Transport of thyrotropin releasing hormone in rabbit buccal mucosa in vitro.

Abstract:

:The transport of thyrotropin releasing hormone (TRH) in rabbit buccal mucosa in vitro has been investigated with respect to (a) rate and type of metabolism of TRH on mucosal and serosal sides of buccal mucosa, (b) mechanism of TRH transport including charge effect on its permeability, and (c) pathway and rate-limiting regions of TRH movement. In addition, the integrity of excised buccal mucosa has been evaluated for purposes of in vitro solute diffusion experiments using tissue ATP level data, transmission electron microscopy, and TRH transport kinetic data. The results indicate that excised rabbit buccal mucosa can be used for TRH diffusion studies for approximately 6 hr. In addition, TRH apparently traverses buccal mucosa by simple diffusion with a steady-state permeability of about 10(-7) cm/sec, and this permeability is independent of pH. Moreover, the primary pathway appears to be via the intercellular space in the rate-limiting barrier, i.e., the upper 50 microns of the epithelium. Finally, TRH is degraded predominantly by deamidase activity, which is followed by, to a lesser degree, carboxypeptidase metabolism.

journal_name

Pharm Res

journal_title

Pharmaceutical research

authors

Dowty ME,Knuth KE,Irons BK,Robinson JR

doi

10.1023/a:1015883217858

subject

Has Abstract

pub_date

1992-09-01 00:00:00

pages

1113-22

issue

9

eissn

0724-8741

issn

1573-904X

journal_volume

9

pub_type

杂志文章
  • The use of disaccharides in inhibiting enzymatic activity loss and secondary structure changes in freeze-dried β-galactosidase during storage.

    abstract:PURPOSE:The purpose of this study is to show how disaccharides differ in their ability to protect lyophilized β-galactosidase from enzymatic activity loss and secondary structure changes during storage. METHODS:β-galactosidase was lyophilized with trehalose, sucrose, cellobiose or melibiose at 2:1, 20:1 and 40:1 excip...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-010-0300-x

    authors: Heljo VP,Jouppila K,Hatanpää T,Juppo AM

    更新日期:2011-03-01 00:00:00

  • Synthesis and calcium channel antagonist activity of 3-arylmethyl 5-isopropyl 1,4-dihydro-2,6-dimethyl-4-(pyridyl)-3,5-pyridinedicarboxylates.

    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

    pub_type: 杂志文章

    doi:10.1023/a:1015941706008

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

    更新日期:1990-09-01 00:00:00

  • Prodrugs of peptides. 13. Stabilization of peptide amides against alpha-chymotrypsin by the prodrug approach.

    abstract::Various derivatives of the C-terminal amide group in N-protected amino acid and peptide amides were synthesized to assess their suitability as prodrug forms with the aim of protecting the amide or peptide bond against cleavage by alpha-chymotrypsin. Whereas N-acetylation, N-hydroxymethylation, and N-phthalidylation di...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015854718903

    authors: Kahns AH,Bundgaard H

    更新日期:1991-12-01 00:00:00

  • Rapid-Acting and Human Insulins: Hexamer Dissociation Kinetics upon Dilution of the Pharmaceutical Formulation.

    abstract:PURPOSE:Comparison of the dissociation kinetics of rapid-acting insulins lispro, aspart, glulisine and human insulin under physiologically relevant conditions. METHODS:Dissociation kinetics after dilution were monitored directly in terms of the average molecular mass using combined static and dynamic light scattering....

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-017-2233-0

    authors: Gast K,Schüler A,Wolff M,Thalhammer A,Berchtold H,Nagel N,Lenherr G,Hauck G,Seckler R

    更新日期:2017-11-01 00:00:00

  • Interactions of phosphodiester and phosphorothioate oligonucleotides with intestinal epithelial Caco-2 cells.

    abstract:PURPOSE:Oral bioavailability for antisense oligonucleotides has recently been reported but the mechanistic details are not known. The proposed oral delivery of nucleic acids will, therefore, require an understanding of the membrane binding interactions, cell uptake and transport of oligonucleotides across the human gas...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1016002606705

    authors: Beck GF,Irwin WJ,Nicklin PL,Akhtar S

    更新日期:1996-07-01 00:00:00

  • Enhancement of nasal salmon calcitonin absorption by lauroylcarnitine chloride in rats.

    abstract:PURPOSE:We investigated optimum formulation characteristics in the nasal absorption of salmon calcitonin (sCT) by incorporation of acylcarnitines. METHODS:Nasal sCT formulations were administered to anesthetized rats. Plasma calcium level was measured and pharmacological bioavailability (P.bioav) was calculated. RESU...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1016051600828

    authors: Kagatani S,Shinoda T,Fukui M,Ohmura T,Hasumi S,Sonobe T

    更新日期:1996-05-01 00:00:00

  • Dependence of dissolution rate on surface area: is a simple linear relationship valid for co-compressed drug mixtures?

    abstract::A quantitative analysis of the dependence of dissolution rate on the relative surface area occupied by two non-interacting drug mixtures from co-compressed slabs is described. The results from the experimental dissolution rates of each component from naproxen/phenytoin co-compressed slabs under laminar flow conditions...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018979419714

    authors: Neervannan S,Southard MZ,Stella VJ

    更新日期:1994-10-01 00:00:00

  • Release of plasmid DNA-encoding IL-10 from PLGA microparticles facilitates long-term reversal of neuropathic pain following a single intrathecal administration.

    abstract:PURPOSE:Interleukin-10 (IL-10) is an anti-inflammatory molecule that has achieved interest as a therapeutic for neuropathic pain. In this work, the potential of plasmid DNA-encoding IL-10 (pDNA-IL-10) slowly released from biodegradable microparticles to provide long-term pain relief in an animal model of neuropathic pa...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-010-0077-y

    authors: Soderquist RG,Sloane EM,Loram LC,Harrison JA,Dengler EC,Johnson SM,Amer LD,Young CS,Lewis MT,Poole S,Frank MG,Watkins LR,Milligan ED,Mahoney MJ

    更新日期:2010-05-01 00:00:00

  • Effect of polymer content and molecular weight on the morphology and heat- and moisture-induced transformations of spray-dried composite particles of amorphous lactose and poly(vinylpyrrolidone).

    abstract:PURPOSE:The aim was to investigate the influence of polymer content and molecular weight on the morphology and heat- and moisture-induced transformations, as indicators of stability, of spray-dried composite particles of amorphous lactose and poly(vinylpyrrolidone) (PVP). METHODS:Amorphous lactose and composite partic...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1024462306941

    authors: Berggren J,Alderborn G

    更新日期:2003-07-01 00:00:00

  • Pharmaceutical properties of loracarbef: the remarkable solution stability of an oral 1-carba-1-dethiacephalosporin antibiotic.

    abstract::Loracarbef is an oral 1-carba-1-dethiacephalosporin antibiotic structurally related to cefaclor. Like many beta-lactam antibiotics, loracarbef exists in several hydrated crystalline forms. The pH-solubility profile curve for loracarbef monohydrate is U-shaped, resembling those of other zwitterionic cephalosporins. Lor...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018949709797

    authors: Pasini CE,Indelicato JM

    更新日期:1992-02-01 00:00:00

  • The determinants of physician attitudes and subjective norms toward drug information sources: modification and test of the theory of reasoned action.

    abstract:PURPOSE:To improve upon the theory of reasoned action and apply it to pharmaceutical research, we investigated the effects of relevant appraisals attributes, and past behavior of physicians on the use of drug information sources. We also examined the moderating effects of practice characteristics. METHODS:A mail quest...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1012143915886

    authors: Gaither CA,Bagozzi RP,Ascione FJ,Kirking DM

    更新日期:1997-10-01 00:00:00

  • Fetal membrane transport enhancement using ultrasound for drug delivery and noninvasive detection.

    abstract:PURPOSE:The purpose of this research was to evaluate the effect of ultrasound on mass transport across fetal membrane for direct fetal drug delivery and sensing of the amniotic fluid in a noninvasive manner. METHODS:Post-delivery human fetal membranes (chorioamnion) were used for in vitro experiments, in which the eff...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-014-1470-8

    authors: Wolloch L,Azagury A,Goldbart R,Traitel T,Groisman G,Hallak M,Kost J

    更新日期:2015-02-01 00:00:00

  • Microbial metabolism studies of the antimalarial drug arteether.

    abstract::Microbial metabolism studies of the antimalarial drug arteether (1) have shown that arteether is metabolized by a number of microorganisms. Large-scale fermentation with Aspergillus niger (ATCC 10549) and Nocardia corallina (ATCC 19070) have resulted in the isolation of four microbial metabolites which have been chara...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015845306124

    authors: Lee IS,ElSohly HN,Hufford CD

    更新日期:1990-02-01 00:00:00

  • Systematic Investigation of the Role of Surfactant Composition and Choice of oil: Design of a Nanoemulsion-Based Adjuvant Inducing Concomitant Humoral and CD4+ T-Cell Responses.

    abstract:PURPOSE:Induction of cell-mediated immune (CMI) responses is crucial for vaccine-mediated protection against difficult vaccine targets, e.g., Chlamydia trachomatis (Ct). Adjuvants are included in subunit vaccines to potentiate immune responses, but many marketed adjuvants stimulate predominantly humoral immune response...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-017-2180-9

    authors: Schmidt ST,Neustrup MA,Harloff-Helleberg S,Korsholm KS,Rades T,Andersen P,Christensen D,Foged C

    更新日期:2017-08-01 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

    doi:10.1007/s11095-010-0157-z

    authors: Tang C,Prueksaritanont T

    更新日期:2010-09-01 00:00:00

  • The use of solution theories for predicting water vapor absorption by amorphous pharmaceutical solids: a test of the Flory-Huggins and Vrentas models.

    abstract::The limitations of traditional gas adsorption models for describing water vapor sorption by amorphous pharmaceutical solids are described and an alternative approach based on polymer solution theories is proposed. The approach is tested by comparing a priori predicted isotherms with literature data for the poly(vinylp...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018901325842

    authors: Hancock BC,Zografi G

    更新日期:1993-09-01 00:00:00

  • Phase behavior of binary and ternary amorphous mixtures containing indomethacin, citric acid, and PVP.

    abstract:PURPOSE:To better understand the nature of drug-excipient interactions we have studied the phase behavior of amorphous binary and ternary mixtures of citric acid, indomethacin and PVP, as model systems. METHODS:We have prepared amorphous mixtures by co-melting or coprecipitation from solvents, and have measured glass ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1011983606606

    authors: Lu Q,Zografi G

    更新日期:1998-08-01 00:00:00

  • The use of multiple doses and pharmacodynamic system analysis to distinguish between dispositional delays and time-variant pharmacodynamics.

    abstract::Pharmacokinetic-pharmacodynamic modeling algorithms, in general, rely on hysteresis minimization techniques that assume time-invariant pharmacodynamics (constant biophase concentration-effect relationships). When time-variant pharmacodynamics are observed, a specific model for tolerance or sensitization is required. H...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018940122382

    authors: Gastonguay MR,Schwartz SL

    更新日期:1994-12-01 00:00:00

  • The effect of probenecid on the pharmacokinetics of zalcitabine in HIV-positive patients.

    abstract:PURPOSE:The purpose of this study was to determine the potential effect of probenecid on the pharmacokinetics of zalcitabine in HIV-positive patients. METHODS:Twelve patients received single oral 1.5 mg doses of zalcitabine alone and during probenecid treatment (500 mg at 8 and 2 hours before and 4 hours after zalcita...

    journal_title:Pharmaceutical research

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1023/a:1016009029536

    authors: Massarella JW,Nazareno LA,Passe S,Min B

    更新日期:1996-03-01 00:00:00

  • Pharmacokinetics of Colistin Methansulphonate (CMS) and Colistin after CMS Nebulisation in Baboon Monkeys.

    abstract:PURPOSE:The objective of this study was to compare two different nebulizers: Eflow rapid® and Pari LC star® by scintigraphy and PK modeling to simulate epithelial lining fluid concentrations from measured plasma concentrations, after nebulization of CMS in baboons. METHODS:Three baboons received CMS by IV infusion and...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-015-1716-0

    authors: Marchand S,Bouchene S,de Monte M,Guilleminault L,Montharu J,Cabrera M,Grégoire N,Gobin P,Diot P,Couet W,Vecellio L

    更新日期:2015-10-01 00:00:00

  • Formulation and physical characterization of large porous particles for inhalation.

    abstract:PURPOSE:Relatively large (>5 microm) and porous (mass density <0.4 g/cm3) particles present advantages for the delivery of drugs to the lungs, e.g., excellent aerosolization properties. The aim of this study was, first, to formulate such particles with excipients that are either FDA-approved for inhalation or endogenou...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018910200420

    authors: Vanbever R,Mintzes JD,Wang J,Nice J,Chen D,Batycky R,Langer R,Edwards DA

    更新日期:1999-11-01 00:00:00

  • Relation between individual and ensemble release kinetics of indomethacin from microspheres.

    abstract::Indomethacin microspheres based on a combination of ethylcellulose and polyethyleneglycol were prepared using the solvent evaporation process. Release profiles of ensemble and individual microspheres were measured. Both were found to follow first-order kinetics, in contrast to what was expected. This was attributed to...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015917023949

    authors: Benita S,Babay D,Hoffman A,Donbrow M

    更新日期:1988-03-01 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

  • Electrospun Zein/PCL Fibrous Matrices Release Tetracycline in a Controlled Manner, Killing Staphylococcus aureus Both in Biofilms and Ex Vivo on Pig Skin, and are Compatible with Human Skin Cells.

    abstract:PURPOSE:To investigate the destruction of clinically-relevant bacteria within biofilms via the sustained release of the antibiotic tetracycline from zein-based electrospun polymeric fibrous matrices and to demonstrate the compatibility of such wound dressing matrices with human skin cells. METHODS:Zein/PCL triple laye...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-015-1782-3

    authors: Alhusein N,Blagbrough IS,Beeton ML,Bolhuis A,De Bank PA

    更新日期:2016-01-01 00:00:00

  • Dual Receptor Targeting Cell Penetrating Peptide Modified Liposome for Glioma and Breast Cancer Postoperative Recurrence Therapy.

    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

    pub_type: 杂志文章

    doi:10.1007/s11095-018-2399-0

    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

  • Correction to: Bioreducible Poly(Amino Ethers) Based mTOR siRNA Delivery for Lung Cancer.

    abstract::Under the heading "Methods-Synthesis of the Bioreducible Modified-PAE (mPAE)", on page 3, line 14-17, there is an error. The quantity unit of PAE and 2-iminothiolane hydrochloride needs to be corrected to mg instead of g. ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章,已发布勘误

    doi:10.1007/s11095-018-2488-0

    authors: Gandhi NS,Godeshala S,Koomoa-Lange DT,Miryala B,Rege K,Chougule MB

    更新日期:2018-09-05 00:00:00

  • The role of polysorbate 80 and HPβCD at the air-water interface of IgG solutions.

    abstract:PURPOSE:To test the hypothesis of surface displacement as the underlying mechanism for IgG stabilization by polysorbates and HPβCD against surface-induced aggregation. METHODS:Adsorption/desorption-kinetics of IgG-polysorbate 80/-HPβCD were monitored. Maximum bubble pressure method was used for processes within second...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-012-0854-x

    authors: Serno T,Härtl E,Besheer A,Miller R,Winter G

    更新日期:2013-01-01 00:00:00

  • Renin inhibitor: transport mechanism in rat small intestinal brush-border membrane vesicles.

    abstract::The transport characteristics of the renin inhibitor ((3S,4S)-4-[N-morpholinoacetyl-(1-naphthyl)-L-alanyl-N-methyl-(4-t hiazolyl)-L- alanyl]amino-3-hydroxy-5-cyclohexyl-1-(4-pyridyl)-1-pentanone; CH3-18) in rat small intestinal brush-border membrane vesicles (BBMV) were examined by a rapid filtration technique. The up...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018900124257

    authors: Hashimoto N,Fujioka T,Toyoda T,Muranushi N,Hirano K

    更新日期:1994-10-01 00:00:00

  • Novel delivery of antioxidant enzyme catalase to alveolar macrophages by Fc receptor-mediated endocytosis.

    abstract::Excessive production of reactive oxygen species by alveolar macrophages (AMs) in response to inhaled toxic substances is a major cause of oxidative lung injury. Therapeutic approaches designed to protect the lungs from oxidative injury by administering native antioxidant enzymes such as catalase and superoxide dismuta...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018976529766

    authors: Harrison J,Shi X,Wang L,Ma JK,Rojanasakul Y

    更新日期:1994-08-01 00:00:00

  • Immunopotentiator-Loaded Polymeric Microparticles as Robust Adjuvant to Improve Vaccine Efficacy.

    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

    pub_type: 杂志文章

    doi:10.1007/s11095-015-1666-6

    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