Estimation of bioavailability on a single occasion after semisimultaneous drug administration.


:A method for determination of absorption rate and bioavailability was developed to reduce the influence of intraindividual variability and applied to the absolute intraperitoneal availability of lithium in the rat. In this method the test and the reference doses are given with a few hours' interval, and the resulting concentration-time data are analyzed by nonlinear regression. The bioavailability estimation by this approach was compared to that of the traditional method, with test and reference doses given on separate days. The mean estimates of availability were 1.035 +/- 0.109 (N = 7) and 0.984 +/- 0.052 (N = 11) for the traditional and the alternative method, respectively. Thus, the precision was better in the latter. Major influences of dose- or time-dependent kinetics of lithium on the availability estimates were excluded by the design used. The estimation of bioavailability was robust with respect to the choice of absorption and disposition model and the duration of sampling. The plasma clearance of lithium was 169 +/- 15 ml/hr/kg, with a terminal half-life of 5.0 +/- 0.5 hr (N = 5).


Pharm Res


Pharmaceutical research


Karlsson MO,Bredberg U




Has Abstract


1989-09-01 00:00:00












  • Cancer immunotherapy and nanomedicine.

    abstract::The immune system has the ability to recognize and kill pre-cancer and cancer cells. However, with the immune system's surveillance, the survival tumor cells learn how to escape the immune system after immunoselection. Cancer immunotherapy develops strategies to overcome these problems. Nanomedicine applications in ca...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章,评审


    authors: Sheng WY,Huang L

    更新日期:2011-02-01 00:00:00

  • Topically applied phospho-sulindac hydrogel is efficacious and safe in the treatment of experimental arthritis in rats.

    abstract:PURPOSE:Formulate phospho-sulindac (P-S, OXT-328) in a Pluronic hydrogel to be used as a topical anti-inflammatory agent and study its efficacy, safety and pharmacokinetics in an arthritis model. METHODS:LEW/crlBR rats with Freund's adjuvant-induced arthritis were treated with P-S formulated in Pluronic hydrogel (PSH)...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Mattheolabakis G,Mackenzie GG,Huang L,Ouyang N,Cheng KW,Rigas B

    更新日期:2013-06-01 00:00:00

  • A photo-activated targeting chemotherapy using glutathione sensitive camptothecin-loaded polymeric micelles.

    abstract:PURPOSE:A novel photo-activated targeted chemotherapy was developed by photochemical internalization (PCI) of glutathione-sensitive polymeric micelles incorporating camptothecin (CPT) prepared from thiolated CPT (CPT-DP) and thiolated poly(ethylene glycol)-b-poly(glutamic acid) (PEG-b-P(Glu-DP)) METHODS: PEG-b-P(Glu-DP...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Cabral H,Nakanishi M,Kumagai M,Jang WD,Nishiyama N,Kataoka K

    更新日期:2009-01-01 00:00:00

  • Probing the Distribution of Water in a Multi-Component System by Solid-State NMR Spectroscopy.

    abstract:PURPOSE:To characterize the distribution of water among various components in a powder blend using solid-state NMR spectroscopy. METHODS:Water sorption behavior of theophylline anhydrate and excipients was determined by dynamic vapor sorption (DVS) and Karl Fischer Titration (KFT) after storing them in humidity chambe...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Mistry P,Chakravarty P,Lubach JW

    更新日期:2016-10-01 00:00:00

  • FoxM1 is a novel target of a natural agent in pancreatic cancer.

    abstract:PURPOSE:Pancreatic cancer remains the fourth most common cause of cancer-related death in the United States. Therefore, novel strategies for the prevention and/or treatment are urgently needed. Genistein has been found to be responsible for lowering the rate of pancreatic cancer. However, the molecular mechanisms by wh...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Wang Z,Ahmad A,Banerjee S,Azmi A,Kong D,Li Y,Sarkar FH

    更新日期:2010-06-01 00:00:00

  • Self-micellization of gemfibrozil 1-O-beta acyl glucuronide in aqueous solution.

    abstract:PURPOSE:Phase II metabolism involves the conjugation of a polar moiety, such as sulfate or glucuronic acid, to a (relatively) nonpolar xenobiotic. Although it might be expected that such conjugates may exhibit amphiphilic character (e.g., surface activity and potential to form micelles), no detailed study of the micell...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Shackleford DM,Prankerd RJ,Scanlon MJ,Charman WN

    更新日期:2003-03-01 00:00:00

  • Use of in vivo animal models to assess pharmacokinetic drug-drug interactions.

    abstract::Animal models are used commonly in various stages of drug discovery and development to aid in the prospective assessment of drug-drug interaction (DDI) potential and the understanding of the underlying mechanism for DDI of a drug candidate. In vivo assessments in an appropriate animal model can be very valuable, when ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章,评审


    authors: Tang C,Prueksaritanont T

    更新日期:2010-09-01 00:00:00

  • Chemical and enzymatic degradation of ganciclovir prodrugs: enhanced stability of the diadamantoate prodrug under acid conditions.

    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

    pub_type: 杂志文章


    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

  • Accelerated blood clearance phenomenon upon repeated injection of PEG-modified PLA-nanoparticles.

    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

    pub_type: 杂志文章


    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

  • Profiling the role of deacylation-reacylation in the lymphatic transport of a triglyceride-mimetic prodrug.

    abstract:PURPOSE:Recent studies have demonstrated the potential for a triglyceride (TG) mimetic prodrug to promote the delivery of mycophenolic acid (MPA) to the lymphatic system. Here, the metabolic pathways that facilitate the lymphatic transport of the TG prodrug (1,3-dipalmitoyl-2-mycophenoloyl glycerol, 2-MPA-TG) were exam...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Han S,Hu L,Quach T,Simpson JS,Trevaskis NL,Porter CJ

    更新日期:2015-05-01 00:00:00

  • Natural and synthetic polymers as inhibitors of drug efflux pumps.

    abstract::Inhibition of efflux pumps is an emerging approach in cancer therapy and drug delivery. Since it has been discovered that polymeric pharmaceutical excipients such as Tweens or Pluronics can inhibit efflux pumps, various other polymers have been investigated regarding their potential efflux pump inhibitory activity. Am...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章,评审


    authors: Werle M

    更新日期:2008-03-01 00:00:00

  • Direct observation of single particle electrostatic charging by atomic force microscopy.

    abstract:PURPOSE:To show that atomic force microscopy (AFM) can be used to directly study the electrostatic charging and dissipation of single pharmaceutical particles. MATERIALS AND METHODS:Particles of lactose attached to AFM cantilevers were charged on a glass surface at a relative humidity (RH) of 0.1%. By recording force-...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Bunker MJ,Davies MC,James MB,Roberts CJ

    更新日期:2007-06-01 00:00:00

  • Mishandling of the therapeutic peptide glucagon generates cytotoxic amyloidogenic fibrils.

    abstract:PURPOSE:Some therapeutic peptides exhibit amyloidogenic properties that cause insolubility and cytotoxicity against neuronal cells in vitro. Here, we characterize the conformational change in monomeric therapeutic peptide to its fibrillar aggregate in order to prevent amyloidogenic formation during clinical application...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Onoue S,Ohshima K,Debari K,Koh K,Shioda S,Iwasa S,Kashimoto K,Yajima T

    更新日期:2004-07-01 00:00:00

  • Major involvement of low-density lipoprotein receptor-related protein 1 in the clearance of plasma free amyloid beta-peptide by the liver.

    abstract:PURPOSE:To identify the molecules responsible for amyloid beta-peptide (1-40) (Abeta(1-40)) uptake by the liver, which play a major role in the systemic clearance of Abeta(1-40). METHODS:The liver uptake index method was used to examine the mechanisms of Abeta(1-40) uptake by the liver in vivo. RESULTS:[125I]Abeta(1-...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Tamaki C,Ohtsuki S,Iwatsubo T,Hashimoto T,Yamada K,Yabuki C,Terasaki T

    更新日期:2006-07-01 00:00:00

  • Development and in vivo evaluation of an oral delivery system for low molecular weight heparin based on thiolated polycarbophil.

    abstract:PURPOSE:It was the purpose of this study to develop a new oral drug delivery system for low molecular weight heparin (LMWH) providing an improved bioavailability and a prolonged therapeutic effect. METHODS:The permeation enhancing polycarbophil-cysteine conjugate (PCP-Cys) used in this study displayed 111.4 +/- 6.4 mi...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Kast CE,Guggi D,Langoth N,Bernkop-Schnürch A

    更新日期:2003-06-01 00:00:00

  • Sugar-Grafted Cyclodextrin Nanocarrier as a "Trojan Horse" for Potentiating Antibiotic Activity.

    abstract:PURPOSE:The use of "Trojan Horse" nanocarriers for antibiotics to enhance the activity of antibiotics against susceptible and resistant bacteria is investigated. METHODS:Antibiotic carriers (CD-MAN and CD-GLU) are prepared from β-cyclodextrin grafted with sugar molecules (D-mannose and D-glucose, respectively) via azi...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Li M,Neoh KG,Xu L,Yuan L,Leong DT,Kang ET,Chua KL,Hsu LY

    更新日期:2016-05-01 00:00:00

  • Development of Thiolated-Graphene Quantum Dots for Regulation of ROS in macrophages.

    abstract:PURPOSE:The current study was designed to develop thiolated-graphene quantum dots (SH-GQDs) as a theranostic nanocarrier and evaluate its potential for the optimal scavenging of reactive oxygen species (ROS) in macrophages. METHODS:SH-GQDs were prepared by hydrothermal pyrolysis of carbon source (citric acid) in the p...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Oh B,Lee CH

    更新日期:2016-11-01 00:00:00

  • Supramolecular Chitosan Micro-Platelets Synergistically Enhance Anti-Candida albicans Activity of Amphotericin B Using an Immunocompetent Murine Model.

    abstract:PURPOSE:The aim of this work is to design new chitosan conjugates able to self-organize in aqueous solution in the form of micrometer-size platelets. When mixed with amphotericin B deoxycholate (AmB-DOC), micro-platelets act as a drug booster allowing further improvement in AmB-DOC anti-Candida albicans activity. METH...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Grisin T,Bories C,Bombardi M,Loiseau PM,Rouffiac V,Solgadi A,Mallet JM,Ponchel G,Bouchemal K

    更新日期:2017-05-01 00:00:00

  • Determination of Depth-Dependent Intradermal Immunogenicity of Adjuvanted Inactivated Polio Vaccine Delivered by Microinjections via Hollow Microneedles.

    abstract:PURPOSE:The aim of this study was to investigate the depth-dependent intradermal immunogenicity of inactivated polio vaccine (IPV) delivered by depth-controlled microinjections via hollow microneedles (HMN) and to investigate antibody response enhancing effects of IPV immunization adjuvanted with CpG oligodeoxynucleoti...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Schipper P,van der Maaden K,Romeijn S,Oomens C,Kersten G,Jiskoot W,Bouwstra J

    更新日期:2016-09-01 00:00:00

  • Acylation of exenatide by glycolic acid and its anti-diabetic activities in db/db mice.

    abstract:PURPOSE:To prepare acylated exenatide analogues and investigate their biological properties for guiding the development of PLGA formulations of exenatide. METHODS:The acylated exenatide analogues were prepared by reaction with glycolic acid (GA), one constitutional unit of PLGA, and characterized by HPLC-MS/MS and Cir...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Liang R,Li X,Zhang R,Shi Y,Wang A,Chen D,Sun K,Liu W,Li Y

    更新日期:2014-08-01 00:00:00

  • Biodistribution and Toxicity of X-Ray Iodinated Contrast Agent in Nano-emulsions in Function of Their Size.

    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

    pub_type: 杂志文章


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

    更新日期:2016-03-01 00:00:00

  • In vitro gastrointestinal lipolysis of four formulations of piroxicam and cinnarizine with the self emulsifying excipients Labrasol and Gelucire 44/14.

    abstract:PURPOSE:Labrasol and Gelucire 44/14 are defined admixtures of acylglycerols and PEG esters which are substrates for digestive lipases. METHODS:We investigated their in vitro gastrointestinal lipolysis to understand which compounds are, after digestion, responsible for keeping poorly water-soluble drugs in solution. Th...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Fernandez S,Chevrier S,Ritter N,Mahler B,Demarne F,Carrière F,Jannin V

    更新日期:2009-08-01 00:00:00

  • Exploring Variation in Known Pharmacogenetic Variants and its Association with Drug Response in Different Mexican Populations.

    abstract:PURPOSE:Information on genetic variants that affect the pharmacokinetics and pharmacodynamics (PK/PD) of drugs in different populations from Mexico is still an ongoing endeavor. Here, we investigate allele frequencies on pharmacogenetic targets in Mexican Mestizos and Natives from three different States and its associa...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Gonzalez-Covarrubias V,Martínez-Magaña JJ,Coronado-Sosa R,Villegas-Torres B,Genis-Mendoza AD,Canales-Herrerias P,Nicolini H,Soberón X

    更新日期:2016-11-01 00:00:00

  • High variability in drug pharmacokinetics complicates determination of bioequivalence: experience with verapamil.

    abstract:PURPOSE:For the assessment of bioequivalence it is assumed that drug clearance in each subject on each of the study days is the same and any observed differences in AUC and/or Cmax between a brand and generic formulation are due to differences in bioavailability. We hypothesized that this assumption was invalid for hig...

    journal_title:Pharmaceutical research

    pub_type: 临床试验,杂志文章


    authors: Tsang YC,Pop R,Gordon P,Hems J,Spino M

    更新日期:1996-06-01 00:00:00

  • EGFR Targeted Theranostic Nanoemulsion for Image-Guided Ovarian Cancer Therapy.

    abstract:PURPOSE:Platinum-based therapies are the first line treatments for most types of cancer including ovarian cancer. However, their use is associated with dose-limiting toxicities and resistance. We report initial translational studies of a theranostic nanoemulsion loaded with a cisplatin derivative, myrisplatin and pro-a...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Ganta S,Singh A,Kulkarni P,Keeler AW,Piroyan A,Sawant RR,Patel NR,Davis B,Ferris C,O'Neal S,Zamboni W,Amiji MM,Coleman TP

    更新日期:2015-08-01 00:00:00

  • Role of viscosity in influencing the glass-forming ability of organic molecules from the undercooled melt state.

    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

    pub_type: 杂志文章


    authors: Baird JA,Santiago-Quinonez D,Rinaldi C,Taylor LS

    更新日期:2012-01-01 00:00:00

  • Cell-penetrating antimicrobial peptides - prospectives for targeting intracellular infections.

    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

    pub_type: 杂志文章


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

    更新日期:2015-05-01 00:00:00

  • PCBP2 siRNA reverses the alcohol-induced pro-fibrogenic effects in hepatic stellate cells.

    abstract:PURPOSE:Type I collagen accumulates during liver fibrosis primarily because α-complex protein-2 (αCP(2)), encoded by the poly(rC) binding protein 2 (PCBP2) gene, binds to the 3' end of the collagen mRNA and increases its half-life. This study aimed to reverse the pro-fibrogenic effect of alcohol on hepatic stellate cel...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Shukla RS,Qin B,Wan YJ,Cheng K

    更新日期:2011-12-01 00:00:00

  • Bilateral Effects of Excipients on Protein Stability: Preferential Interaction Type of Excipient and Surface Aromatic Hydrophobicity of Protein.

    abstract:PURPOSE:Understanding the mechanism of protein-excipient interaction and illuminating the influencing factors on protein stability are key steps in the rational design of protein formulations. The objective of this study was to assess effects of preferential interaction type of excipient and surface aromatic hydrophobi...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Wen L,Zheng X,Wang X,Lan H,Yin Z

    更新日期:2017-07-01 00:00:00

  • Acid-responsive polymeric nanocarriers for topical adapalene delivery.

    abstract:PURPOSE:The acne skin is characteristic of a relatively lower pH microenvironment compared to the healthy skin. The aim of this work was to utilize such pH discrepancy as a site-specific trigger for on-demand topical adapalene delivery. METHODS:The anti-acne agent, adapalene, was encapsulated in acid-responsive polyme...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章


    authors: Guo C,Khengar RH,Sun M,Wang Z,Fan A,Zhao Y

    更新日期:2014-11-01 00:00:00