Factors that restrict intestinal cell permeation of cyclic prodrugs of an opioid peptide (DADLE): Part II. Role of metabolic enzymes in the intestinal mucosa.

abstract：:The antifungal activity of amphotericin B (AmB) incorporated in three cholesteryl carbonate esters (CCEs), sodium cholesteryl carbonate, cholesteryl palmityl carbonate, and dicholesteryl carbonate, was examined to assess their potential for use in a dry powder aerosol. Formulations containing dissolved AmB were stable...

journal_title：Journal of pharmaceutical sciences

authors： Chuealee R,Wiedmann TS,Srichana T

更新日期：2011-05-01 00:00:00

abstract：:X-ray diffraction and infrared spectroscopy measurements for the N,N-dimethylformamide (DMF) and dimethyl sulfoxide (DMSO) solvatomorphs of betulonic acid (BA) were investigated. BA [3-oxolup-20(29)-en-28-oic acid, C(30)H(46)O(3)] exhibits a wide spectrum of biological activities and is considered to be a promising na...

journal_title：Journal of pharmaceutical sciences

authors： Boryczka S,Jastrzebska M,Bębenek E,Kusz J,Zubko M,Kadela M,Michalik E

更新日期：2012-12-01 00:00:00

abstract：:Drug transporters expressed in liver and kidney play a critical role in the elimination of a wide range of drugs and xenobiotics and inhibition of these transporters may therefore cause clinically significant drug-drug interactions (DDIs). Currently, in vitro transporter inhibition data are used to assess the risk tha...

journal_title：Journal of pharmaceutical sciences

authors： Chu X,Chan GH,Evers R

更新日期：2017-09-01 00:00:00

abstract：:Nanocrystals have emerged as a potential formulation strategy to eliminate the bioavailability-related problems by enhancing the initial dissolution rate and moderately super-saturating the thermodynamic solubility. This review contains an in-depth knowledge of, the processing method for formulation, an accurate quant...

journal_title：Journal of pharmaceutical sciences

authors： Shah DA,Murdande SB,Dave RH

更新日期：2016-01-01 00:00:00

abstract：:DB844 (CPD-594-12), N-methoxy-6-{5-[4-(N-methoxyamidino)phenyl]-furan-2-yl}-nicotinamidine, is an oral prodrug that has shown promising efficacy in both mouse and monkey models of second stage human African trypanosomiasis. However, gastrointestinal (GI) toxicity was observed with high doses in a vervet monkey safety ...

journal_title：Journal of pharmaceutical sciences

authors： Ju W,Yang S,Ansede JH,Stephens CE,Bridges AS,Voyksner RD,Ismail MA,Boykin DW,Tidwell RR,Hall JE,Wang MZ

更新日期：2014-01-01 00:00:00

abstract：:Spray freeze-drying is an evolving technology that combines the benefits of spray-drying and conventional lyophilization techniques to produce drug substance and drug product as free-flowing powders. The high surface-to-volume ratio associated to the submillimeter spray-frozen particles contributes to shorter drying a...

journal_title：Journal of pharmaceutical sciences

authors： Sebastião IB,Bhatnagar B,Tchessalov S,Ohtake S,Plitzko M,Luy B,Alexeenko A

更新日期：2019-06-01 00:00:00

abstract：:Time and resource constraints necessitate increasingly early decision making to accelerate or stop preclinical drug discovery programs. Early discovery drug candidates may be potent inhibitors of new targets, but all too often exhibit poor pharmaceutical and pharmacokinetic properties that limit the in vivo exposure. ...

journal_title：Journal of pharmaceutical sciences

authors： Chiang PC,South SA,Foster KA,Daniels JS,Wene SP,Albin LA,Thompson DC

更新日期：2010-07-01 00:00:00

abstract：:The cobalt 60 radiolytic degradation products have been identified in the following corticosteroids: cortisone, cortisone acetate, hydrocortisone, hydrocortisone acetate, hydrocortisone sodium succinate, isoflupredone acetate, methylprednisolone, methylprednisolone acetate, prednisolone, prednisolone acetate, and pred...

journal_title：Journal of pharmaceutical sciences

authors： Kane MP,Tsuji K

更新日期：1983-01-01 00:00:00

abstract：:This paper describes the synthesis and characterization of cationic copolymers with different macromolecular architecture and drug delivery properties of the corresponding dexamethasone sodium phosphate (DSP)-loaded systems. Copolyelectrolytes comprising poly[2-(acryloyloxy)ethyl] trimethylammonium chloride (PAETMAC) ...

journal_title：Journal of pharmaceutical sciences

authors： Georgieva D,Kostova B,Ivanova S,Rachev D,Tzankova V,Kondeva-Burdina M,Christova D

更新日期：2014-08-01 00:00:00

abstract：:The estimates of infinity values obtained using Prony's method are shown to be subject to significant error arising from small errors in the assigned sample times. The error of the estimate may be reduced by increasing the time interval between samples. ...

journal_title：Journal of pharmaceutical sciences

authors： Newburger J,Stavchansky S,Pearlman RS

更新日期：1980-10-01 00:00:00

abstract：:Heckel analysis, tablet tensile strength, and indentation hardness were determined for a series of sieved and roller compacted microcrystalline cellulose mixtures under both unlubricated and lubricated conditions with magnesium stearate. These results have been used to evaluate the loss of reworkability following roll...

journal_title：Journal of pharmaceutical sciences

authors： He X,Secreast PJ,Amidon GE

更新日期：2007-05-01 00:00:00

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

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

更新日期：2012-01-01 00:00:00

abstract：:The aim of this study was to characterize the in vitro hepatic uptake kinetics of sodium fluorescein (NaFluo) and identify the transporters involved. NaFluo exhibited saturable uptake kinetics in suspended rat and human hepatocytes as reflected by K(m) values of 22.5 and 14.1 µM, and V(max) values of 98.3 and 5.8 pmol...

journal_title：Journal of pharmaceutical sciences

authors： De Bruyn T,Fattah S,Stieger B,Augustijns P,Annaert P

更新日期：2011-11-01 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：:Recently developed techniques were applied in a preformulation program to select a compound and a suitable salt for use in a one-month toxicological test. The program showed that valuable information can be obtained prior to the choice of a compound as a candidate for a solid-dosage form. Information about the physica...

journal_title：Journal of pharmaceutical sciences

authors： Graffner C,Johansson ME,Nicklasson M,Nyqvist H

更新日期：1985-01-01 00:00:00

abstract：:The adsorption of cimetidine on selected pharmaceuticals including kaolin, activated charcoal, talc, and nonsystemic antacids was determined at pH 5.0 and 25 degrees. The Langmuir and Freundlich adsorption isotherms showed that cimetidine adsorption was significant with activated charcoal, kaolin, talc, and magnesium ...

journal_title：Journal of pharmaceutical sciences

authors： Ganjian F,Cutie AJ,Jochsberger T

更新日期：1980-03-01 00:00:00

abstract：:Water/n-octanol partition coefficients (log P) for 33 1,2-dithiole-3-thiones and for 18 1,2-dithiol-3-ones were determined by RP-HPLC measurement of the concentration of the solute in aqueous solution after equilibrium. Depending on the nature of the substituents (alkyl or aryl) and their position(s) (4,5, or both) on...

journal_title：Journal of pharmaceutical sciences

authors： Bona M,Boudeville P,Zekri O,Christen MO,Burgot JL

更新日期：1995-09-01 00:00:00

abstract：:Owing to proliferation of antibiotic-resistant bacteria, the use of antibiotics for livestock growth promotion is banned in many countries and alternatives to in-feed antibiotics are needed. Cinnamon essential oil exhibits strong in vitro antibacterial activity; however, direct addition of essential oils to animal fee...

journal_title：Journal of pharmaceutical sciences

authors： Ma YH,Wang Q,Gong J,Wu XY

更新日期：2016-03-01 00:00:00

abstract：:The influence of commonly used excipients, spray-dried lactose (SDL), microcrystalline cellulose (MCC), and partially pregelatinized maize starch (Starch 1500) on drug release from hydroxypropyl methylcellulose (HPMC, hypromellose) matrix system has been investigated. A model formulation contained 30%w/w drug, 20%w/w ...

journal_title：Journal of pharmaceutical sciences

authors： Levina M,Rajabi-Siahboomi AR

更新日期：2004-11-01 00:00:00

abstract：:The blood-brain barrier (BBB) limits the distribution of systemically administered therapeutics to the central nervous system (CNS). Intranasal delivery is a noninvasive method that targets drugs to the brain and spinal cord along olfactory and trigeminal neural pathways, bypassing the BBB and minimizing systemic expo...

journal_title：Journal of pharmaceutical sciences

authors： Dhuria SV,Hanson LR,Frey WH 2nd

更新日期：2009-07-01 00:00:00

abstract：:The purpose of the present study was to clarify the expression levels of transporter proteins in human lung tissue and to analyze regional and interindividual differences in primary cultured epithelial cells. Organic cation/carnitine tranporter 1 (OCTN1) protein expression was highest (2.08 ± 1.19 fmol/μg protein) in ...

journal_title：Journal of pharmaceutical sciences

authors： Sakamoto A,Matsumaru T,Yamamura N,Uchida Y,Tachikawa M,Ohtsuki S,Terasaki T

更新日期：2013-09-01 00:00:00

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

authors： Hwang SS,Bayne W,Theeuwes F

更新日期：1993-11-01 00:00:00

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

authors： Bhat PG,Flanagan DR,Donovan MD

更新日期：1996-06-01 00:00:00

abstract：:A direct high-performance liquid chromatographic (HPLC) method was applied to monitor 2,5-diaziridinyl-3,6-bis(carboethoxyamino)-1,4-benzoquinone (I) and its degradation products in pharmaceutical vehicles at 25 +/- 0.1 degrees. At the optimal pH for stability of I, an increase in buffer concentration [phosphate and t...

journal_title：Journal of pharmaceutical sciences

authors： Poochikian GK,Kelley JA

更新日期：1981-02-01 00:00:00

abstract：:Both bovine enamel and hydroxyapatite pellets were remineralized in a fluoride-containing remineralization solution after prior demineralization for various lengths of time. In both the enamel and pellet systems, the degree of remineralization attainable was directly related to the extent of prior demineralization, al...

journal_title：Journal of pharmaceutical sciences

authors： Yonese M,Fox JL,Nambu N,Hefferren JJ,Higuchi WI

更新日期：1981-08-01 00:00:00

abstract：:The Setschenow constant, K(salt), of a nonelectrolyte in a NaCl solution is shown to be related to the logarithm of its octanol-water partition coefficient, log K(ow), determined by K(salt) = A log K(ow) + B, where K(ow) is the octanol-water partition coefficient of the solute and the coefficients A and B are constant...

journal_title：Journal of pharmaceutical sciences

authors： Ni N,El-Sayed MM,Sanghvi T,Yalkowsky SH

更新日期：2000-12-01 00:00:00

abstract：:The absorption, protein binding, blood-to-plasma ratio, renal excretion, and pharmacokinetics of the dopamine-2 agonists (D2-agonists) 4-(2-di-n-propylaminoethyl)-7-hydroxy-2-(3H)-indolone (1), N-(2'-hydroxy-5'-[N,N-di-n-propylaminoethylphenyl])methanesulfonamide (2), and 4-(2-di-n-propylaminoethyl)-2-(3H)-indolone (3...

journal_title：Journal of pharmaceutical sciences

authors： Swagzdis JE,Wittendorf RW,DeMarinis RM,Mico BA

更新日期：1986-10-01 00:00:00

abstract：:(-)-1-Cyclopropylmethyl-4-(3-trifluoromethylthio-5H-dibenzo [a,d]cyclohepten-5-ylidene)piperidine (MK-160) was extracted from human plasma and urine with petroleum ether and quantitated by GLC using a nitrogen-sensitive detector. A homologue of the drug served as the internal standard. The method is specific for the d...

journal_title：Journal of pharmaceutical sciences

authors： Hucker HB,Hutt JE

更新日期：1983-07-01 00:00:00

abstract：:The use of pharmacological responses such as pupil diameter for dosage individualization, bioavailability, and pharmacokinetic analyses is becoming more widespread. Attempts to use pupil diameter to assess morphine bioavailability illuminate the fact that multiple responses, nonlinearities, and the condition of the su...

journal_title：Journal of pharmaceutical sciences

authors： Kramer PA

更新日期：1977-04-01 00:00:00

abstract：:The pharmaceutical preparation, chromatography, and biological distribution of a series of new chemical analogs of palmitic acid and diethylenetriaminepentaacetic acid, ethylenediaminetetraacetic acid, or diethylenetriamine are described. The biological distribution in rabbits 30 min after intravenous administration o...

journal_title：Journal of pharmaceutical sciences

authors： Karesh SM,Eckelman WC,Reba RC

更新日期：1977-02-01 00:00:00