Abstract:
:Losartan, an antihypertensive agent in clinical development, was found to exist in two enantiotropic polymorphic forms, a low-temperature stable form (Form I) and a high-temperature stable form (Form II), the temperatures at which they are stable being related to the transition temperature. X-ray powder diffraction patterns indicated differences in the crystal packing of the two forms. The vibrational data from infrared and Raman spectroscopy suggested a subtle change in molecular conformation and crystal packing in the two forms. Solid-state 13C NMR data of the polymorphs concurred with the vibrational data and indicated that, while the observed line widths reflect no major changes in crystallinity, signal multiplicities and chemical shifts do reflect differences in molecular packing in the respective unit cells. Thus, in the absence of crystallographic data, useful structural information could be derived from spectroscopic results to identify each of the crystalline forms.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Raghavan K,Dwivedi A,Campbell GC Jr,Johnston E,Levorse D,McCauley J,Hussain Mdoi
10.1023/a:1018973530443subject
Has Abstractpub_date
1993-06-01 00:00:00pages
900-4issue
6eissn
0724-8741issn
1573-904Xjournal_volume
10pub_type
杂志文章abstract::Colonic absorption of recombinant human insulin-like growth factor I (rhIGF-I) was measured in vitro using both rat and minipig colon. The permeability coefficients were 8.03 +/- 1.03 and 4.75 +/- 0.43 x 10(-8) cm sec-1 in the rat and minipig, respectively. The steady-state flux in rat colon was linearly related to th...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018999106684
更新日期:1994-02-01 00:00:00
abstract::The pharmacokinetics of trilostane and one of its metabolites ketotrilostane are described and characterized in the rat following the separate intravenous administration of trilostane and ketotrilostane. It was noted during these studies that the parent compound and its metabolite undergo metabolic interconversion-tri...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015828027060
更新日期:1992-04-01 00:00:00
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
更新日期:1992-02-01 00:00:00
abstract::Azo polymers based upon 2-hydroxyethyl methacrylate, methyl methacrylate, and methacrylic acid, and containing N,N'-bis [(methacryloyloxyethyl)oxy(carbonylamino)]azobenzene as azo aromatic agent were evaluated in vivo as coating for colon-specific drug delivery. The gastrointestinal absorption of theophylline from cap...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016283027139
更新日期:1995-02-01 00:00:00
abstract::Esmolol hydrochloride degrades in aqueous solutions by the hydrolysis of a labile aliphatic carboxyester group. The products are methanol and ASL-8123. The resulting aliphatic carboxylic acid moiety (ASL-8123) has a pK of 4.80, which is within 1 pH unit of the pH of the formulation. ASL-8123 therefore acts as a "secon...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015973425708
更新日期:1988-08-01 00:00:00
abstract:PURPOSE:Near-infrared reflectance spectroscopy (NIRS) was used to evaluate and quantify the effect of compression force on the NIR spectra of tablets. METHODS:Flat, white tablets with no orientation (scoring, etc.) were manufactured on a Stokes Rotary Tablet Press. NIRS was used to predict tablet hardness on the follo...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1012071904673
更新日期:1997-01-01 00:00:00
abstract:PURPOSE:The purpose of this work was to investigate the mechanisms of cocrystal formation during cogrinding and storage of solid reactants, and to establish the effects of water by cogrinding with hydrated form of reactants and varying RH conditions during storage. METHODS:The hydrogen bonded 1:1 carbamazepine-sacchar...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-9110-6
更新日期:2006-10-01 00:00:00
abstract:PURPOSE:One of the major hurdles facing nanomedicines is the antibody production against nanoparticles that subsequently results in their opsonization and clearance by macrophages. The objective of this research was to examine and identify the sequence of a low-immunogenic peptide based on recombinant elastin-like poly...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-015-1683-5
更新日期:2015-09-01 00:00:00
abstract:PURPOSE:Penetration enhancers (PEs) enhancing efficacy depends on two processes: PEs release from patches and action on skin. Compared with their action on skin, PEs release process was poorly understood. Therefore, the purpose of this study was to make a mechanistic understanding of PEs release from acrylic pressure-s...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-020-02901-0
更新日期:2020-08-13 00:00:00
abstract::Photodegradation of solutions of metronidazole in the presence and absence of sodium urate was studied. Photodegradation appeared to follow zero-order kinetics and was found to be dependent on the pH, buffer species, sodium urate concentration, and light source. Complex formation between metronidazole and sodium urate...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015851719579
更新日期:1989-01-01 00:00:00
abstract:PURPOSE:The purpose of the present study was to use the human colorectal carcinoma cell line. Caco-2, as a human intestinal epithelial model for studying the effects of cyclodextrins as absorption enhancers. METHODS:Cyclodextrins of varying sizes and physicochemical characters were investigated. The effects of the cyc...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016225707807
更新日期:1995-09-01 00:00:00
abstract:PURPOSE:To assess the effects of selective lipid extraction and tape stripping on transepidermal water loss (TEWL) at three body regions in the pig. METHODS:Lipids were extracted from the abdominal, inguinal. and back regions using three different solvent extraction procedures or cellophane tape stripping (15x) on Yor...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1010944529387
更新日期:2001-07-01 00:00:00
abstract:PURPOSE:Bioadhesion is an important property of biological membranes, that can be utilized in pharmaceutical and biomedical applications. In this study, we have fabricated mucoadhesive drug releasing films with bio-based, non-toxic and biodegradable polymers that do not require chemical modifications. METHODS:Nanofibr...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-018-2428-z
更新日期:2018-05-22 00:00:00
abstract:PURPOSE:The intratumoral heterogeneity observed in breast cancer (BC), in particular with regard to cell surface receptor expression, can hinder the success of many targeted cancer therapies. The development of novel therapeutic agents that target more than one receptor can overcome this inherent property of tumors and...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-019-2684-6
更新日期:2020-01-21 00:00:00
abstract:PURPOSE:To study the pulmonary absorption and tolerability of various formulations of the decapeptide cetrorelix acetate in rats by a new aerosol delivery system (ASTA-ADS) for intratracheal application. METHODS:Using the ASTA-ADS, cetrorelix liquid formulations (aqueous solutions for ultrasonic nebulization) were fir...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011028227155
更新日期:2001-06-01 00:00:00
abstract::Aucubin, a promising hepatoprotecting iridoid glucoside, was given intravenously (iv), orally (po), intraperitoneally (ip), and hepatoportally (pv) to rats. A linear pharmacokinetic behavior was obtained after iv administation of 400-400 mg/kg of aucubin. The half-life of aucubin in the postdistributive phase (t1/2, b...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015821527621
更新日期:1991-08-01 00:00:00
abstract:PURPOSE:The objective of the work was to evaluate the potential of hyaluronan-based nanoparticles as tumor-targeting nano-systems for CD44-overexpressed cancer therapy. METHODS:The synthesized amphiphilic cholesteryl succinoyl hyaluronan (Chol-Suc-HA) conjugates self-assembled into docetaxel(DTX)-loaded nanoparticles ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1393-4
更新日期:2014-11-01 00:00:00
abstract::A liposomal formulation of methylprednisolone (L-MPL) was developed to improve localization of this immunosuppressant in lymphatic tissues. Liposomes containing MPL were formulated from a mixture of phosphatydylcholine and phosphatydylglycerol (molar ratio, 9:1) and sized by extrusion through a 0.1-micron membrane. Ma...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018954704886
更新日期:1993-10-01 00:00:00
abstract:PURPOSE AND METHODS:Data from 358 pharmacist-patient encounters in 12 community pharmacies were used to investigate the association of prescription status, patient age, patient gender, and patient question asking with the content of pharmacist-patient communication. RESULTS:There was an association between prescriptio...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1012084207399
更新日期:1997-02-01 00:00:00
abstract:PURPOSE:Ultrasound can be used to release a therapeutic payload encapsulated within a perfluorocarbon (PFC) emulsion via acoustic droplet vaporization (ADV), a process whereby the PFC phase is vaporized and the agent is released. ADV-generated microbubbles have been previously used to selectively occlude blood vessels ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-010-0277-5
更新日期:2010-12-01 00:00:00
abstract:PURPOSE:Doxorubicin was chemically conjugated to a terminal end group of poly(D,L-lactic-co-glycolic acid) [PLGA] and the doxorubicin-PLGA conjugate was formulated into nanoparticles to sustain the release of doxorubicin. METHODS:A hydroxyl terminal group of PLGA was activated by p-nitrophenyl chloroformate and reacte...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018908421434
更新日期:1999-07-01 00:00:00
abstract:PURPOSE:The purpose of this work was to determine whether a new modeling methodology using fuzzy logic c an predict skin permeability coefficients that are given compound descriptors that have been proven to affect percutaneous penetration. METHOD:Three fuzzy inference models were developed using subtractive clusterin...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1022273115847
更新日期:2003-02-01 00:00:00
abstract:PURPOSE:To develop a semi-distributed liver model for the evaluation of saturable sinusoidal uptake and binding kinetics of the Oatp1a4 substrate digoxin. METHODS:In the perfused rat liver, two successive digoxin doses of 42 and 125 microg were administered, and the outflow concentration was determined by LC/MS/MS. [1...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-010-0204-9
更新日期:2010-09-01 00:00:00
abstract:PURPOSE:To investigate influence of ion induced mesophasic transformation on pharmaceutical performance of in situ gelling system consisting of glyceryl monooleate. METHODS:The prepared system showed mesophasic transformation during its conversion from sol to gel upon controlled hydration. The process of mesophasic tr...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-013-1033-4
更新日期:2013-07-01 00:00:00
abstract:PURPOSE:Myricetin (MYR) flavonoid is well-recognized for its antioxidant, anti-inflammatory and anti-tumor potential. Introducing nanomedicine was the ultimate resort to solve the imperfections of this nutraceutical, namely solubility, stability and delivery issues. The study, thus, aims at developing inhalable micropa...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-020-02794-z
更新日期:2020-04-14 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:A theoretical study was performed to generate a pharmacophore model for chemically diverse structures that specifically interact with the diltiazem binding site of L-type calcium channels. METHODS:Via molecular mechanics and quantum chemical methods solvation energies, logP values, conformational and electroni...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015037800903
更新日期:1999-10-01 00:00:00
abstract::New generation vaccines, particularly those based on recombinant proteins and DNA, are likely to be less reactogenic than traditional vaccines but are also less immunogenic. Therefore, there is an urgent need for the development of new and improved vaccine adjuvants. Adjuvants can be broadly separated into two classes...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1023/a:1016104910582
更新日期:2002-06-01 00:00:00
abstract:PURPOSE:The present investigation describes a formulative study for the development of innovative drug delivery systems for bromocriptine. METHODS:Solid lipid nanoparticles (SLN) based on different lipidic components have been produced and characterized. Morphology and dimensional distribution have been investigated b...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-007-9514-y
更新日期:2008-07-01 00:00:00
abstract:PURPOSE:The purpose of this study was (a) to suggest a novel dermatopharmacokinetic (DPK) approach from which pharmacokinetic parameters relevant to the bioequivalence (BE) assessment of a topical formulation can be deduced while circumventing the need for numerous measurements and assumptions, and (b) to investigate w...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-019-2724-2
更新日期:2020-01-02 00:00:00