Abstract：
:Previous work from this laboratory showed site-dependent variations in the apparent permeability of insulin as measured using the everted rat gut sac technique, with the greatest permeability in the distal jejunum and the lowest in the duodenum (5). To quantify better the rate and extent of insulin absorption from the small intestine, closed-loop in situ experiments were performed in nondiabetic rats. Results correlated with the everted gut sac technique in that the absolute bioavailability determined in situ was higher for insulin solution administered to the more distal region of the intestine (0.133%) than that absorbed from an earlier portion of the intestine (0.059%). While the difference in regional bioavailabilities was not significant (P = 0.08), the blood glucose response showed highly significant differences (P = 0.0015), with severe and prolonged hypoglycemia resulting from insulin delivered to the distal jejunum/proximal ileum. Insulin administered iv followed a two-compartment pharmacokinetic model. Whole-body elimination rate constants were similar for both iv and enteral insulin. Although therapeutic quantities of insulin were absorbed from the distal small intestine, absorption enhancers would be necessary to decrease the dose of insulin required.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Schilling RJ,Mitra AKdoi
10.1023/a:1015894125611subject
Has Abstractpub_date
1992-08-01 00:00:00pages
1003-9issue
8eissn
0724-8741issn
1573-904Xjournal_volume
9pub_type
杂志文章abstract：PURPOSE:To investigate whether conjunctival epithelial cells express transport processes for opioid peptides. METHODS:We monitored the uptake of [(3)H]deltorphin II and [(3)H]DADLE, two hydrolysis-resistant synthetic opioid peptides, in the rabbit conjunctival epithelial cell line CJVE and elucidated the characteristi...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-008-9709-x
更新日期：2009-05-01 00:00:00
abstract：PURPOSE:Orally absorbable anticancer medications have great advantages for conventional cancer therapies to patients. Here we evaluated the potent anticancer effect of orally absorbable LHD, a chemical conjugate of low-molecular-weight heparin and deoxycholic acid, on tumor graft growth models. METHODS:We characterize...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-009-9989-9
更新日期：2009-12-01 00:00:00
abstract：:The binding of 1-anilino-8-naphthalenesulfonate (ANS) to bovine serum albumin (BSA), human serum albumin (HSA), and human plasma has been studied by potentiometric titration utilizing a laboratory constructed ion selective electrode (ISE) of ANS. Three classes of ANS binding sites were found on BSA, HSA, and plasma at...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015855613083
更新日期：1991-07-01 00:00:00
abstract：PURPOSE:The purpose of this work was to study the influence of cell differentiation on the mRNA expression of transporters and channels in Caco-2 cells and to assess Caco-2 cells as a model for carrier-mediated drug transport in the intestines. METHOD:Gene mRNA expression was measured using a custom-designed microarra...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1022282221530
更新日期：2003-01-01 00:00:00
abstract：PURPOSE:The purpose of the present study was to investigate changes of blood-brain barrier (BBB) and brain parenchymal protein expression due to type II diabetes mellitus (T2DM) induced by a high-fat diet (HFD) by using SWATH-based quantitative proteomics. METHODS:Mice were fed a HFD for 2 or 10 weeks, and then SWATH-...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-019-2674-8
更新日期：2019-07-31 00:00:00
abstract：PURPOSE:The lack of effective delivery vehicles impedes in vivo applications of siRNA. The trimethyl chitosan-cysteine (TC) nanoparticles (NPs) were developed for in vivo delivery of tumor necrosis factor α (TNF-α) siRNA via oral gavage and intraperitoneal injection. METHODS:The nanoparticles formulated from TC conjug...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1086-4
更新日期：2013-10-01 00:00:00
abstract：PURPOSE:The aim was to design and thoroughly characterize monodisperse Fe3O4@SiO2-Ag nanoparticles with strong antibacterial properties, which makes them a candidate for targeting bacterial infections. METHODS:The monodisperse Fe3O4 nanoparticles were prepared by oleic acid-stabilized thermal decomposition of Fe(III) ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-019-2680-x
更新日期：2019-08-14 00:00:00
abstract：PURPOSE:The objective of this work was to assess, in vitro, the passage of P-glycoprotein dependent drugs across brain capillary endothelial cells, when these drugs are associated with a reversing agent. METHODS:An in vitro model of the blood-brain barrier consisting of a coculture of brain capillary endothelial cells...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1011913723928
更新日期：1998-07-01 00:00:00
abstract：PURPOSE:1. The assessment of the role of hair follicles and sweat glands in skin resistance and percutaneous iontophoretic flux of 9-desglycinamide, 8-arginine vasopressin (DGAVP) by comparing two skin species: human stratum corneum which contained hair follicles, sweat and sebaceous glands, and shed snake skin which l...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016243706415
更新日期：1995-10-01 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
pub_type： 杂志文章
doi：10.1007/s11095-011-0540-4
更新日期：2012-01-01 00:00:00
abstract：:Primaquine, an 8-aminoquinoline antimalarial, is shown to undergo unexpectedly rapid aromatic proton exchange with the medium. At a pH less than 4, the exchange of C-5 is so fast as to be unmeasurable by proton nmr methods. At a pH of 6-6.5 the half-time for exchange is 4 to 5 minutes. This unexpectedly high rate of e...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/A:1016356926714
更新日期：1984-07-01 00:00:00
abstract：:The pharmacokinetic parameters of leuprolide acetate, a potent analogue of LH-RH, were determined in rats and dogs after i.v. and s.c. dosing with leuprolide solution. The effective human dose of once-a-month injectable microspheres of leuprolide was estimated to be about 3.2 to 8.1 mg analogue/month using these param...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015818504906
更新日期：1991-06-01 00:00:00
abstract：PURPOSE:Scutellarin, a flavonoid derived from the plant Erigeron breviscapus, is currently widely used to treat cerebrovascular diseases, liver-related diseases, and hyperlipidemia in china and other East Asian countries. This study was to investigate the effect of scutellarin on the uptake of rosuvastatin in HEK293T c...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-020-02950-5
更新日期：2020-10-29 00:00:00
abstract：PURPOSE:The sensitivity and effectiveness of indirect metrics proposed for the assessment of comparative absorption rates in bioequivalence studies [Cmax, Tmax, partial AUC (AUCp), feathered slope (SLf), intercept metric (I)] were originally tested by assuming first-order absorption. The present study re-evaluates thei...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1007521016985
更新日期：2000-05-01 00:00:00
abstract：PURPOSE:To characterize the pharmacokinetic/pharmacodynamic (PK/PD) properties of a new polyethylene glycol (PEG) conjugate formulation of interferon (IFN)-beta la following subcutaneous (SC) administration in monkeys. METHODS:Single SC injections of 0.3, 1, and 3 million international units (MIU)/kg of PEG-IFN-beta 1...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-004-9009-z
更新日期：2005-01-01 00:00:00
abstract：PURPOSE:The aim was to investigate anticancer drug-loaded poly(carbonate-ester) nanospheres as potential drug delivery systems for cancer therapy. METHODS:Functional poly(carbonate-ester) copolymers (HPCP-SD) were synthesized by the incorporation of sulfadiazine as the tumor-targeting groups to hydroxyl groups of poly...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-010-0275-7
更新日期：2010-12-01 00:00:00
abstract：:We describe an assay for acrolein in urine, employing derivatization with m-aminophenol in the presence of ferrous sulfate solution in sulfuric acid. The derivative (7-OH quinoline; DER) and the internal standard (quinine-bisulfate; IS) were separated on a 10-micron particle, 8 mm x 10-cm C18 cartridge in conjunction ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018964401677
更新日期：1993-11-01 00:00:00
abstract：PURPOSE:Our previous studies indicated that drug leaked from discoidal reconstituted high density lipoprotein (d-rHDL) during the remodeling behaviors induced by lecithin cholesterol acyl transferase (LCAT) abundant in circulation, thus decreasing the drug amount delivered into the target. In this study, arachidonic ac...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1273-3
更新日期：2014-07-01 00:00:00
abstract：PURPOSE:To develop a method for drawing statistical inferences from differences between multiple experimental pair distribution function (PDF) transforms of powder X-ray diffraction (PXRD) data. METHODS:The appropriate treatment of initial PXRD error estimates using traditional error propagation algorithms was tested ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-010-0259-7
更新日期：2010-12-01 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
pub_type： 杂志文章
doi：10.1023/a:1016270103863
更新日期：1995-01-01 00:00:00
abstract：PURPOSE:To investigate the potential of chitosan nanoparticles as a system for improving the systemic absorption of insulin following nasal instillation. METHODS:Insulin-loaded chitosan nanoparticles were prepared by ionotropic gelation of chitosan with tripolyphosphate anions. They were characterized for their size a...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018908705446
更新日期：1999-10-01 00:00:00
abstract：:The area function method for assessing zero-order (ko) drug absorption rates was compared to four other methods under conditions where variation occurs in the plasma concentration data and in the elimination rate constant (kel or k10) for one- or two-compartment models. For deviant kel values of a one-compartment mode...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015843811150
更新日期：1990-01-01 00:00:00
abstract：PURPOSE:The purpose was to develop a population pharmacokinetic model for montelukast after intravenous administration. Clinical trial simulations were conducted using the model developed to identify the lowest intravenous dose in 6- to 14-year-old children that would give montelukast systemic exposures that were compa...
journal_title：Pharmaceutical research
pub_type： 杂志文章,随机对照试验
doi：10.1007/s11095-005-2493-y
更新日期：2005-04-01 00:00:00
abstract：PURPOSE:To compare the adjuvanticity of polymeric particles (new-generation adjuvant) and alum (the traditional and FDA-approved adjuvant) for H5N1 influenza split vaccine, and to investigate respective action mode. METHODS:Vaccine formulations were prepared by incubating lyophilized poly(lactic acid) (PLA) microparti...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1224-z
更新日期：2014-04-01 00:00:00
abstract：:Turbidimetric or light scattering assays can be used to determine the extent of aggregation in protein formulations. Using low molecular weight urokinase (LMW-UK) as a model protein, the effect of polymeric additives on heat-induced aggregation was evaluated. Previous work has shown that under 60 degrees C heat treatm...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018935420680
更新日期：1994-07-01 00:00:00
abstract：PURPOSE:Design of intravaginal rings (IVRs) for delivery of antiretrovirals is often guided by in vitro release under sink conditions, based on the assumption that in vivo release will follow a similar release profile. METHODS:We conducted a dose-ranging study in the female reproductive tract of pigtail macaques using...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-017-2224-1
更新日期：2017-10-01 00:00:00
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
更新日期：1999-11-01 00:00:00
abstract：PURPOSE:To investigate plasmid DNA interactions with liposomes prepared from dimyristoylglyceroethylphosphocholine (EDMPC) and DOPE using high sensitivity differential scanning calorimetry (HSDSC). MATERIALS AND METHODS:Large unilamellar liposomes of EDMPC with DOPE (mol ratio 0-50%) were prepared. Plasmid DNA was add...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-007-9325-1
更新日期：2007-10-01 00:00:00
abstract：:This review describes the design and current development of leukotriene biosynthesis inhibitors as potential antiinflammatory agents. Knowledge of the enzymatic mechanism of 5-lipoxygenase led to specific inhibitors of this enzyme which catalyzes a key step in the leukotriene pathway. Competitive inhibitors include ir...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/A:1016381215385
更新日期：1985-11-01 00:00:00
abstract：PURPOSE:To engineer optimized near-infrared (NIR) active thermosensitive liposomes to potentially achieve image-guided delivery of chemotherapeutic agents. METHODS:Thermosensitive liposomes were surface-coated with either polyethylene glycol or dextran. Differential scanning calorimetry and calcein release studies wer...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0738-0
更新日期：2012-08-01 00:00:00
