abstract：:Our research on topical application of lidocaine-loaded non-ionic surfactant vesicles (NSVs) was prompted by the great interest on new delivery systems for local anaesthetics. This study is focused on a novel formulation of NSVs entrapping lidocaine in the form of a free base (LID) and a hydrochloride (LIDHCl). NSVs w...

journal_title：International journal of pharmaceutics

authors： Carafa M,Santucci E,Lucania G

更新日期：2002-01-01 00:00:00

abstract：:Poloxamer-407 (P-407) is a nonionic surfactant that induces atheroma formation in the aortas of C57BL/6 mice with long-term (14 weeks) administration. The objectives of the present study were to determine the mechanism(s) responsible for the induction of hypercholesterolemia as well as to determine whether this animal...

journal_title：International journal of pharmaceutics

authors： Johnston TP,Nguyen LB,Chu WA,Shefer S

更新日期：2001-10-23 00:00:00

abstract：:The dose-dependency in the pharmacokinetics of a macromolecular prodrug of methylprednisolone (MP), dextran-methylprednisolone succinate (DMP), was investigated in rats. Single doses (MP equivalent) of 2.5, 5.0, 10, 20, and 30 mg/kg of DMP were administered intravenously to rats (n=5/group), and serial blood samples (...

journal_title：International journal of pharmaceutics

authors： Zhang X,Mehvar R

更新日期：2001-10-23 00:00:00

abstract：:Clonazepam and lorazepam are two anxiolytics, antidepressant agents, having suitable features for transdermal delivery. The objectives of this study were to evaluate the in vitro percutaneous absorption of these drugs through excised human skin (stratum corneum and epidermis, SCE) and to determine their in vitro perme...

journal_title：International journal of pharmaceutics

authors： Puglia C,Bonina F,Trapani G,Franco M,Ricci M

更新日期：2001-10-09 00:00:00

abstract：:Effects of pH and co-solvents on the bio-mimetic artificial membrane permeation assay were investigated to determine the optimal conditions for the prediction of oral absorption. The permeability (P(am)) of 33 structurally diverse drugs to the PC/PE/PS/PI/CHO/1,7-octadiene membrane system (bio-mimetic lipid (BML) memb...

journal_title：International journal of pharmaceutics

authors： Sugano K,Hamada H,Machida M,Ushio H,Saitoh K,Terada K

更新日期：2001-10-09 00:00:00

abstract：:Triboelectrification of pharmaceutical powders with stainless steel and polymer contact surfaces was investigated. alpha-Lactose monohydrate, from 90 to 125 up to 355-500 microm, was used to quantify electrostatic interactions with negligible powder adhesion to the contact surface. Size fractions down to 53-75 microm ...

journal_title：International journal of pharmaceutics

authors： Rowley G

更新日期：2001-10-04 00:00:00

abstract：:The aim of this study was to assess the in vitro stability of ranitidine to colonic bacteria by utilising a batch culture fermentation system to simulate the conditions of the colon. Three quantities of ranitidine, 100, 200 and 500 mg, in the form of the hydrochloride salt, were introduced into individual 100 ml ferme...

journal_title：International journal of pharmaceutics

authors： Basit AW,Lacey LF

更新日期：2001-10-04 00:00:00

abstract：:The effect of nicotinamide on the properties of aqueous hydroxypropylmethylcellulose (HPMC) solutions was studied. Rheological studies showed that solutions of HPMC of concentration less than 3.0 w/v.% did not form gels and exhibited Newtonian flow patterns at 25 degrees C. The inclusion of nicotinamide increased the ...

journal_title：International journal of pharmaceutics

authors： Hino T,Ford JL

更新日期：2001-09-11 00:00:00

abstract：:Distribution of PLGA-microparticles in porcine skin, after its topical application, was studied in vitro using microparticles containing rhodamine as a fluorescent probe. PLGA-microparticles loaded with rhodamine were prepared using a solvent evaporation technique. Skin distribution of fluorescent microparticles was p...

journal_title：International journal of pharmaceutics

authors： de Jalón EG,Blanco-Príeto MJ,Ygartua P,Santoyo S

更新日期：2001-09-11 00:00:00

abstract：:Exposure of a drug to irradiation can influence the stability of the formulation, leading to changes in the physicochemical properties of the product. The influence of excipients of frequently used stabilizers is often difficult to predict and, therefore, stability testing of the final preparation is important. The se...

journal_title：International journal of pharmaceutics

authors： Tønnesen HH

更新日期：2001-08-28 00:00:00

abstract：:Liquid dosage forms, generally based on aqueous solutions, take an important role in drug administration. The approaches to a theoretical description of solvent and solubility properties have not yet proved completely satisfying. In this work, the Debye equation, which describes well polar and nonpolar molecules in an...

journal_title：International journal of pharmaceutics

authors： Stengele A,Rey S,Leuenberger H

更新日期：2001-08-28 00:00:00

abstract：:The influence of temperature, pH, keratinase concentration, substrate concentration and incubation time on the soluble proteins released by a new keratinase from Doratomyces microsporus was studied with a second-order experimental design. Only 15 or 18 spectrophotometric analyses were required to determine the optimal...

journal_title：International journal of pharmaceutics

authors： Vignardet C,Guillaume YC,Michel L,Friedrich J,Millet J

更新日期：2001-08-14 00:00:00

abstract：:The purpose of this study was to investigate the use of 6-carboxycellulose (OC), a biocompatible and bioresorbable polymer, as a prodrug carrier for amine drugs. Phenylpropanolamine hydrochloride (PPA.HCl) was used as a model drug. OC and PPA were reacted in dimethylformamide (DMF) in the presence of 1,3-dicyclohexylc...

journal_title：International journal of pharmaceutics

authors： Zhu L,Kumar V,Banker GS

更新日期：2001-07-31 00:00:00

abstract：:The enhancing effects of non-ionic surfactants on the permeation of piroxicam from the poloxamer gels were evaluated using Franz diffusion cells fitted with excised rat skins. The effectiveness of penetration enhancers, the ratio of piroxicam flux in the presence or absence of enhancers, was defined as the enhancement...

journal_title：International journal of pharmaceutics

authors： Shin SC,Cho CW,Oh IJ

更新日期：2001-07-17 00:00:00

abstract：:The pharmacokinetics of acetaminophen have been well studied in different populations, especially in Caucasians. However, limited studies on acetaminophen pharmacokinetics have been conducted in the native Chinese and few such data have been reported in the English language literature. Previous published studies sugge...

journal_title：International journal of pharmaceutics

authors： Yin OQ,Tomlinson B,Chow AH,Chow MS

更新日期：2001-07-17 00:00:00

abstract：:The melting point of lidocaine was significantly lowered when mixed with thymol and/or aqueous ethanol. Mixtures of lidocaine and thymol at ratios within the range of 30:70-70:30 (w:w) became homogeneous oils at 25 degrees C. In a pH 9.2 carbonate buffer containing 25% ethanol, lidocaine (5%, w:w) also liquefied at 25...

journal_title：International journal of pharmaceutics

authors： Kang L,Jun HW,Mani N

更新日期：2001-07-03 00:00:00

abstract：:Solid dispersions were prepared with the extremely poorly water soluble drug, probucol and the water soluble polymers, polyvinyl pyrrolidone (PVP), polyacrylic acid (PAA) or polyethylene oxide (PEO) and blends of these polymers. The solid dispersions were prepared either by the solvent evaporation method, or by compre...

journal_title：International journal of pharmaceutics

authors： Broman E,Khoo C,Taylor LS

更新日期：2001-07-03 00:00:00

abstract：:A new system for prediction of drug absorption that takes into account drug dissolution and pH change in the gastro-intestinal tract was developed. In this new system, a drug (solid form) is added into a drug-dissolving vessel (pH 1.0) and the dissolved drug is transferred to a pH adjustment vessel (pH 6.0). Then the ...

journal_title：International journal of pharmaceutics

authors： Kobayashi M,Sada N,Sugawara M,Iseki K,Miyazaki K

更新日期：2001-06-19 00:00:00

abstract：:Changes in the rheological properties of four o/w cream formulations differing in the combination of surfactants were studied. The non-ionic surfactants used were soybean derivatives, polyethylene glycol 10 and 25 soya sterol, and sorbitol derivatives, sorbitan monooleate and trioleate. Combinations of the soybean and...

journal_title：International journal of pharmaceutics

authors： Korhonen M,Hellen L,Hirvonen J,Yliruusi J

更新日期：2001-06-19 00:00:00

abstract：:Stimulated acoustic relaxation emissions from maize starch tablets after compression were detected and recorded in the audible region. Stimulation was found to enhance the detected acoustic emission and to maintain recordable acoustic emission level longer. Based on the fact, that the stimulation by a halogen lamp and...

journal_title：International journal of pharmaceutics

authors： Mellin V,Salonen J,Laine E

更新日期：2001-06-04 00:00:00

abstract：:The effect of the solvent systems water, ethanol (EtOH), propylene glycol (PG) and their binary combinations was studied on the ex vivo permeation profile of the opioid receptor antagonist, naloxone, through rat skin. Fourier transform-infrared (FT-IR) spectroscopic studies were done to investigate the effect of enhan...

journal_title：International journal of pharmaceutics

authors： Panchagnula R,Salve PS,Thomas NS,Jain AK,Ramarao P

更新日期：2001-05-21 00:00:00

abstract：:The purpose of the present study was to investigate the effects of molecular weight (MW) of polyvinylpyrrolidone (PVP) on glass transition and crystallization of sucrose. Thus, sucrose was co-lyophilized with 2.5 and 5.0% w/w PVP of different molecular weights, which were characterized using gel permeation chromatogra...

journal_title：International journal of pharmaceutics

authors： Zeng XM,Martin GP,Marriott C

更新日期：2001-05-07 00:00:00

abstract：:Dissolution profiles of diltiazem hydrochloride (DIL) contained in core tablets from press-coated (PC) tablets with hydroxypropylmethylcellulose acetate succinate (HPMCAS) and plasticizers-adsorbent in the outer shell were investigated. Although, on the addition of triethyl citrate (TEC), triacetin (TA), and acetyltri...

journal_title：International journal of pharmaceutics

authors： Fukui E,Miyamura N,Yoneyama T,Kobayashi M

更新日期：2001-04-17 00:00:00

abstract：:The present study deals with controlled drug delivery from hydrocolloid tablets by polymer particle erosion. The influence of excipients and formulation factors on the dissolution behaviour of the methyl hydroxyethyl cellulose (MHEC)-tablets is investigated. Linear drug release with low susceptibility to hydrodynamic ...

journal_title：International journal of pharmaceutics

authors： Zuleger S,Lippold BC

更新日期：2001-04-17 00:00:00

abstract：:The static electricity generated by triggering a piezo gas igniter is shown to cause electroporation of the skin to deliver antigen. Mice were immunized with chicken albumin by electroporation using a piezo gas igniter and in another experiment, the gas igniter was replaced by a power supply. In both the groups identi...

journal_title：International journal of pharmaceutics

authors： Upadhyay P

更新日期：2001-04-17 00:00:00

abstract：:Lipid emulsions can be used as a vehicle for the production of low-volume injectable preparations with minimally water-soluble active ingredients. First, we focus on the galenic and technological conditions established by ultrasound techniques. A 2(5) factorial design was used to optimize the carrier emulsion. The stu...

journal_title：International journal of pharmaceutics

authors： Medina J,Salvadó A,del Pozo A

更新日期：2001-03-23 00:00:00

abstract：:The rate constants for transfer of a homologous series of nicotinic acid esters from oil vehicles to aqueous buffer phases were determined using a rotating dialysis cell. The chemical stability of butyl nicotinate has been investigated at 60 degrees C over pH range 0.5--10. Maximum stability occurs at pH 4--5 and an i...

journal_title：International journal of pharmaceutics

authors： Weng Larsen S,Engelbrecht Thomsen AE,Rinvar E,Friis GJ,Larsen C

更新日期：2001-03-23 00:00:00

abstract：:A simple and readily manoeuverable method for preparing immuno-magnetic liposomes that indigenously contain binding sites for attaching other molecules like antibodies on their exterior surface is described. In this method magnetic unilamellar vesicles are prepared from a mixture of phosphatidylcholine, cholesterol, s...

journal_title：International journal of pharmaceutics

authors： Elmi MM,Sarbolouki MN

更新日期：2001-03-14 00:00:00

abstract：:The pharmacokinetic parameters of nitrendipine were determined in 40 healthy male volunteers and a very high degree of intersubject variability was observed (CV = 39-71%). Since the distribution of nitrendipine to erythrocytes could influence the overall pharmacokinetic variability the correlation between hematocrit a...

journal_title：International journal of pharmaceutics

authors： Antolic G,Kozjek F,Primozic S

更新日期：2001-03-14 00:00:00

abstract：:The dehydration of nedocromil magnesium (NM) pentahydrate proceeds in two steps, corresponding to the loss of four water molecules in the first step and one water molecule in the second step. The effects of temperature, particle size, sample weight, water vapor pressure and dehydration-rehydration cycle on both the ki...

journal_title：International journal of pharmaceutics

authors： Zhu H,Grant DJ

更新日期：2001-03-14 00:00:00

abstract：:A novel delivery concept based on the encapsulation of liposomes in biodegradable dextran microspheres was developed. The microspheres were prepared using a two-phase system, consisting of water/poly(ethylene glycol), and water/methacrylated dextran. Liposomes were encapsulated almost quantitatively and in their intac...

journal_title：International journal of pharmaceutics

authors： Stenekes RJ,Loebis AE,Fernandes CM,Crommelin DJ,Hennink WE

更新日期：2001-02-19 00:00:00

abstract：:Amphipathic partial dendrimers having three lipidic (C(14)) chains coupled to dendritic lysine head groups with eight, 16 or 32 free terminal amino groups have been synthesised by solid-phase peptide synthesis. Liposomes were prepared with positive, negative and neutral charge using the dehydration-rehydration method ...

journal_title：International journal of pharmaceutics

authors： Purohit G,Sakthivel T,Florence AT

更新日期：2001-02-19 00:00:00

abstract：:Size reduction of microcrystalline cellulose (MCC, Avicel PH-101) powder by ball milling was poorly effective, particularly in the presence of sodium lauryl sulphate (SLS), which tended to form a protective foam. Ultrasonic homogenisation of an aqueous suspension more readily produced ultra-fine MCC, even in the prese...

journal_title：International journal of pharmaceutics

authors： Levis SR,Deasy PB

更新日期：2001-02-01 00:00:00

abstract：:This investigation has examined possible causes of the poor bioavailability of the beta(3)-adrenoceptor agonist BTA-243. The aqueous solubility of BTA-243 is pH dependent with a solubility minimum at pH 1.5. However, the dissolution rate of the disodium salt of BTA-243 is similar at both pH 2.0 and 7.4 indicating that...

journal_title：International journal of pharmaceutics

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

更新日期：2001-02-01 00:00:00

abstract：:The effect of 35 newly synthesized O-ethylmenthol (MET) derivatives on percutaneous absorption of ketoprofen was investigated in rats. In order to understand the relationship between the structure of compounds and promoting activity (structure-activity relationship), an artificial neural network (ANN) was employed. In...

journal_title：International journal of pharmaceutics

authors： Obata Y,Li CJ,Fujikawa M,Takayama K,Sato H,Higashiyama K,Isowa K,Nagai T

更新日期：2001-01-16 00:00:00

abstract：:It has been demonstrated that orally administered cholestyramine is distributed throughout the stomach and provides prolonged gastric residence via mucoadhesion. Gamma scintigraphy was used to compare the gastric emptying and residence of this resin with two formulations known to exhibit retentive or bioadhesive prope...

journal_title：International journal of pharmaceutics

authors： Jackson SJ,Bush D,Perkins AC

更新日期：2001-01-05 00:00:00

abstract：:The objective of the present study was to establish several methods for the introduction of thiol groups onto the surface of human serum albumin (HSA) nanoparticles. Besides the epsilon-amino groups of lysine, the carboxyl groups of asparaginic and glutaminic acid, and the carbonyl groups of the cross-linker glutarald...

journal_title：International journal of pharmaceutics

authors： Weber C,Reiss S,Langer K

更新日期：2000-12-15 00:00:00

abstract：:A procedure is developed that allows particles inhaled with realistic breath patterns to be sized by cascade impaction at a constant flow rate. This procedure is then used to examine the difference between particle sizes obtained with constant flow rate (step profile) versus actual-subject breath patterns for two dry ...

journal_title：International journal of pharmaceutics

authors： Finlay WH,Gehmlich MG

更新日期：2000-12-04 00:00:00

abstract：:This investigation is a contribution to standardization in in vitro drug penetration measurements using excised human skin and to statistical treatment of the observations. The wide variations observed in measurements of drug accumulation in and drug permeation through the stratum corneum are caused not only by analyt...

journal_title：International journal of pharmaceutics

authors： Loth H,Hauck G,Borchert D,Theobald F

更新日期：2000-11-19 00:00:00

abstract：:Amphipathic asymmetric dendrimers have been investigated for use in delivery of genes into cells, with the objective of optimising transfection efficiency and maintaining cell viability. We have synthesised amphipathic asymmetric dendrimers by solid phase methods. The ability of two of these to transfect BHK cells in ...

journal_title：International journal of pharmaceutics

authors： Shah DS,Sakthivel T,Toth I,Florence AT,Wilderspin AF

更新日期：2000-11-04 00:00:00