Potential of immobilized artificial membranes for predicting drug penetration across the blood-brain barrier.

abstract：PURPOSE:To study the biorelevant drug release from novel starch-based polyvinyl alcohol capsules (S-PVA-C). The effect of the shell material is studied by considering microstructural formulation changes during hydration. METHODS:Two different self-emulsifying systems containing either fenofibrate or probucol were fill...

journal_title：Pharmaceutical research

authors： Misic Z,Urbani R,Pfohl T,Muffler K,Sydow G,Kuentz M

更新日期：2014-01-01 00:00:00

abstract：PURPOSE:Cell penetrating peptides (CPPs) were widely used as motifs for drug delivery to tumor. In former study, an RGD reverse sequence dGR was used to develop active-targeting liposome R8dGR-Lip, which showed well penetrating ability and treatment efficiency on glioma model. However, recurrence after tumor resection ...

journal_title：Pharmaceutical research

authors： Qiu Y,Yu Q,Liu Y,Tang J,Wang X,Lu Z,Xu Z,He Q

更新日期：2018-04-26 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：PURPOSE:To apply physiologically-based pharmacokinetic (PBPK) modeling to investigate the consequences of reduction in activity of hepatic and intestinal uptake and efflux transporters by cyclosporine and its metabolite AM1. METHODS:Inhibitory potencies of cyclosporine and AM1 against OATP1B1, OATP1B3 and OATP2B1 were...

journal_title：Pharmaceutical research

authors： Gertz M,Cartwright CM,Hobbs MJ,Kenworthy KE,Rowland M,Houston JB,Galetin A

更新日期：2013-03-01 00:00:00

abstract：PURPOSE:To develop a non-viral gene delivery system in the form of an oil-in-water (o/w) lipid emulsion. METHOD:Cationic lipid emulsions were formulated with soybean oil, 1,2-dioleoyl-sn-glycero-3-trimethylammonium-propane (DOTAP) as a cationic emulsifier and other co-emulsifiers. The physical characteristics of the l...

journal_title：Pharmaceutical research

authors： Yi SW,Yune TY,Kim TW,Chung H,Choi YW,Kwon IC,Lee EB,Jeong SY

更新日期：2000-03-01 00:00:00

abstract：:A method to provide near-constant sustained release of high molecular weight, water-soluble proteins from polyanhydride microspheres is described. The polyanhydrides used were poly(fatty acid dimer) (PFAD), poly(sebacic acid) (PSA), and their copolymers [P(FAD-SA)]. P(FAD-SA) microspheres containing proteins of differ...

journal_title：Pharmaceutical research

authors： Tabata Y,Gutta S,Langer R

更新日期：1993-04-01 00:00:00

abstract：PURPOSE:Good glycaemic control is essential to minimize the risk for diabetes-induced complications. Also, compliance is likely to be higher if the procedure is simple and painless. This study was designed to validate painless intradermal delivery via a patch-like microneedle array. MATERIALS AND METHODS:Diabetes was ...

journal_title：Pharmaceutical research

authors： Nordquist L,Roxhed N,Griss P,Stemme G

更新日期：2007-07-01 00:00:00

abstract：PURPOSES:To evaluate the effects of component contents in different colistin methanesulfonate (CMS) formulas on their clinical pharmacokinetics of the prodrug CMS and the formed colistin. METHODS:Two CMS formulas (CTTQ and Parkedale) were investigated in a single dose, randomized, open-label, crossover study conducted...

journal_title：Pharmaceutical research

authors： Fan YX,Chen YC,Li Y,Yu JC,Bian XC,Li X,Li WZ,Guo BN,Wu HL,Liu XF,Wang Y,Xu XY,Hu JL,Wang JJ,Wu XJ,Cao GY,Wu JF,Xue CJ,Feng J,Zhang YY,Zhang J

更新日期：2021-01-26 00:00:00

abstract：PURPOSE:We have shown that the three human prostate xenograft tumors, i.e. the androgen-dependent CWR22 tumor, and the androgen-resistant CWR22R and CWR91 tumors, are comparable to patient tumors in their expression of prostate specific antigen, multidrug resistance p-glycoprotein, p53 and Bcl-2 and in their sensitivit...

journal_title：Pharmaceutical research

authors： Gan Y,Au JL,Lu J,Wientjes MG

更新日期：1998-11-01 00:00:00

abstract：:Defined size fractions of polyethyleneglycol powder (MW = 10,000) were mixed with defined size fractions of alpha-lactose monohydrate in order to study the effect of compaction as a function of the weight ratios of the two excipients. For a precise control of the compression cycle, tablets were compressed on a Univers...

journal_title：Pharmaceutical research

authors： Blattner D,Kolb M,Leuenberger H

更新日期：1990-02-01 00:00:00

abstract：:The plasma concentration-time profiles and pharmacokinetics were characterized for nicotine and its major metabolite, cotinine, after multiple daily application of a nicotine user-activated transdermal therapeutic system (UATTS) to nine healthy smokers. The volunteers abstained from smoking 24 hr prior to and during t...

journal_title：Pharmaceutical research

authors： Ross HD,Chan KK,Piraino AJ,John VA

更新日期：1991-03-01 00:00:00

abstract：PURPOSE:Within-subject dependency of observations has a strong impact on the evaluation of population pharmacokinetic (PK) and/or pharmacodynamic (PD) models. To our knowledge, none of the current model evaluation tools correctly address this issue. We present a new method with a global test and easy diagnostic plot wh...

journal_title：Pharmaceutical research

authors： Laffont CM,Concordet D

更新日期：2011-08-01 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：PURPOSE:A plasmid-based gene expression system was complexed with protective, interactive, and non-condensing (PINC) polymer system and administered with Medi-Jector, a needle-free injection device (NFID), to achieve high and sustained levels of antigen-specific antibodies in blood circulation. METHODS:Human growth ho...

journal_title：Pharmaceutical research

authors： Anwer K,Earle KA,Shi M,Wang J,Mumper RJ,Proctor B,Jansa K,Ledebur HC,Davis S,Eaglstein W,Rolland AP

更新日期：1999-06-01 00:00:00

abstract：PURPOSE:The described structure pharmacokinetic pharmacodynamic relationships (SPPR) study explored the utilization of tetramethylcyclopropane analogues of valpromide (VPD), or tetramethylcyclopropane carboxamide derivatives of valproic acid (VPA) as new antiepileptics. METHODS:The study was carried out by investigati...

journal_title：Pharmaceutical research

authors： Bialer M,Hadad S,Kadry B,Abdul-Hai A,Haj-Yehia A,Sterling J,Herzig Y,Yagen B

更新日期：1996-02-01 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：: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:To explain thermal stability enhancement of an organic compound, sucralose, with cyclodextrin based metal organic frameworks. METHODS:Micron and nanometer sized basic CD-MOFs were successfully synthesized by a modified vapor diffusion method and further neutralized with glacial acetic acid. Sucralose was loade...

journal_title：Pharmaceutical research

authors： Lv N,Guo T,Liu B,Wang C,Singh V,Xu X,Li X,Chen D,Gref R,Zhang J

更新日期：2017-02-01 00:00:00

abstract：PURPOSE:Nasal delivery is a favorable route for vaccination against most respiratory infections, as antigen deposited in the nasal turbinate and Waldeyer's ring areas induce mucosal and systemic immune responses. However, little is known about the nasal distribution of the vaccines, specifically for infants. METHODS:A...

journal_title：Pharmaceutical research

authors： Wilkins JV Jr,Golshahi L,Rahman N,Li L

更新日期：2021-01-15 00:00:00

abstract：PURPOSE:The heparin-paclitaxel conjugates using amino acid as linker (HD2), with low anticoagulant activity, the similar anticancer activity as paclitaxel, offer great potential for further investigation. METHODS:Two types of heparin-paclitaxel conjugates (HD) have been developed, in which O-acetylated heparin as carr...

journal_title：Pharmaceutical research

authors： Wang Y,Xin D,Liu K,Xiang J

更新日期：2009-04-01 00:00:00

abstract：:The pharmacokinetics of 2',3'-dideoxyinosine (ddI) were examined in rats given intravenous doses of 8, 40, or 200 mg/kg. The concentrations of ddI in whole blood and plasma were identical. The concentration decline was multiexponential, with mean half-lives of 2 and 20 min for the first and second phases, respectively...

journal_title：Pharmaceutical research

authors： Wientjes MG,Mukherji E,Au JL

更新日期：1992-08-01 00:00:00

abstract：PURPOSE:To devise experimental and computational models to predict aqueous drug solubility. METHODS:A simple and reliable modification of the shake flask method to a small-scale format was devised, and the intrinsic solubilities of 17 structurally diverse drugs were determined. The experimental solubility data were us...

journal_title：Pharmaceutical research

authors： Bergström CA,Norinder U,Luthman K,Artursson P

更新日期：2002-02-01 00:00:00

abstract：PURPOSE:The feasibility of using iontophoresis to enhance the permeation rate of a model peptide was investigated in vitro using hairless mouse skin. METHODS:Angiotensin 2 (AT 2) was employed as a permeant probe, using optimum iontophoresis conditions. A number of physicochemical parameters (donor ionic strength; vale...

journal_title：Pharmaceutical research

authors： Clemessy M,Couarraze G,Bevan B,Puisieux F

更新日期：1995-07-01 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：:During protein lyophilization, it is common practice to complete the freezing step as fast as possible in order to avoid protein denaturation, as well as to obtain a final product of uniform quality. We report a contradictory observation made during lyophilization of recombinant tissue-type plasminogen activator (t-PA...

journal_title：Pharmaceutical research

authors： Hsu CC,Nguyen HM,Yeung DA,Brooks DA,Koe GS,Bewley TA,Pearlman R

更新日期：1995-01-01 00:00:00

abstract：PURPOSE:SN-38, a potent chemotherapeutic drug, has not been used clinically because of its severe side effects and poor solubility. In this work, we aimed to evaluate the effect of dose and multiple injections of SN-38-loaded polymeric depots on antitumor efficacy and toxicity in vivo. METHODS:Preparation and characte...

journal_title：Pharmaceutical research

authors： Manaspon C,Nasongkla N,Chaimongkolnukul K,Nittayacharn P,Vejjasilpa K,Kengkoom K,Boongird A,Hongeng S

更新日期：2016-12-01 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 effects of skin storage, skin preparation, skin pretreatment with a penetration enhancer, and skin barrier removal by adhesive tape-stripping on the concurrent cutaneous transport and metabolism of nitroglycerin (GTN) have been studied in vitro using hairless mouse skin. Storing the skin for 10 days at 4 degrees C...

journal_title：Pharmaceutical research

authors： Higo N,Hinz RS,Lau DT,Benet LZ,Guy RH

更新日期：1992-03-01 00:00:00

abstract：OBJECTIVES:We recently demonstrated that fibrin-based tissue engineered blood vessels (TEV) exhibited vascular reactivity, matrix remodeling and sufficient strength for implantation into the veins of an ovine animal model, where they remained patent for 15 weeks. Here we present an approach to improve the mechanical pr...

journal_title：Pharmaceutical research

authors： Yao L,Liu J,Andreadis ST

更新日期：2008-05-01 00:00:00

abstract：PURPOSE:In this work, the alacepril thiolesterase, which catalyzes the hydrolyzing reaction of the thiolester linkage in alacepril and the conversion from alacepril to deacetylalacepril, was purified from rat liver cytosol and characterized. METHODS:A purification procedure for the thiolesterase consisted of ammonium ...

journal_title：Pharmaceutical research

authors： Usui S,Kubota M,Iguchi K,Kiho T,Sugiyama T,Katagiri Y,Hirano K

更新日期：2003-08-01 00:00:00