abstract：:The role of water activity (a(w)), relative humidity (RH) and temperature on the hydration state of theophylline has been investigated. Slurry bridging experiments at controlled water activities, using powder X-ray diffraction (PXRD) and thermogravimetric analysis (TGA) to characterise the solid phase, established tha...

journal_title：International journal of pharmaceutics

authors： Ticehurst MD,Storey RA,Watt C

更新日期：2002-10-24 00:00:00

abstract：:The objective of this study was to investigate the presence of amino acid transporters on the corneal epithelium and to enhance corneal drug absorption through prodrug modification targeted to the amino acid transporters. SIRC was used as a model cell line representing the corneal epithelium. Uptake studies were carri...

journal_title：International journal of pharmaceutics

authors： Balakrishnan A,Jain-Vakkalagadda B,Yang C,Pal D,Mitra AK

更新日期：2002-10-24 00:00:00

abstract：:The optimized formulation of N-4472, N-[2-(3,5-di-tert-butyl-4-hydroxyphenethyl)-4,6-difluorophenyl]-N'-[4-(N-benzylpiperidyl)] urea, which was a poorly water-soluble drug, was developed by utilizing the complexation between N-4472 and L-ascorbic acid (VC). It was found that the formulation with Gelucire((R)) 44/14, H...

journal_title：International journal of pharmaceutics

authors： Itoh K,Matsui S,Tozuka Y,Oguchi T,Yamamoto K

更新日期：2002-10-10 00:00:00

abstract：:The potential of gels formed in situ by dilute aqueous solutions of a xyloglucan polysaccharide derived from tamarind seed as sustained release vehicles for percutaneous administration of non-steroidal anti-inflammatory drugs has been assessed by in vitro and in vivo studies. Chilled aqueous solutions of xyloglucan th...

journal_title：International journal of pharmaceutics

authors： Takahashi A,Suzuki S,Kawasaki N,Kubo W,Miyazaki S,Loebenberg R,Bachynsky J,Attwood D

更新日期：2002-10-10 00:00:00

abstract：:An investigation was carried out to determine the behavior of moisture gain by four anti-tuberculosis drugs, viz. rifampicin, isoniazid, pyrazinamide and ethambutol, when exposed in pure form and in combinations to accelerated conditions of 40 degrees C and 75% RH, in the absence and the presence of light. Weight gain...

journal_title：International journal of pharmaceutics

authors： Singh S,Bhutani H,Mariappan TT,Kaur H,Bajaj M,Pakhale S

更新日期：2002-10-01 00:00:00

abstract：:This study explores the potential of the monoglyceride monocaprin as an enhancer of the epithelial permeability of the beta(3)-adrenoceptor agonist BTA-243, as an approach to improving the bioavailability of this drug. The permeabilities of BTA-243 and mannitol (paracellular marker) in Caco-2 cell monolayer and everte...

journal_title：International journal of pharmaceutics

authors： Brown JR,Collett JH,Attwood D,Ley RW,Sims EE

更新日期：2002-10-01 00:00:00

abstract：:The purpose of the present study was to investigate the effect of secondary structure of three model polypeptides on their apparent permeability (P(app)) across a synthetic, microporous membrane. Poly-L-lysine (PL), poly-L-glutamate (PGlu), and poly-L-lysine-L-phenylalanine (1:1) (PLP) were selected because a solution...

journal_title：International journal of pharmaceutics

authors： Salamat-Miller N,Chittchang M,Mitra AK,Johnston TP

更新日期：2002-09-05 00:00:00

abstract：:Nanoparticles formulated from biodegradable polymers such as poly (lactic acid) and poly (D,L-lactide-co-glycolide) (PLGA) are being extensively investigated as non-viral gene delivery systems due to their sustained release characteristics and biocompatibility. PLGA nanoparticles for DNA delivery are mainly formulated...

journal_title：International journal of pharmaceutics

authors： Prabha S,Zhou WZ,Panyam J,Labhasetwar V

更新日期：2002-09-05 00:00:00

abstract：:The aim of the present work was to evaluate the effect of sustained release of potassium chloride semi-solid matrices prepared with different kinds and added amounts of Gelucires by the in vitro dissolution test and in vivo oral absorption study, and compared with a commercial product (slow-K). The results indicating ...

journal_title：International journal of pharmaceutics

authors： Wu PC,Tsai MJ,Huang YB,Chang JS,Tsai YH

更新日期：2002-08-28 00:00:00

abstract：:Amorphous nanoparticle suspensions of a poorly water-soluble drug, cyclosporine A, are produced by a new process, evaporative precipitation into aqueous solution (EPAS). The rapid evaporation of a heated organic solution of the drug, which is atomized into an aqueous solution, results in fast nucleation leading to nan...

journal_title：International journal of pharmaceutics

authors： Chen X,Young TJ,Sarkari M,Williams RO 3rd,Johnston KP

更新日期：2002-08-21 00:00:00

abstract：:Spray-freezing into liquid (SFL) is a novel particle engineering technology where a feed solution containing an active pharmaceutical ingredient (API) and pharmaceutical excipient(s) is atomized beneath the surface of a cryogenic liquid, such as liquid nitrogen. Intense atomization results from the impingement that oc...

journal_title：International journal of pharmaceutics

authors： Rogers TL,Hu J,Yu Z,Johnston KP,Williams RO 3rd

更新日期：2002-08-21 00:00:00

abstract：:This study proposed a method to understand the surfactant role in the first step of the formulation of a novel generation of lipidic nanocapsules. A dynamic rheological protocol was applied using a pendant drop tensiometer in order to determine the interfacial properties of the initial mixture implied in the first for...

journal_title：International journal of pharmaceutics

authors： Heurtault B,Saulnier P,Pech B,Proust JE,Benoît JP

更新日期：2002-08-21 00:00:00

abstract：:A novel method to include poorly water-soluble substances into the polyelectrolyte capsules of defined size, stability, composition and affinity properties is proposed. Encapsulation explores the polarity gradient across the capsule wall. Capsules creation makes use of electrostatic interaction and can involve many su...

journal_title：International journal of pharmaceutics

authors： Radtchenko I,Sukhorukov G,Möhwald H

更新日期：2002-08-21 00:00:00

abstract：:In order to protect protein and peptide drugs against inactivation by different barriers in the gastro-intestinal tract and to improve their absorption, alginate microparticles as a carrier of L-lactate dehydrogenase, were developed by spray-drying technique. However, alginate complexation and spray-drying conditions ...

journal_title：International journal of pharmaceutics

authors： Coppi G,Iannuccelli V,Bernabei M,Cameroni R

更新日期：2002-08-21 00:00:00

abstract：:The sublingual administration of nifedipine (NIF) is currently used in clinical practice. The sublingual administration of NIF solid dispersions (SD), by using a suitable dispenser, appears an interesting approach in the treatment of moderate and severe hypertensive emergencies. With this aim nine SD made of NIF and a...

journal_title：International journal of pharmaceutics

authors： Cilurzo F,Minghetti P,Casiraghi A,Montanari L

更新日期：2002-08-21 00:00:00

abstract：:Marinosomes are liposomes based on a natural marine lipid extract containing a high polyunsaturated fatty acid (PUFA) ratio. They were prepared and characterized in conditions that mimic that of topical application in terms of pH, temperature and calcium. Marinosomes were stable in storage conditions for 1 month. At l...

journal_title：International journal of pharmaceutics

authors： Moussaoui N,Cansell M,Denizot A

更新日期：2002-08-21 00:00:00

abstract：:Supra Molecular Biovectors (SMBV) are nanoparticles composed by a polysaccharidic core surrounded by a lipid bilayer. They are designed for drug delivery and vaccine and can be administrated by nasal route. The association rate and the stability of association between active principle (AP) or antigens (Ag) with SMBV c...

journal_title：International journal of pharmaceutics

authors： Siguier JP,Major M,Balland O

更新日期：2002-08-21 00:00:00

abstract：:The kinetics of fenoprofen release from poly[alpha,beta-(N-2-hydroxyethyl-DL-aspartamide)]-fenoprofen conjugate (PHEA-Fen) in aqueous buffer solutions (pH 10 and 1.1), simulated gastric (SGF) and intestinal fluids (SIF) was studied. In borate buffer pH 10, the following rate constants were obtained: k=0.2659 (t=60 deg...

journal_title：International journal of pharmaceutics

authors： van der Merwe T,Boneschans B,Zorc B,Breytenbach J,Zovko M

更新日期：2002-07-25 00:00:00

abstract：:The purpose of this study was to optimize in vitro experimental conditions for the measurement of Delta(9)-tetrahydrocannabinol (Delta(9)-THC) permeation across human skin using a flow-through diffusion cell system. The drug permeation rates through intact and stripped (stratum corneum (SC) removed) skin were also com...

journal_title：International journal of pharmaceutics

authors： Challapalli PV,Stinchcomb AL

更新日期：2002-07-25 00:00:00

abstract：:The purpose of this study was to develop Pluronic F127 (PF127) based formulations of timolol maleate (TM) aimed at enhancing its ocular bioavailability. The effect of isotonicity agents and PF127 concentrations on the rheological properties of the prepared formulations was examined. In an attempt to reduce the concent...

journal_title：International journal of pharmaceutics

authors： El-Kamel AH

更新日期：2002-07-08 00:00:00

abstract：:Spherical hydroxyapatite cores were prepared by using carboxylic acid terminated half-generation poly(amidoamine) (PAMAM) dendrimer as templates or crystal modifiers. The hydroxyapatite cores were characterized by infrared spectroscopy (IR), X-ray diffraction (XRD) and transmission electron microscopy (TEM). The spher...

journal_title：International journal of pharmaceutics

authors： Khopade AJ,Khopade S,Jain NK

更新日期：2002-07-08 00:00:00

abstract：:The use of non-linear mixed effects models to describe dissolution data has been evaluated. A theoretical part is included to introduce this approach to scientists who are not familiar with this type of statistics. The standard settings of the statistical software package (S-plus) are used as much as possible. Several...

journal_title：International journal of pharmaceutics

authors： Adams E,Coomans D,Smeyers-Verbeke J,Massart DL

更新日期：2002-06-20 00:00:00

abstract：:The gel forming characteristics of alginate in the presence of calcium ions and further crosslinking with poly-L-lysine led to the formation of sponge-like nano- and microparticles. The particle size was varied by adjusting the final concentrations of and proportions between the components. The region for particle for...

journal_title：International journal of pharmaceutics

authors： González Ferreiro M,Tillman L,Hardee G,Bodmeier R

更新日期：2002-06-04 00:00:00

abstract：:A new chemical entity (NCE) was evaluated in the Clickhaler (Innovata Biomed Ltd.) dry powder inhaler, a reservoir-based multidose delivery system. The standard device metering system was modified to handle higher doses (nominally 20 mm(3) of lactose based blend). The micronized drug was formulated at 12.5% w/w in lac...

journal_title：International journal of pharmaceutics

authors： Thibert R,Parry-Billings M,Shott M

更新日期：2002-06-04 00:00:00

abstract：:Chitosan (CH) was dissolved in aqueous solutions containing aspartic, glutamic, hydrochloric, lactic and citric acids to obtain different chitosan salts. Chitosan salts were collected from the solutions by spray-drying and the powders obtained were mixed with Sodium Diclofenac (SD), taken as a model anti-inflammatory ...

journal_title：International journal of pharmaceutics

authors： Orienti I,Cerchiara T,Luppi B,Bigucci F,Zuccari G,Zecchi V

更新日期：2002-05-15 00:00:00

abstract：:The buccal administration of ergotamine tartrate (ET) combined with polyvinyl alcohol (PVA) gel brought about higher plasma concentration of ET compared with that of oral administration of capsules in guinea-pigs. T(max) of ET in plasma of buccal administration was significantly smaller than that of oral administratio...

journal_title：International journal of pharmaceutics

authors： Tsutsumi K,Obata Y,Nagai T,Loftsson T,Takayama K

更新日期：2002-05-15 00:00:00

abstract：:From the viewpoint of effective utilization of natural resources and development of new pharmaceutical materials, acid-treated yeast cell wall (AYC) was prepared via a novel approach involving acidification of brewers' yeast cell wall. AYC aqueous dispersion containing 5% (w/v) AYC and 0.5% (w/v) glycerol was prepared...

journal_title：International journal of pharmaceutics

authors： Yuasa H,Kaneshige J,Ozeki T,Kasai T,Eguchi T,Ishiwaki N

更新日期：2002-04-26 00:00:00

abstract：:In vivo drug release from solid lipid nanoparticles (SLN) takes place by diffusion and degradation of the lipid matrix. SLN with different degree of crystallinity were prepared to study the effect of crystallinity on the degradation velocity. These SLN were produced by using glycerides with different length of fatty a...

journal_title：International journal of pharmaceutics

authors： Olbrich C,Kayser O,Müller RH

更新日期：2002-04-26 00:00:00

abstract：:To examine whether the dietary lectin wheat germ agglutinin (WGA) can facilitate binding and uptake of protein drugs due to its cytoadhesive and cytoinvasive properties, conjugates were prepared by covalent coupling of fluorescein-labeled bovine serum albumin (F-BSA) to WGA using divinylsulfone for crosslinking. Incre...

journal_title：International journal of pharmaceutics

authors： Gabor F,Schwarzbauer A,Wirth M

更新日期：2002-04-26 00:00:00

abstract：:The effects of vehicles and penetration enhancers on the in vitro permeation of tenoxicam from saturated solutions through dorsal hairless mouse skin were investigated. Various types of vehicles, including ester-, alcohol-, and ether-types and their mixtures, were used as vehicles, and then a series of fatty acids and...

journal_title：International journal of pharmaceutics

authors： Gwak HS,Chun IK

更新日期：2002-04-02 00:00:00

abstract：:The aims of this study were to develop novel liposome formulations for tranexamic acid (TA) from various lipid compositions [neutral (hydrogenated soya phosphatidylcholine and cholesterol), positive (stearylamine) or negative (dicetyl phosphate) charged lipid], and to investigate the effects of concentrations of TA (5...

journal_title：International journal of pharmaceutics

authors： Manosroi A,Podjanasoonthon K,Manosroi J

更新日期：2002-03-20 00:00:00

abstract：:Isomalt, a sugar alcohol, was melt-extruded prior to compression in order to improve its tabletting properties. After fusion, crystalline isomalt was transformed into an amorphous form as shown by X-ray diffraction and differential scanning calorimetry (DSC). The tabletting properties of amorphous isomalt were dramati...

journal_title：International journal of pharmaceutics

authors： Ndindayino F,Henrist D,Kiekens F,Van den Mooter G,Vervaet C,Remon JP

更新日期：2002-03-20 00:00:00

abstract：:In the present study, the features of two new thiolated polymers--the so-called thiomers--were investigated. Mediated by a carbodiimide cysteamine was covalently attached to sodium carboxymethylcellulose (Na-CMC) and neutralised polycarbophil (Na-PCP). Depending on the weight-ratio polymer to cysteamine during the cou...

journal_title：International journal of pharmaceutics

authors： Kast CE,Bernkop-Schnürch A

更新日期：2002-03-02 00:00:00

abstract：:We developed several kinds of fentanyl-loaded poly(L-lactide-co-glycolide) (PLGA) microspheres (FMS) for sustained release of fentanyl. FMS were prepared by an emulsion solvent-evaporation method. In this study, the influences of several preparation parameters, such as initial drug loading, polymer concentration, and ...

journal_title：International journal of pharmaceutics

authors： Choi HS,Seo SA,Khang G,Rhee JM,Lee HB

更新日期：2002-03-02 00:00:00

abstract：:Endothelium is an important target for drug or gene therapy because of its important role in the biological system. In this paper, we have characterized nanoparticle uptake by endothelial cells in cell culture. Nanoparticles were formulated using poly DL-lactide-co-glycolide polymer containing bovine serum albumin as ...

journal_title：International journal of pharmaceutics

authors： Davda J,Labhasetwar V

更新日期：2002-02-21 00:00:00

abstract：:The purpose of the present study is to prepare chemically and physically stable rhEGF/poloxamer gel and to investigate its possibility of ophthalmic delivery. The rhEGF/HP-beta-CD complex markedly increased rhEGF stability compared with rhEGF solution at 4 degrees C. The poloxamer gel was composed of poloxamer 407 (16...

journal_title：International journal of pharmaceutics

authors： Kim EY,Gao ZG,Park JS,Li H,Han K

更新日期：2002-02-21 00:00:00

abstract：:Topical poultices of ketoprofen were prepared using deionized water, propylene glycol (X1), and glycerin (X2) as the vehicle in combination with hydrophilic matrix materials, including gelatin (X3) and sodium polyacrylate. A mixture design was utilized to evaluate the influence of these constituents (X1-X3) on the adh...

journal_title：International journal of pharmaceutics

authors： Sheu MT,Chen LC,Ho HO

更新日期：2002-02-21 00:00:00

abstract：:The objectives of this work were to develop a liposomal fasudil, an antivasospastic drug, as a possible means to deliver the encapsulated drug to the brain, and to characterize the stability of the liposomal formulation in vitro. Transmembrane electrochemical gradients of H+ or ammonium sulfate were created, and their...

journal_title：International journal of pharmaceutics

authors： Ishida T,Takanashi Y,Doi H,Yamamoto I,Kiwada H

更新日期：2002-01-31 00:00:00

abstract：:The release properties of steroids from a combined contraceptive vaginal ring have been investigated. The product design is based on a coaxial fiber consisting of two types of polyethylene vinylacetate copolymers. Inside the core of the fiber, two steroids are present in a molecularly dissolved state. In order to desi...

journal_title：International journal of pharmaceutics

authors： van Laarhoven JA,Kruft MA,Vromans H

更新日期：2002-01-31 00:00:00

abstract：:The process of systemic absorption and tissue targeting efficacy of salicylate (SA) following intracutaneous (i.c.), subcutaneous (s.c.) and intramuscular (i.m.) injections of its sodium salt in rats were evaluated by determining the drug concentration at the injection site and surrounding tissues. After i.c. and s.c....

journal_title：International journal of pharmaceutics

authors： Yoshida D,Hasegawa T,Sugibayashi K

更新日期：2002-01-14 00:00:00