Solubility of small-molecule crystals in polymers: D-mannitol in PVP, indomethacin in PVP/VA, and nifedipine in PVP/VA.

abstract：:Azo polymers based upon 2-hydroxyethyl methacrylate, methyl methacrylate, and methacrylic acid, and containing N,N'-bis [(methacryloyloxyethyl)oxy(carbonylamino)]azobenzene as azo aromatic agent were evaluated in vivo as coating for colon-specific drug delivery. The gastrointestinal absorption of theophylline from cap...

journal_title：Pharmaceutical research

authors： Van den Mooter G,Samyn C,Kinget R

更新日期：1995-02-01 00:00:00

abstract：PURPOSE:Due to protease inhibitor (PI) efflux transport by P-glycoprotein (P-gp), insufficient PI concentrations result in low ongoing HIV replication in the so-called virus sanctuaries (brain and testes). The aim of the present study was to evaluate indinavir-loaded nanocapsules (Ind-LNC) including Solutol HS15, an ex...

journal_title：Pharmaceutical research

authors： Pereira de Oliveira M,Garcion E,Venisse N,Benoit JP,Couet W,Olivier JC

更新日期：2005-11-01 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:Adjuvants are required to ensure the efficacy of subunit vaccines. Incorporating molecular immunopotentiators within particles could overcome drawbacks of molecular adjuvants (such as solubility and toxicity), and improve adjuvanticity of particles, achieving stronger adjuvant activity. Aim of this study is to ...

journal_title：Pharmaceutical research

authors： Zhang W,Wang L,Yang T,Liu Y,Chen X,Liu Q,Jia J,Ma G

更新日期：2015-09-01 00:00:00

abstract：PURPOSE:Grapefruit juice (GJ) is known to increase the oral bioavailability of many CYP3A-substrates by inhibiting intestinal phase-I metabolism. However, the magnitude of AUC increase is often insignificant and highly variable. Since we earlier suggested that CYP3A and P-glycoprotein (P-gp) form a concerted barrier to...

journal_title：Pharmaceutical research

authors： Soldner A,Christians U,Susanto M,Wacher VJ,Silverman JA,Benet LZ

更新日期：1999-04-01 00:00:00

abstract：:The effects of process and storage conditions of solid-state emulsions were studied. Oil-in-water emulsions may be prepared from solid state emulsions by adding an aqueous phase to the solid. Solid-state emulsions are prepared by processing an oil phase and an aqueous solution of matrix material via a solvent removal ...

journal_title：Pharmaceutical research

authors： Shively ML,Myers S

更新日期：1993-07-01 00:00:00

abstract：:A sensitive radioreceptor assay (RRA) to determine the serum concentrations of fentanyl, pentazocine and morphine was developed on the basis of the drug's competition with a labeled tracer ((3)H-naloxone) for the membrane bound opioid receptor in rat brain homogenates. The binding data were computer-fitted to a standa...

journal_title：Pharmaceutical research

authors： Grevel J,Thomas J,Richards ML,Sadée W

更新日期：1984-09-01 00:00:00

abstract：PURPOSE:To compare the ability of alkyl-aryl isothiocyanates (ITCs) to increase the activities of the Phase 2 detoxification enzymes NAD[P]H:quinone acceptor oxidoreductase 1 (NQO1) and glutathione S-transferases (GST) in rat tissues in vivo and in cells in vitro. MATERIALS AND METHODS:Twelve alkyl-aryl ITCs and the f...

journal_title：Pharmaceutical research

authors： Munday R,Zhang Y,Munday CM,Bapardekar MV,Paonessa JD

更新日期：2008-09-01 00:00:00

abstract：PURPOSE:Adenoviruses are being developed for diseases of the gastrointestinal tract. Several in vitro assays were used to predict stability of PEGylated adenovirus along the GI tract and determine in vivo gene transfer after oral administration. METHODS:Recombinant adenovirus was modified with monomethoxypoly(ethylene...

journal_title：Pharmaceutical research

authors： Cheng X,Ming X,Croyle MA

更新日期：2003-09-01 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:The study was performed for clarifying the mechanism of interaction between indoxyl sulfate (IS), a typical uremic toxin bound to site II, and site I-ligands when bound to human serum albumin (HSA). The effect of the N to B transition on the interactions was also examined. METHODS:Quantitative investigation of...

journal_title：Pharmaceutical research

authors： Sakai T,Yamasaki K,Sako T,Kragh-Hansen U,Suenaga A,Otagiri M

更新日期：2001-04-01 00:00:00

abstract：PURPOSE:The major goal of this study was to compare the relative utility of the Hanson Microette and the Van Kel apparatus, two fully automated devices, as in vitro release tests (IVRT) for semisolids. We attempted to develop methodology that can be used to discriminate formulation changes, and to evaluate the precisio...

journal_title：Pharmaceutical research

authors： Rapedius M,Blanchard J

更新日期：2001-10-01 00:00:00

abstract：:The interdependent relationship between pharmacology and toxicology is fundamental to the concepts of efficacy and safety of both drugs and xenobiotics. The traditional concept of establishing efficacious and tolerated doses to define a 'therapeutic window' appears simplistic in the context of an exponentially increas...

journal_title：Pharmaceutical research

authors： Sayes CM,Staats H,Hickey AJ

更新日期：2014-09-01 00:00:00

abstract：PURPOSE:We recently developed prostaglandin E(1) (PGE(1))-encapsulated nanoparticles, prepared with a poly(lactide) homopolymer (PLA, Mw = 17,500) and monomethoxy poly(ethyleneglycol)-PLA block copolymer (PEG-PLA) (NP-L20). In this study, we tested whether the accelerated blood clearance (ABC) phenomenon is observed wi...

journal_title：Pharmaceutical research

authors： Ishihara T,Takeda M,Sakamoto H,Kimoto A,Kobayashi C,Takasaki N,Yuki K,Tanaka K,Takenaga M,Igarashi R,Maeda T,Yamakawa N,Okamoto Y,Otsuka M,Ishida T,Kiwada H,Mizushima Y,Mizushima T

更新日期：2009-10-01 00:00:00

abstract：:Monte Carlo simulation technique used to evaluate the effect of the arrangement of concentrations on the efficiency of estimation of population pharmacokinetic parameters in the preclinical setting is described. Although the simulations were restricted to the one compartment model with intravenous bolus input, they pr...

journal_title：Pharmaceutical research

authors： Ette EI,Howie CA,Kelman AW,Whiting B

更新日期：1995-05-01 00:00:00

abstract：:Significant efforts are made to characterize molecular liabilities and degradation of the drug substance (DS) and drug product (DP) during various product life-cycle stages. The in vivo fate of a therapeutic protein is usually only considered in terms of pharmacokinetics (PKs) and pharmacodynamics (PDs). However, the ...

journal_title：Pharmaceutical research

authors： Schuster J,Koulov A,Mahler HC,Detampel P,Huwyler J,Singh S,Mathaes R

更新日期：2020-01-03 00:00:00

abstract：PURPOSE:This study was conducted to investigate in vivo the impact of interferon-alpha (IFN)-alpha on P-glycoprotein (P-gp) activity in rats by studying how its administration modifies the bioavailability of digoxin, a fairly pure P-gp substrate. METHODS:Human recombinant IFN-alpha was given to rats (n = 5-7 per group...

journal_title：Pharmaceutical research

authors： Ben Reguiga M,Bonhomme-Faivre L,Orbach-Arbouys S,Farinotti R

更新日期：2005-11-01 00:00:00

abstract：:Unsymmetrical aryl(heteroaryl)methyl isopropyl ester analogues of nifedipine, in which the 2-nitrophenyl group at C-4 is replaced by a 2- or 3-pyridyl substituent, were synthesized and evaluated as calcium-channel antagonists using guinea pig ileal longitudinal smooth muscle. The point of attachment of the C-4 pyridyl...

journal_title：Pharmaceutical research

authors： Akula MR,Matowe WC,Wolowyk MW,Knaus EE

更新日期：1990-09-01 00:00:00

abstract：:We studied the effects of two verapamil analogs, anipamil and ronipamil, in traumatic shock. Noble-Collip drum trauma produced a shock state characterized by an eight-fold increase in plasma cathepsin D activity, a 13-fold increase in the rate of plasma myocardial depressant factor (MDF) accumulation, and a survival t...

journal_title：Pharmaceutical research

authors： Hock CE,Daitch JS,Lefer AM

更新日期：1985-05-01 00:00:00

abstract：:A procedure is described that is suitable for the radioimmunoassay (RIA) of 9-[(l,3-dihydroxy-2-propoxy)-methyl]guanine (DHPG) in plasma or serum at concentrations as low as 0.7 ng/ml (2.75 × 10(-9) M). Antiserum was prepared by coupling DHPG monohemisuccinate to bovine serum albumin and immunizing rabbits with the re...

journal_title：Pharmaceutical research

authors： Nerenberg C,McClung S,Martin J,Fass M,La Fargue J,Kushinsky S

更新日期：1986-04-01 00:00:00

abstract：:The bioavailability of dipyridamole, a poorly soluble weak base, was evaluated in 11 healthy, older subjects (> or = 65 years), 6 with a low fasting gastric pH (control) and 5 with a fasting gastric pH > 5 (achlorhydric), in a randomized, crossover design. Subjects received 50 mg dipyridamole as a single oral dose bot...

journal_title：Pharmaceutical research

authors： Russell TL,Berardi RR,Barnett JL,O'Sullivan TL,Wagner JG,Dressman JB

更新日期：1994-01-01 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：: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:To determine the factors influencing "solid solubility" and phase separation kinetics of drugs from amorphous solid dispersions. METHODS:Solid dispersions of griseofulvin-poly(vinyl pyrrolidone) (PVP) and indoprofen-PVP were prepared using solvent evaporation technique. Dispersions demonstrating single Tg were...

journal_title：Pharmaceutical research

authors： Vasanthavada M,Tong WQ,Joshi Y,Kislalioglu MS

更新日期：2005-03-01 00:00:00

abstract：:Apigenin, a naturally occurring plant flavone, abundantly present in common fruits and vegetables, is recognized as a bioactive flavonoid shown to possess anti-inflammatory, antioxidant and anticancer properties. Epidemiologic studies suggest that a diet rich in flavones is related to a decreased risk of certain cance...

journal_title：Pharmaceutical research

authors： Shukla S,Gupta S

更新日期：2010-06-01 00:00:00

abstract：:Solution calorimetry has been employed to evaluate the stability constants and enthalpy changes associated with complex formation between alpha-, beta, or gamma-cyclodextrin (CD) and a group of amine compounds having the diphenylmethyl functionality. Data from thermal titrations of the compounds were analyzed using no...

journal_title：Pharmaceutical research

authors： Tong WQ,Lach JL,Chin TF,Guillory JK

更新日期：1991-07-01 00:00:00

abstract：PURPOSE:Simvastatin (SIM), a HMG-CoA reductase inhibitor widely prescribed for hypercholesterolemia, has been reported to ameliorate inflammation and promote osteogenesis. Its clinical applications on these potential secondary indications, however, have been hampered by its lack of osteotropicity and poor water solubil...

journal_title：Pharmaceutical research

authors： Wang X,Jia Z,Almoshari Y,Lele SM,Reinhardt RA,Wang D

更新日期：2018-06-25 00:00:00

abstract：PURPOSE:Reverse micellar solutions of diclofenac sodium were encapsulated in soft gelatine capsules. On contact with aqueous media they exhibited an application induced transformation (AIT) into a semisolid system of liquid crystals (SSLC) which slows down drug release. The aim of the present paper was to study in vitr...

journal_title：Pharmaceutical research

authors： Schneeweis A,Müller-Goymann CC

更新日期：1997-12-01 00:00:00

abstract：PURPOSE:To investigate how likely two extended release formulations are to be bioequivalent when they demonstrate f2 similarity. METHOD:Dissolution profiles were simulated using the Weibull model and varying model parameters around those of a reference profile. The f2 values were calculated for the comparisons of each...

journal_title：Pharmaceutical research

authors： Duan JZ,Riviere K,Marroum P

更新日期：2011-05-01 00:00:00

abstract：PURPOSE:N-terminal site-specific mono-PEGylation of recombinant human epidermal growth factor (EGF) was accomplished using polyethyleneglycol (PEG) derivatives (Mw = 2000 and 5000) through a reactive terminal aldehyde group. METHODS:The site-specific PEG conjugation was conducted ata slightly acidic pH condition (pH 5...

journal_title：Pharmaceutical research

authors： Lee H,Jang IH,Ryu SH,Park TG

更新日期：2003-05-01 00:00:00