Physicochemical, crystallographic, thermal, and spectroscopic behavior of crystalline and X-ray amorphous ciclesonide.

Abstract:

:Single crystal structure experiments revealed that the orthorhombic needles of Ciclesonide crystallized in P2(1)2(1)2(1) space group with four independent molecules in the unit cell. Amorphous Ciclesonide was prepared by lyophilization and characterized in comparison with crystalline material by differential scanning calorimetry (DSC), Fourier transformed (FT)-Raman spectroscopy, powder X-ray diffraction, dissolution, and saturation solubility experiments. Significant differences in the dissolution, thermal, and spectrometric behavior were observed for both solid-state phases. DSC- and FT-Raman methods for the determination of amorphous content in crystalline Ciclesonide samples were established. Isothermal and dynamical recrystallization studies on amorphous Ciclesonide were conducted using dispersive hot-stage Raman microscopy. The recrystallization was observed to be a two-step process with an induction period (most likely nuclei formation) followed by the actual recrystallization (crystal growth). The recrystallization rate constants and Avrami exponents (n = 2) were determined from the isothermal experiments at various temperatures using Johnson-Mehl-Avrami theory. Isothermal activation energies were obtained from Arrhenius plots using the temperature dependence of (a) the rate constants (160.4 kJ/mol) and (b) the induction time (140.9 kJ/mol) of the isothermal hot-stage experiments.

journal_name

J Pharm Sci

authors

Feth MP,Volz J,Hess U,Sturm E,Hummel RP

doi

10.1002/jps.21223

subject

Has Abstract

pub_date

2008-09-01 00:00:00

pages

3765-80

issue

9

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(16)32707-1

journal_volume

97

pub_type

杂志文章
  • Optimal Dosing Regimen of Phenytoin for Korean Epilepsy Patients: From Premature Babies to the Elderly.

    abstract::Phenytoin has been decreasingly used because of the high interindividual variability in drug concentration and the narrow therapeutic window. Despite such drawbacks, phenytoin is still essential as a second-line therapy for status epilepticus when patients are resistant to benzodiazepines. This study aimed to develop ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2019.03.022

    authors: Guk J,Lee SG,Chae D,Kim JH,Park K

    更新日期:2019-08-01 00:00:00

  • In vivo evaluation of controlled-release products.

    abstract::A theoretical investigation has been conducted to understand the deconvolution method used for evaluating the in vivo release rate of an oral controlled-release product from the plasma drug concentration versus time profile. The theory is based on well-accepted pharmacokinetic compartmental models. The cumulative amou...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600821116

    authors: Hwang SS,Bayne W,Theeuwes F

    更新日期:1993-11-01 00:00:00

  • Pharmacokinetics of transdermal drug delivery.

    abstract::The pharmacokinetics of drug delivery from transdermal controlled-release devices consisting of (a) a membrane plus a reservoir or (b) a monolithic slab are examined. For the period when the devices act as if the drug reservoir were infinite, simple relationships for the steady-state slope and time lag are derived and...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600740704

    authors: Berner B

    更新日期:1985-07-01 00:00:00

  • Extreme sensitivity of botulinum neurotoxin domains towards mild agitation.

    abstract::Botulinum neurotoxins (BoNTs) and their fragments are targets of therapeutic developments and are increasingly used as therapeutic, prophylactic, and research reagents. However, published data on their properties vary widely. In order to gain a better understanding of these variations, we initiated a systematic invest...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21676

    authors: Toth SI,Smith LA,Ahmed SA

    更新日期:2009-09-01 00:00:00

  • Evaluation of degradation pathways for plasmid DNA in pharmaceutical formulations via accelerated stability studies.

    abstract::The stability of highly purified supercoiled plasmid DNA formulated in simple phosphate or Tris-buffered saline solutions has been characterized to establish the overall degradation processes that occur during storage in aqueous solution. Plasmid DNA stability was monitored during accelerated stability studies (at 50 ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/(SICI)1520-6017(200001)89:1<76::AID-JPS8>3

    authors: Evans RK,Xu Z,Bohannon KE,Wang B,Bruner MW,Volkin DB

    更新日期:2000-01-01 00:00:00

  • Zinc(II) in saliva: determination of concentrations produced by different formulations of zinc gluconate lozenges containing common excipients.

    abstract::A study of the pH of saliva produced by humans sucking hard candy lozenges containing zinc gluconate and citric acid demonstrated the probability that the formulation delivered an insignificant amount of the contained zinc as Zn2+. This could account for the negative results of several clinical studies of this lozenge...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600810205

    authors: Zarembo JE,Godfrey JC,Godfrey NJ

    更新日期:1992-02-01 00:00:00

  • Assay and disposition of carvedilol enantiomers in humans and monkeys: evidence of stereoselective presystemic metabolism.

    abstract::Carvedilol is a new beta-blocking agent with vasodilating activities, which is a racemic mixture of R(+)- and S(-)-enantiomers. Since the two enantiomers differ in pharmacological properties, it is necessary to individually measure their plasma concentrations in order to evaluate the pharmacological effects of racemic...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600790704

    authors: Fujimaki M,Murakoshi Y,Hakusui H

    更新日期:1990-07-01 00:00:00

  • Developability index: a rapid in silico tool for the screening of antibody aggregation propensity.

    abstract::Determining the aggregation propensity of protein-based biotherapeutics is an important step in the drug development process. Typically, a great deal of data collected over a large period of time is needed to estimate the aggregation propensity of biotherapeutics. Thus, candidates cannot be screened early on for aggre...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22758

    authors: Lauer TM,Agrawal NJ,Chennamsetty N,Egodage K,Helk B,Trout BL

    更新日期:2012-01-01 00:00:00

  • Application of neural networks to pharmacodynamics.

    abstract::Neural networks (NN) are computational systems implemented in software or hardware that attempt to simulate the neurological processing abilities of biological systems. A synopsis is presented of the operational characteristics, structures, and applications of NN. The NN technology has primarily been aimed at recognit...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600820910

    authors: Veng-Pedersen P,Modi NB

    更新日期:1993-09-01 00:00:00

  • Properties and stability of a liquid crystal form of cyclosporine-the first reported naturally occurring peptide that exists as a thermotropic liquid crystal.

    abstract::A new solid-state form of cyclosporine produced by spray-drying exhibited characteristics consistent with a liquid crystal. No sharp diffraction peaks were observed by powder X-ray diffraction; however, analysis by both small-angle X-ray diffraction (SAXR) and microscopic under polarized light (PLM) confirmed the exis...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.10444

    authors: Lechuga-Ballesteros D,Abdul-Fattah A,Stevenson CL,Bennett DB

    更新日期:2003-09-01 00:00:00

  • Chloride ion nuclear magnetic resonance spectroscopy probe studies of copper and nickel binding to serum albumins.

    abstract::The binding of Cu2+ and Ni2+ to bovine, dog, and human serum albumin has been studied by the 35Cl NMR probe technique. The number of primary copper sites were estimated to be 1.3 for human serum albumin, 3.1 for bovine serum albumin, and 6.6 for dog serum albumin. A similar number of primary nickel sites was determine...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600740116

    authors: Mohanakrishnan P,Chignell CF,Cox RH

    更新日期:1985-01-01 00:00:00

  • Analysis and prediction of partition coefficients of meta- and para-disubstituted benzenes in terms of substituent effects.

    abstract::The hydrophobic substituent parameter for a system of meta- and para-disubstituted benzenes, XC6H4Y, defined as pi X/PhY = log PXC6H4Y - log PC6H5Y, where P is the octanol-water partition coefficient and X and Y are variable and fixed substituents, respectively, varies from one system to another, according to the vari...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600720319

    authors: Fujita T

    更新日期:1983-03-01 00:00:00

  • Nanoparticle formation of organic compounds with retained biological activity.

    abstract::Many pharmaceuticals are formulated as powders to aid drug delivery. A major problem is how to produce powders having high purity, controlled morphology, and retained bioactivity. We demonstrate the use of supercritical carbon dioxide as an antisolvent for meeting this need for two model drug systems, quercetin, a spa...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22035

    authors: Jacobson GB,Shinde R,McCullough RL,Cheng NJ,Creasman A,Beyene A,Hickerson RP,Quan C,Turner C,Kaspar RL,Contag CH,Zare RN

    更新日期:2010-06-01 00:00:00

  • "Predicting" Polymorphs of Pharmaceuticals Using Hydrogen Bond Propensities: Probenecid and Its Two Single-Crystal-to-Single-Crystal Phase Transitions.

    abstract::The recently developed hydrogen-bonding propensity tool in the Cambridge Structural Database software package (Mercury) was tested to predict polymorphs. The compounds for the study were chosen from a list of approximately 300 pharmaceutically important compounds, for which multiple crystal forms had not been previous...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.24449

    authors: Nauha E,Bernstein J

    更新日期:2015-06-01 00:00:00

  • Interaction of L-tryptophan with alpha-cyclodextrin: studies with calorimetry and proton nuclear magnetic resonance spectroscopy.

    abstract::The interaction of L-tryptophan with alpha-cyclodextrin was investigated in a 0.1 M phosphate buffer at pH 7.4 with a LKB 2277 microcalorimeter, using flow mixed mode at 25 degrees C. The thermodynamic parameters for inclusion complex formation obtained are as follows; DeltaG(0) = - 7.03 kJ/mol (K = 17.0), DeltaH(0) =...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/1520-6017(200102)90:2<134::aid-jps4>3.0.co

    authors: Nishijo J,Tsuchitani M

    更新日期:2001-02-01 00:00:00

  • Buccal drug absorption. II: In vitro diffusion across the hamster cheek pouch.

    abstract::The in vitro diffusion of a series of substituted acetanilides across the hamster cheek pouch was studied. The keratinized epithelial layer of the cheek pouch appeared to provide the major barrier to diffusion of these compounds. Linear relationships were found for plots of log epithelial permeability (Pe) versus the ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600780218

    authors: Garren KW,Repta AJ

    更新日期:1989-02-01 00:00:00

  • Prostaglandin prodrugs VI: structure-thermodynamic activity and structure-aqueous solubility relationships.

    abstract::Solubilities in isoctane and water were determined for several C1-phenolic esters of prostaglandin F2 alpha and prostaglandin E2 and acetates having the same phenol moiety. Linear free energy relationships for solubility among the series were observed with slopes of approximately 1. These results suggest that the cont...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600690417

    authors: Anderson BD,Conradi RA

    更新日期:1980-04-01 00:00:00

  • Drug diffusion through cystic fibrotic mucus: steady-state permeation, rheologic properties, and glycoprotein morphology.

    abstract::One manifestation of cystic fibrosis (CF) is the presence of a viscid mucus secretion in the lungs. The clearance of this mucus is significantly slower than in "normals" due to uncoordinated beating of the cilia and the increased viscosity of the mucus. In these studies, the permeabilities of p-aminosalicylic acid, is...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js950381s

    authors: Bhat PG,Flanagan DR,Donovan MD

    更新日期:1996-06-01 00:00:00

  • Myocardial effect compartment modeling of metoprolol and sotalol: importance of myocardial subsite drug concentration.

    abstract::We have recently reported the time course of acute myocardial drug uptake and simultaneous pharmacodynamic effects for metoprolol (4 mg; n = 12) and sotalol (20 mg; n = 10) in patients with ischemic heart disease. The acute pharmacodynamic effects of the two drugs included reductions in both spontaneous heart rate and...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 临床试验,杂志文章

    doi:10.1021/js9702776

    authors: Ritchie RH,Morgan DJ,Horowitz JD

    更新日期:1998-02-01 00:00:00

  • Preparation and characterization of quercetin nanocrystals.

    abstract::This study is to enhance the dissolution rate of a poorly water-soluble drug, quercetin, by fabricating nanocrystals using high-pressure homogenization. The particle size, crystallinity, dissolution, and antioxidant effects of fabricated quercetin nanocrystals have been investigated. Characterization of the original q...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22446

    authors: Sahoo NG,Kakran M,Shaal LA,Li L,Müller RH,Pal M,Tan LP

    更新日期:2011-06-01 00:00:00

  • Compressibility of anhydrous tricalcium phosphate.

    abstract::It is shown that tricalcium phosphate follows a simple Heckel relationship in pressures of usual tablet compression, only if a density of 1.92 g/mL is used. This coincides with the density obtained by wet pycnometry, whereas the crystallographical density is 3.1 g/mL. The interpretation is that some of the pore space ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600740419

    authors: Hou XP,Carstensen JT

    更新日期:1985-04-01 00:00:00

  • A mechanistic study of griseofulvin dissolution into surfactant solutions under laminar flow conditions.

    abstract::The in vivo dissolution of many poorly soluble drugs is enhanced by the action of surfactants secreted into the upper gastrointestinal (GI) tract. These substances may act by solubilizing individual drug molecules into two separate liquid phases: the free aqueous phase and a micellar phase in which the drug is incorpo...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js9604974

    authors: Rao VM,Lin M,Larive CK,Southard MZ

    更新日期:1997-10-01 00:00:00

  • Slow motion picture of protein inactivation during single-droplet drying: a study of inactivation kinetics of L-glutamate dehydrogenase dried in an acoustic levitator.

    abstract::A novel technique is presented to allow measurement of the kinetics of protein inactivation during drying of an acoustically levitated single droplet. Droplets/particles are removed from the acoustic field after various times during drying, and the state of the protein within them is analyzed. The influence of drying ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23129

    authors: Lorenzen E,Lee G

    更新日期:2012-06-01 00:00:00

  • Formation of insoluble particulates in a spray-dried F(ab')(2) fragment.

    abstract::An F(ab')2 fragment of an IgG has been spray-dried on a bench-top machine to examine the presence of insoluble particulates in the redissolved powder product. Preliminary experiments showed that treatment of the F(ab')2 in aqueous solution in a water bath at 65°C for 1 h produced fragmentation and also insoluble parti...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23891

    authors: Lassner P,Adler M,Lee G

    更新日期:2014-04-01 00:00:00

  • Drug release from hydrophilic matrices. 2. A mathematical model based on the polymer disentanglement concentration and the diffusion layer.

    abstract::A comprehensive model is developed to describe the swelling/dissolution behaviors and drug release from hydrophilic matrices. The major thrust of this model is to employ an important physical property of the polymer, the polymer disentanglement concentration, rho p,dis, the polymer concentration below which polymer ch...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600841214

    authors: Ju RT,Nixon PR,Patel MV,Tong DM

    更新日期:1995-12-01 00:00:00

  • Stabilization of proteins by recombinant human gelatins.

    abstract::Porcine gelatins have been widely used as stabilizers of macromolecular based pharmaceuticals but the mechanism by which they stabilize has not been precisely established. Their variability and immunogenicity, however, make them less than ideal excipients. In this work, we take advantage of the availability of recombi...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20980

    authors: Thyagarajapuram N,Olsen D,Middaugh CR

    更新日期:2007-12-01 00:00:00

  • Preparation and characterization of a customized cellulose acetate butyrate dispersion for controlled drug delivery.

    abstract::The purpose of the present experiment was to prepare and characterize the aqueous-based pseudolatex system of cellulose acetate butyrate (CAB) for controlled drug delivery. Aqueous pseudolatex systems are advantageous over organic-based coating systems because these systems are devoid of criteria pollutants such as ca...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.10155

    authors: Vaithiyalingam S,Nutan M,Reddy I,Khan M

    更新日期:2002-06-01 00:00:00

  • Dosing Recommendations Based on Population Pharmacokinetics of Lamotrigine in Mexican Adult Patients With Epilepsy.

    abstract::Dose individualization is essential in epilepsy treatment, especially in antiepileptic drugs that present high interindividual variability such as lamotrigine. We aimed an observational study to develop a population pharmacokinetic model for quantitative evaluation of the factors that influence lamotrigine pharmacokin...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2020.05.030

    authors: Chávez-Castillo CE,Medellín-Garibay SE,Milán-Segovia RDC,Rodríguez-Leyva I,Romano-Moreno S

    更新日期:2020-09-01 00:00:00

  • Alginate-Based Delivery Systems for Bevacizumab Local Therapy: In Vitro Structural Features and Release Properties.

    abstract::Alginate-based polyelectrolyte complexes (PECs) and hydrogel were engineered as platforms for local bevacizumab (BVZ) therapy. This study provides deep comprehension on the microstructures of such systems, and their correlation with drug-release patterns. PECs and hydrogel were characterized using Fourier transform in...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2018.11.038

    authors: Ferreira NN,Caetano BL,Boni FI,Sousa F,Magnani M,Sarmento B,Ferreira Cury BS,Daflon Gremião MP

    更新日期:2019-04-01 00:00:00

  • Oral apomorphine delivery from solid lipid nanoparticles with different monostearate emulsifiers: pharmacokinetic and behavioral evaluations.

    abstract::Apomorphine, a dopamine receptor agonist for treating Parkinson's disease, has very poor oral bioavailability (<2%) due to the first-pass effect. The aim of this work was to investigate whether the oral bioavailability and brain regional distribution of apomorphine could be improved by utilizing solid lipid nanopartic...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22285

    authors: Tsai MJ,Huang YB,Wu PC,Fu YS,Kao YR,Fang JY,Tsai YH

    更新日期:2011-02-01 00:00:00