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

Abstract:

: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).

journal_name

Pharm Res

journal_title

Pharmaceutical research

authors

Karlsson MO,Bredberg U

doi

10.1023/a:1015939917646

subject

Has Abstract

pub_date

1989-09-01 00:00:00

pages

817-21

issue

9

eissn

0724-8741

issn

1573-904X

journal_volume

6

pub_type

杂志文章
  • Assessment of physical stability of an antibody drug conjugate by higher order structure analysis: impact of thiol- maleimide chemistry.

    abstract:PURPOSE:To provide a systematic biophysical approach towards a better understanding of impact of conjugation chemistry on higher order structure and physical stability of an antibody drug conjugate (ADC). METHODS:ADC was prepared using thiol-maleimide chemistry. Physical stabilities of ADC and its parent IgG1 mAb were...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-013-1274-2

    authors: Guo J,Kumar S,Prashad A,Starkey J,Singh SK

    更新日期:2014-07-01 00:00:00

  • Solute absorption from the airways of the isolated rat lung. I. The use of absorption data to quantify drug dissolution or release in the respiratory tract.

    abstract::Coprecipitates of fluorescein and magnesium hydroxide demonstrate delayed absorption relative to fluorescein solutions when administered to the airways of the isolated perfused rat lung (IPRL). Perfusate concentration vs time profiles showed that dissolution and not epithelial permeability was the rate-controlling fac...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015942013413

    authors: Niven RW,Byron PR

    更新日期:1988-09-01 00:00:00

  • Oral delivery of ionic complex of ceftriaxone with bile acid derivative in non-human primates.

    abstract:PURPOSE:Since the absorption of ceftriaxone (CTO) in the intestine is restricted by its natural physiological characteristics, we developed a series of small synthetic compounds derived from bile acids to promote the absorption of CTO in the gastrointestinal tract. METHODS:Several bile acid derivatives were screened b...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-012-0932-0

    authors: Jeon OC,Hwang SR,Al-Hilal TA,Park JW,Moon HT,Lee S,Park JH,Byun Y

    更新日期:2013-04-01 00:00:00

  • Phase behavior of amorphous molecular dispersions II: Role of hydrogen bonding in solid solubility and phase separation kinetics.

    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

    pub_type: 杂志文章

    doi:10.1007/s11095-004-1882-y

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

    更新日期:2005-03-01 00:00:00

  • Enhanced Anti-Tumor Efficacy of Lipid-Modified Platinum Derivatives in Combination with Survivin Silencing siRNA in Resistant Non-Small Cell Lung Cancer.

    abstract:PURPOSE:Cisplatin, is recognized as a first line therapeutic for the treatment of non-small cell lung cancer (NSCLC). Cisplatin resistance is identified as the most detrimental complication during treatment and has been associated with upregulation of several genes, such as the anti-apoptotic gene survivin. In this stu...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-016-2016-z

    authors: Mattheolabakis G,Ling D,Ahmad G,Amiji M

    更新日期:2016-12-01 00:00:00

  • Buprenorphine is an Antagonist at the ϰ Opioid Receptor.

    abstract::The effect of buprenorphine on bremazocine-induced diuresis was tested in the rat to determine the nature of buprenorphine's action at the ϰ opioid receptor. Both morphine-tolerant and naive rats were used to account for possible antidiuretic effects of buprenorphine at the µ site. Separate experiments established tha...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/A:1016340106299

    authors: Richards ML,Sadée W

    更新日期:1985-07-01 00:00:00

  • Hypolipidemic Agents of Phthalimide Derivatives 6. Effects of Aromatic vs. Non-Aromatic Imides.

    abstract::A number of substituted phthalimide, 1, 8-naphthalimide, succinimide and glutarimide derivatives demonstrated significant hypolipidemic activity at 20 mg/kg/ day, I.P. after 16 days dosing. The N-(n-pentyl) succinimide proved to be the most potent analogue of the new compounds, lowering serum triglyceride levels 51 % ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/A:1016346018962

    authors: Chapman JM Jr,Wyrick SD,Maguire JH,Cocolas GH,Hall IH

    更新日期:1984-11-01 00:00:00

  • Nonisothermal stability assessment of stable pharmaceuticals: testing of a clindamycin phosphate formulation.

    abstract::The stability of an antibiotic formulation (clindamycin phosphate in dextrose), which is stable at room temperature, was assessed by nonisothermal kinetic analysis at elevated temperatures. A preliminary study, conducted to establish apparent rate order, verified the appropriateness of a first-order kinetic model. The...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015840320410

    authors: Kipp JE,Hlavaty JJ

    更新日期:1991-05-01 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

    doi:10.1007/s11095-017-2152-0

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

    更新日期:2017-07-01 00:00:00

  • The effect of conformation on membrane permeability of an acyloxyalkoxy-linked cyclic prodrug of a model hexapeptide.

    abstract:PURPOSE:To determine the different conformations of the acyloxyalkoxy-linked cyclic prodrug 1 of the model hexapeptide 2 in solution and to investigate the relationship between these solution conformations and the cellular permeability characteristics of this prodrug. METHODS:Two-dimensional Homonuclear Hartmann-Hahn ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1016484522113

    authors: Gangwar S,Jois SD,Siahaan TJ,Vander Velde DG,Stella VJ,Borchardt RT

    更新日期:1996-11-01 00:00:00

  • Recent developments in cyclic acetal biomaterials for tissue engineering applications.

    abstract::At an ever increasing pace, synthetic biomaterials are being developed with specific functionalities for tissue engineering applications. These biomaterials possess properties including biocompatibility, mechanical strength, and degradation as well as functionalities such as specific cell adhesion and directed cell mi...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章,评审

    doi:10.1007/s11095-008-9620-5

    authors: Falco EE,Patel M,Fisher JP

    更新日期:2008-10-01 00:00:00

  • Dissolution testing of hardly soluble materials by surface sensitive techniques: clotrimazole from an insoluble matrix.

    abstract:PURPOSE:The low aqueous solubility of many drugs impedes detailed investigation as the detection limit of standard testing routines is limited. This is further complicated within application relevant thin films typical used in patches or stripes for buccal or topical routes. METHODS:In this work a model system is deve...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-014-1368-5

    authors: Ehmann HM,Winter S,Griesser T,Keimel R,Schrank S,Zimmer A,Werzer O

    更新日期:2014-10-01 00:00:00

  • The effects of bile salts and lipids on the physicochemical behavior of gemfibrozil.

    abstract::Physicochemical effects caused by intestinal fluids on drugs in the gastrointestinal (GI) tract can be a contributing factor in food induced changes in bioavailability. To identify physicochemical properties of gemfibrozil that may be altered by endogenous and dietary lipids, in vitro studies were conducted in model s...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018967401000

    authors: Luner PE,Babu SR,Radebaugh GW

    更新日期:1994-12-01 00:00:00

  • Effects of pluronic P85 on GLUT1 and MCT1 transporters in the blood-brain barrier.

    abstract:PURPOSE:The amphiphilic block copolymer Pluronic P85 (P85) increases the permeability of the blood-brain barrier (BBB) with respect to a broad spectrum of drugs by inhibiting the drug efflux transporter, P-glycoprotein (Pgp). In this regard, P85 serves as a promising component for CNS drug delivery systems. To assess t...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/b:pham.0000048189.79606.6e

    authors: Batrakova EV,Zhang Y,Li Y,Li S,Vinogradov SV,Persidsky Y,Alakhov VY,Miller DW,Kabanov AV

    更新日期:2004-11-01 00:00:00

  • Nanotechnology-based cancer therapeutics--promise and challenge--lessons learned through the NCI Alliance for Nanotechnology in Cancer.

    abstract::The new generation of nanotechnology-based drug formulations is challenging the accepted ways of cancer treatment. Multi-functional nanomaterial constructs have the capability to be delivered directly to the tumor site and eradicate cancer cells selectively, while sparing healthy cells. Tailoring of the nano-construct...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-010-0214-7

    authors: Farrell D,Ptak K,Panaro NJ,Grodzinski P

    更新日期:2011-02-01 00:00:00

  • Tissue Chips in Space: Modeling Human Diseases in Microgravity.

    abstract:PURPOSE:Microphysiological systems (MPS), also known as "organs-on-chips" or "tissue chips," leverage recent advances in cell biology, tissue engineering, and microfabrication to create in vitro models of human organs and tissues. These systems offer promising solutions for modeling human physiology and disease in vitr...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章,评审

    doi:10.1007/s11095-019-2742-0

    authors: Low LA,Giulianotti MA

    更新日期:2019-12-17 00:00:00

  • Correlation of rFVIII inactivation with aggregation in solution.

    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

    pub_type: 杂志文章

    doi:10.1023/a:1023271405005

    authors: Wang W,Kelner DN

    更新日期:2003-04-01 00:00:00

  • ATP-binding cassette transporter G2 mediates the efflux of phototoxins on the luminal membrane of retinal capillary endothelial cells.

    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

    pub_type: 杂志文章

    doi:10.1007/s11095-006-0067-2

    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

  • A physiologic model for simulating gastrointestinal flow and drug absorption in rats.

    abstract:PURPOSE:The development of a physiologically based absorption model for orally administered drugs in rats is described. METHODS:Unlike other models that use a multicompartmental approach, the GI tract is modeled as a continuous tube with spatially varying properties. The mass transport through the intestinal lumen is ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/b:pham.0000003373.72652.c0

    authors: Willmann S,Schmitt W,Keldenich J,Dressman JB

    更新日期:2003-11-01 00:00:00

  • A pH-Sensitive Nanocarrier for Tumor Targeting : Delivery of Ruthenium Complex for Tumor Theranostic by pH-Sensitive Nanocapsule.

    abstract:PURPOSE:Ruthenium complex is a potentially theranostic agent for cancer imaging and therapy, however its application is limited due to poor water-solubility and lack of tumor selectivity. To overcome the above drawbacks, pH-sensitive nanocapsule as a novel targeting carrier was designed to deliver ruthenium complex for...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-016-2021-2

    authors: Chen L,Fu C,Deng Y,Wu W,Fu A

    更新日期:2016-12-01 00:00:00

  • The effect of octanoic acid on the binding of the enantiomers of ibuprofen and naproxen to human serum albumin: a chromatographic implication.

    abstract:PURPOSE:The heats of reaction between the enantiomers and racemates of ibuprofen and naproxen and human serum albumin (HSA) are to be measured with and without the addition of octanoic acid. The effects of octanoic acid on the free energies of interaction between the drugs and HSA is to be determined and compared to th...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1016066325476

    authors: Cheruvallath VK,Riley CM,Narayanan SR,Lindenbaum S,Perrin JH

    更新日期:1996-01-01 00:00:00

  • Effect of polymer blending on the release of ganciclovir from PLGA microspheres.

    abstract:PURPOSE:The aim of the study is to investigate the effect of polymer blending on entrapment and release of ganciclovir (GCV) from poly(D,L-lactide-co-glycolide) (PLGA) microspheres using a set of empirical equations. METHODS:Two grades of PLGA, PLGA 7525 [D,L-lactide:glycolide(75:25), MW 90,000-126,000 Da] and Resomer...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-005-9042-6

    authors: Duvvuri S,Gaurav Janoria K,Mitra AK

    更新日期:2006-01-01 00:00:00

  • Population Pharmacokinetics, Efficacy Exposure-response Analysis, and Model-based Meta-analysis of Fenebrutinib in Subjects with Rheumatoid Arthritis [corrected].

    abstract:PURPOSE:Fenebrutinib (GDC-0853), a Bruton's tyrosine kinase (BTK) inhibitor was investigated in a Phase 2 clinical trial in patients with rheumatoid arthritis (RA). Our aim was to apply a model-informed drug development (MIDD) approach to examine the totality of available clinical efficacy data. METHODS:Population pha...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-019-2752-y

    authors: Chan P,Yu J,Chinn L,Prohn M,Huisman J,Matzuka B,Hanley W,Tuckwell K,Quartino A

    更新日期:2020-01-06 00:00:00

  • Physical approaches to masking bitter taste: lessons from food and pharmaceuticals.

    abstract::Many drugs and desirable phytochemicals are bitter, and bitter tastes are aversive. Food and pharmaceutical manufacturers share a common need for bitterness-masking strategies that allow them to deliver useful quantities of the active compounds in an acceptable form and in this review we compare and contrast the chall...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章,评审

    doi:10.1007/s11095-014-1480-6

    authors: Coupland JN,Hayes JE

    更新日期:2014-11-01 00:00:00

  • Photokinetic Drug Delivery: Near infrared (NIR) Induced Permeation Enhancement of Bevacizumab, Ranibizumab and Aflibercept through Human Sclera.

    abstract:PURPOSE:Permeation studies, with near infrared (NIR) light and anti-aggregation antibody formulation, were used to investigate the in vitro permeation of bevacizumab, ranibizumab and aflibercept through human sclera. METHODS:A vertical, spherical Franz cell diffusion apparatus was used for this scleral tissue permeati...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-018-2392-7

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

    更新日期:2018-03-29 00:00:00

  • High-performance liquid chromatographic (HPLC) assay using fluorescence detection for the simultaneous determination of gallopamil and norgallopamil in human plasma.

    abstract::Gallopamil is a calcium-channel antagonist with reported activity in experimental animals three to five times higher than that of verapamil. An automated high-performance liquid chromatographic (HPLC) method with fluorescence detection is described for the simultaneous determination of gallopamil and its metabolite no...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1016401405119

    authors: McLean AM,Babcock-Atkinson E,Rein K,Ruggirello DA,Gonzalez MA,Noonan PK

    更新日期:1987-08-01 00:00:00

  • Antiangiogenic effect of docetaxel and everolimus as individual and dual-drug-loaded micellar nanocarriers.

    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

    pub_type: 杂志文章

    doi:10.1007/s11095-013-1188-z

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

    更新日期:2014-03-01 00:00:00

  • Local Application of Pyrophosphorylated Simvastatin Prevents Experimental Periodontitis.

    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

    pub_type: 杂志文章

    doi:10.1007/s11095-018-2444-z

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

    更新日期:2018-06-25 00:00:00

  • Enhanced oral delivery of curcumin from N-trimethyl chitosan surface-modified solid lipid nanoparticles: pharmacokinetic and brain distribution evaluations.

    abstract:PURPOSE:Solid lipid nanoparticles (SLNs) have been proposed as a colloidal carrier system that could enhance the oral bioavailability of curcumin. However, a burst release of the loaded drug, which occurs in acidic environments, has been a main obstacle to the oral delivery of curcumin by using SLNs as a carrier system...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-014-1469-1

    authors: Ramalingam P,Ko YT

    更新日期:2015-02-01 00:00:00

  • Effects of solute characteristics and concentration on a lyotropic liquid crystal: solute-induced phase change.

    abstract::We investigated the effects of increased concentrations of the solutes, salicylic acid, benzoic acid, and o-, m-, and p-methoxy benzoic acids, on the anisotropic properties of a liquid crystal solvent. The lamellar liquid crystal was composed of 37% polyoxyethylene (20) isohexadecyl ether in aqueous buffer of pH 1. Ph...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018920118631

    authors: Ibrahim HG,Sallam ES,Takieddin M,Habboub M

    更新日期:1993-05-01 00:00:00