Pharmacokinetics and bioinversion of ibuprofen enantiomers in humans.

abstract：PURPOSE:We recently developed prostaglandin E(1) (PGE(1))-encapsulated nanoparticles, prepared with a poly(lactide) homopolymer (PLA, Mw = 17,500) and monomethoxy poly(ethyleneglycol)-PLA block copolymer (PEG-PLA) (NP-L20). In this study, we tested whether the accelerated blood clearance (ABC) phenomenon is observed wi...

journal_title：Pharmaceutical research

authors： Ishihara T,Takeda M,Sakamoto H,Kimoto A,Kobayashi C,Takasaki N,Yuki K,Tanaka K,Takenaga M,Igarashi R,Maeda T,Yamakawa N,Okamoto Y,Otsuka M,Ishida T,Kiwada H,Mizushima Y,Mizushima T

更新日期：2009-10-01 00:00:00

abstract：PURPOSE:Chitosan-based polymeric micelles (CBPMs) are considered as promising carriers for delivery of anticancer drugs, imaging agents and genes. To optimize the physicochemical, pharmaceutical and biological properties of CBPMs, the molecular mechanisms behind the self-assembly behavior of chitosan (CHI) amphiphilic ...

journal_title：Pharmaceutical research

authors： Mahmoudzadeh M,Fassihi A,Dorkoosh F,Heshmatnejad R,Mahnam K,Sabzyan H,Sadeghi A

更新日期：2015-12-01 00:00:00

abstract：PURPOSE:To investigate in vitro if P-glycoprotein (P-gp) transport can differentiate between antibiotic drugs exhibiting increased active renal clearance (CL(r)) in cystic fibrosis (CF) patients (i.e., dicloxacillin, trimethoprim) and drugs that do not exhibit this phenomenon (i.e.. cefsulodin, sulfamethoxazole). METH...

journal_title：Pharmaceutical research

authors： Susanto M,Benet LZ

更新日期：2002-04-01 00:00:00

abstract：PURPOSE:Highly lipophilic basic drugs, the antiestrogens AE 1 (log P = 5.82) and AE 2 (log P = 7.8) shall be delivered transdermally. METHODS:Transdermal permeation of drugs, enhancers, and solvents from various fluid formulations were characterized by in-vitro permeation studies through excised skin of hairless mice....

journal_title：Pharmaceutical research

authors： Funke AP,Schiller R,Motzkus HW,Günther C,Müller RH,Lipp R

更新日期：2002-05-01 00:00:00

abstract：:Pediatric brain tumors are most common cancers in childhood and among the leading causes of death in children. Chemotherapy has been used as adjuvant (i.e. after) or neoadjuvant (i.e. before) therapy to surgery and radiotherapy for the management of pediatric brain tumors for more than four decades and gained more att...

journal_title：Pharmaceutical research

authors： Wu L,Li X,Janagam DR,Lowe TL

更新日期：2014-03-01 00:00:00

abstract：PURPOSE:To develop a semi-physiological-based model describing simultaneously the time course of immature and mature B-lymphocytes after topotecan (TPT) administration to tumor-bearing rats. METHODS:Twenty-four tumor-bearing BDIX male rats received a single 6 mg/kg intra-peritoneal dose of TPT or saline. Mature and im...

journal_title：Pharmaceutical research

authors： Vélez de Mendizábal N,Martínez-Forero I,Garrido MJ,Bandrés E,García-Foncillas J,Segura C,Trocóniz IF

更新日期：2010-03-01 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：PURPOSES:To evaluate the effects of component contents in different colistin methanesulfonate (CMS) formulas on their clinical pharmacokinetics of the prodrug CMS and the formed colistin. METHODS:Two CMS formulas (CTTQ and Parkedale) were investigated in a single dose, randomized, open-label, crossover study conducted...

journal_title：Pharmaceutical research

authors： Fan YX,Chen YC,Li Y,Yu JC,Bian XC,Li X,Li WZ,Guo BN,Wu HL,Liu XF,Wang Y,Xu XY,Hu JL,Wang JJ,Wu XJ,Cao GY,Wu JF,Xue CJ,Feng J,Zhang YY,Zhang J

更新日期：2021-01-26 00:00:00

abstract：PURPOSE:The long-term stability and nasal absorption characteristics of a basic nasal formulation of azetirelin, a thyrotropin-releasing hormone analog and its absorption enhancement by incorporation of acylcarnitines in the formulation were investigated. METHODS:The long-term stability of basic nasal azetirelin formu...

journal_title：Pharmaceutical research

authors： Kagatani S,Inaba N,Fukui M,Sonobe T

更新日期：1998-01-01 00:00:00

abstract：PURPOSE:The relationship between rat intestinal permeability (Papp) of a range of hydrophilic probe molecules and probe geometry was examined. METHODS:Molecules studies included mannitol, the polyethylene glycols (PEGs) 400, 900, and 4000, the dextran conjugated dye Texas Red (MW 3000) and the polysaccharide inulin (M...

journal_title：Pharmaceutical research

authors： Lane ME,O'Driscoll CM,Corrigan OI

更新日期：1996-10-01 00:00:00

abstract：PURPOSE:To analyze the mechanics of some pharmaceutical agglomerates during uniaxial confined compression by using compression parameters derived from the Heckel, Kawakita and Adams equations, and to study the influence of these compression parameters on the tablet-forming ability of agglomerates. METHODS:Force and di...

journal_title：Pharmaceutical research

authors： Nicklasson F,Alderborn G

更新日期：2000-08-01 00:00:00

abstract：PURPOSE:The described structure pharmacokinetic pharmacodynamic relationships (SPPR) study explored the utilization of tetramethylcyclopropane analogues of valpromide (VPD), or tetramethylcyclopropane carboxamide derivatives of valproic acid (VPA) as new antiepileptics. METHODS:The study was carried out by investigati...

journal_title：Pharmaceutical research

authors： Bialer M,Hadad S,Kadry B,Abdul-Hai A,Haj-Yehia A,Sterling J,Herzig Y,Yagen B

更新日期：1996-02-01 00:00:00

abstract：PURPOSE:The objective of this study is to evaluate the feasibility of using coated microneedles to deliver vaccines into the oral cavity to induce systemic and mucosal immune responses. METHOD:Microneedles were coated with sulforhodamine, ovalbumin and two HIV antigens. Coated microneedles were inserted into the inner...

journal_title：Pharmaceutical research

authors： Ma Y,Tao W,Krebs SJ,Sutton WF,Haigwood NL,Gill HS

更新日期：2014-09-01 00:00:00

abstract：PURPOSE:The gastric mucoadhesive property of tetracycline-sucralfate acidic complex (CO) was evaluated by using a novel method in vitro to compare with the in vivo test. The mucoadhesive mechanism of the acidic complex was also studied. METHODS:The gastric mucosa removed from a rat was placed covering the end of a plu...

journal_title：Pharmaceutical research

authors： Higo S,Ori K,Takeuchi H,Yamamoto H,Hino T,Kawashima Y

更新日期：2004-03-01 00:00:00

abstract：PURPOSE:The objective of the present work was to prepare safe and effective Ciclosporin A Lipid nanocapsule (CsA-LNC) eye-drops for the treatment of DED. METHODS:The phase-inversion method was used to prepared different sizes CsA-LNC. CsA biodistribution in ocular after topical administration in rabbits was analyzed b...

journal_title：Pharmaceutical research

authors： Zhang A,Sun R,Ran M,Deng Y,Ge Y,Zhu Y,Tao X,Shang L,Gou J,He H,Yin T,Wang Y,Zhang Y,Tang X

更新日期：2020-07-14 00:00:00

abstract：PURPOSE:To produce and characterize a nonviral ultrasound-controlled release system of plasmid DNA (pDNA) encapsulated in gas-filled poly(D,L-lactide-co-glycolide) microparticles (PLGA-MPs). METHODS:Different cationic polymers were used to form pDNA/polymer complexes to enhance the stability of pDNA during micropartic...

journal_title：Pharmaceutical research

authors： Seemann S,Hauff P,Schultze-Mosgau M,Lehmann C,Reszka R

更新日期：2002-03-01 00:00:00

abstract：PURPOSE:To compare the systemic delivery of deslorelin following intratracheal administration of different deslorelin formulations. The formulations included dry powders of deslorelin, large-porous deslorelin-poly(lactide-co-glycolide) (PLGA) particles, and small conventional deslorelin-PLGA particles. Also, solution f...

journal_title：Pharmaceutical research

authors： Koushik K,Dhanda DS,Cheruvu NP,Kompella UB

更新日期：2004-07-01 00:00:00

abstract：PURPOSE:This study examined the rheological and textural characteristics (hardness, compressibilty, adhesiveness and cohesiveness) of bioadhesive oral gels containing the antimicrobial agent chlorhexidine. METHODS:Textural analysis was performed using a Stable Micro Systems texture analyser (model TA-XT 2) in texture ...

journal_title：Pharmaceutical research

authors： Jones DS,Woolfson AD,Brown AF

更新日期：1997-04-01 00:00:00

abstract：PURPOSE:This prospective study aimed to evaluate the effects of genetic polymorphisms in sulindac-related metabolizing enzyme genes including FMO3 and AOX1 on the population pharmacokinetics of sulindac in 58 pregnant women with preterm labor. METHODS:Plasma samples were collected at 1.5, 4, and 10 h after first oral ...

journal_title：Pharmaceutical research

authors： Sung JW,Yun HY,Park S,Kim YJ,Yee J,Lee KE,Song B,Chung JE,Gwak HS

更新日期：2020-01-28 00:00:00

abstract：:A number of substituted phthalimide, 1, 8-naphthalimide, succinimide and glutarimide derivatives demonstrated significant hypolipidemic activity at 20 mg/kg/ day, I.P. after 16 days dosing. The N-(n-pentyl) succinimide proved to be the most potent analogue of the new compounds, lowering serum triglyceride levels 51 % ...

journal_title：Pharmaceutical research

authors： Chapman JM Jr,Wyrick SD,Maguire JH,Cocolas GH,Hall IH

更新日期：1984-11-01 00:00:00

abstract：PURPOSE:To characterize factor(s) contained in apical medium of primary cultured rat alveolar epithelial type II cell-like monolayers (RAECM-II) that enhance insulin absorption across alveolar epithelial cells. MATERIALS AND METHODS:Primary rat alveolar epithelial cell monolayers cultured on Transwells in the presence...

journal_title：Pharmaceutical research

authors： Bahhady R,Kim KJ,Borok Z,Crandall ED,Shen WC

更新日期：2007-09-01 00:00:00

abstract：PURPOSE:To develop a semi-distributed liver model for the evaluation of saturable sinusoidal uptake and binding kinetics of the Oatp1a4 substrate digoxin. METHODS:In the perfused rat liver, two successive digoxin doses of 42 and 125 microg were administered, and the outflow concentration was determined by LC/MS/MS. [1...

journal_title：Pharmaceutical research

authors： Weiss M,Li P,Roberts MS

更新日期：2010-09-01 00:00:00

abstract：:Diltiazem (DTZ) is a calcium channel blocker widely used in the treatment of angina and hypertension. DTZ undergoes extensive metabolism yielding several metabolites, some of which are active like N-desmethyldiltiazem (MA), desacetyldiltiazem (M1) and N-desmethyl,desacetyldiltiazem (M2). Due to the nature of its biotr...

journal_title：Pharmaceutical research

authors： Homsy W,Lefebvre M,Caillé G,du Souich P

更新日期：1995-04-01 00:00:00

abstract：PURPOSE:The sensitivity and effectiveness of indirect metrics proposed for the assessment of comparative absorption rates in bioequivalence studies [Cmax, Tmax, partial AUC (AUCp), feathered slope (SLf), intercept metric (I)] were originally tested by assuming first-order absorption. The present study re-evaluates thei...

journal_title：Pharmaceutical research

authors： Ring A,Tothfalusi L,Endrenyi L,Weiss M

更新日期：2000-05-01 00:00:00

abstract：PURPOSE:Simvastatin (SIM), a HMG-CoA reductase inhibitor widely prescribed for hypercholesterolemia, has been reported to ameliorate inflammation and promote osteogenesis. Its clinical applications on these potential secondary indications, however, have been hampered by its lack of osteotropicity and poor water solubil...

journal_title：Pharmaceutical research

authors： Wang X,Jia Z,Almoshari Y,Lele SM,Reinhardt RA,Wang D

更新日期：2018-06-25 00:00:00

abstract：PURPOSE:To investigate the suitability of three antimicrobial peptides (AMPs) as cell-penetrating antimicrobial peptides. METHODS:Cellular uptake of three AMPs (PK-12-KKP, SA-3 and TPk) and a cell-penetrating peptide (penetratin), all 5(6)-carboxytetramethylrhodamine-labeled, were tested in HeLa WT cells and analyzed ...

journal_title：Pharmaceutical research

authors： Bahnsen JS,Franzyk H,Sayers EJ,Jones AT,Nielsen HM

更新日期：2015-05-01 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

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：:The three-dimensional structures and molecular electrostatic potentials of the cis(Z) and trans(E)-isomers of flupenthixol and clopenthixol were examined by computer graphics and molecular mechanical and quantum mechanical calculations, and their internal molecular motions were studied by molecular dynamics simulation...

journal_title：Pharmaceutical research

authors： Sylte I,Dahl SG

更新日期：1991-04-01 00:00:00

abstract：PURPOSE:To examine the inhibitory potential of enalapril [and other angiotensin converting enzyme (ACE) inhibitors] on glycylsarcosine (GlySar) transport by the high-affinity renal peptide transporter. METHODS:Studies were performed in rabbit renal brush border membrane vesicles in which the uptake of radiolabeled Gly...

journal_title：Pharmaceutical research

authors： Lin CJ,Akarawut W,Smith DE

更新日期：1999-05-01 00:00:00