Poly(lactide-co-glycolide) nanocapsules containing benzocaine: influence of the composition of the oily nucleus on physico-chemical properties and anesthetic activity.

abstract：:Biotherapeutics, including recombinant or plasma-derived human proteins and antibody-based molecules, have emerged as an important class of pharmaceuticals. Aggregation and immunogenicity are among the major bottlenecks during discovery and development of biotherapeutics. Computational tools that can predict aggregati...

journal_title：Pharmaceutical research

authors： Kumar S,Singh SK,Wang X,Rup B,Gill D

更新日期：2011-05-01 00:00:00

abstract：PURPOSE:Under different charging conditions, particles can be either attracted or repulsed by each other, causing powder agglomeration or segregation. Such behavior can be detrimental in many processes aimed at achieving particulate mixture homogeneity. Consequently, the effects of electrostatic charges on mixing kinet...

journal_title：Pharmaceutical research

authors： Desrosiers Lachiver E,Abatzoglou N,Cartilier L,Simard JS

更新日期：2006-05-01 00:00:00

abstract：PURPOSE:We evaluated the effect of luminal bacterial metabolism on intestinal absorption of azetirelin in rats. In vitro characteristics of bacterial metabolism of azetirelin were also investigated with the goal of overcoming the low stability of the peptidic drug against luminal microorganisms. METHODS:Plasma azetire...

journal_title：Pharmaceutical research

authors： Sasaki I,Tamura T,Shibakawa T,Fujita T,Murakami M,Yamamoto A,Muranishi S

更新日期：1997-08-01 00:00:00

abstract：PURPOSE:Oral bioavailability for antisense oligonucleotides has recently been reported but the mechanistic details are not known. The proposed oral delivery of nucleic acids will, therefore, require an understanding of the membrane binding interactions, cell uptake and transport of oligonucleotides across the human gas...

journal_title：Pharmaceutical research

authors： Beck GF,Irwin WJ,Nicklin PL,Akhtar S

更新日期：1996-07-01 00:00:00

abstract：PURPOSE:The purpose of this study is to show how disaccharides differ in their ability to protect lyophilized β-galactosidase from enzymatic activity loss and secondary structure changes during storage. METHODS:β-galactosidase was lyophilized with trehalose, sucrose, cellobiose or melibiose at 2:1, 20:1 and 40:1 excip...

journal_title：Pharmaceutical research

authors： Heljo VP,Jouppila K,Hatanpää T,Juppo AM

更新日期：2011-03-01 00:00:00

abstract：PURPOSE:To evaluate micronized powder retention and detachment from inhaler surfaces following reproducible deposition by impaction, coupled with centrifugal particle detachment (CPD). METHODS:Micronized albuterol sulfate (AS) and beclomethasone dipropionate (BDP) were aerosolized as dry powders and deposited by casca...

journal_title：Pharmaceutical research

authors： Clarke MJ,Peart J,Cagnani S,Byron PR

更新日期：2002-03-01 00:00:00

abstract：PURPOSE:The preparation of drug/cyclodextrin complexes is a suitable method to improve the dissolution of poor soluble drugs. The efficacy of the Controlled Particle Deposition (CPD) as a new developed method to prepare these complexes in a single stage process using supercritical carbon dioxide is therefore compared w...

journal_title：Pharmaceutical research

authors： Hussein K,Türk M,Wahl MA

更新日期：2007-03-01 00:00:00

abstract：:Celiac disease (CD) is an immune-mediated enteropathy triggered by the ingestion of gluten-containing grains that affects ~1% of the white ethnic population. In the last decades, a rise in prevalence of CD has been observed that cannot be fully explained by improved diagnostics. Genetic predisposition greatly influenc...

journal_title：Pharmaceutical research

authors： Matoori S,Fuhrmann G,Leroux JC

更新日期：2013-03-01 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: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:To quantitatively compare in vitro dissolution data in biorelevant and compendial media, to investigate whether in vitro differences are reflected in the simulated plasma profile and to specify under which circumstances prediction of the plasma profile of orally administered lipophilic drugs can be achieved. M...

journal_title：Pharmaceutical research

authors： Nicolaides E,Symillides M,Dressman JB,Reppas C

更新日期：2001-03-01 00:00:00

abstract：PURPOSE:To evaluate the mechanism of renal transport of quinolone antibacterial drugs, we examined the interaction of levofloxacin with p-aminohippurate (PAH) transport systems and the transport of levofloxacin in renal epithelial cells. METHODS:Transport of [14C]PAH or [14C]levofloxacin was measured using OK cell mon...

journal_title：Pharmaceutical research

authors： Matsuo Y,Yano I,Habu Y,Katsura T,Hashimoto Y,Inui K

更新日期：2001-05-01 00:00:00

abstract：:The pharmacokinetics of cefixime, a new orally active cephalosporin, was studied after an intravenous dose of 50 mg/kg to four beagle dogs. Cefixime was shown to exhibit concentration dependent serum protein binding and saturable tubular reabsorption. The drug was excreted mainly in the urine, the net result of glomer...

journal_title：Pharmaceutical research

authors： Tonelli AP,Bialer M,Look ZM,Carson S,Yacobi A

更新日期：1986-06-01 00:00:00

abstract：:Seven healthy, male volunteers were entered into a randomized, open crossover study of the gastrointestinal transit of two enteric-coated 500-mg naproxen tablets. Two radiolabeled tablets were given to each volunteer on two occasions separated by 7 days, once in the fasted state and once after breakfast. Radiolabeling...

journal_title：Pharmaceutical research

authors： Wilding IR,Hardy JG,Sparrow RA,Davis SS,Daly PB,English JR

更新日期：1992-11-01 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:It was the aim of this study to synthesize and characterize a novel chitosan-glutathione (GSH) conjugate providing improved mucoadhesive and permeation-enhancing properties. METHODS:Mediated by carbodiimide and N-hydroxysuccinimide, glutathione was covalently attached to chitosan via the formation of an amide ...

journal_title：Pharmaceutical research

authors： Kafedjiiski K,Föger F,Werle M,Bernkop-Schnürch A

更新日期：2005-09-01 00:00:00

abstract：PURPOSE:Grapefruit juice (GJ) is known to increase the oral bioavailability of many CYP3A-substrates by inhibiting intestinal phase-I metabolism. However, the magnitude of AUC increase is often insignificant and highly variable. Since we earlier suggested that CYP3A and P-glycoprotein (P-gp) form a concerted barrier to...

journal_title：Pharmaceutical research

authors： Soldner A,Christians U,Susanto M,Wacher VJ,Silverman JA,Benet LZ

更新日期：1999-04-01 00:00:00

abstract：:Over the last few decades, intraperitoneal (IP) local drug delivery, providing high drug concentrations with prolonged retention in the peritoneal cavity, has opened a new horizon for the management of life-threatening peritoneal disorders, such as peritoneal carcinomatosis (PC). However, clinical translation of this ...

journal_title：Pharmaceutical research

authors： Alavi S,Haeri A,Mahlooji I,Dadashzadeh S

更新日期：2020-06-03 00:00:00

abstract：PURPOSE:To determine the correlation among progesterone dose, rate of import of progesterone-occupied progesterone receptor (PR) complexes into the nucleus of cells, and transcriptional activity of progesterone-PR complexes. METHODS:Live cell imaging and time-lapse microscopy of green fluorescent protein-tagged PR wer...

journal_title：Pharmaceutical research

authors： Li H,Yan G,Kern SE,Lim CS

更新日期：2003-10-01 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：PURPOSE:Induction of cell-mediated immune (CMI) responses is crucial for vaccine-mediated protection against difficult vaccine targets, e.g., Chlamydia trachomatis (Ct). Adjuvants are included in subunit vaccines to potentiate immune responses, but many marketed adjuvants stimulate predominantly humoral immune response...

journal_title：Pharmaceutical research

authors： Schmidt ST,Neustrup MA,Harloff-Helleberg S,Korsholm KS,Rades T,Andersen P,Christensen D,Foged C

更新日期：2017-08-01 00:00:00

abstract：:A liposomal formulation of methylprednisolone (L-MPL) was developed to improve localization of this immunosuppressant in lymphatic tissues. Liposomes containing MPL were formulated from a mixture of phosphatydylcholine and phosphatydylglycerol (molar ratio, 9:1) and sized by extrusion through a 0.1-micron membrane. Ma...

journal_title：Pharmaceutical research

authors： Mishina EV,Straubinger RM,Pyszczynski NA,Jusko WJ

更新日期：1993-10-01 00:00:00

abstract：PURPOSE:Since the absorption of ceftriaxone (CTO) in the intestine is restricted by its natural physiological characteristics, we developed a series of small synthetic compounds derived from bile acids to promote the absorption of CTO in the gastrointestinal tract. METHODS:Several bile acid derivatives were screened b...

journal_title：Pharmaceutical research

authors： Jeon OC,Hwang SR,Al-Hilal TA,Park JW,Moon HT,Lee S,Park JH,Byun Y

更新日期：2013-04-01 00:00:00

abstract：:The interaction between several marker solutes and a polyolefin laminate polymer was studied in several solutions. Solutions studied included mixtures of sodium chloride and dextrose (at concentrations more less typical of i.v. administration solutions) and several actual i.v. products [lactated Ringer's injection, Di...

journal_title：Pharmaceutical research

authors： Jenke DR

更新日期：1991-06-01 00:00:00

abstract：PURPOSE:With the aim of developing multivalent vaccines for single-injection, we examined the feasibility of combining antigens in biodegradable microspheres. Such vaccines are expected to improve vaccination coverage by reducing the number of vaccination sessions required to generate immunity. METHODS:Mono- and multi...

journal_title：Pharmaceutical research

authors： Boehm G,Peyre M,Sesardic D,Huskisson RJ,Mawas F,Douglas A,Xing D,Merkle HP,Gander B,Johansen P

更新日期：2002-09-01 00:00:00

abstract：:The plasma concentration-time profiles and pharmacokinetics were characterized for nicotine and its major metabolite, cotinine, after multiple daily application of a nicotine user-activated transdermal therapeutic system (UATTS) to nine healthy smokers. The volunteers abstained from smoking 24 hr prior to and during t...

journal_title：Pharmaceutical research

authors： Ross HD,Chan KK,Piraino AJ,John VA

更新日期：1991-03-01 00:00:00

abstract：:Interogan variation in tissue distribution of weakly basic drugs such as quinidine, propranolol, and imipramine was investigated as a function of binding to phosphatidylserine (PhS) in tissues. Tissue distributions of these drugs were determined using 10 different tissues at a steady-state plasma concentration and wer...

journal_title：Pharmaceutical research

authors： Yata N,Toyoda T,Murakami T,Nishiura A,Higashi Y

更新日期：1990-10-01 00:00:00

abstract：:During protein lyophilization, it is common practice to complete the freezing step as fast as possible in order to avoid protein denaturation, as well as to obtain a final product of uniform quality. We report a contradictory observation made during lyophilization of recombinant tissue-type plasminogen activator (t-PA...

journal_title：Pharmaceutical research

authors： Hsu CC,Nguyen HM,Yeung DA,Brooks DA,Koe GS,Bewley TA,Pearlman R

更新日期：1995-01-01 00:00:00

abstract：PURPOSE:This study aimed to characterize the transepithelial transport of miltefosine (HePC), the first orally effective drug against visceral leishmaniasis, across the intestinal barrier to further understand its oral absorption mechanism. MATERIALS AND METHODS:Caco-2 cell monolayers were used as an in vitro model of...

journal_title：Pharmaceutical research

authors： Ménez C,Buyse M,Dugave C,Farinotti R,Barratt G

更新日期：2007-03-01 00:00:00

abstract：:Various diesters of 9-[(1,3-dihydroxy-2-propoxy)-methyl]guanine (DHPG) were screened in order to identify a derivative with improved oral absorption. The solubilities and dissolution rates decreased with increasing chain length and branching of the ester group. However, the dipropionate ester showed an anomalously fas...

journal_title：Pharmaceutical research

authors： Benjamin EJ,Firestone BA,Bergstrom R,Fass M,Massey I,Tsina I,Lin YY

更新日期：1987-04-01 00:00:00