Investigation into the influence of primary crystallization conditions on the mechanical properties and secondary processing behaviour of fluticasone propionate for carrier based dry powder inhaler formulations.

abstract：PURPOSE:This study aimed to investigate the impact of the size of X-ray iodinated contrast agent in nano-emulsions, on their toxicity and fate in vivo. METHODS:A new compound, triiodobenzoate cholecalciferol, was synthetized, formulated as nano-emulsions, and followed after i.v. administration in mice by X-ray imaging...

journal_title：Pharmaceutical research

authors： Attia MF,Anton N,Akasov R,Chiper M,Markvicheva E,Vandamme TF

更新日期：2016-03-01 00:00:00

abstract：:The relative effectiveness of two beta-cyclodextrin derivatives, i.e., dimethyl-beta-cyclodextrin (DM beta CD) and hydroxypropyl-beta-cyclodextrin (HP beta CD), in enhancing enteral absorption of insulin was evaluated in the lower jejunal/upper ileal segments of the rat by means of an in situ closed loop method. The i...

journal_title：Pharmaceutical research

authors： Shao Z,Li Y,Chermak T,Mitra AK

更新日期：1994-08-01 00:00:00

abstract：PURPOSE:To study the influence of cytotoxicity of macromolecules, VEGF gene expression, and vascular permeability on the enhanced permeability and retention (EPR) effect. METHODS:Mice bearing xenografts of A2780 multidrug resistant human ovarian carcinoma were treated by free doxorubicin (DOX) and N-(2-hydroxypropyl)m...

journal_title：Pharmaceutical research

authors： Minko T,Kopeckova P,Pozharov V,Jensen KD,Kopecek J

更新日期：2000-05-01 00:00:00

abstract：PURPOSE:Safe, targeted delivery of therapeutics remains a focus of drug/gene delivery, the aim being to achieve optimal efficacy while minimising off-target delivery. Dendrimers have a vast array of potential applications and have great potential as gene and drug delivery tools. We previously reported the development o...

journal_title：Pharmaceutical research

authors： Shah ND,Parekh HS,Steptoe RJ

更新日期：2014-11-01 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:Studies were conducted to investigate dilute solutions of the monoclonal antibody (mAb) bevacizumab, mAb fragment ranibizumab and fusion protein aflibercept, develop common procedures for formulation of low concentration mAbs and identify a stabilizing formulation for anti-VEGF mAbs for use in in vitro permeati...

journal_title：Pharmaceutical research

authors： Giannos SA,Kraft ER,Zhao ZY,Merkley KH,Cai J

更新日期：2018-02-28 00:00:00

abstract：PURPOSE:The purpose of this human intestinal perfusion study was to investigate the transport and metabolism of R/S-verapamil in the human jejunum (in vivo). METHODS:A regional single-pass perfusion of the jejunum was performed using a Loc-I-Gut perfusion tube in 12 healthy volunteers. Each perfusion lasted for 200 mi...

journal_title：Pharmaceutical research

authors： Sandström R,Karlsson A,Knutson L,Lennernäs H

更新日期：1998-06-01 00:00:00

abstract：:Using brine shrimp lethality to direct fractionation, extracts of the bark of Annona bullata Rich. (Annonaceae) have yielded 16 alpha-hydroxy-(-)-kauranoic acid as a bioactive plant constituent. This previously known diterpene showed significant (ED50 8.25 x 10(-2) micrograms/ml) and selective cytotoxicity against A-5...

journal_title：Pharmaceutical research

authors： Hui YH,Chang CJ,Smith DL,McLaughlin JL

更新日期：1990-04-01 00:00:00

abstract：:Nonstereospecific studies have indicated that the pharmacokinetics of propranolol (PR) are altered in inflammatory conditions such as arthritis. However, as the kinetics and dynamics of PR are stereoselective, we examined the effect of adjuvant arthritis (AA) on the disposition of the individual enantiomers. A novel n...

journal_title：Pharmaceutical research

authors： Piquette-Miller M,Jamali F

更新日期：1993-02-01 00:00:00

abstract：PURPOSE:To elucidate the key parameters affecting solute transport from semi-interpenetrating networks (sIPNs) comprised of poly(ethylene glycol) diacrylate (PEGdA) and gelatin that are partially crosslinked, water-swellable and biodegradable. Effects of material compositions, solute size, solubility, and loading densi...

journal_title：Pharmaceutical research

authors： Fu Y,Kao WJ

更新日期：2009-09-01 00:00:00

abstract：:We describe an assay for acrolein in urine, employing derivatization with m-aminophenol in the presence of ferrous sulfate solution in sulfuric acid. The derivative (7-OH quinoline; DER) and the internal standard (quinine-bisulfate; IS) were separated on a 10-micron particle, 8 mm x 10-cm C18 cartridge in conjunction ...

journal_title：Pharmaceutical research

authors： al-Rawithi S,el-Yazigi A,Nicholls PJ

更新日期：1993-11-01 00:00:00

abstract：PURPOSE:To investigate the effects of small aliphatic pendent groups conjugated through an acid-sensitive linker to the core of brushed block copolymer micelles on particle properties. METHODS:The brushed block copolymers were synthesized by conjugating five types of 2-alkanone (2-butanone, 2-hexanone, 2-octanone, 2-d...

journal_title：Pharmaceutical research

authors： Lee HJ,Bae Y

更新日期：2013-08-01 00:00:00

abstract：PURPOSE:The purpose of this study was to clarify the localization and function of the ATP-binding cassette transporter G2 (ABCG2; BCRP/MXR/ABCP) in retinal capillary endothelial cells, which form the inner blood-retinal barrier, as an efflux transport system. METHODS:The expression was determined by reverse transcript...

journal_title：Pharmaceutical research

authors： Asashima T,Hori S,Ohtsuki S,Tachikawa M,Watanabe M,Mukai C,Kitagaki S,Miyakoshi N,Terasaki T

更新日期：2006-06-01 00:00:00

abstract：PURPOSE:To dynamically analyze the processes of oral absorption and hepatobiliary distribution of telmisartan using positron emission tomography (PET). METHODS:(11)C-labeled telmisartan ([(11)C]TEL) was orally administered to rats with or without non-radiolabeled telmisartan (0.5, and 10 mg/kg). PET scanning of abdomi...

journal_title：Pharmaceutical research

authors： Kataoka M,Takashima T,Shingaki T,Hashidzume Y,Katayama Y,Wada Y,Oh H,Masaoka Y,Sakuma S,Sugiyama Y,Yamashita S,Watanabe Y

更新日期：2012-09-01 00:00:00

abstract：PURPOSE:Bioadhesion is an important property of biological membranes, that can be utilized in pharmaceutical and biomedical applications. In this study, we have fabricated mucoadhesive drug releasing films with bio-based, non-toxic and biodegradable polymers that do not require chemical modifications. METHODS:Nanofibr...

journal_title：Pharmaceutical research

authors： Laurén P,Paukkonen H,Lipiäinen T,Dong Y,Oksanen T,Räikkönen H,Ehlers H,Laaksonen P,Yliperttula M,Laaksonen T

更新日期：2018-05-22 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:Ultrasound can be used to release a therapeutic payload encapsulated within a perfluorocarbon (PFC) emulsion via acoustic droplet vaporization (ADV), a process whereby the PFC phase is vaporized and the agent is released. ADV-generated microbubbles have been previously used to selectively occlude blood vessels ...

journal_title：Pharmaceutical research

authors： Fabiilli ML,Lee JA,Kripfgans OD,Carson PL,Fowlkes JB

更新日期：2010-12-01 00:00:00

abstract：BACKGROUND:Little is known about the affinity and stability of 99mTc-labeled 2-methoxyisobutylisonitrile (99mTc-MIBI) and tetrofosmin (99mTc-TF) for imaging of multiple drug resistance transporters in cancer. We examined the affinity of 99mTc-labeled compounds for these transporters and their stability. METHODS:99mTc-...

journal_title：Pharmaceutical research

authors： Kobayashi M,Tsujiuchi T,Okui Y,Mizutani A,Nishi K,Nakanishi T,Nishii R,Fukuchi K,Tamai I,Kawai K

更新日期：2018-11-29 00:00:00

abstract：PURPOSE:The purpose was to develop a population pharmacokinetic model for montelukast after intravenous administration. Clinical trial simulations were conducted using the model developed to identify the lowest intravenous dose in 6- to 14-year-old children that would give montelukast systemic exposures that were compa...

journal_title：Pharmaceutical research

authors： Ramakrishnan R,Migoya E,Knorr B

更新日期：2005-04-01 00:00:00

abstract：PURPOSE:Studies were conducted to evaluate whether the use of an in vitro model of the blood-brain barrier (BBB) resulted in more accurate predictions of the in vivo transport of compounds compared to the use of a human intestinal cell line (Caco-2). METHODS:The in vitro BBB model employs bovine brain capillary endoth...

journal_title：Pharmaceutical research

authors： Lundquist S,Renftel M,Brillault J,Fenart L,Cecchelli R,Dehouck MP

更新日期：2002-07-01 00:00:00

abstract：:The limitations of traditional gas adsorption models for describing water vapor sorption by amorphous pharmaceutical solids are described and an alternative approach based on polymer solution theories is proposed. The approach is tested by comparing a priori predicted isotherms with literature data for the poly(vinylp...

journal_title：Pharmaceutical research

authors： Hancock BC,Zografi G

更新日期：1993-09-01 00:00:00

abstract：PURPOSE:We evaluated the effect of luminal bacterial metabolism on intestinal absorption of azetirelin in rats. In vitro characteristics of bacterial metabolism of azetirelin were also investigated with the goal of overcoming the low stability of the peptidic drug against luminal microorganisms. METHODS:Plasma azetire...

journal_title：Pharmaceutical research

authors： Sasaki I,Tamura T,Shibakawa T,Fujita T,Murakami M,Yamamoto A,Muranishi S

更新日期：1997-08-01 00:00:00

abstract：PURPOSE:Reverse iontophoresis is an alternative to blood sampling for the monitoring of endogenous molecules. Here, the potential of the technique to measure urea and potassium levels non-invasively, and to track their concentrations during hemodialysis, has been examined. MATERIALS AND METHODS:In vitro experiments we...

journal_title：Pharmaceutical research

authors： Wascotte V,Delgado-Charro MB,Rozet E,Wallemacq P,Hubert P,Guy RH,Préat V

更新日期：2007-06-01 00:00:00

abstract：PURPOSE:To study the pulmonary absorption and tolerability of various formulations of the decapeptide cetrorelix acetate in rats by a new aerosol delivery system (ASTA-ADS) for intratracheal application. METHODS:Using the ASTA-ADS, cetrorelix liquid formulations (aqueous solutions for ultrasonic nebulization) were fir...

journal_title：Pharmaceutical research

authors： Lizio R,Klenner T,Sarlikiotis AW,Romeis P,Marx D,Nolte T,Jahn W,Borchard G,Lehr CM

更新日期：2001-06-01 00:00:00

abstract：PURPOSE:TXA9, a novel cardiac glycoside, has a potent anti-proliferative effect against A549 human lung cancer cells, however, possesses a poor water-solubility and a rapid metabolic rate in vivo which limited the further development of TXA9. To overcome the shortcomings of TXA9, four polymer prodrugs of TXA9 were desi...

journal_title：Pharmaceutical research

authors： Li Y,Ye C,Cai C,Zhao M,Han N,Liu Z,Zhai J,Yin J

更新日期：2020-03-12 00:00:00

abstract：PURPOSE:Hydrogen/deuterium (H/D) exchange over a range of temperatures suggests a protein structural/mobility transition in the solid state below the system glass transition temperature (Tg). The purpose of this study was to determine whether solid-state protein stability correlates with the difference between storage ...

journal_title：Pharmaceutical research

authors： Fang R,Obeidat W,Pikal MJ,Bogner RH

更新日期：2020-08-13 00:00:00

abstract：PURPOSE:The fate of inhaled salmon calcitonin (sCT) at the respiratory epithelial barrier was studied with particular emphasis on enzymatic degradation by trypsin, chymotrypsin, and neutrophil elastase. METHODS:Degradation of sCT was assessed by HPLC in cell homogenate, supernatant and intact monolayers of human respi...

journal_title：Pharmaceutical research

authors： Baginski L,Tewes F,Buckley ST,Healy AM,Bakowsky U,Ehrhardt C

更新日期：2012-01-01 00:00:00

abstract：PURPOSE:LY3015014 is a humanized immunoglobulin G4 (IgG4) monoclonal antibody that binds to the catalytic domain of PCSK9 and reduce low-density lipoprotein cholesterol (LDL-C) in patients with hypercholesterolemia that is poorly controlled by maximally tolerated statin therapy. The objective of this pharmacokinetic/ph...

journal_title：Pharmaceutical research

authors： Shen T,James DE,Krueger KA

更新日期：2017-01-01 00:00:00

abstract：:Dihydropyridine ⇄ pyridinium salt-based brain-selective delivery systems were synthesized for the progestins, ethisterone, norethindrone, and norgestrel. After initial lipophilicity and in vitro studies indicated the feasibility of applying these compounds to brain-specific delivery, in vivo distribution studies were ...

journal_title：Pharmaceutical research

authors： Brewster ME,Estes KS,Bodor N

更新日期：1986-10-01 00:00:00

abstract：:A biopharmaceutics drug classification scheme for correlating in vitro drug product dissolution and in vivo bioavailability is proposed based on recognizing that drug dissolution and gastrointestinal permeability are the fundamental parameters controlling rate and extent of drug absorption. This analysis uses a transp...

journal_title：Pharmaceutical research

authors： Amidon GL,Lennernäs H,Shah VP,Crison JR

更新日期：1995-03-01 00:00:00