarboxylate transporter (MCT) inhibition represents a potential treatment strategy for γ-hydroxybutyric acid (GHB) overdose by blocking its renal reabsorption in the kidney. This study further evaluated the effects of a novel, highly potent MCT inhibitor, AR-C155858, on GHB toxicokinetics/toxicodynamics (TK...

journal_title：Pharmaceutical research

authors： Vijay N,Morse BL,Morris ME

更新日期：2015-06-01 00:00:00

abstract：PURPOSE:To study the oxidative degradation of drugs using a hydrophilic free radical initiator, 2,2'-Azobis(-amidinopropane) dihydrochloride (AAPH). METHODS:AAPH was used as the free radical initiator to study oxidation of three model compounds (A, B, and C), which represent different oxidizable moieties. In the solut...

journal_title：Pharmaceutical research

authors： Betigeri S,Thakur A,Raghavan K

更新日期：2005-02-01 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:Targeted delivery of aerosols could not only improve efficacy of inhaled drugs but also reduce side effects resulting from their accumulation in healthy tissue. Here we investigated the impact of magnetized aerosols on model drug accumulation and transgene expression in magnetically targeted lung regions of una...

journal_title：Pharmaceutical research

authors： Hasenpusch G,Geiger J,Wagner K,Mykhaylyk O,Wiekhorst F,Trahms L,Heidsieck A,Gleich B,Bergemann C,Aneja MK,Rudolph C

更新日期：2012-05-01 00:00:00

abstract：:The transport characteristics of the renin inhibitor ((3S,4S)-4-[N-morpholinoacetyl-(1-naphthyl)-L-alanyl-N-methyl-(4-t hiazolyl)-L- alanyl]amino-3-hydroxy-5-cyclohexyl-1-(4-pyridyl)-1-pentanone; CH3-18) in rat small intestinal brush-border membrane vesicles (BBMV) were examined by a rapid filtration technique. The up...

journal_title：Pharmaceutical research

authors： Hashimoto N,Fujioka T,Toyoda T,Muranushi N,Hirano K

更新日期：1994-10-01 00:00:00

abstract：PURPOSE:The purpose of this study was to investigate the effects of formulation factors including varying wax concentration, drug loading and drug particle size, on drug release characteristics from both pure oil and gel formulations prepared with a combination of derivatized vegetable oil (Labrafil 1944 CS) and glycer...

journal_title：Pharmaceutical research

authors： Gao ZH,Shukla AJ,Johnson JR,Crowley WR

更新日期：1995-06-01 00:00:00

abstract：:The effects of tertiary amine-containing basic drugs on the enzymes located in the mitochondria and the effect of monoamine oxidase inhibitors (MAOIs) on drug accumulation in lung mitochondria have been studied. Various basic drugs inhibited MAO activity but not other mitochondrial marker enzymes. The potency of MAO i...

journal_title：Pharmaceutical research

authors： Yoshida H,Kamiya A,Okumura K,Hori R

更新日期：1989-10-01 00:00:00

abstract：:Cyclosporine (CsA) is commercially available for oral administration as a solution in olive oil with alcohol and an emulsifier. To improve its variable absorption and low patient acceptability, several oral formulations were prepared and tested in vitro and in vivo in dogs. A tablet formulation prepared by direct comp...

journal_title：Pharmaceutical research

authors： Abdallah HY,Mayersohn M

更新日期：1991-04-01 00:00:00

abstract：PURPOSE:Tissue partitioning is an important component of drug distribution and half-life. Protein binding and lipid partitioning together determine drug distribution. METHODS:Two structure-based models to predict partitioning into microsomal membranes are presented. An orientation-based model was developed using a mem...

journal_title：Pharmaceutical research

authors： Nagar S,Korzekwa K

更新日期：2017-03-01 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：:An oral formulation of controlled-release isosorbide-5-nitrate pellets has been used to investigate the location of pellets in the gastrointestinal (GI) tract and, in parallel, to measure the drug absorption from these locations. Using the method of gamma scintigraphy the transit times and spreading of pellets in the ...

journal_title：Pharmaceutical research

authors： Fischer W,Boertz A,Davis SS,Khosla R,Cawello W,Sandrock K,Cordes G

更新日期：1987-12-01 00:00:00

abstract：:Four lipophilic, low molecular weight drugs solubilized in phosphatidylcholine-bile salt mixed micelles were injected s.c. into the hind legs of sheep and their cumulative recoveries in lymph draining from the site of application were determined. Surprisingly, the cumulative recoveries (percentage of dose) varied betw...

journal_title：Pharmaceutical research

authors： Supersaxo A,Hein WR,Steffen H

更新日期：1991-10-01 00:00:00

abstract：PURPOSE:Understanding the critical factors governing the crystallization tendency of organic compounds is vital when assessing the feasibility of an amorphous formulation to improve oral bioavailability. The objective of this study was to investigate potential links between viscosity and crystallization tendency for or...

journal_title：Pharmaceutical research

authors： Baird JA,Santiago-Quinonez D,Rinaldi C,Taylor LS

更新日期：2012-01-01 00:00:00

abstract：:Interogan variation in tissue distribution of weakly basic drugs such as quinidine, propranolol, and imipramine was investigated as a function of binding to phosphatidylserine (PhS) in tissues. Tissue distributions of these drugs were determined using 10 different tissues at a steady-state plasma concentration and wer...

journal_title：Pharmaceutical research

authors： Yata N,Toyoda T,Murakami T,Nishiura A,Higashi Y

更新日期：1990-10-01 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：:The delivery of therapeutic nucleic acids to neurons has the potential to treat neurological disease and spinal cord injury. While select viral vectors have shown promise as gene carriers to neurons, their potential as therapeutic agents is limited by their toxicity and immunogenicity, their broad tropism, and the cos...

journal_title：Pharmaceutical research

authors： Bergen JM,Park IK,Horner PJ,Pun SH

更新日期：2008-05-01 00:00:00

abstract：PURPOSE:To show, using a model study, how electronic structure theory can be applied in combination with LC/UV/MS/MS for the prediction and identification of oxidative degradants. METHODS:The benzyloxazole 1, was used to represent an active pharmaceutical ingredient for oxidative forced degradation studies. Bond disso...

journal_title：Pharmaceutical research

authors： Reid DL,Calvitt CJ,Zell MT,Miller KG,Kingsmill CA

更新日期：2004-09-01 00:00:00

abstract：PURPOSE:Platinum-based therapies are the first line treatments for most types of cancer including ovarian cancer. However, their use is associated with dose-limiting toxicities and resistance. We report initial translational studies of a theranostic nanoemulsion loaded with a cisplatin derivative, myrisplatin and pro-a...

journal_title：Pharmaceutical research

authors： Ganta S,Singh A,Kulkarni P,Keeler AW,Piroyan A,Sawant RR,Patel NR,Davis B,Ferris C,O'Neal S,Zamboni W,Amiji MM,Coleman TP

更新日期：2015-08-01 00:00:00