Effects of epinephrine pretreatment and solution pH on ocular and systemic absorption of ocularly applied timolol in rabbits.

Abstract:

:The ratio between ocular and systemic drug concentrations describes the relative safety of ophthalmic dosage forms of the same drug in terms of its systemic side effects. In this study, we evaluated the effects of epinephrine pretreatment and solution pH on the aqueous humor:plasma and iris-ciliary body:plasma ratios of peak timolol concentrations after ocular application of timolol. Timolol eyedrops (5 mg/mL, 25 microL) were applied ocularly in pigmented rabbits. Raising pH of the eyedrops from 6.2 to 7.5 did not affect the ratio between ocular and systemic peak drug concentrations, since both ocular and systemic concentrations of timolol were increased. Administration of epinephrine (20 mg/mL, 50 microL) 5 min prior to timolol eyedrop administration reduced the peak timolol concentrations in plasma 65-80%. Epinephrine did not affect the ocular concentrations of timolol. The decreased peak concentrations in plasma were due to the conjunctival and nasal vasoconstricting effects of epinephrine and to the subsequent slower absorption of timolol. Our study demonstrates that compared with currently available eyedrops (pH 6.9), the ocular:systemic concentration ratio of ophthalmic timolol can be improved four- to sixfold in rabbits by combining epinephrine-induced conjunctival and nasal vasoconstriction and improved ocular absorption from pH 7.5 eyedrops.

journal_name

J Pharm Sci

authors

Kyyrönen K,Urtti A

doi

10.1002/jps.2600790808

subject

Has Abstract

pub_date

1990-08-01 00:00:00

pages

688-91

issue

8

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(15)48306-6

journal_volume

79

pub_type

杂志文章
  • A hot-melt extruded intravaginal ring for the sustained delivery of the antiretroviral microbicide UC781.

    abstract::Microbicide intravaginal rings (IVRs) are a promising woman-controlled strategy for preventing sexual transmission of human immunodeficiency virus (HIV). An IVR was prepared and developed from polyether urethane (PU) elastomers for the sustained delivery of UC781, a highly potent nonnucleoside reverse transcriptase in...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22781

    authors: Clark MR,Johnson TJ,McCabe RT,Clark JT,Tuitupou A,Elgendy H,Friend DR,Kiser PF

    更新日期:2012-02-01 00:00:00

  • Development of a Minimal Physiologically-Based Pharmacokinetic Model to Simulate Lung Exposure in Humans Following Oral Administration of Ivermectin for COVID-19 Drug Repurposing.

    abstract::SARS-CoV-2 utilizes the IMPα/β1 heterodimer to enter host cell nuclei after gaining cellular access through the ACE2 receptor. Ivermectin has shown antiviral activity by inhibiting the formation of the importin-α (IMPα) and IMPβ1 subunits as well as dissociating the IMPα/β1 heterodimer and has in vitro efficacy agains...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2020.08.024

    authors: Jermain B,Hanafin PO,Cao Y,Lifschitz A,Lanusse C,Rao GG

    更新日期:2020-12-01 00:00:00

  • Facile synthesis of glycol metabolites of phenethylamine drugs.

    abstract::High yields of potential glycol metabolites of p-synephrine, epinephrine, octopamine, and normacromerine can be obtained from the readily available monosubstituted and disubstituted acetophenones. The general procedure involves alpha-bromination followed by displacement with acetate ion and reduction with lithium alum...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600750621

    authors: Holshouser MH,Kolb M

    更新日期:1986-06-01 00:00:00

  • Preparation and biological evaluation of tumor-specific Ara-C liposomal preparations containing RGDV motif.

    abstract::Arginine-glycine-aspartate (RGD) has been shown to be essential for the recognition of integrins overexpressed in tumor cells, especially during tumor invasion, angiogenesis, and metasis. In this study, a novel tetrapeptide, RGD-valine (RGDV), was designed and attached to the N position of 1-β-D-arabinofuranosylcytosi...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23326

    authors: Wang F,Cui C,Ren Z,Wang L,Liu H,Cui G

    更新日期:2012-12-01 00:00:00

  • Targeted Drug Delivery via Folate Receptors for the Treatment of Brain Cancer: Can the Promise Deliver?

    abstract::Brain cancers are among the most lethal tumors due to their rapid development and poor prognosis. Despite the existing potential of novel therapeutic strategies for the treatment of brain cancer, the major remaining challenge associated with clinical translation is the lack of effective and safe delivery strategies to...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.xphs.2017.08.009

    authors: Guo J,Schlich M,Cryan JF,O'Driscoll CM

    更新日期:2017-12-01 00:00:00

  • Relative bioavailability of commercially available ibuprofen oral dosage forms in humans.

    abstract::Two human bioavailability studies were conducted to assess the in vivo performances of recently marketed 200-, 300-, and 400-mg ibuprofen capsules relative to the innovator's 300- and 400-mg tablets when administered as single oral 300- or 400-mg doses. An ibuprofen oral solution was also administered in each trial. W...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600710920

    authors: Gillespie WR,DiSanto AR,Monovich RE,Albert KS

    更新日期:1982-09-01 00:00:00

  • Adhesive tablet effective for treating canker sores in humans.

    abstract::A new mucoadhesive tablet, which releases natural active agents for pain reduction and rapid healing of canker sores, has been prepared and characterized. Adhesive tablets were prepared by compression molding of mixed powders of crosslinked polyacrylic acid and hydroxypropyl cellulose, absorbed with citrus oil and mag...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 临床试验,杂志文章

    doi:10.1002/jps.20193

    authors: Mizrahi B,Golenser J,Wolnerman JS,Domb AJ

    更新日期:2004-12-01 00:00:00

  • Long-term stability of aqueous solutions of luteinizing hormone-releasing hormone assessed by an in vitro bioassay and liquid chromatography.

    abstract::The stability of aqueous solutions of luteinizing hormone-releasing hormone (LHRH) after extended storage at various temperatures was investigated using a newly developed HPLC assay and an in vitro dispersed pituitary cell culture bioassay. Good correlations were obtained between the potency obtained by HPLC and bioas...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600730628

    authors: Shi YF,Sherins RJ,Brightwell D,Gallelli JF,Chatterji DC

    更新日期:1984-06-01 00:00:00

  • Enhancement of dissolution and absorption of mefenamic acid by egg albumin.

    abstract::The dissolution behavior and absorption of mefenamic acid following oral and rectal administration from drug:egg albumin solid dispersions have been studied in comparison with those of the drug alone. The interaction of drug with egg albumin in aqueous solution and solid state were examined by solubility analysis, dia...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600800517

    authors: Imai T,Nohdomi K,Acartürk F,Otagiri M

    更新日期:1991-05-01 00:00:00

  • Correlation of absorption of sulfamethazine boluses with dissolution using a new dissolution apparatus for veterinary tablets.

    abstract::A rotating-basket apparatus for dissolution testing of veterinary bolus tablets was designed and constructed. Sulfamethazine boluses containing different disintegrating agents were evaluated in vitro and by blood level data following administration to cattle. The dissolution t50 and various pharmacokinetic parameters ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600651231

    authors: Frazier WF,Nuessle NO

    更新日期:1976-12-01 00:00:00

  • VLDL-resembling phospholipid-submicron emulsion for cholesterol-based drug targeting.

    abstract::The objective of the current study was to develop and evaluate VLDL-resembling phospholipid-submicron emulsion (PSME) as a carrier system for new cholesterol-based compounds for targeted delivery to cancer cells. BCH, a boronated cholesterol compound, was originally developed in our laboratory to mimic the cholesterol...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.10117

    authors: Shawer M,Greenspan P,ØIe S,Lu DR

    更新日期:2002-06-01 00:00:00

  • Novel method of derivatization of an amidinourea (lidamidine) for GLC analysis.

    abstract::A new quantitative GLC method for analysis of lidamidine hydrochloride (I) was developed. The method was based on derivatization of I to 1-(2,6-dimethylphenyl)-4-methylamino-dihydro-1,3,5-triazin-2-one (II) using dimethylformamide dimethylacetal reagent. Compound II was synthesized and characterized by IR, NMR, mass s...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600710327

    authors: Won CM,Zalipsky JJ,Patel DM,Grim WM

    更新日期:1982-03-01 00:00:00

  • Influence of non-water-soluble placebo pellets of different sizes on the characteristics of orally disintegrating tablets manufactured by freeze-drying.

    abstract::The present study describes the development of an orally disintegrating tablet containing a non-water-soluble drug delivery system. A model system was applied to evaluate the effect of different-sized particles on tablet characteristics. Cellets were incorporated into tablets prepared by freeze-drying from a 100 mg/mL...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23517

    authors: Stange U,Führling C,Gieseler H

    更新日期:2013-06-01 00:00:00

  • InVitro, Ex Vivo, and In Vivo Evaluation of a Dual pH/Redox Responsive Nanoliposomal Sludge for Transdermal Drug Delivery.

    abstract::A dual pH/redox responsive copper-glyglycine-prednisolone succinate-loaded nanoliposomal (NL) sludge was successfully synthesized and optimized using a Box-Behnken design of experiments. Preformulation design variables indicated that relative ratios of phospholipids, considerably influences NL size, thus altering the ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2017.11.011

    authors: Mavuso S,Marimuthu T,Kumar P,Kondiah PPD,du Toit LC,Choonara YE,Pillay V

    更新日期:2018-04-01 00:00:00

  • Bioavailability of sulfadiazine in rabbits using tablets prepared by direct compression and fluidized-bed granulation.

    abstract::Experimental sulfadiazine tablets prepared by direct compression, using a commercially available direct compression tablet mass, were compared with experimental sulfadiazine tablets prepared by fluidized-bed granulation and commercially available sulfadiazine tablets USP. The values for friability and the time require...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600661023

    authors: Ritschel WA,Erni W

    更新日期:1977-10-01 00:00:00

  • Development of a thermally responsive nanogel based on chitosan-poly(N-isopropylacrylamide-co-acrylamide) for paclitaxel delivery.

    abstract::A thermally responsive nanogel was developed through the radical polymerization based on chitosan (CTS) and N-isopropylacrylamide (NIPAAm) with acrylamide (AAm) blended to explore the possibility of increasing the volume phase transition temperature (VPTT). The thermally sensitive features of resultant nanogels were s...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23995

    authors: Wang Y,Xu H,Wang J,Ge L,Zhu J

    更新日期:2014-07-01 00:00:00

  • Bioavailability and efficacy of antisense morpholino oligomers targeted to c-myc and cytochrome P-450 3A2 following oral administration in rats.

    abstract::Antisense phosphorodiamidate Morpholino oligomers (PMO) are resistant to degradation by cellular hydrolases, DNases, RNases, and phosphodiesterases, but remain sensitive to prolonged exposure to low pH. The present studies evaluate the oral fractional bioavailability, stability, and efficacy of two distinct PMO sequen...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.10088

    authors: Arora V,Knapp DC,Reddy MT,Weller DD,Iversen PL

    更新日期:2002-04-01 00:00:00

  • Structural requirements for binding of nonsteroidal anti-inflammatory drugs to human serum albumin.

    abstract::The binding of representative chemical classes of nonsteroidal anti-inflammatory drugs (NSAIDs) to human serum albumin (HSA) was investigated by equilibrium dialysis. Warfarin enantiomers were used as specific markers in displacement studies. Data were analyzed by a computerized nonlinear least squares approach design...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600770314

    authors: Li KL,Thakur AK,Kapoor AL

    更新日期:1988-03-01 00:00:00

  • Stabilizing effect of fructose on aqueous solutions of hydrocortisone.

    abstract::Accelerated stability studies (37 degrees, 47 degrees, and 57 degrees) were conducted on buffered aqueous solutions (pH 7.4, 8.4, and 9.4) of hydrocortisone in the presence of various molar ratios of D-fructose. First-order degradation was observed. Significant improvement in hydrocortisone stability was seen in those...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600720930

    authors: Bansal NP,Holleran EM,Jarowski CI

    更新日期:1983-09-01 00:00:00

  • Structural characterization of anhydrous naloxone- and naltrexone hydrochloride by high resolution laboratory X-ray powder diffraction and thermal analysis.

    abstract::The crystal structures of the analgesic compounds anhydrous naloxone and naltrexone hydrochloride were determined ab initio from high resolution laboratory X-ray powder diffraction data. Both compounds crystallize in the orthorhombic space group P2(1)2(1)2(1) with lattice parameters of a = 14.6588(10) A, b = 17.4363(9...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20972

    authors: Sugimoto K,Dinnebier RE,Zakrzewski M

    更新日期:2007-12-01 00:00:00

  • High-speed liquid chromatographic determination of canrenone in pharmaceutical dosage forms.

    abstract::Canrenone can be determined by high-speed liquid chromatography in pharmaceutical dosage forms without interference from common excipients or degradation products. This stability-indicating assay, using o-nitroaniline as the internal standard, is rapid and accurate. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600650135

    authors: Williamson DE

    更新日期:1976-01-01 00:00:00

  • GLC analysis of theophylline, hydroxyethyltheophylline, and diphenylpyraline hydrochloride syrup.

    abstract::A GLC method for determining theophylline, hydroxyethyltheophylline, and diphenylpyraline hydrochloride is presented. The method permits the separation and quantitative determination of the therapeutically active ingredients with a single injection in an overall time of approximately 2.5 hr. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600680438

    authors: de Fabrizio F

    更新日期:1979-04-01 00:00:00

  • Physicochemical and structural characterization of quercetin-beta-cyclodextrin complexes.

    abstract::Quercetin is a bioactive flavonoid widely used as a health supplement. Being sparingly soluble and chemically unstable in aqueous intestinal fluids, quercetin is poorly absorbed orally. This study aimed to investigate the effects of three beta-cyclodextrins, namely, unsubstituted beta-cyclodextrin (beta-CD), hydroxypr...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20325

    authors: Zheng Y,Haworth IS,Zuo Z,Chow MS,Chow AH

    更新日期:2005-05-01 00:00:00

  • A solid-state NMR study of phase structure, molecular interactions, and mobility in blends of citric acid and paracetamol.

    abstract::Citric acid anhydrate (CAA) and paracetamol (PARA), prepared as crystalline physical mixtures and as amorphous blends, were studied using (13)C solid-state cross polarization magic angle spinning (CPMAS) NMR. Amorphous blends showed significant line broadening from the conformational distribution as compared to the cr...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21559

    authors: Schantz S,Hoppu P,Juppo AM

    更新日期:2009-05-01 00:00:00

  • Micro and macro GLC determination of ethambutol in biological fluids.

    abstract::Previously available GLC methods for ethambutol may only be used to measure quantities of drugs much greater than those found in biological fluids such as plasma and dialysate. A previously published GLC method for plasma samples is extended to measure ethambutol in dialysate. A second GLC method, involving derivatiza...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600670407

    authors: Lee CS,Benet LZ

    更新日期:1978-04-01 00:00:00

  • Applications of circular dichroism (CD) for structural analysis of proteins: qualification of near- and far-UV CD for protein higher order structural analysis.

    abstract::Circular dichroism (CD) spectroscopy is routinely used in the biopharmaceutical industry to study the effects of manufacturing, formulation, and storage conditions on protein conformation and stability, and these results are often included in regulatory filings. In this context, the purpose of CD spectroscopy is often...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22695

    authors: Li CH,Nguyen X,Narhi L,Chemmalil L,Towers E,Muzammil S,Gabrielson J,Jiang Y

    更新日期:2011-11-01 00:00:00

  • Solubility profiling of HIV protease inhibitors in human intestinal fluids.

    abstract::The present study pursued to profile the intestinal solubility of nine HIV protease inhibitors (PIs) in fasted- and fed-state human intestinal fluids (FaHIF, FeHIF) aspirated from four volunteers. In addition, the ability of fasted- and fed-state simulated intestinal fluids (FaSSIF, FeSSIF) to predict the intestinal s...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23698

    authors: Wuyts B,Brouwers J,Mols R,Tack J,Annaert P,Augustijns P

    更新日期:2013-10-01 00:00:00

  • Prediction of distribution coefficient from structure. 1. Estimation method.

    abstract::A method has been developed for the estimation of the distribution coefficient (D), which considers the microspecies of a compound. D is calculated from the microscopic dissociation constants (microconstants), the partition coefficients of the microspecies, and the counterion concentration. A general equation for the ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js960177k

    authors: Csizmadia F,Tsantili-Kakoulidou A,Panderi I,Darvas F

    更新日期:1997-07-01 00:00:00

  • Variations in compaction behaviour for tablets of different size and shape, revealed by small-angle X-ray scattering.

    abstract::Local variations in compaction behaviour were investigated, for specimens of different shapes and thickness, comparing predictions from finite element (FE) modelling and results from a recently developed method using small-angle X-ray scattering (SAXS). Good agreement was generally obtained between these methods, in t...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22144

    authors: Laity PR,Han L,Elliott J,Cameron RE

    更新日期:2010-10-01 00:00:00

  • Raster image correlation spectroscopy as a novel tool for the quantitative assessment of protein diffusional behaviour in solution.

    abstract::The application of raster image correlation spectroscopy (RICS) as a tool for the characterisation of protein diffusion was assessed using a model protein, bovine serum albumin (BSA), as a function of formulation and denaturing conditions. RICS results were also validated against dynamic light scattering and fluoresce...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23105

    authors: Hamrang Z,Pluen A,Zindy E,Clarke D

    更新日期:2012-06-01 00:00:00