Pharmacokinetic study of methotrexate following intra-articular injection of methotrexate loaded poly(L-lactic acid) microspheres in rabbits.

abstract：:Regional permeability coefficients of 19 drugs with different physicochemical properties were determined using excised segments from three regions of rat intestine: jejunum, ileum, and colon. The results are discussed in relation to the characteristics of the drug, i.e., MW (range 113-1071 Da), pKa, log D (octanol/wat...

journal_title：Journal of pharmaceutical sciences

authors： Ungell AL,Nylander S,Bergstrand S,Sjöberg A,Lennernäs H

更新日期：1998-03-01 00:00:00

abstract：:This article discusses the evaluation of drug candidates as hepatic transporter substrates. Recently, research on the applications of hepatic transporters in the pharmaceutical industry has improved to meet the requirements of the regulatory guidelines for the evaluation of drug interactions. To identify the risk of t...

journal_title：Journal of pharmaceutical sciences

authors： Okudaira N

更新日期：2017-09-01 00:00:00

abstract：:Cytochrome P450 1B1 (CYP1B1) has been reported to have a major role in metabolizing arachidonic acid (AA) into cardiotoxic metabolites, mid-chain hydroxyeicosatetraenoic acids (HETEs). Recently, we have shown that fluconazole decreases the level of mid-chain HETEs in human liver microsomes. Therefore, the objectives o...

journal_title：Journal of pharmaceutical sciences

authors： Alammari AH,Shoieb SM,Maayah ZH,El-Kadi AOS

更新日期：2020-07-01 00:00:00

abstract：:It is shown that a suitable dosage interval, tau, can be estimated by a factor times the sum of the mean residence time (MRT) of the central compartment (MRTC) and the MRT of the absorption site (MRTA). This value of tau will provide a ratio, maximum steady-state plasma concentration: minimum steady-state plasma conce...

journal_title：Journal of pharmaceutical sciences

authors： Wagner JG

更新日期：1987-01-01 00:00:00

abstract：:The physiological pH changes and peristalsis activities in gastrointestinal (GI) tract have big impact on the dissolution of oral drug products, when those oral drug products include APIs with pH-dependent solubility. It is well documented that predicting the bioperformance of those oral drug products can be challengi...

journal_title：Journal of pharmaceutical sciences

authors： Tsume Y,Patel S,Wang M,Hermans A,Kesisoglou F

更新日期：2020-11-01 00:00:00

abstract：:Oral Almotriptan maleate (ALM) is used in the treatment of migraine; however, due to its extreme aqueous solubility, shows poor penetration and lesser concentration in the brain thus requiring frequent oral dosing. Being flexible and lipophilic in nature, nanostructured lipid carriers (NLCs) represent a promising tool...

journal_title：Journal of pharmaceutical sciences

authors： Salem LH,El-Feky GS,Fahmy RH,El Gazayerly ON,Abdelbary A

更新日期：2020-07-01 00:00:00

abstract：:A crossover experiment was utilized to compare the pharmacokinetics of a 1-g dose of cephalexin tablets, cephalexin capsules, or cephradine capsules in nine normal human volunteers. These antibiotics were administered as three formulations: two 500-mg capsulin every 6 hr for five doses, and one 1000-mg tablet of cepha...

journal_title：Journal of pharmaceutical sciences

authors： Finkelstein E,Quintiliani R,Lee R,Bracci A,Nightingale CH

更新日期：1978-10-01 00:00:00

abstract：:Determination of the kinetics of water-soluble degradation products inside poly(lactide-co-glycolide) (PLGA) delivery systems during polymer degradation is important to evaluate the polymer microclimate conditions, particularly microclimate pH changes for optimization of encapsulated drug stability. A pre-derivatizati...

journal_title：Journal of pharmaceutical sciences

authors： Ding AG,Schwendeman SP

更新日期：2004-02-01 00:00:00

abstract：:Mixing Fungizone with a fat emulsion used for nutritional purpose (Intralipid or Lipofundin ) was reported to decrease Amphotericin B (AmB) toxicity in clinical use. In an effort to understand the reason for this phenomenon, spectral and morphological analyses were done for the Fungizone and Fungizone /Lipofundin admi...

journal_title：Journal of pharmaceutical sciences

authors： Egito ES,Araújo IB,Damasceno BP,Price JC

更新日期：2002-11-01 00:00:00

abstract：:The pharmacokinetics of fluorouracil were examined after single 250-mg iv doses and 500-mg oral doses to female patients with breast cancer. In five patients who received intravenous fluorouracil, the mean peak plasma level of unchanged drug was 13.4 microgram/ml, the elimination half-life was 6.3 min, and the plasma ...

journal_title：Journal of pharmaceutical sciences

authors： Phillips TA,Howell A,Grieve RJ,Welling PG

更新日期：1980-12-01 00:00:00

abstract：:The pharmacokinetics of the antirheumatic proquazone and its conjugated and unconjugated m-hydroxy metabolites were investigated in five healthy male volunteers after both intravenous (75 and 122 mg) and peroral (300 and 900 mg via capsules) administration. For adequate intravenous dosing of the poorly water-soluble p...

journal_title：Journal of pharmaceutical sciences

authors： Hinderling PH,Roos A

更新日期：1984-03-01 00:00:00

abstract：:Both developing (Days --1-+12 relative to inoculation) and established (Days +18-+29) stages of Mycobacterium butyricum adjuvant-induced polyarthritis in rats were treated orally with cryogenine (100 mg/kg/day), a prototype anti-inflammatory (phenylbutazone, 100 mg/kg/day), or a prototype immunosuppressive (cyclophosp...

journal_title：Journal of pharmaceutical sciences

authors： Watson WC,Malone MH

更新日期：1977-09-01 00:00:00

abstract：:Therapeutic use of anti-inflammatory steroids is limited due to their potential suppressive effects on pituitary-adrenal function and the immune system. Based on the antedrug concept, a new class of potent locally active compounds with reduced risk of side effects has been synthesized from prednisolone by introducing ...

journal_title：Journal of pharmaceutical sciences

authors： Heiman AS,Taraporewala IB,McLean HM,Hong D,Lee HJ

更新日期：1990-07-01 00:00:00

abstract：:Magnetic resonance imaging (MRI) with chemical shift resolution is a recent extension of MRI and it provides information about species resolved molecular transport on the macroscopic scale in complex systems. In this contribution, we show that by using this novel method, one can predict the behavior of drug and food m...

journal_title：Journal of pharmaceutical sciences

authors： Lafitte G,Thuresson K,Söderman O

更新日期：2007-02-01 00:00:00

abstract：:Product temperature (Tb) and drying time constitute critical material attributes and process parameters in the lyophilization process and especially during the primary drying stage. In the study, we performed a temperature measurement by the sublimation rate (TMbySR) to monitor the Tb value and determine the end point...

journal_title：Journal of pharmaceutical sciences

authors： Kawasaki H,Shimanouchi T,Sawada H,Hosomi H,Hamabe Y,Kimura Y

更新日期：2019-07-01 00:00:00

abstract：:A physically based method for arriving at topological indexes is described. The derived indexes correlate with molecular surface areas and with the molecular connectivity index. The newly derived index seems to account better for the expected distinctions among primary, secondary, and tertiary alcohol aqueous solubili...

journal_title：Journal of pharmaceutical sciences

authors： Cammarata A

更新日期：1979-07-01 00:00:00

abstract：:Quantitative determination of serum concentrations of carvedilol [(+/-)-1-(carbazol-4-yloxy)-3-[[2-(o-methoxyphenoxy)ethyl) amino]-2-propanol], a combined alpha- and beta-adrenergic receptor antagonist, was obtained using HPLC with spectrofluorometric detection. Carvedilol was extracted from alkalinized serum with eth...

journal_title：Journal of pharmaceutical sciences

authors： Varin F,Cubeddu LX,Powell JR

更新日期：1986-12-01 00:00:00

abstract：:Disintegration performance was measured by analysing both water ingress and tablet swelling of pure microcrystalline cellulose (MCC) and in mixture with croscarmellose sodium using terahertz pulsed imaging (TPI). Tablets made from pure MCC with porosities of 10% and 15% showed similar swelling and transport kinetics: ...

journal_title：Journal of pharmaceutical sciences

authors： Yassin S,Goodwin DJ,Anderson A,Sibik J,Ian Wilson D,Gladden LF,Axel Zeitler J

更新日期：2015-10-01 00:00:00

abstract：:The effect of pretreating callus membranes with dimethyl sulfoxide, dimethylacetamide, dimethylformamide, formamide, dioxane, or methyl orthoformate on sarin permeability was studied at three temperatures to determine the activation energy for transport. In addition, the effect of membrane pretreatment on permeability...

journal_title：Journal of pharmaceutical sciences

authors： Matheson LE,Wurster DE,Ostrenga JA

更新日期：1979-11-01 00:00:00

abstract：:A difference spectrophotometric analytical method was developed for the selective determination of p-hydroxybenzoic acid in the presence of its alkyl esters without prior separation. Based on the spectral shift to a shorter wavelength accompanyint carboxyl dissociation, the procedure measures as little as 2% of this a...

journal_title：Journal of pharmaceutical sciences

authors： Fink DW,Fink HC,Tolan JW,Blodinger J

更新日期：1978-06-01 00:00:00

abstract：:Aliphatic polyesters have great utility as temporary prosthetics and surgical aids, and in drug delivery systems. Knowledge of the mechanism and pathways of hydrolysis can form a basis for the design and selection of a controlled-release system. Because of the importance of hydrolysis to the properties of such a syste...

journal_title：Journal of pharmaceutical sciences

authors： Maniar ML,Kalonia DS,Simonelli AP

更新日期：1991-08-01 00:00:00

abstract：:We describe the key issues and possibilities for continuous final dosage formation, otherwise known as downstream processing or drug product manufacturing. A distinction is made between heterogeneous processing and homogeneous processing, the latter of which is expected to add more value to continuous manufacturing. W...

journal_title：Journal of pharmaceutical sciences

authors： Byrn S,Futran M,Thomas H,Jayjock E,Maron N,Meyer RF,Myerson AS,Thien MP,Trout BL

更新日期：2015-03-01 00:00:00

abstract：:An analysis of the disintegration-dissolution sequence of drug release from a tablet leads to a mathematical expression relating disintegration to the dissolution profile of the tablet and the dissolution rate of the primary drug particles in the tablet. The equation describing the disintegration of an acetaminophen t...

journal_title：Journal of pharmaceutical sciences

authors： Nelson KG,Wang LY

更新日期：1978-01-01 00:00:00

abstract：:A rapid solubility-screening assay was developed with a focus on Biopharmaceutic Classification Scheme (BCS) class II drug solubility in animal and simulated human gastrointestinal (GI) fluids. The assay enables biologically promising drug leads to be evaluated for solubility limitations earlier in the drug developmen...

journal_title：Journal of pharmaceutical sciences

authors： Guo J,Elzinga PA,Hageman MJ,Herron JN

更新日期：2008-04-01 00:00:00

abstract：:The highly lipid soluble, free-base form of halofantrine (Hf base; approximately 50 mg/mL in triglyceride lipids), a highly lipophilic (calculated log P approximately 8.5) antimalarial, has recently been shown to undergo significant intestinal lymphatic transport (54% of administered dose) after postprandial administr...

journal_title：Journal of pharmaceutical sciences

authors： Khoo SM,Prankerd RJ,Edwards GA,Porter CJ,Charman WN

更新日期：2002-03-01 00:00:00

abstract：:Quantitative prediction of unbound drug fraction (fu) is essential for scaling pharmacokinetics through physiologically based approaches. However, few attempts have been made to evaluate the projection of fu values under pathological conditions. The primary objective of this study was to predict fu values (n = 105) of...

journal_title：Journal of pharmaceutical sciences

authors： Li GF,Yu G,Li Y,Zheng Y,Zheng QS,Derendorf H

更新日期：2018-07-01 00:00:00

abstract：:Application of low-frequency ultrasound has been shown to enhance transdermal transport of drugs (low-frequency sonophoresis). In this paper, we show that the efficacy of low-frequency ultrasound in enhancing transdermal transport can be further increased by its combination with sodium lauryl sulfate (SLS), a well-kno...

journal_title：Journal of pharmaceutical sciences

authors： Mitragotri S,Ray D,Farrell J,Tang H,Yu B,Kost J,Blankschtein D,Langer R

更新日期：2000-07-01 00:00:00

abstract：:The phase diagram for the binary system nafcillin sodium-water, was determined using differential scanning calorimetry (DSC) and polarized light microscopy. In the temperature range of -20-30 degrees, three crystalline forms and an amphiphilic liquid crystalline phase were detected. The stable crystalline form of nafc...

journal_title：Journal of pharmaceutical sciences

authors： Bogardus JB

更新日期：1982-01-01 00:00:00

abstract：:A stability-indicating reversed-phase high-performance liquid chromatographic method using a refractive index detector is described for the determination of propylene carbonate in pharmaceutical formulations. Good precision and accuracy of the method was demonstrated using an aqueous formulation. This method is also a...

journal_title：Journal of pharmaceutical sciences

authors： Cheng H,Gadde RR

更新日期：1985-06-01 00:00:00

abstract：:In an attempt to explain the mechanism of protein stabilization conferred by detergents, we investigated the effect of Tween 80 on aggregation of bovine serum albumin (BSA) using circular dichroism (CD) and native gel electrophoresis. CD thermal scans showed that BSA denatures at about 54 degrees C in 20 mM Tris, pH 7...

journal_title：Journal of pharmaceutical sciences

authors： Arakawa T,Kita Y

更新日期：2000-05-01 00:00:00