Estimation of aqueous solubility for some guanine derivatives using partition coefficient and melting temperature.

abstract：:Pinacidil [(+/-)-2-cyano-1-(4-pyridyl)-3-(1,2,2-trimethylpropyl)guanidine monohydrate] is a novel, direct-acting vasodilator antihypertensive agent. The cyano 14C-labeled drug is rapidly and completely absorbed after an oral 12.5-mg dose in solution. The blood:plasma concentration ratios (0.8-0.9) indicate transient p...

journal_title：Journal of pharmaceutical sciences

authors： DeLong AF,Oldham SW,DeSante KA,Nell G,Henry DP

更新日期：1988-02-01 00:00:00

abstract：:Nanospheres with D,L-lactide/glycolide copolymer (PLGA) were prepared as a biodegradable and biocompatible polymeric carrier for peptide drugs by a novel spontaneous emulsification solvent diffusion method. Nafarelin acetate (NA), a luteinizing hormone-releasing hormone analogue, was employed as a model peptide drug t...

journal_title：Journal of pharmaceutical sciences

authors： Niwa T,Takeuchi H,Hino T,Kunou N,Kawashima Y

更新日期：1994-05-01 00:00:00

abstract：:Although inaccurate true density affects analysis of powder compaction data, such effects have not been systematically evaluated in the literature. This work is aimed at quantitatively evaluating effects of inaccurate true density on tableting data analysis using the Ryshkewitch equation, sigma = sigma0 e - bepsilon, ...

journal_title：Journal of pharmaceutical sciences

authors： Sun CC

更新日期：2005-09-01 00:00:00

abstract：:Male and female rats treated with a single 20-mg/kg ip dose of pregnenolone-16alpha-carbonitrile (PCN) produced parallel increases in hepatic cytochrome P-450 and aniline hydroxylase activity. However, the onset of increase in aniline hydroxylase activity and cytochrome P-450 content was slower in male than female ani...

journal_title：Journal of pharmaceutical sciences

authors： Stohs SJ,Rosenberg H

更新日期：1976-04-01 00:00:00

abstract：:Boron analogues of carbamoylcholine and thiocholine and esters of these analogues were prepared. These compounds were fairly stable toward hydrolysis and demonstrated moderate anti-inflammatory and hypolipidemic activities in mice. The hypolipidemic activity of the compounds at a dose of 8 mg/kg/day was equivalent in ...

journal_title：Journal of pharmaceutical sciences

authors： Sood A,Sood CK,Spielvogel BF,Hall IH,Wong OT

更新日期：1992-05-01 00:00:00

abstract：:Poor dissolution performance is one of the challenges encountered in dosage form design of amorphous solid dispersions (ASDs). This study was aimed to investigate the effect of solid-liquid interactions of an encapsulated ASD on drug release. Drug release profiles of a molecularly interacting amorphous celecoxib solid...

journal_title：Journal of pharmaceutical sciences

authors： Puri V,Dantuluri AK,Bansal AK

更新日期：2011-06-01 00:00:00

abstract：:One of the challenges with predictive modeling is how to quantify the reliability of the models' predictions on new objects. In this work we give an introduction to conformal prediction, a framework that sits on top of traditional machine learning algorithms and which outputs valid confidence estimates to predictions ...

journal_title：Journal of pharmaceutical sciences

authors： Alvarsson J,Arvidsson McShane S,Norinder U,Spjuth O

更新日期：2021-01-01 00:00:00

abstract：:Ketoconazole and posaconazole are both Biopharmaceutics Classification System class 2 drugs (highly permeable, poorly soluble), are structurally similar, and are administered at the same doses. Nevertheless, the duodenal concentration profile and the magnitude of the positive food effect observed for these 2 drugs are...

journal_title：Journal of pharmaceutical sciences

authors： Cristofoletti R,Patel N,Dressman JB

更新日期：2016-09-01 00:00:00

abstract：:Certain disulfide analogues of cystamine were prepared and evaluated for the ability to inhibit gamma-glutamylcysteine synthetase (GCS), the rate-limiting enzyme in glutathione synthesis. The compound SAPH-3 disulfide (2a) was found to be the most effective inactivator of GCS reported to date. Studies of structural an...

journal_title：Journal of pharmaceutical sciences

authors： Schor NF,Cheng B,Siuda JF

更新日期：1991-04-01 00:00:00

abstract：:This investigation was designed to quantitate and compare in the rat the oral absorption characteristics of micronized griseofulvin from a corn oil-in-water emulsion dosage form containing suspended drug and a control aqueous suspension after single-dose (50 mg/kg) and multiple-dose (50 mg/kg every 12 hr for five dose...

journal_title：Journal of pharmaceutical sciences

authors： Bates TR,Carrigan PJ

更新日期：1975-09-01 00:00:00

abstract：:The disposition of the beta-blocking drug talinolol is controlled by P-glycoprotein in man. Because talinolol is marketed as a racemate, we reevaluated the serum-concentration time profiles of talinolol of a previously published study with single intravenous (30 mg) and repeated oral talinolol (100 mg for 14 days) bef...

journal_title：Journal of pharmaceutical sciences

authors： Zschiesche M,Lemma GL,Klebingat KJ,Franke G,Terhaag B,Hoffmann A,Gramatté T,Kroemer HK,Siegmund W

更新日期：2002-02-01 00:00:00

abstract：:In pharmaceutical development alternative drug delivery modalities are being increasingly employed. One example is an implant, which achieves gradual drug release in patients over a period of many months or years. Due to the complexity of these long-acting formulations, advanced physical characterization methods are d...

journal_title：Journal of pharmaceutical sciences

authors： Skomski D,Liu Z,Su Y,John CT,Doty A,Forster SP,Teller R,Barrett SE,Xu W

更新日期：2020-09-01 00:00:00

abstract：:We have shown that adsorbability of local anesthetics onto activated carbon, expressed by the partition coefficients at infinite dilution, correlated well with the pharmacological activity. However, there is no parameter that can singly express the tendency to be adsorbed. Adsorbability is a loosely defined term and i...

journal_title：Journal of pharmaceutical sciences

authors： Abe I,Kamaya H,Ueda I

更新日期：1990-04-01 00:00:00

abstract：:The hepatic distribution, biliary excretion, and mass balance of liposomal amphotericin B (L-AmB) were investigated in recirculated isolated perfused rat liver. The results were compared with those from the conventional AmB formulation, amphotericin B deoxycholate (D-AmB). L-AmB was introduced as a bolus into the perf...

journal_title：Journal of pharmaceutical sciences

authors： Hong Y,Ramzan I,McLachlan AJ

更新日期：2005-01-01 00:00:00

abstract：:Human insulin exists in different association states, from monomer to hexamer, depending on the conditions. In the presence of zinc the "normal" state is a hexamer. The structural properties of 20 variants of human insulin were studied by near-UV circular dichroism, fluorescence spectroscopy, and small-angle X-ray sca...

journal_title：Journal of pharmaceutical sciences

authors： Uversky VN,Garriques LN,Millett IS,Frokjaer S,Brange J,Doniach S,Fink AL

更新日期：2003-04-01 00:00:00

abstract：:Thymoquinone (TQ) is the main bioactive component isolated from Nigella sativa essential oil and seeds and has been used for the treatment of inflammations, liver disorders, arthritis, and is of great importance as a promising therapeutic drug for different diseases including cancer. This paper reports the first exper...

journal_title：Journal of pharmaceutical sciences

authors： Lupidi G,Camaioni E,Khalifé H,Avenali L,Damiani E,Tanfani F,Scirè A

更新日期：2012-07-01 00:00:00

abstract：:An immune response for a nasal ovalbumin (OVA) powder formulation with an applied nasal delivery platform technology, consisting of a powdery nasal carrier and a device, was evaluated in monkeys with similar upper respiratory tracts and immune systems to those of humans, in order to assess the applicability to a vacci...

journal_title：Journal of pharmaceutical sciences

authors： Torikai Y,Sasaki Y,Sasaki K,Kyuno A,Haruta S,Tanimoto A

更新日期：2020-12-03 00:00:00

abstract：:Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release (IR) solid oral dosage forms containing ethambutol dihydrochloride as the only active pharmaceutical ingredient (API) are reviewed. Ethambutol dihydrochloride is a Biopharmaceutics Cl...

journal_title：Journal of pharmaceutical sciences

authors： Becker C,Dressman JB,Amidon GL,Junginger HE,Kopp S,Midha KK,Shah VP,Stavchansky S,Barends DM

更新日期：2008-04-01 00:00:00

abstract：:The aim was to study a new method of dissolution in vitro, the "Bio-Dis" apparatus, and to compare it with the classical rotating bottle method. Several theophylline controlled-release drug dosage forms were studied. Dissolution testing was performed in increasing pH in standard conditions and after treatment with pea...

journal_title：Journal of pharmaceutical sciences

authors： Esbelin B,Beyssac E,Aiache JM,Shiu GK,Skelly JP

更新日期：1991-10-01 00:00:00

abstract：:The utility of inhaled protein therapeutics to treat lung-resident diseases is limited by protein degradation in the lungs and rapid clearance. This study therefore aimed to evaluate the impact of PEGylation on the lung and systemic exposure of interferon (IFN) α2 after intratracheal administration to rats. An inverse...

journal_title：Journal of pharmaceutical sciences

authors： Mcleod VM,Chan LJ,Ryan GM,Porter CJ,Kaminskas LM

更新日期：2015-04-01 00:00:00

abstract：:Because the ionized species is more polar than its un-ionized counterpart, it is often assumed that the ionized species of the drug does not make a meaningful contribution to solubilization by either cosolvents or surfactants. This report extends previous studies on solubilization of the ionic species by a combination...

journal_title：Journal of pharmaceutical sciences

authors： Li P,Tabibi SE,Yalkowsky SH

更新日期：1999-05-01 00:00:00

abstract：:Using liquid scintillation counting and liquid chromatographic techniques, it has been demonstrated that the anthracycline antibiotics, doxorubicin hydrochloride, N-trifluoroacetyladriamycin-14-valerate, and N-trifluoroacetyladriamycin-14-octanoate, can be strongly absorbed to the walls of containers, depending on the...

journal_title：Journal of pharmaceutical sciences

authors： Tomlinson E,Malspeis L

更新日期：1982-10-01 00:00:00

abstract：:The relationship between chemical structure and antifungal activity of quaternary imidazolium compounds is analyzed. The compounds are described by a set of condition attributes concerning structure and by a decision attribute concerning activity. The description builds up an information system. The smallest set of co...

journal_title：Journal of pharmaceutical sciences

authors： Krysiński J

更新日期：1995-02-01 00:00:00

abstract：:Alkyl 2-imidazolyl disulfide compounds are novel antitumor agents, one of which is currently being evaluated in Phase I clinical trials. These molecules contain an unsymmetrical disulfide fragment, the lipophilic and electronic contributions of which are still not defined in the literature. Lipophilicity, ionization, ...

journal_title：Journal of pharmaceutical sciences

authors： Hashash A,Kirkpatrick DL,Lazo JS,Block LH

更新日期：2002-07-01 00:00:00

abstract：:The pKa values of benzoic acid, p-methylbenzoic, and p-aminobenzoic acid (PABA) were determined by potentiometric titration in mixtures of 0-0.5 volume fractions of various cosolvents and water. The differences between the aqueous and semiaqueous pKa values were similar for the three solutes at a particular cosolvent-...

journal_title：Journal of pharmaceutical sciences

authors： Rubino JT,Berryhill WS

更新日期：1986-02-01 00:00:00

abstract：:Safety evaluation of self-assembled polymeric micelles is important for biomedical involvement in drug delivery systems in the future. In this study, biodegradable monomethyl poly (ethylene glycol)-poly (ε-caprolactone)-poly (trimethylene carbonate) [MPEG-P(CL-co-TMC)] copolymer was synthesized and characterized by Fo...

journal_title：Journal of pharmaceutical sciences

authors： Yang X,Cao D,Wang N,Sun L,Li L,Nie S,Wu Q,Liu X,Yi C,Gong C

更新日期：2014-01-01 00:00:00

abstract：:Most of the global healthcare issues facing us--from expanding access to care, to providing medical and dental care in the aftermath of disasters--are far too complex for any single sector to successfully solve. Industry, the healthcare profession, government, academia and non-governmental organizations (NGOs) are all...

journal_title：Journal of pharmaceutical sciences

authors： Bergman SM

更新日期：2008-12-01 00:00:00

abstract：:The α-keto carboxylic acid, pyruvic acid (1) was found to be a very effective peroxide scavenger but is subject to an aldol-like self-condensation/polymerization reaction. The purpose of this study was to evaluate the hydrogen peroxide, H2O2, scavenging ability of 3-methyl-2-oxobutanoic acid (2), 4-methyl-2-oxopentano...

journal_title：Journal of pharmaceutical sciences

authors： Lopalco A,Stella VJ

更新日期：2016-09-01 00:00:00

abstract：:The blood-brain barrier permeation has been investigated by using a topological substructural molecular design approach (TOPS-MODE). A linear regression model was developed to predict the in vivo blood-brain partitioning coefficient on a data set of 119 compounds, treated as the logarithm of the blood-brain concentrat...

journal_title：Journal of pharmaceutical sciences

authors： Cabrera MA,Bermejo M,Pérez M,Ramos R

更新日期：2004-07-01 00:00:00

abstract：:Treatment of systemic diseases by means of the inhalation route is hampered by uncertainties of the drug dose applied by inhalation. In this study, the hypothesis was tested that by standardization of the breathing maneuver used for inhalation, the interindividual variability of the dose deposited intrathoracically ca...

journal_title：Journal of pharmaceutical sciences

authors： Brand P,Friemel I,Meyer T,Schulz H,Heyder J,Häubetainger K

更新日期：2000-06-01 00:00:00