In vivo and in vitro diclofenac sodium evaluation after rectal application of soft gelatine capsules enabling application induced transformation (AIT) into a semisolid system of liquid crystals (SSLC) for controlled release.

abstract：PURPOSE:The blood-brain barrier (BBB) essentially restricts therapeutic drugs from entering into the brain. This study tests the hypothesis that brain endothelial cell derived exosomes can deliver anticancer drug across the BBB for the treatment of brain cancer in a zebrafish (Danio rerio) model. MATERIALS AND METHODS...

journal_title：Pharmaceutical research

authors： Yang T,Martin P,Fogarty B,Brown A,Schurman K,Phipps R,Yin VP,Lockman P,Bai S

更新日期：2015-06-01 00:00:00

abstract：PURPOSE:The aim of the study is to determine whether a biodegradable elastomeric device that uses an osmotic pressure delivery mechanism can release different therapeutic proteins at a nearly constant rate in nanomolar concentrations with high bioactivity, given the same formulation conditions. Vascular endothelial gro...

journal_title：Pharmaceutical research

authors： Gu F,Neufeld R,Amsden B

更新日期：2006-04-01 00:00:00

abstract：PURPOSE:Radial basis function artificial neural networks and theoretical descriptors were used to develop a quantitative structure-pharmacokinetic relationship for structurally diverse drug compounds. METHODS:Human bioavailability values were taken from the literature and descriptors were generated from the drug struc...

journal_title：Pharmaceutical research

authors： Turner JV,Maddalena DJ,Agatonovic-Kustrin S

更新日期：2004-01-01 00:00:00

abstract：PURPOSE:The possibility of direct delivery of steroids through the skin to the trachea and the effect of iontophoresis on delivery efficacy were evaluated after the application of an ionic steroidal prodrug, prednisolone sodium succinate (PS-Na), to the throat skin. METHODS:Fluorescein sodium salt (FL-Na) and PS-Na we...

journal_title：Pharmaceutical research

authors： Ishii H,Suzuki T,Todo H,Kamimura M,Sugibayashi K

更新日期：2011-04-01 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 investigate the suitability of three antimicrobial peptides (AMPs) as cell-penetrating antimicrobial peptides. METHODS:Cellular uptake of three AMPs (PK-12-KKP, SA-3 and TPk) and a cell-penetrating peptide (penetratin), all 5(6)-carboxytetramethylrhodamine-labeled, were tested in HeLa WT cells and analyzed ...

journal_title：Pharmaceutical research

authors： Bahnsen JS,Franzyk H,Sayers EJ,Jones AT,Nielsen HM

更新日期：2015-05-01 00:00:00

abstract：PURPOSE:Calculation of the ideal solubility of a crystalline solute in a liquid solvent requires knowledge of the difference in the molar heat capacity at constant pressure of the solid and the supercooled liquid forms of the solute, delta Cp. Since this parameter is not usually known, two assumptions have been used to...

journal_title：Pharmaceutical research

authors： Neau SH,Bhandarkar SV,Hellmuth EW

更新日期：1997-05-01 00:00:00

abstract：PURPOSE:For passive dry powder inhalers (DPIs) entrainment and emission of the aerosolized drug dose depends strongly on device geometry and the patient's inhalation manoeuvre. We propose a computational method for optimizing the entrainment part of a DPI. The approach assumes that the pulmonary delivery location of ae...

journal_title：Pharmaceutical research

authors： Kopsch T,Murnane D,Symons D

更新日期：2016-11-01 00:00:00

abstract：PURPOSE:We aimed to assess the fate of β-arteether lipid-based drug delivery systems (AE-LBDDS) in terms of resistance to lipolysis and permeation across intestinal cells. METHODS:AE-LBDDS contained Tween 80 or Cremophor EL as surfactants, ethanol, Maisine 35-1 and vegetable oil. The solubilization behavior of AE was ...

journal_title：Pharmaceutical research

authors： Memvanga PB,Eloy P,Gaigneaux EM,Préat V

更新日期：2013-10-01 00:00:00

abstract：PURPOSE:Performance of a transdermal delivery system (TDS) can be affected by exposure to elevated temperature, which can lead to unintended safety issues. This study investigated TDS and skin temperatures and their relationship in vivo, characterized the effective thermal resistance of skin, and identified the in vitr...

journal_title：Pharmaceutical research

authors： Zhang Q,Murawsky M,LaCount T,Hao J,Kasting GB,Newman B,Ghosh P,Raney SG,Li SK

更新日期：2017-07-01 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：:Microbial metabolism studies of the antimalarial drug arteether (1) have shown that arteether is metabolized by a number of microorganisms. Large-scale fermentation with Aspergillus niger (ATCC 10549) and Nocardia corallina (ATCC 19070) have resulted in the isolation of four microbial metabolites which have been chara...

journal_title：Pharmaceutical research

authors： Lee IS,ElSohly HN,Hufford CD

更新日期：1990-02-01 00:00:00

abstract：PURPOSE:A major challenge facing nanoparticle-based delivery of chemotherapy agents is the natural and unavoidable accumulation of these particles in healthy tissue resulting in local toxicity and dose-limiting side effects. To address this issue, we have designed and characterized a new prodrug nanoparticle with contr...

journal_title：Pharmaceutical research

authors： Schutt C,Ibsen S,Zahavy E,Aryal S,Kuo S,Esener S,Berns M,Esener S

更新日期：2017-10-01 00:00:00

abstract：:The new generation of nanotechnology-based drug formulations is challenging the accepted ways of cancer treatment. Multi-functional nanomaterial constructs have the capability to be delivered directly to the tumor site and eradicate cancer cells selectively, while sparing healthy cells. Tailoring of the nano-construct...

journal_title：Pharmaceutical research

authors： Farrell D,Ptak K,Panaro NJ,Grodzinski P

更新日期：2011-02-01 00:00:00

abstract：:The stability of an antibiotic formulation (clindamycin phosphate in dextrose), which is stable at room temperature, was assessed by nonisothermal kinetic analysis at elevated temperatures. A preliminary study, conducted to establish apparent rate order, verified the appropriateness of a first-order kinetic model. The...

journal_title：Pharmaceutical research

authors： Kipp JE,Hlavaty JJ

更新日期：1991-05-01 00:00:00

abstract：PURPOSE:This study aimed to develop a sustained-release formulation of exenatide (EXT) for the long-term therapeutic efficacy in the treatment of type II diabetes. METHODS:In this study, we present an injectable phospholipid gel by mixing biocompatible phospholipid S100, medium chain triglyceride (MCT) with 85% (w/w) ...

journal_title：Pharmaceutical research

authors： Hu M,Zhang Y,Xiang N,Zhong Y,Gong T,Zhang ZR,Fu Y

更新日期：2016-06-01 00:00:00

abstract：:A colorless, parallelepiped crystal of methyl (2R,3S)-N-benzoyl-3-phenylisoserinate belonging to the space group P2(1) with a = 5.414(4), b = 7.813(1), c = 17.802(7) A, beta = 90.87(4) degrees, Z = 2, V = 752.9 A3, Dcalc = 1.32 g cm-3, and mu calc = 1.02 cm-1 was selected and the structure solved using direct methods....

journal_title：Pharmaceutical research

authors： Peterson JR,Do HD,Rogers RD

更新日期：1991-07-01 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：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：PURPOSE:To identify materials and processes which effect supersaturation of the GI milieu for low solubility drugs in order to increase oral bioavailability. METHODS:A variety of small and polymeric molecules were screened for their ability to inhibit drug precipitation in supersaturated solutions. The best polymeric ...

journal_title：Pharmaceutical research

authors： Curatolo W,Nightingale JA,Herbig SM

更新日期：2009-06-01 00:00:00

abstract：PURPOSE:To determine the extent of lateral spread and stratum corneum (SC) penetration of caffeine (CAF), hydrocortisone (HC) and ibuprofen (IBU) using a novel concentric tape stripping technique. METHOD:Ethanolic solutions of CAF, HC or IBU were applied to the forearm of 8 volunteers. At various time points, 10 succe...

journal_title：Pharmaceutical research

authors： Gee CM,Nicolazzo JA,Watkinson AC,Finnin BC

更新日期：2012-08-01 00:00:00

abstract：PURPOSE:Relatively large (>5 microm) and porous (mass density <0.4 g/cm3) particles present advantages for the delivery of drugs to the lungs, e.g., excellent aerosolization properties. The aim of this study was, first, to formulate such particles with excipients that are either FDA-approved for inhalation or endogenou...

journal_title：Pharmaceutical research

authors： Vanbever R,Mintzes JD,Wang J,Nice J,Chen D,Batycky R,Langer R,Edwards DA

更新日期：1999-11-01 00:00:00

abstract：PURPOSE:A conventional approach to assess cytochrome P450 (CYP) induction in preclinical animal models involves daily dosing for a least a week followed by Western blot and/or enzyme activity analysis. To evaluate the potential benefit of a third more specific and sensitive assay, real-time quantitative reverse transcr...

journal_title：Pharmaceutical research

authors： Goodsaid FM,Palamanda JR,Montgomery D,Mandakas G,Gu C,Li Z,You X,Norton L,Smith R,Chu I,Soares T,Alton K,Kishnani NS,Rosenblum IY

更新日期：2003-09-01 00:00:00

abstract：PURPOSE:The purpose of this study is to investigate the characteristics of pGlu-L-Dopa-Pro as a prodrug of L-Dopa. METHODS:pGlu-L-Dopa-Pro and L-Dopa-Pro were synthesized using the standard procedures of peptide synthesis. The conversion of pGlu-L-Dopa-Pro to L-Dopa was studied using pyroglutamyl aminopeptidase I and ...

journal_title：Pharmaceutical research

authors： Bai JP

更新日期：1995-07-01 00:00:00

abstract：PURPOSE:Chemically modified heparin-DOCA was prepared and found to have markedly lower anticoagulant activity than heparin. In the present study, we elucidated the antiangiogenic and antitumoral activities of heparin-DOCA derivative. METHODS:To evaluate the antiangiogenic and antitumoral effects of heparin-DOCA, capil...

journal_title：Pharmaceutical research

authors： Park K,Kim YS,Lee GY,Nam JO,Lee SK,Park RW,Kim SY,Kim IS,Byun Y

更新日期：2007-01-01 00:00:00

abstract：:Transport studies using intestinal brush-border membrane vesicles isolated from rats and rabbits have failed to demonstrate proton- or Na(+)-dependent carrier-mediated transport of thyrotropin-releasing hormone (TRH), despite a pharmacologically relevant oral bioavailability. To examine the hypothesis that reported le...

journal_title：Pharmaceutical research

authors： Thwaites DT,Hirst BH,Simmons NL

更新日期：1993-05-01 00:00:00

abstract：:Many drugs and desirable phytochemicals are bitter, and bitter tastes are aversive. Food and pharmaceutical manufacturers share a common need for bitterness-masking strategies that allow them to deliver useful quantities of the active compounds in an acceptable form and in this review we compare and contrast the chall...

journal_title：Pharmaceutical research

authors： Coupland JN,Hayes JE

更新日期：2014-11-01 00:00:00

abstract：PURPOSE:To evaluate the use of an in vitro intestinal permeability model to predict rat and human absorption as well as to evaluate the use of an internal standard to control for intra- and inter-rat variability. METHODS:In vivo peroral absorption and in vitro steady-state intestinal permeability coefficients were det...

journal_title：Pharmaceutical research

authors： Dowty ME,Dietsch CR

更新日期：1997-12-01 00:00:00

abstract：PURPOSE:The purpose of the study is to characterize glycine crystallization during freezing of aqueous solutions as a function of the glycine salt form (i.e., neutral glycine, glycine hydrochloride, and sodium glycinate), pH, and ionic strength. METHODS:Crystallization was studied by thermal analysis, microscopy, x-ra...

journal_title：Pharmaceutical research

authors： Akers MJ,Milton N,Byrn SR,Nail SL

更新日期：1995-10-01 00:00:00

abstract：PURPOSE:To study the miscibility of proteins and polymer excipients in frozen solutions and freeze-dried solids as protein formulation models. METHODS:Thermal profiles of frozen solutions and freeze-dried solids containing various proteins (lysozyme, ovalbumin, BSA), nonionic polymers (Ficoll, polyvinylpyrrolidone [PV...

journal_title：Pharmaceutical research

authors： Izutsu K,Kojima S

更新日期：2000-10-01 00:00:00