Effects of variation in drug elimination on five methods for assessing zero-order drug absorption rates.

abstract：PURPOSE:Chemically modified heparin-DOCA was prepared and found to have markedly lower anticoagulant activity than heparin. In the present study, we elucidated the antiangiogenic and antitumoral activities of heparin-DOCA derivative. METHODS:To evaluate the antiangiogenic and antitumoral effects of heparin-DOCA, capil...

journal_title：Pharmaceutical research

authors： Park K,Kim YS,Lee GY,Nam JO,Lee SK,Park RW,Kim SY,Kim IS,Byun Y

更新日期：2007-01-01 00:00:00

abstract：:Molecular dynamics simulations and the generation of ad hoc chemical libraries are playing an increasingly important and recognized role in structure-based virtual screening. These approaches are important for treating target flexibility and improving the drug discovery pipeline. In this article I will comment on thes...

journal_title：Pharmaceutical research

authors： Rastelli G

更新日期：2013-05-01 00:00:00

abstract：:The pharmacokinetics of 2',3'-dideoxyinosine (ddI) were examined in rats given intravenous doses of 8, 40, or 200 mg/kg. The concentrations of ddI in whole blood and plasma were identical. The concentration decline was multiexponential, with mean half-lives of 2 and 20 min for the first and second phases, respectively...

journal_title：Pharmaceutical research

authors： Wientjes MG,Mukherji E,Au JL

更新日期：1992-08-01 00:00:00

abstract：PURPOSE:The possibility of direct delivery of steroids through the skin to the trachea and the effect of iontophoresis on delivery efficacy were evaluated after the application of an ionic steroidal prodrug, prednisolone sodium succinate (PS-Na), to the throat skin. METHODS:Fluorescein sodium salt (FL-Na) and PS-Na we...

journal_title：Pharmaceutical research

authors： Ishii H,Suzuki T,Todo H,Kamimura M,Sugibayashi K

更新日期：2011-04-01 00:00:00

abstract：PURPOSE:The aim of this study was to investigate whether biodegradable nanocapsules could be obtained by the emulsification-diffusion technique. METHODS:This technique consists of emulsifying an organic solution containing an oil, a polymer, and a drug in an aqueous solution of a stabilizing agent. The subsequent addi...

journal_title：Pharmaceutical research

authors： Quintanar-Guerrero D,Allémann E,Doelker E,Fessi H

更新日期：1998-07-01 00:00:00

abstract：:Chimeric L6 is a mouse-human monoclonal antibody specific for tumor cell-associated antigens. The factors affecting the physical and chemical stability of chimeric L6 were assessed at elevated temperatures (30-60 degrees C) and by multiple freezing and thawing. Three routes of degradation were observed: chemical degra...

journal_title：Pharmaceutical research

authors： Paborji M,Pochopin NL,Coppola WP,Bogardus JB

更新日期：1994-05-01 00:00:00

abstract：PURPOSE:Chitosan and its derivatives possess several unique properties relevant in the field of pharmaceutics and medicinal chemistry. This study aimed to evaluate the pharmaceutical performance of an innovative chitosan derivative, methyl acrylate chitosan bearing p-nitrobenzaldehyde (MA*CS*pNBA) Schiff base. METHODS...

journal_title：Pharmaceutical research

authors： Ali SS,Kenawy ER,Sonbol FI,Sun J,Al-Etewy M,Ali A,Huizi L,El-Zawawy NA

更新日期：2018-11-07 00:00:00

abstract：:Despite substantial research carried out over the last decades, it remains difficult to understand the wide range of pharmacological effects of dopaminergic agents. The dopaminergic system is involved in several neurological disorders, such as Parkinson's disease and schizophrenia. This complex system features multipl...

journal_title：Pharmaceutical research

authors： van den Brink WJ,Palic S,Köhler I,de Lange ECM

更新日期：2018-02-15 00:00:00

abstract：PURPOSE:To investigate, for the first time, the performance of a dry powder inhaler (DPI, Aerolizer(®)) in the case of a model drug (i.e. albuterol sulphate) formulated with spray dried mannitol carrier particles with homogeneous shape and solid-state form but different sizes. METHODS:Spray dried mannitol (SDM) partic...

journal_title：Pharmaceutical research

authors： Kaialy W,Hussain T,Alhalaweh A,Nokhodchi A

更新日期：2014-01-01 00:00:00

abstract：:The mechanical properties of dry and wet polymeric films prepared from various aqueous polymeric dispersions were evaluated by a puncture test. They were studied with respect to type of polymer dispersion [cellulosic: Aquacoat and Surelease; acrylic: Eudragit NE, L, RS, and RL 30 D], plasticizer type (water-soluble or...

journal_title：Pharmaceutical research

authors： Bodmeier R,Paeratakul O

更新日期：1994-06-01 00:00:00

abstract：:Emulsions (o/w) were prepared from solid-state emulsions comprised of various matrix materials and oils and the resultant particle size properties determined. Results suggest that for those matrices that can form solid-state emulsions, the droplet size decreased as a function of time, as previously observed. The final...

journal_title：Pharmaceutical research

authors： Shively ML

更新日期：1993-08-01 00:00:00

abstract：PURPOSE:The possibility of preparing nanoparticles in the supercooled thermotropic liquid crystalline state from cholesterol esters with saturated acyl chains as well as the incorporation of model drugs into the dispersions was investigated using cholesteryl myristate (CM) as a model cholesterol ester. METHODS:Nanopar...

journal_title：Pharmaceutical research

authors： Kuntsche J,Westesen K,Drechsler M,Koch MH,Bunjes H

更新日期：2004-10-01 00:00:00

abstract：:Published permeability coefficient (Kp) data for the transport of a large group of compounds through mammalian epidermis were analyzed by a simple model based upon permeant size [molecular volume (MV) or molecular weight (MW)] and octanol/water partition coefficient (Koct). The analysis presented is a facile means to ...

journal_title：Pharmaceutical research

authors： Potts RO,Guy RH

更新日期：1992-05-01 00:00:00

abstract：PURPOSE:Cationic host defence peptides constitute a promising class of therapeutic drug leads with a wide range of therapeutic applications, including anticancer therapy, immunomodulation, and antimicrobial activity. Although potent and efficacious, systemic toxicity and low chemical stability have hampered their comme...

journal_title：Pharmaceutical research

authors： Water JJ,Kim Y,Maltesen MJ,Franzyk H,Foged C,Nielsen HM

更新日期：2015-08-01 00:00:00

abstract：PURPOSE:This study aimed to investigate the impact of the size of X-ray iodinated contrast agent in nano-emulsions, on their toxicity and fate in vivo. METHODS:A new compound, triiodobenzoate cholecalciferol, was synthetized, formulated as nano-emulsions, and followed after i.v. administration in mice by X-ray imaging...

journal_title：Pharmaceutical research

authors： Attia MF,Anton N,Akasov R,Chiper M,Markvicheva E,Vandamme TF

更新日期：2016-03-01 00:00:00

abstract：PURPOSE:To test the hypothesis that coating particles with a highly bonding polymer is effective in improving tabletability of poorly compressible drugs. METHODS:Micronized acetaminophen (d (90) < 10 μm, Form I) was coated with 1%-10% (wt%) hydroxypropyl cellulose (HPC) by spray-drying. Phase nature of acetaminophen p...

journal_title：Pharmaceutical research

authors： Shi L,Sun CC

更新日期：2011-12-01 00:00:00

abstract：:The influence of varying protein and fat content in milk of New Zealand White rabbits on the milk-to-plasma drug concentration (M/P) ratio of diazepam was studied. At various time points after littering, a bolus dose (1.5 mg/kg) followed by a 26-hr infusion (1.8 mg/h) of diazepam was administered to freely moving rabb...

journal_title：Pharmaceutical research

authors： Stebler T,Guentert TW

更新日期：1992-10-01 00:00:00

abstract：:One thousand milligrams of aspirin, as its lysine salt was administered intravenously, orally, and intramuscularly to nine male and nine female young healthy adult volunteers. After intravenous injection mean (+/- SD) values of clearance, steady-state volume of distribution, and terminal half-life were 12.2 +/- 2.2 ml...

journal_title：Pharmaceutical research

authors： Aarons L,Hopkins K,Rowland M,Brossel S,Thiercelin JF

更新日期：1989-08-01 00:00:00

abstract：:The transport characteristics of the renin inhibitor ((3S,4S)-4-[N-morpholinoacetyl-(1-naphthyl)-L-alanyl-N-methyl-(4-t hiazolyl)-L- alanyl]amino-3-hydroxy-5-cyclohexyl-1-(4-pyridyl)-1-pentanone; CH3-18) in rat small intestinal brush-border membrane vesicles (BBMV) were examined by a rapid filtration technique. The up...

journal_title：Pharmaceutical research

authors： Hashimoto N,Fujioka T,Toyoda T,Muranushi N,Hirano K

更新日期：1994-10-01 00:00:00

abstract：PURPOSE:The purpose of this study was to assess the effect of several chemical permeation enhancers on the buccal permeability of nicotine and to image the spatial distribution of nicotine in buccal mucosa with and without buccal permeation enhancers. METHODS:The impact of sodium taurodeoxycholate (STDC), sodium dodec...

journal_title：Pharmaceutical research

authors： Marxen E,Jin L,Jacobsen J,Janfelt C,Hyrup B,Nicolazzo JA

更新日期：2018-02-21 00:00:00

abstract：PURPOSE:The aim of this study was to examine if sparging with CO2(g) could be used to establish stable biorelevant bicarbonate buffers, in aqueous medium, for use in dissolution characterization of low-solubility ionizable drugs. METHODS:Preparation of the bicarbonate-containing dissolution medium was monitored by use...

journal_title：Pharmaceutical research

authors： McNamara DP,Whitney KM,Goss SL

更新日期：2003-10-01 00:00:00

abstract：PURPOSE:Recent studies have demonstrated the potential for a triglyceride (TG) mimetic prodrug to promote the delivery of mycophenolic acid (MPA) to the lymphatic system. Here, the metabolic pathways that facilitate the lymphatic transport of the TG prodrug (1,3-dipalmitoyl-2-mycophenoloyl glycerol, 2-MPA-TG) were exam...

journal_title：Pharmaceutical research

authors： Han S,Hu L,Quach T,Simpson JS,Trevaskis NL,Porter CJ

更新日期：2015-05-01 00:00:00

abstract：PURPOSE:The aim of this study was to identify new surfactants with low skin irritant properties for use in pharmaceutical and cosmetic formulations, employing cell culture as an alternative method to in vivo testing. In addition, we sought to establish whether potential cytotoxic properties were related to the size of ...

journal_title：Pharmaceutical research

authors： Sanchez L,Mitjans M,Infante MR,Vinardell MP

更新日期：2004-09-01 00:00:00

abstract：:Primaquine, an 8-aminoquinoline antimalarial, is shown to undergo unexpectedly rapid aromatic proton exchange with the medium. At a pH less than 4, the exchange of C-5 is so fast as to be unmeasurable by proton nmr methods. At a pH of 6-6.5 the half-time for exchange is 4 to 5 minutes. This unexpectedly high rate of e...

journal_title：Pharmaceutical research

authors： McChesney JD,Sarangan S

更新日期：1984-07-01 00:00:00

abstract：PURPOSE:At elevated temperatures, the rate of drug release and skin permeation from transdermal delivery systems (TDS) may be higher than at a normal skin temperature. The aim of this study was to compare the effect of heat on the transdermal delivery of two model drugs, nicotine and fentanyl, from matrix-type TDSs wit...

journal_title：Pharmaceutical research

authors： Shin SH,Ghosh P,Newman B,Hammell DC,Raney SG,Hassan HE,Stinchcomb AL

更新日期：2017-09-01 00:00:00

abstract：:The immune system has the ability to recognize and kill pre-cancer and cancer cells. However, with the immune system's surveillance, the survival tumor cells learn how to escape the immune system after immunoselection. Cancer immunotherapy develops strategies to overcome these problems. Nanomedicine applications in ca...

journal_title：Pharmaceutical research

authors： Sheng WY,Huang L

更新日期：2011-02-01 00:00:00

abstract：PURPOSE:The trial-and-error approach is still predominantly used in pharmaceutical development of nanosuspensions. Physicochemical dispersion stability is a primary focus and therefore, various analytical bulk methods are commonly employed. Clearly less attention is directed to surface changes of nanoparticles even tho...

journal_title：Pharmaceutical research

authors： Aleandri S,Schönenberger M,Niederquell A,Kuentz M

更新日期：2018-02-21 00:00:00

abstract：PURPOSE:4-Phenylbutyrate (4-PBA) is expected to be a potential therapeutic for several neurodegenerative diseases. These activities require 4-PBA transport into the brain across the blood-brain barrier (BBB). The objective of the present study was to characterize the brain transport mechanism of 4-PBA through the BBB. ...

journal_title：Pharmaceutical research

authors： Lee NY,Kang YS

更新日期：2016-07-01 00:00:00

abstract：PURPOSE:Cationic liposomes are expected to be useful as nonviral vectors for gene delivery. Cationic liposomes showed cytotoxicity, and we proposed that the cytotoxicity is through apoptosis. In this study, we examined the effects of liposomal properties, such as liposomal charge, size, membrane fluidity, and PEG coati...

journal_title：Pharmaceutical research

authors： Takano S,Aramaki Y,Tsuchiya S

更新日期：2003-07-01 00:00:00

abstract：:Using brine shrimp lethality to direct fractionation, extracts of the bark of Annona bullata Rich. (Annonaceae) have yielded 16 alpha-hydroxy-(-)-kauranoic acid as a bioactive plant constituent. This previously known diterpene showed significant (ED50 8.25 x 10(-2) micrograms/ml) and selective cytotoxicity against A-5...

journal_title：Pharmaceutical research

authors： Hui YH,Chang CJ,Smith DL,McLaughlin JL

更新日期：1990-04-01 00:00:00