Tuning the Phytoglycogen Size and Aggregate Structure with Solvent Quality: Influence of Water-Ethanol Mixtures Revealed by X-ray and Light Scattering Techniques.

Phytoglycogen (PG) is a hyperbranched polysaccharide with promising properties for biomedical and pharmaceutical applications. Herein, we explore the size and structure of sweet corn PG nanoparticles and their aggregation in water-ethanol mixtures up to the ethanol mole fraction = 0.364 in dilute concentrations using small-angle X-ray scattering (SAXS) and dynamic light scattering (DLS) measurements.

Preparation and Spectroscopic Characterization of Inclusion Complexes of 3D Ball-Milled Rifampicin with β-cyclodextrin and γ-cyclodextrin : 3D Ball-Milled Rifampicin with β-cyclodextrin and γ-cyclodextrin.

Rifampicin (RFP) solutions, intended to reduce incidence of prosthetic graft infection, were prepared as three-dimensional ground mixtures (3DGMs) using β-cyclodextrin (βCD) and γ-cyclodextrin (γCD) and characterized for their spectroscopic properties and solubility. Phase solubility diagrams revealed that 3DGMs (RFP/βCD and RFP/γCD) produced a complex at 1:1 molar ratio. Pulsed field gradient nuclear magnetic resonance experiments indicated that the diffusion coefficients for RFP/βCD and RFP/γCD were similar to the respective diffusion coefficients for βCD and γCD.

Inclusion Complexes of Daidzein with Cyclodextrin-Based Metal-Organic Framework-1 Enhance Its Solubility and Antioxidant Capacity.

Daidzein, an aglycone-type isoflavone, is useful in the prevention of atherosclerotic cardiovascular diseases. However, the solubility of daidzein remains relatively low even with pharmaceutical interventions (e.g.

Preparation and characterization of triamterene complex with ascorbic acid derivatives.

The purpose of this study was to prepare solid dispersions of triamterene (TRT) with ascorbic acid (AA) or ascorbic acid 2 glucoside (AA2G) and to evaluate their physical properties. Solid dispersions were prepared by dissolving each sample in an organic solvent and evaporation (EVP). Powder X-ray diffraction (PXRD) revealed a halo pattern for EVP1 (AA/TRT = 1/1) and EVP2 (AA2G/TRT = 1/1).

Photochemically stabilized formulation of dacarbazine with reduced production of algogenic photodegradants.

The present study aimed to develop a photochemically stabilized formulation of dacarbazine [5-(3,3-dimethyl-1-triazeno)imidazole-4-carboxamide; DTIC] for reducing the production of algogenic photodegradant (5-diazoimidazole-4-carboxamide; Diazo-IC). Photochemical properties of DTIC were characterized by UV-visible light spectral analysis, reactive oxygen species (ROS) assay, and photostability testing. A pharmacokinetic study was conducted after intravenous administration of DTIC formulations (1 mg-DTIC/kg) to rats.

Photochemical Mechanism of Riboflavin-Induced Degradation of Famotidine and a Suggested Pharmaceutical Strategy for Improving Photostability.

The present study aimed to clarify the mechanism of photodegradation of famotidine with riboflavin (FMT/RF), and to develop a photochemically stabilized formulation of FMT/RF. Photochemical properties of RF were characterized by UV-VIS spectral analysis, reactive oxygen species (ROS) assay, and photostability testing. Pharmacokinetic study was conducted in rats after intravenous administration of FMT (1 mg/kg) formulation containing RF (0.

[Specific variability of teicoplanin protein binding in patients receiving continuous hemodiafiltration-comparison with hypoalbuminemia patients].

Variation in protein binding ratio (PBR) of teicoplanin (TEIC) was investigated in continuous hemodiafiltration (CHDF) patients. TEIC is classified as a high PBR drug (≧90%), and it was reported that the PBR of TEIC decreased with an decrease in the serum albumin level in hypoalbuminemia patients. However, few reports can be found about the variation of PBR of TEIC for CHDF patient.

[Questionnaire survey of air extruded jelly dosage form (I) - oral condition of elder patients and applicability of air extruded jelly formulation - ].

Elderly patients tend to have troubles with oral conditions such as the impairment of deglutition capability (difficulty in swallowing), in addition to a decline in physical performance. An air extruded jelly formulation (AEJF) has been developed as a new formulation consisting of jelly and clean air under increased pressure. As jelly is discharged smoothly by pushing the air portion, elderly patients are able to easily take jelly from the package.

Formulation study on retinoic acid gel composed of iota-carrageenan, polyethylene oxide and Emulgen® 408.

In the present study, all-trans retinoic acid (RA) gels formulated with various compositions of polyethylene oxide (Emulgen®) and iota-carrageenan (ι-CG) were prepared and their physicochemical properties were evaluated. The compression energy, which is the work required to compress the product through a fixed distance, increased with increasing amount of ι-CG or Emulgen®. The adhesion energy and displacement decreased with increasing amount of ι-CG or Emulgen® due to the progression of gel formation.

Molecular states of p-dimethylaminobenzonitrile coground with β-cyclodextrin investigated using solid-state fluorescence spectroscopy.

Changes in molecular states of p-dimethylaminobenzonitrile (DMABN) coground with β-cyclodextrin (β-CD) were examined using solid-state fluorescence measurements. Formation of a DMABN/β-CD inclusion complex by coprecipitation was confirmed by powder X-ray diffraction measurement. The powder X-ray diffraction pattern of the ground mixture was a halo pattern and differed from the pattern of the mixture prepared by coprecipitation.

Guest molecular size-dependent inclusion complexation of parabens with cholic acid by cogrinding.

Effects of p-hydroxybenzoate (paraben) ester chain length on the stoichiometry and structure of grinding-induced inclusion complexes with cholic acid (CA) were investigated. Physicochemical properties of the ground mixture were evaluated by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), Fourier transform infrared (FT-IR) spectroscopy, and solid-state nuclear magnetic resonance (NMR) measurements. Ethyl-, n-propyl-, and isopropyl-parabens formed equimolar inclusion complexes with CA, and the complex structures were of the β-trans bilayer type.

Development of sarpogrelate external preparation for intractable pain control. I. Pre-formulation study on application of modified beta-cyclodextrins.

To optimize the formulation of in-hospital sarpogrelate (SPG) preparation for external use, various cyclodextrins (CDs) were investigated for their ability to improve the aqueous solubility and chemical stability of SPG. Although hydrolysis of SPG was markedly accelerated at above pH 7.0 in aqueous solution, the addition of modified beta-CD resulted in suppressed SPG hydrolysis.

Participation of pharmacist CRC in practical on-site training--a survey by questionnaires for pharmacy students.

In order to estimate the 4th grade-students' knowledge regarding clinical trials, we carried out the questionnaire survey to the students being about to take practice in hospitals, and could collect answers from 163 students. This survey revealed that about 25% of the students could not draw the difference between "clinical trial" and "clinical research". As for the question about the technical terms regarding the clinical trial, clear correlation between students' learning experience and their knowledge was suggested.

[Solid states fluorescence study of p-dimethylaminobenzonitrile by co-grinding with cyclodextrins].

The molecular status of a freeze-dried sample or a ground mixture of p-dimethylaminobenzonitrile (DMABN) with alpha-, beta-, or gamma-cyclodextrins (CDs) was examined using solid-state fluorescence measurements. A twisted intramolecular charge transfer (TICT) emission of DMABN crystals was shown at 475 nm. Emission peaks of freeze-dried samples were observed at 450, 380, and 393 nm in alpha-CD/DMABN, beta-CD/DMABN, and gamma-CD/DMABN systems, respectively.

Formulation study of intravesical oxybutynin instillation solution with enhanced retention in bladder.

A formulation study of intravesical oxybutynin (OB) preparations was carried out in order to improve the effectiveness in intravesical instillation therapy for spastic neurogenetic bladder. Sodium hyaluronate (HYA) was introduced to enhance the muco-adhesiveness of the instillation preparation, and the physicochemical properties of the OB formulation were evaluated in comparison with a conventional formulation containing hydroxypropylcellulose (HPC). The viscous properties and in vitro adhesiveness increased with the amount of the polymeric additives, and retention properties of OB in rabbit bladder were comparable after addition of 0.

[Evidence-based quality management of clinical formulations: determination of expiration date of powdered medicine prepared by grinding tablets].

Beraprost sodium (BPS) is often used for pediatric patients with pulmonary hypertension. The purpose of this study was to determine the expiration date of the powdered medicine prepared by grinding tablets. In the present study, the hygroscopicity and stability of the beraprost tablet (DORNER tablet), ground Dorner tablet and powder formulation (Dorner powder) consisting of the ground DORNER tablet and lactose (EFC lactose) were investigated after storage at various relative humidities (RHs) and light exposures.

Preparation of drug nanoparticles by co-grinding with cyclodextrin: formation mechanism and factors affecting nanoparticle formation.

The aim of this study was to investigate the factors affecting the formation of pranlukast nanoparticle prepared by co-grinding with beta-cyclodextrin (beta-CD) and to elucidate the mechanism of nanoparticle formation. The effects of grinding time, moisture content and CD content on the nanoparticle formation were evaluated by means of UV quantitative determination and particle size analysis. High-resolution scanning electron microscopy (HRSEM) was employed to observe drug nanoparticles in the ground mixture.

Specific inclusion mode of guest compounds in the amylose complex analyzed by solid state NMR spectroscopy.

The inclusion compound formation between linear amylose of molecular weight 102500 (AS100) and p-aminobenzoic acid (PA) during the sealed-heating process was investigated by powder X-ray diffractometry, infrared spectroscopy and solid state NMR spectroscopy. Sealed-heating of AS100 and PA at 100 degrees C for 6 h provided an inclusion compound with 6(1)-helix structure, while a 7(1)-helix structure was found when sealed-heating was carried out at 150 degrees C for 1 h. The formation of an inclusion compound was not observed when sealed-heating was performed at 50 degrees C for 6 h.

Solid-state fluorescence study of naphthalene adsorption on porous material.

Naphthalene adsorption profile on porous materials was studied using solid-state fluorescence spectroscopy. When naphthalene crystals were simply mixed with porous crystalline cellulose (PCC), excimer emission of naphthalene was observed after 1 min of mixing, suggesting a drastic change in the naphthalene molecular environment during the mixing procedure. For the naphthalene-octadesyl silane (ODS)-80A or naphthalene-ODS-2 systems, the changes in adsorption profiles and fluorescence spectral pattern of naphthalene were similar to those of the naphthalene-PCC system.

Micronization of phenylbutazone by rapid expansion of supercritical CO2 solution.

Rapid expansion of supercritical solutions (RESS) technique was applied for the preparation of phenylbutazone fine particles. The operating temperature and pressure affected the yield of the drug fine particles, which was evaluated by dissolving the sprayed product of drug into ethanol. Effect of pre- and post-expansion conditions on the particle size distribution of phenylbutazone was investigated and the smallest sample (mean particle size: 1.

Rapid adsorption and entrapment of benzoic acid molecules onto mesoporous silica (FSM-16).

Changes in the molecular state of benzoic acid (BA) in the presence of folded sheet mesoporous material (FSM-16), which has uniformly sized cylindrical mesopores and a large surface area, were assessed with several analyses. When BA was blended with FSM-16 for 5 min (BA content=30%), the X-ray diffraction peaks of BA crystals disappeared, suggesting an amorphous state. Fluorescence analysis of the mixture showed a new fluorescence emission peak for BA at 386 nm after mixing with FSM-16.

Release behavior of diethylhexyl phthalate from the polyvinyl-chloride tubing used for intravenous administration and the plasticized PVC membrane.

The release behavior of diethylhexyl phthalate (DEHP) from polyvinyl-chloride (PVC) tubing, which composes materials in an intravenous administration set, was investigated using polysorbate 80 (Tween 80) aqueous solutions. When Tween 80 solution was circulated in PVC tubing, the amount of DEHP released increased with increasing circulation velocity and temperature. In order to clarify the effect of temperature on the release behavior of DEHP, PVC films containing varying amounts of DEHP were mounted on a cylindrical shaft and rotated at 5 and 40 degrees C.

Water vapor adsorption behavior of sodium deoxycholate anhydrous forms.

Pseudopolymorphism of sodium deoxycholate (NaDC) was investigated. Intact NaDC (dihydrate) was dried at 60 degrees C under reduced pressure resulting an anhydrous amorphous phase. On the other hand, intact NaDC was altered to an anhydrous crystalline form by heating at 200 degrees C.

Influence of dehydration temperature on water vapor adsorption, dissolution behavior and surface property of ampicillin.

Several specimens of anhydrous ampicillin were prepared by heating the ampicillin trihydrate at 100, 120, 140 and 160 degrees C. The effects of dehydration temperature on water vapor adsorption, dissolution behavior and surface property were investigated. The water vapor adsorption of anhydrous ampicillin was studied at 89% relative humidity, 40 degrees C and the water vapor adsorption rate was found to decrease with increase of dehydration temperature.