Abstract：
PURPOSE:(i) To use trehalose as a model compound to evaluate the concept of crystallinity in pharmaceuticals. (ii) To understand the structural nature of dehydrated trehalose dihydrate. MATERIALS AND METHODS:Trehalose dihydrate was dehydrated isothermally at several temperatures below 100 degrees C and the anhydrous product was characterized by XRD, DSC and water vapor sorption. RESULTS:XRD and DSC suggested that the dehydration product was a partially crystalline alpha-polymorphic form of anhydrous trehalose (T(alpha)). An increase in the temperature of dehydration resulted in a decrease in lattice order. In agreement with earlier findings, the ordered regions in the dehydrated lattice (T(alpha)) converted to the dihydrate at much lower RH values than amorphous trehalose. However, the lattice order in the dehydrated product dictated the RH at which this conversion was initiated--the higher the lattice order the lower this RH. The structural nature of these samples can be explained based on the one-state model of crystallinity. In dehydrated trehalose, there is a continuum in lattice order ranging from highly crystalline (T(alpha)) to a completely disordered (i.e., amorphous) state. CONCLUSION:The extent of lattice order in anhydrous trehalose T(alpha) was dictated by the kinetics of water removal from trehalose dihydrate. The partially crystalline nature of anhydrous trehalose produced by dehydration could be described on a continuous scale of lattice order based on the one-state model of crystallinity.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Rani M,Govindarajan R,Surana R,Suryanarayanan Rdoi
10.1007/s11095-006-9058-6subject
Has Abstractpub_date
2006-10-01 00:00:00pages
2356-67issue
10eissn
0724-8741issn
1573-904Xjournal_volume
23pub_type
杂志文章abstract：PURPOSE:The purpose of this study was to investigate the effects of formulation factors including varying wax concentration, drug loading and drug particle size, on drug release characteristics from both pure oil and gel formulations prepared with a combination of derivatized vegetable oil (Labrafil 1944 CS) and glycer...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016209020160
更新日期：1995-06-01 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 study the expression of P-glycoprotein (P-gp), lung resistance-related protein (LRP), and caveolin-1 (cav-1) in the human bronchial epithelial cell line 16HBE14o-. METHODS:The presence of P-gp, LRP, and cav-1 in 16HBE14o- cell layers was evaluated using immunocytochemical staining and visualization with con...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1023230328687
更新日期：2003-04-01 00:00:00
abstract：PURPOSE:To provide the physicochemical properties of vitrified trehalose for predicting its recrystallization. METHODS:Thin films of vitrified trehalose solutions were prepared at room temperature and exposed to various humid and temperature atmospheres. The in-situ amount of retained water in the vacuum-dried trehalo...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-018-2420-7
更新日期：2018-05-10 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：PURPOSE:To describe the pharmacokinetics of SK&F 107647, a synthetic hematoregulatory peptide, in healthy volunteers and in patients with adenocarcinoma. METHODS:SK&F 107647 pharmacokinetics were evaluated in 2 dose-escalation studies. Volunteers received SK&F 107647 as single 15-minute iv infusion doses of 1, 10, 100...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1007512617139
更新日期：2000-04-01 00:00:00
abstract：:The application of supercritical fluid (SF) processing in pharmaceutical research is increasing particularly in the field of particle formation for drug delivery systems. The SF processes have benefits over the existing particle formation methods in terms of improved control, flexibility and operational ease. This rev...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1023/a:1011957512347
更新日期：1999-07-01 00:00:00
abstract：PURPOSE:A polysaccharide-flavonoid conjugate was developend and proposed for the treatment of pancreatic ductal adenocarcinoma (PDAC). METHODS:The conjugate was synthesized by free radical grafting reaction between catechin and dextran. The chemical characterization of the conjugate was obtained by UV-Vis, 1H-NMR, FT-...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0790-9
更新日期：2012-09-01 00:00:00
abstract：PURPOSE:The purpose of this study was to establish a useful methodology, possibly providing information on the stoichiometry of pharmaceutical drug salts obtained from salt screening by using a multiwell plate and a Raman microscope. METHODS:Tamoxifen salt screening was conducted with monobasic and polybasic acids on ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-006-9644-7
更新日期：2006-04-01 00:00:00
abstract：PURPOSE:This study examines methylprednisolone (MPL) effects on the dynamics of hepatic low-density lipoprotein receptor (LDLR) mRNA and plasma lipids associated with increased risks for atherosclerosis. MATERIALS AND METHODS:Normal male Wistar rats were given 50 mg/kg MPL intramuscularly (IM) and sacrificed at variou...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-007-9371-8
更新日期：2008-04-01 00:00:00
abstract：PURPOSE:To quantitatively compare in vitro dissolution data in biorelevant and compendial media, to investigate whether in vitro differences are reflected in the simulated plasma profile and to specify under which circumstances prediction of the plasma profile of orally administered lipophilic drugs can be achieved. M...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1011071401306
更新日期：2001-03-01 00:00:00
abstract：PURPOSE:Predicting human skin permeability of chemical compounds accurately and efficiently is useful for developing dermatological medicines and cosmetics. However, previous work have two problems; 1) quality of databases used, and 2) methods for prediction models. In this paper, we attempt to solve these two problems...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-015-1629-y
更新日期：2015-07-01 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：:Knowledge Management (KM) is a key enabler for achieving quality in a lifecycle approach for production of biopharmaceuticals. Due to the important role that it plays towards successful implementation of Quality by Design (QbD), an analysis of KM solutions is needed. This work provides a comprehensive review of the in...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1007/s11095-016-2043-9
更新日期：2017-02-01 00:00:00
abstract：PURPOSE:To investigate the potential of a novel lipid carrier, comprising beads of alpha-cyclodextrin and soybean oil, for topical drug delivery. Adapalene was chosen as a model drug to explore the ability of the beads to encapsulate and release a highly lipophilic compound. MATERIALS AND METHODS:Adapalene-loaded bead...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-007-9395-0
更新日期：2008-02-01 00:00:00
abstract：PURPOSE:To develop a semi-physiological-based model describing simultaneously the time course of immature and mature B-lymphocytes after topotecan (TPT) administration to tumor-bearing rats. METHODS:Twenty-four tumor-bearing BDIX male rats received a single 6 mg/kg intra-peritoneal dose of TPT or saline. Mature and im...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-009-0025-x
更新日期：2010-03-01 00:00:00
abstract：PURPOSE:HSP90 (Heat shock protein 90kD) has been validated as a therapeutic target in Castrate Resistant Prostate Cancer. Unfortunately, HSP90 inhibitors suffer from dose-limiting toxicities that hinder their clinical applications. Previously developed polymeric delivery systems for HSP90 inhibitors had either low drug...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-017-2249-5
更新日期：2017-12-01 00:00:00
abstract：PURPOSE:To determine the different conformations of the acyloxyalkoxy-linked cyclic prodrug 1 of the model hexapeptide 2 in solution and to investigate the relationship between these solution conformations and the cellular permeability characteristics of this prodrug. METHODS:Two-dimensional Homonuclear Hartmann-Hahn ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016484522113
更新日期：1996-11-01 00:00:00
abstract：PURPOSE:To analyze the mechanics of some pharmaceutical agglomerates during uniaxial confined compression by using compression parameters derived from the Heckel, Kawakita and Adams equations, and to study the influence of these compression parameters on the tablet-forming ability of agglomerates. METHODS:Force and di...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1007575120817
更新日期：2000-08-01 00:00:00
abstract：PURPOSE:Modulation of 5-HT3 receptor in the central nervous system (CNS) is a promising approach for treatment of neuropathic pain. The goal was to evaluate the role of P-glycoprotein (Pgp) in limiting exposure of different parts of the CNS to ondansetron (5-HT3 receptor antagonist) using wild-type and genetic knockout...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-020-02929-2
更新日期：2020-09-28 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：: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
更新日期：2010-09-01 00:00:00
abstract：PURPOSE:Fusogenic liposomes (FLs) are unique delivery vehicles capable of introducing their contents directly into the cytoplasm with the aid of envelope glycoproteins of Sendai virus (SeV). The objective of this study was to evaluate the potential of FL to improve the mucosal absorption of insulin from rat intestinal ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-005-9175-7
更新日期：2006-02-01 00:00:00
abstract：PURPOSE:This work describes the synthesis of block co-polymeric micelles, methoxy-poly(ethylene glycol)-poly(D,L-lactide) (mPEG-PLA) to encapsulate Curcumin (CUR), thereby improving the dispersibility and chemical stability of curcumin, prolonging its cellular uptake and enhancing its bioavailability. METHODS:CUR-mPEG...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-015-1830-z
更新日期：2016-04-01 00:00:00
abstract：:Gene delivery systems are designed to control the location of administered therapeutic genes within a patient's body. Successful in vivo gene transfer may require (i) the condensation of plasmid and its protection from nuclease degradation, (ii) cellular interaction and internalization of condensed plasmid, (iii) esca...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1023/a:1012187414126
更新日期：1997-07-01 00:00:00
abstract：PURPOSE:We aimed to assess the fate of β-arteether lipid-based drug delivery systems (AE-LBDDS) in terms of resistance to lipolysis and permeation across intestinal cells. METHODS:AE-LBDDS contained Tween 80 or Cremophor EL as surfactants, ethanol, Maisine 35-1 and vegetable oil. The solubilization behavior of AE was ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1094-4
更新日期：2013-10-01 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：:To evaluate the effects of a neutron activation radiolabeling technique on an enteric-coated multiparticulate formulation of erythromycin, test quantities were produced under industrial pilot scale conditions. The pellets contained the stable isotope erbium oxide (Er-170), which was later converted by neutron activati...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015826229323
更新日期：1990-03-01 00:00:00
abstract：:Various diesters of 9-[(1,3-dihydroxy-2-propoxy)-methyl]guanine (DHPG) were screened in order to identify a derivative with improved oral absorption. The solubilities and dissolution rates decreased with increasing chain length and branching of the ester group. However, the dipropionate ester showed an anomalously fas...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016462801968
更新日期：1987-04-01 00:00:00
abstract：:A sensitive activity assay for high volume evaluation of human renin inhibitory peptides (RIPs) in rat sera (range 2-80 ng/ml) was developed based on the low affinity of RIPs to rat renin and their high affinity to human renin. The utility of this activity assay was tested by measuring concentrations of a human RIP, U...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015883709275
更新日期：1990-04-01 00:00:00
