Abstract：
:The mechanism of release from sustained-release adinazolam mesylate tablets was assessed by the Higuchi equation and by analysis of drug release profiles through 60% released using the Peppas equation. Computed values of the diffusional exponent, n, ranged from 0.59 to 0.66. Values of n in this range are consistent with a mixed mechanism of release, with diffusion of drug through the hydrated polymer matrix and relaxation of this matrix being the principal processes controlling release. The rate of in vitro drug release was increased for half tablets relative to whole tablets and is attributed to an increase in the surface to volume ratio of half tablets of about 16%. This increase in surface-to-volume ratio of half tablets was reflected by an increase in the constant, k, from the Peppas equation of 20-23% and by an increase in the slope of Higuchi plots of 12-18% for four lots of tablets. In vivo/in vitro relationships from two bioavailability studies were thoroughly evaluated. Using either a linear or a quadratic relationship, an in vivo/in vitro correlation exists for sustained-release adinazolam mesylate tablets.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Skoug JW,Borin MT,Fleishaker JC,Cooper AMdoi
10.1023/a:1015834114359subject
Has Abstractpub_date
1991-12-01 00:00:00pages
1482-8issue
12eissn
0724-8741issn
1573-904Xjournal_volume
8pub_type
杂志文章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
更新日期：1993-09-01 00:00:00
abstract：PURPOSE:To develop a dose dependent version of BCS and identify a critical dose after which the amount absorbed is independent from the dose. METHODS:We utilized a mathematical model of drug absorption in order to produce simulations of the fraction of dose absorbed (F) and the amount absorbed as function of the dose ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0815-4
更新日期：2012-11-01 00:00:00
abstract：:One of the authors has his name incorrectly indexed in PubMed and SpringerLink as "Laird Forrest M" (last name "Laird Forrest"). His name should index as "Forrest M. Laird" with last name as "Forrest". ...
journal_title：Pharmaceutical research
pub_type： 杂志文章,已发布勘误
doi：10.1007/s11095-018-2463-9
更新日期：2018-07-25 00:00:00
abstract：PURPOSE:Tissue partitioning is an important component of drug distribution and half-life. Protein binding and lipid partitioning together determine drug distribution. METHODS:Two structure-based models to predict partitioning into microsomal membranes are presented. An orientation-based model was developed using a mem...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-016-2085-z
更新日期：2017-03-01 00:00:00
abstract：:The mechanical properties of dry and wet polymeric films prepared from various aqueous polymeric dispersions were evaluated by a puncture test. They were studied with respect to type of polymer dispersion [cellulosic: Aquacoat and Surelease; acrylic: Eudragit NE, L, RS, and RL 30 D], plasticizer type (water-soluble or...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018942127524
更新日期：1994-06-01 00:00:00
abstract：:Silk is a remarkable biopolymer with a long history of medical use. Silk fabrications have a robust track record for load-bearing applications, including surgical threads and meshes, which are clinically approved for use in humans. The progression of top-down and bottom-up engineering approaches using silk as the basi...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1007/s11095-018-2534-y
更新日期：2018-11-05 00:00:00
abstract：:A new transdermal therapeutic system (TTS) for nitroglycerin is presented that controls release of the active substance by means of desorption and diffusion. The drug release, in the dosage range examined under sink conditions, is independent of electrolytes and pH of the aqueous acceptor medium, but it does depend on...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/A:1016361921803
更新日期：1985-01-01 00:00:00
abstract：:A method of immobilizing urokinase on albumin microspheres has been developed. Laser scattering, which was used to follow particle size from the initial emulsification stage to the final aqueous resuspension of the microsphere stage, showed that particle coalescence and crosslinking were critical parameters in manufac...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015855622459
更新日期：1992-06-01 00:00:00
abstract：PURPOSE:To develop a new intradermal antigen delivery system by coating microneedle arrays with lipid bilayer-coated, antigen-loaded mesoporous silica nanoparticles (LB-MSN-OVA). METHODS:Synthesis of MSNs with 10-nm pores was performed and the nanoparticles were loaded with the model antigen ovalbumin (OVA), and coate...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-017-2177-4
更新日期：2017-08-01 00:00:00
abstract：:The glass transition temperature of an amorphous pharmaceutical solid is a critical physical property which can dramatically influence its chemical stability, physical stability, and viscoelastic properties. Water frequently acts as a potent plasticizer for such materials, and since many amorphous solids spontaneously...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018941810744
更新日期：1994-04-01 00:00:00
abstract：PURPOSE:The aim of the study was to evaluate organogel nanoparticles as a lipophilic vehicle to increase the oral bioavailability of poorly soluble compounds. Efavirenz (EFV), a Biopharmaceutical Classification System (BCS) Class II, was used as drug model. METHODS:Organogel nanoparticles loaded with EFV were formulat...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-020-02808-w
更新日期：2020-05-11 00:00:00
abstract：PURPOSE:Safe, targeted delivery of therapeutics remains a focus of drug/gene delivery, the aim being to achieve optimal efficacy while minimising off-target delivery. Dendrimers have a vast array of potential applications and have great potential as gene and drug delivery tools. We previously reported the development o...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-014-1408-1
更新日期：2014-11-01 00:00:00
abstract：PURPOSE:To determine the extent of lateral spread and stratum corneum (SC) penetration of caffeine (CAF), hydrocortisone (HC) and ibuprofen (IBU) using a novel concentric tape stripping technique. METHOD:Ethanolic solutions of CAF, HC or IBU were applied to the forearm of 8 volunteers. At various time points, 10 succe...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0731-7
更新日期：2012-08-01 00:00:00
abstract：PURPOSE:The objective of this study was to elucidate the different mechanisms of action of different excipients on the oxidation of Met1, Met122, Met127, and Met138 in granulocyte colony-stimulating factor (G-CSF) by using hydrogen peroxide as the oxidant. METHODS:The oxidation of Met1, Met127, and Met138 was quantifi...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-004-9019-x
更新日期：2005-01-01 00:00:00
abstract：PURPOSE:The pharmacokinetics of corticosteroids in pregnancy were analyzed to assess maternal/fetal disposition and factors controlling fetal exposure. Area/Moment equations and compartmental models for estimating pharmacokinetic parameters from single dose data during pregnancy were developed. METHODS:Betamethasone i...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-004-7681-7
更新日期：2004-12-01 00:00:00
abstract：PURPOSE:To investigate in vitro if P-glycoprotein (P-gp) transport can differentiate between antibiotic drugs exhibiting increased active renal clearance (CL(r)) in cystic fibrosis (CF) patients (i.e., dicloxacillin, trimethoprim) and drugs that do not exhibit this phenomenon (i.e.. cefsulodin, sulfamethoxazole). METH...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015191511817
更新日期：2002-04-01 00:00:00
abstract：:The pulmonary deposition and pharmacokinetics of human growth hormone (hGH), administered by aerosol and instillate, in formulations containing 99mTc-DTPA (for gamma scintigraphic imaging) have been studied in five male New Zealand White rabbits. Gamma scintigraphy indicated that the peripheral:central deposition tend...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016292232513
更新日期：1995-03-01 00:00:00
abstract：PURPOSE:To assess the efficacy of the novel clinical formulation of fenretinide (LAU-7b) for the treatment of allergic asthma. To study the association between LAU-7b treatment in allergic asthma and the modulation of very long chain ceramides (VLCC). METHODS:We used two allergens (OVA and HDM) to induce asthma in mou...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-019-2743-z
更新日期：2020-01-08 00:00:00
abstract：PURPOSE:Tumor vascular normalization by antiangiogenic agents may increase tumor perfusion but reestablish vascular barrier properties in CNS tumors. Vascular priming via nanoparticulate carriers represents a mechanistically distinct alternative. This study investigated mechanisms by which sterically-stabilized liposom...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0823-4
更新日期：2012-12-01 00:00:00
abstract：PURPOSE:Characterization of virosomes, in late stage preclinical development as vaccines for Respiratory Syncytial Virus (RSV), with a membrane-incorporated synthetic monophosphoryl lipid A, 3D-PHAD® adjuvant. METHODS:Virosomes were initially formed by contacting a lipid film containing 3D-PHAD® with viral membranes s...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-018-2453-y
更新日期：2018-07-03 00:00:00
abstract：PURPOSE:To compare the systemic delivery of deslorelin following intratracheal administration of different deslorelin formulations. The formulations included dry powders of deslorelin, large-porous deslorelin-poly(lactide-co-glycolide) (PLGA) particles, and small conventional deslorelin-PLGA particles. Also, solution f...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/b:pham.0000032997.96823.88
更新日期：2004-07-01 00:00:00
abstract：:The possible mechanism of hepatic uptake of colchicine (CLC), a microtubule system disrupting agent, was examined using isolated rat hepatocytes. The existence of a carrier-mediated active transport system for CLC was demonstrated. This transport system is saturable, is affected by metabolic inhibitors (dinitrophenol,...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015917601349
更新日期：1989-03-01 00:00:00
abstract：PURPOSE:The effects of liposomes on nitric oxide (NO) production from mouse peritoneal macrophages following intraperitoneal injection of liposomes were investigated. METHODS:Mouse peritoneal macrophages were collected following intraperitoneal injection of liposomes and cultured with and without lipopolysaccharide (L...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016034303012
更新日期：1996-09-01 00:00:00
abstract：PURPOSE:Levofloxacin, a quinolone antibacterial drug, is a zwitterion at physiological pH. We examined the effect of cationic and anionic drugs on renal excretion of levofloxacin by means of in vivo clearance to characterize the mechanisms of renal excretion of this drug. METHODS:In vivo clearance was studied in male ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1012111902798
更新日期：1997-04-01 00:00:00
abstract：:Sodium taurodihydrofusidate (STDHF) is one of the most promising absorption enhancers for nasal delivery of peptide drugs. Drugs and additives in nasal formulations should not interfere with the self-cleaning capacity of the nose by the ciliary epithelium. Measured in vitro on human adenoid tissue with a photoelectric...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015872617511
更新日期：1990-02-01 00:00:00
abstract：PURPOSE:This study was conducted to investigate in vivo the impact of interferon-alpha (IFN)-alpha on P-glycoprotein (P-gp) activity in rats by studying how its administration modifies the bioavailability of digoxin, a fairly pure P-gp substrate. METHODS:Human recombinant IFN-alpha was given to rats (n = 5-7 per group...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-005-7415-5
更新日期：2005-11-01 00:00:00
abstract：PURPOSE:To study the physical and release properties of different molecular weight (MW) pH- and temperature-responsive statistical terpolymers and beads of N-isopropylacrylamide (NIPAAm), butylmethacrylate (BMA) and acrylic acid (AA). METHODS:Random terpolymers of varying MW were synthesized with NIPAAm/BMA/AA of feed...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018813700535
更新日期：1999-06-01 00:00:00
abstract：:Five aliphatic 5'-esters of 5-iodo-2'deoxyuridine (IDU) were synthesized via an acid chloride alcoholysis reaction. The solubility in pH 7.4 phosphate buffer, lipophilicity as determined by partition experiments in octanol/pH 7.4 buffer, and cytotoxicity of these potential prodrugs were evaluated. The esters showed a ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015968113838
更新日期：1988-11-01 00:00:00
abstract：:The hair follicle, hair shaft, and sebaceous gland collectively form what is recognized as the pilosebaceous unit. This complex, three-dimensional structure within the skin possesses a unique biochemistry, metabolism and immunology. Recent studies have focused on the hair follicle as a potential pathway for both local...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1023/a:1016250422596
更新日期：1995-02-01 00:00:00
abstract：:The effect of freezing on formation of soluble and insoluble aggregates of human growth hormone (hGH) was studied. The amount of soluble aggregates was affected very little by freezing regardless of the cooling rate. In contrast, the formation of insoluble aggregates (particulates), as determined by light scattering i...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015888704365
更新日期：1991-11-01 00:00:00
