Heparin-paclitaxel conjugates using mixed anhydride as intermediate: synthesis, influence of polymer structure on drug release, anticoagulant activity and in vitro efficiency.

abstract：:Sulfasalazine, 60 mg/kg, was administered orally to groups of rats (n = 4) along with 1, 5, or 10 mg/kg of riboflavin. Plasma and urine were assayed for 5-aminosalicylic acid, acetyl-5-aminosalicylic acid, sulfapyridine, and acetyl-sulfapyridine using an HPLC method. The mean percent of dose recovered as total metabol...

journal_title：Pharmaceutical research

authors： Chungi VS,Dittert LW,Shargel L

更新日期：1989-12-01 00:00:00

abstract：PURPOSE:Generalizations based upon behavior of small molecules have established that a crystalline solid is generally much more stable toward chemical degradation than is the amorphous solid. This study examines the validity of this generalization for proteins using biosynthetic human insulin as the model protein. MET...

journal_title：Pharmaceutical research

authors： Pikal MJ,Rigsbee DR

更新日期：1997-10-01 00:00:00

abstract：:A reverse-phase HPLC method for the analysis of tryptic digests of recombinant porcine growth hormone (pGH) has been developed and validated. Digestion was performed at 4 degrees C for a 20-hr period with TPCK-treated trypsin at a 1:20 (w/w) trypsin:pGH ratio. Gradient elution HPLC, using an Aquapore RP300 C8 column, ...

journal_title：Pharmaceutical research

authors： Charman SA,McCrossin LE,Charman WN

更新日期：1993-10-01 00:00:00

abstract：:During the past two decades the nanomedicine field has experienced significant progress. To date, over sixty nanoparticle (NP) formulations have been approved in the US and EU while many others are in clinical or preclinical development, indicating a concerted effort to translate promising bench research to commercial...

journal_title：Pharmaceutical research

authors： Clogston JD,Hackley VA,Prina-Mello A,Puri S,Sonzini S,Soo PL

更新日期：2019-12-11 00:00:00

abstract：PURPOSE:To investigate the influence of nanocarrier molecular size and shape on breast duct retention in normal rats using a non-invasive optical imaging method. METHODS:Fluorescein-labeled PEG nanocarriers of different molecular weights and shapes (linear, two-arm, four-arm, and eight-arm) were intraductally administ...

journal_title：Pharmaceutical research

authors： Singh Y,Gao D,Gu Z,Li S,Rivera KA,Stein S,Love S,Sinko PJ

更新日期：2012-09-01 00:00:00

abstract：PURPOSE:The lack of effective delivery vehicles impedes in vivo applications of siRNA. The trimethyl chitosan-cysteine (TC) nanoparticles (NPs) were developed for in vivo delivery of tumor necrosis factor α (TNF-α) siRNA via oral gavage and intraperitoneal injection. METHODS:The nanoparticles formulated from TC conjug...

journal_title：Pharmaceutical research

authors： He C,Yin L,Tang C,Yin C

更新日期：2013-10-01 00:00:00

abstract：PURPOSE:To evaluate the impact of intestinal first-pass metabolism (Fg) by cytochrome P4503A (CYP3A) and uridine 5'-diphosphate-glucuronosyltransferases (UGT) on in vivo oral absorption of their substrate drugs. METHODS:CYP3A and UGT substrates were orally administered to portal-vein cannulated (PV) rats to evaluate t...

journal_title：Pharmaceutical research

authors： Matsuda Y,Konno Y,Hashimoto T,Nagai M,Taguchi T,Satsukawa M,Yamashita S

更新日期：2015-02-01 00:00:00

abstract：:Since ancient times, natural products, herbs and spices have been used for preventing several diseases, including cancer. The term chemoprevention was coined in the late 1970s and referred to the prevention of cancer by selective use of phytochemicals or their analogs. The field utilizes experimental carcinogenesis mo...

journal_title：Pharmaceutical research

authors： Mehta RG,Murillo G,Naithani R,Peng X

更新日期：2010-06-01 00:00:00

abstract：PURPOSE:The objective of this study was to compare two different nebulizers: Eflow rapid® and Pari LC star® by scintigraphy and PK modeling to simulate epithelial lining fluid concentrations from measured plasma concentrations, after nebulization of CMS in baboons. METHODS:Three baboons received CMS by IV infusion and...

journal_title：Pharmaceutical research

authors： Marchand S,Bouchene S,de Monte M,Guilleminault L,Montharu J,Cabrera M,Grégoire N,Gobin P,Diot P,Couet W,Vecellio L

更新日期：2015-10-01 00:00:00

abstract：:The electrochemical properties of human cadaver skin were studied in a diffusion cell with impedance spectroscopy as a function of time in the absence and presence of penetration enhancers dodecyl N,N-dimethylamino acetate and Azone. An improved electrochemical model of skin is presented, and combining the novel model...

journal_title：Pharmaceutical research

authors： Kontturi K,Murtomäki L,Hirvonen J,Paronen P,Urtti A

更新日期：1993-03-01 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:This work investigated the effect of relative humidity (RH) on bipolar electrostatic charge profiles of dry powder inhaler aerosols using the Bipolar Charge Analyzer (BOLAR). METHODS:Two commercial products, Pulmicort® (400 μg, budesonide) and Bricanyl® (500 μg, terbutaline sulfate) Turbuhaler®, were used as m...

journal_title：Pharmaceutical research

authors： Yu J,Wong J,Ukkonen A,Kannosto J,Chan HK

更新日期：2017-08-01 00:00:00

abstract：PURPOSE:To demonstrate the applicability of thermally stimulated current (TSC) spectrometry for the detection of low levels of the amorphous phase in crystalline pharmaceutical materials. METHODS:A crystalline drug substance was melt quenched to produce an amorphous material. Blends of the crystalline and amorphous ph...

journal_title：Pharmaceutical research

authors： Venkatesh GM,Barnett ME,Owusu-Fordjour C,Galop M

更新日期：2001-01-01 00:00:00

abstract：:Under the heading "Methods-Synthesis of the Bioreducible Modified-PAE (mPAE)", on page 3, line 14-17, there is an error. The quantity unit of PAE and 2-iminothiolane hydrochloride needs to be corrected to mg instead of g. ...

journal_title：Pharmaceutical research

authors： Gandhi NS,Godeshala S,Koomoa-Lange DT,Miryala B,Rege K,Chougule MB

更新日期：2018-09-05 00:00:00

abstract：PURPOSE:To explore whether miR-19 is involved in the regulation of multidrug resistance (MDR), one of the main causes of breast cancer mortality, and modulates sensitivity of tumor cells to chemotherapeutic agents. METHODS:We analyzed miRNA expression levels in three MDR cell lines in comparison with their parent cell...

journal_title：Pharmaceutical research

authors： Liang Z,Li Y,Huang K,Wagar N,Shim H

更新日期：2011-12-01 00:00:00

abstract：PURPOSE:The aim of this study was to examine if sparging with CO2(g) could be used to establish stable biorelevant bicarbonate buffers, in aqueous medium, for use in dissolution characterization of low-solubility ionizable drugs. METHODS:Preparation of the bicarbonate-containing dissolution medium was monitored by use...

journal_title：Pharmaceutical research

authors： McNamara DP,Whitney KM,Goss SL

更新日期：2003-10-01 00:00:00

abstract：PURPOSE:To evaluate the potential of several bis-ester prodrugs of the antiviral agent 9-(2-phosphonylmethoxyethyl)adenine (PMEA, adefovir) to enhance the oral absorption of PMEA. METHODS:Caco-2 monolayers were used to estimate intestinal transport and metabolism of the bis(pivaloyloxymethyl)-ester [bis(POM)-] and a s...

journal_title：Pharmaceutical research

authors： Annaert P,Gosselin G,Pompon A,Benzaria S,Valette G,Imbach JL,Naesens L,Hatse S,de Clercq E,Van den Mooter G,Kinget R,Augustijns P

更新日期：1998-02-01 00:00:00

abstract：PURPOSE:To develop a dose dependent version of BCS and identify a critical dose after which the amount absorbed is independent from the dose. METHODS:We utilized a mathematical model of drug absorption in order to produce simulations of the fraction of dose absorbed (F) and the amount absorbed as function of the dose ...

journal_title：Pharmaceutical research

authors： Charkoftaki G,Dokoumetzidis A,Valsami G,Macheras P

更新日期：2012-11-01 00:00:00

abstract：:Growing tumors develop additional new blood vessels to meet the demand for adequate nutrients and oxygen, a process called angiogenesis. Cancer is a highly complex disease promoted by excess angiogenesis; interfering with this process poses for an attractive approach for controlling tumor growth. This hypothesis led t...

journal_title：Pharmaceutical research

authors： Sudhakar A,Boosani CS

更新日期：2008-12-01 00:00:00

abstract：PURPOSE:To investigate the effect of atomization conditions on particle size and stability of spray-freeze dried protein. METHODS:Atomization variables were explored for excipient-free (no zinc added) and zinc-complexed bovine serum albumin (BSA). Particle size was measured by laser diffraction light scattering follow...

journal_title：Pharmaceutical research

authors： Costantino HR,Firouzabadian L,Hogeland K,Wu C,Beganski C,Carrasquillo KG,Córdova M,Griebenow K,Zale SE,Tracy MA

更新日期：2000-11-01 00:00:00

abstract：PURPOSE:To investigate influence of ion induced mesophasic transformation on pharmaceutical performance of in situ gelling system consisting of glyceryl monooleate. METHODS:The prepared system showed mesophasic transformation during its conversion from sol to gel upon controlled hydration. The process of mesophasic tr...

journal_title：Pharmaceutical research

authors： Patil SS,Venugopal E,Bhat S,Mahadik KR,Paradkar AR

更新日期：2013-07-01 00:00:00

abstract：PURPOSE:The in vitro inhibitory effect of Docetaxel (DTX) and Everolimus (EVR) alone and together in poly(ethylene glycol)-block-poly(D,L-lactic acid) (PEG-b-PLA) nanocarriers on angiogenic processes and acute toxicity in mice was evaluated. METHODS:PEG-b-PLA DTX and/or EVR nanocarriers were characterized for size, dr...

journal_title：Pharmaceutical research

authors： Mishra GP,Doddapaneni BS,Nguyen D,Alani AW

更新日期：2014-03-01 00:00:00

abstract：PURPOSE:To examine whether the glass transition temperature (Tg) of freeze-dried formulations containing polymer excipients can be accurately predicted by molecular dynamics simulation using software currently available on the market. Molecular dynamics simulations were carried out for isomaltodecaose, a fragment of de...

journal_title：Pharmaceutical research

authors： Yoshioka S,Aso Y,Kojima S

更新日期：2003-06-01 00:00:00

abstract：PURPOSE:The objective of this study is to evaluate the feasibility of using coated microneedles to deliver vaccines into the oral cavity to induce systemic and mucosal immune responses. METHOD:Microneedles were coated with sulforhodamine, ovalbumin and two HIV antigens. Coated microneedles were inserted into the inner...

journal_title：Pharmaceutical research

authors： Ma Y,Tao W,Krebs SJ,Sutton WF,Haigwood NL,Gill HS

更新日期：2014-09-01 00:00:00

abstract：PURPOSE:Nanocrystalline drug-polymer dispersions are of significant interest in pharmaceutical delivery. The purpose of this work is to demonstrate the applicability of methods based on two-dimensional (2D) and multinuclear solid-state NMR (SSNMR) to a novel nanocrystalline pharmaceutical dispersion of ebselen with pol...

journal_title：Pharmaceutical research

authors： Vogt FG,Williams GR

更新日期：2012-07-01 00:00:00

abstract：PURPOSE:To study the degradation of oxaliplatin in chloride media and evaluate the cytotoxicity of oxaliplatin in normal and chloride-deficient medium. METHODS:The products of the reaction of oxaliplatin with chloride were separated on a Hypercarb S column with a mobile phase containing 40% methanol in 0.05 M ammonia ...

journal_title：Pharmaceutical research

authors： Jerremalm E,Hedeland M,Wallin I,Bondesson U,Ehrsson H

更新日期：2004-05-01 00:00:00

abstract：PURPOSE:This study was designed to investigate the stability of recombinant FVIII (rFVIII) in solution at different pHs and to probe the cause(s) of rFVIII inactivation under accelerated storage conditions. METHODS:Aqueous stability samples of full-length rFVIII at different pHs were incubated at 40 degrees C for seve...

journal_title：Pharmaceutical research

authors： Wang W,Kelner DN

更新日期：2003-04-01 00:00:00

abstract：:Nasal sprays containing different concentrations of the somatostatin analogue octreotide and sodium tauro-24,25-dihydrofusidate (STDHF) as an absorption promoter were evaluated in two consecutive pharmacokinetic studies in healthy volunteers to characterize their bioavailability and local tolerability. The concentrati...

journal_title：Pharmaceutical research

authors： Kissel T,Drewe J,Bantle S,Rummelt A,Beglinger C

更新日期：1992-01-01 00:00:00

abstract：PURPOSE:Under different charging conditions, particles can be either attracted or repulsed by each other, causing powder agglomeration or segregation. Such behavior can be detrimental in many processes aimed at achieving particulate mixture homogeneity. Consequently, the effects of electrostatic charges on mixing kinet...

journal_title：Pharmaceutical research

authors： Desrosiers Lachiver E,Abatzoglou N,Cartilier L,Simard JS

更新日期：2006-05-01 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