Solubility and partitioning. VII: Solubility of barbiturates in water.

abstract：:Hyperlipidemia (HL) was previously shown to lower liver uptake of the more potent (-) enantiomer of ketoconazole (KTZ) in rat. The current study examined the possible modifying influence of experimental HL on a KTZ pharmacokinetic interaction with midazolam (MDZ). Normolipidemic and hyperlipidemic rats were administer...

journal_title：Journal of pharmaceutical sciences

authors： Hamdy DA,Brocks DR

更新日期：2011-11-01 00:00:00

abstract：:Recent studies have clearly demonstrated that Fourier transform IR spectroscopy can be a powerful tool for the study of protein stabilization during freeze-drying and for optimizing approaches to prevent lyophilization-induced protein aggregation. The purpose of the current review is to provide an overview of these to...

journal_title：Journal of pharmaceutical sciences

authors： Dong A,Prestrelski SJ,Allison SD,Carpenter JF

更新日期：1995-04-01 00:00:00

abstract：:Insulin-degrading enzyme (IDE) has been implicated in the intracellular degradation of insulin in insulin target cells. Knowledge of the existence of this enzyme in the intestine will be beneficial to the achievement of clinical oral efficacy of insulin. A comparative study was conducted with rat intestine, human colo...

journal_title：Journal of pharmaceutical sciences

authors： Chang LL,Stout LE,Wong WD,Buls JG,Rothenberger DA,Shier WT,Sorenson RL,Bai JP

更新日期：1997-01-01 00:00:00

abstract：:The objective of this article was to monitor phase transformation in thiamine hydrochloride, from a nonstoichiometric hydrate (NSH) to a hemihydrate (HH), in stored tablets, prepared both by direct compression and wet granulation, and to relate the storage-induced phase transformation with changes in tablet microstruc...

journal_title：Journal of pharmaceutical sciences

authors： Chakravarty P,Suryanarayanan R,Govindarajan R

更新日期：2012-04-01 00:00:00

abstract：:Isothermal crystallization of amorphous nifedipine, phenobarbital, and flopropione was studied at temperatures above and below their glass transition temperatures (T(g)). A sharp decrease in the crystallization rate with decreasing temperature was observed for phenobarbital and flopropione, such that no crystallizatio...

journal_title：Journal of pharmaceutical sciences

authors： Aso Y,Yoshioka S,Kojima S

更新日期：2000-03-01 00:00:00

abstract：:A characterization and optimization of the in vitro transdermal iontophoretic transport of 5-hydroxy-2-(N,N,-di-n-propylamino)tetralin (5-OH-DPAT) is presented. The utility of acetaminophen as a marker of electroosmotic flow was studied as well. The following parameters of iontophoretic transport of 5-OH-DPAT were exa...

journal_title：Journal of pharmaceutical sciences

authors： Ackaert OW,Van Smeden J,De Graan J,Dijkstra D,Danhof M,Bouwstra JA

更新日期：2010-01-01 00:00:00

abstract：:The recombinant fusion proteins hybrid 1 [H1 (Ag85B-ESAT-6)] and hybrid 56 [H56 (Ag85B-ESAT-6-Rv2660c)] derived from Mycobacterium tuberculosis are promising antigens for subunit vaccines against tuberculosis. Both antigens are early batches of antigens to be enrolled in human clinical trials and it is therefore impor...

journal_title：Journal of pharmaceutical sciences

authors： Hamborg M,Kramer R,Schanté CE,Agger EM,Christensen D,Jorgensen L,Foged C,Middaugh CR

更新日期：2013-10-01 00:00:00

abstract：:Eight analogs of the fentanyl-type analgesics, in which the piperidine ring is restricted into a boat conformation, were evaluated for analgesic activity. All analogs were less active than fentanyl, but interesting conformational and structural relationships were observed. Results of the study are discussed. ...

journal_title：Journal of pharmaceutical sciences

authors： Borne RF,Law SJ,Kapeghian JC,Masten LW

更新日期：1980-09-01 00:00:00

abstract：:Stability of the 1,3,5-triazine derivative (1), a corticotropin-releasing factor inhibitor, was studied in acidic solutions and in solid formulations. Degradant structures were elucidated using liquid chromatography/mass spectrometry (LC/MS) and nuclear magnetic resonance (NMR). Compound 1 was found to undergo hydroly...

journal_title：Journal of pharmaceutical sciences

authors： Badawy S,Hussain M,Zhao F,Ye Q,Huang Y,Palaniswamy V

更新日期：2009-08-01 00:00:00

abstract：:3,6-Diformyl- and 3,6-dipropanoylmorphine and 6-formyl- and 6-propanoylmorphine were prepared to obtain longer acting, heroin-like compounds. The 6-acylated compounds were more potent than heroin subcutaneously and were orally effective, and their duration of action was at least two to three times greater than that of...

journal_title：Journal of pharmaceutical sciences

authors： May EL,Jacobson AE

更新日期：1977-02-01 00:00:00

abstract：:A modified NF method for the quantitative determination of pentaerythritol tetranitrate is reported. A solution of powder is made directly from the dosage form in glacial acetic acid and is then reacted with phenoldisulfonic acid TS. The proposed method saves approximately 75% of the time required with the NF method. ...

journal_title：Journal of pharmaceutical sciences

authors： Gupta VD

更新日期：1978-05-01 00:00:00

abstract：:Three series of 3,4,5-trisubstituted pyrazolesulfonylurea derivatives were prepared and evaluated as hypoglycemic agents. Preliminary biological testing revealed that the new compounds possess moderate hypoglycemic activity. ...

journal_title：Journal of pharmaceutical sciences

authors： Soliman R,Mokhtar H,Mohamed HF

更新日期：1983-09-01 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：:Both nonequilibrium and equilibrium models were proposed to explain the optimal biological response to a set of congeners with respect to the oil-water partition coefficient (P). A detailed analysis of the kinetic model proposed by Hansch demonstrates the bilinear form of the model, with the initial slope of the logar...

journal_title：Journal of pharmaceutical sciences

authors： Cooper ER,Berner B,Bruce RD

更新日期：1981-01-01 00:00:00

abstract：:Statistical assessment of bioavailability and bioequivalence of drug products is generally carried out with a univariate analysis by independently comparing each relevant parameter [such as, area under the drug concentration curve (AUC) and peak drug concentration (Cmax)] of the test and reference products. The assump...

journal_title：Journal of pharmaceutical sciences

authors： Hsu HC,Lu HL,Chan KK

更新日期：1995-06-01 00:00:00

abstract：:Porcine gelatins have been widely used as stabilizers of macromolecular based pharmaceuticals but the mechanism by which they stabilize has not been precisely established. Their variability and immunogenicity, however, make them less than ideal excipients. In this work, we take advantage of the availability of recombi...

journal_title：Journal of pharmaceutical sciences

authors： Thyagarajapuram N,Olsen D,Middaugh CR

更新日期：2007-12-01 00:00:00

abstract：:The presence of subvisible particles in formulations of therapeutic proteins is a risk factor for adverse immune responses. Although the immunogenic potential of particulate contaminants likely depends on particle structural characteristics (e.g., composition, size, and shape), exact structure-immunogenicity relations...

journal_title：Journal of pharmaceutical sciences

authors： Daniels AL,Randolph TW

更新日期：2018-05-01 00:00:00

abstract：:First-order rate constants (k) were determined for the hydrolysis of ceftazidime in the pH range of 0.5 to 8.5 at 45, 55, and 65 degrees C by a stability-indicating HPLC assay. In the absence of buffer effects, the pH-rate expression was k = kH1f1(aH+) + kH2f2(aH+) + kH3f3(aH+) + kSf3 + kOHf3(aOH-), where KH and KOH a...

journal_title：Journal of pharmaceutical sciences

authors： Zhou M,Notari RE

更新日期：1995-05-01 00:00:00

abstract：:Approximately 30% of active pharmaceutical ingredients (APIs) experience agglomeration, granulation, and breakage during agitated drying. Currently, there is no small-scale bench tool to help assess and observe granulation behavior of APIs in the laboratory and subsequently lead to the development of a robust drying m...

journal_title：Journal of pharmaceutical sciences

authors： Zhang S,Lamberto DJ

更新日期：2014-01-01 00:00:00

abstract：:Single-dose oral administration of a commercial polychlorinated biphenyl product containing 54% chlorine provided data with which to plot the time course of total polychlorinated biphenyl and individual components in the blood of swine and sheep. Pharmacokinetic parameters describing absorption from the gut and elimin...

journal_title：Journal of pharmaceutical sciences

authors： Borchard RE,Welborn ME,Wiekhorst WB,Wilson DW,Hansen LG

更新日期：1975-08-01 00:00:00

abstract：:Near-infrared spectroscopy was used to monitor the phase conversion for two solvatomorphs of caffeine, an anhydrous form and a nonstoichiometric hydrate, as a function of time, temperature, and relative humidity. The transformation kinetics between these caffeine forms was determined to increase with temperature. The ...

journal_title：Journal of pharmaceutical sciences

authors： Krzyzaniak JF,Williams GR,Ni N

更新日期：2007-05-01 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：:Near infrared (NIR) spectroscopy was used for quantitatively monitoring polymorph conversion of an active pharmaceutical ingredient (API) in wet granulation. The API under pharmaceutical development has two different polymorphs. Polymorph A is the stable form for drug development and polymorph B is the undesired form ...

journal_title：Journal of pharmaceutical sciences

authors： Li W,Worosila GD,Wang W,Mascaro T

更新日期：2005-12-01 00:00:00

abstract：:Vaults, at 13 MDa, are the largest ribonucleoprotein particles known. In vitro, expression of the major vault protein (MVP) alone in Sf9 insect cells results in the production of recombinant particles with characteristic vault structure. With the ultimate goal of using recombinant vaults as nanocapsules for the delive...

journal_title：Journal of pharmaceutical sciences

authors： Esfandiary R,Kickhoefer VA,Rome LH,Joshi SB,Middaugh CR

更新日期：2009-04-01 00:00:00

abstract：:2 closely related prostaglandins (PGs), A2 and B2, were separated by ion-exchange liquid chromatography. PGA2 and PGB2 are an isomeric pair of PGs which show little resolution on thin-layer chromatography; the pair can be resolved as gas-liquid chromatography, but use of this method requires protection of the C9-carb...

journal_title：Journal of pharmaceutical sciences

authors： Morozowich W

更新日期：1974-05-01 00:00:00

abstract：:A number of biopharmaceuticals are available as lyophilized formulations along with a prefilled syringe (PFS) containing water for injection (WFI). Submicron- and micron-size droplets of lubricating silicone oil (SO) applied to the inner surface of the PFS barrel might migrate into the WFI, to which protein pharmaceut...

journal_title：Journal of pharmaceutical sciences

authors： Krayukhina E,Yokoyama M,Hayashihara KK,Maruno T,Noda M,Watanabe H,Uchihashi T,Uchiyama S

更新日期：2019-07-01 00:00:00

abstract：:Tritium-labeled progesterone was administered to mature female rats in the proestrous stage by three different routes, gastric intubation, subcutaneous injection, and uterine intraluminal instillation, to study the kinetics involved in the uptake and retention of radioactivity by the uterus and various other tissues. ...

journal_title：Journal of pharmaceutical sciences

authors： Fang SM,Lin CS,Lyon V

更新日期：1977-12-01 00:00:00

abstract：:Respirable crystals of cromoglycic acid (CA) were prepared by precipitation of CA with hydrochloric acid from aqueous solutions of cromolyn sodium and subsequent recrystallization from hot water or mixtures of dimethyl sulphoxide and water. The properties of the materials were established by melting point measurements...

journal_title：Journal of pharmaceutical sciences

authors： Chan HK,Gonda I

更新日期：1989-02-01 00:00:00

abstract：:The objective of this study was to generate a water-soluble thiolated chitosan to enable the permeation-enhancing effect of chitosan at pH of at least 5.5 without losing the advantages of improved mucoadhesive properties. Therefore, the thiol-bearing polyoxyethylene ligand {O-(3-carboxylpropyl)-O'-[2-[3-mercaptopropio...

journal_title：Journal of pharmaceutical sciences

authors： Hauptstein S,Bonengel S,Griessinger J,Bernkop-Schnürch A

更新日期：2014-02-01 00:00:00

abstract：:(+-)-Carbovir [(+-)-9-[4 alpha-(hydroxymethyl)-cyclopent-2-ene-1 alpha-yl]guanine; NSC 614846] is a novel carbocyclic nucleoside analogue which has been shown to be a potent and selective inhibitor of HIV in vitro. As part of an effort to develop a parenteral formulation for subsequent clinical and toxicological evalu...

journal_title：Journal of pharmaceutical sciences

authors： Anderson BD,Chiang CY

更新日期：1990-09-01 00:00:00