Bioavailability prediction based on molecular structure for a diverse series of drugs.

abstract：PURPOSE:Some therapeutic peptides exhibit amyloidogenic properties that cause insolubility and cytotoxicity against neuronal cells in vitro. Here, we characterize the conformational change in monomeric therapeutic peptide to its fibrillar aggregate in order to prevent amyloidogenic formation during clinical application...

journal_title：Pharmaceutical research

authors： Onoue S,Ohshima K,Debari K,Koh K,Shioda S,Iwasa S,Kashimoto K,Yajima T

更新日期：2004-07-01 00:00:00

abstract：PURPOSE:The purpose of the current study is to evaluate the solubility advantage offered by celecoxib (CEL) amorphous systems and to characterize and correlate the physical and thermodynamic properties of CEL and its amorphous molecular dispersions containing poly(vinylpyrrolidone) (PVP). METHODS:The measurement of cr...

journal_title：Pharmaceutical research

authors： Gupta P,Kakumanu VK,Bansal AK

更新日期：2004-10-01 00:00:00

abstract：PURPOSE:To identify the key formulation factors controlling the initial drug and polymer dissolution rates from an amorphous solid dispersion (ASD). METHODS:Ketoconazole (KTZ) ASDs using PVP, PVP-VA, HMPC, or HPMC-AS as polymeric matrix were prepared. For each drug-polymer system, two types of formulations with the sa...

journal_title：Pharmaceutical research

authors： Chen Y,Wang S,Wang S,Liu C,Su C,Hageman M,Hussain M,Haskell R,Stefanski K,Qian F

更新日期：2016-10-01 00:00:00

abstract：PURPOSE:The purpose of this study was to develop a new computational fluid dynamics (CFD)-based model of the complex transport and droplet drying kinetics within a laboratory-scale spray dryer, and relate CFD-predicted drying parameters to powder aerosolization metrics from a reference dry powder inhaler (DPI). METHOD...

journal_title：Pharmaceutical research

authors： Longest PW,Farkas D,Hassan A,Hindle M

更新日期：2020-05-21 00:00:00

abstract：PURPOSE:To examine the effect of particle size and morphology on aerosol dispersion using jet-milled and spray-dried mannitol particles in narrow size distributions within the respirable range. METHODS:Particle size and morphology were examined by laser diffraction and scanning electron microscopy, respectively. Aeros...

journal_title：Pharmaceutical research

authors： Louey MD,Van Oort M,Hickey AJ

更新日期：2004-07-01 00:00:00

abstract：PURPOSE:The aim of the study is to investigate the effect of polymer blending on entrapment and release of ganciclovir (GCV) from poly(D,L-lactide-co-glycolide) (PLGA) microspheres using a set of empirical equations. METHODS:Two grades of PLGA, PLGA 7525 [D,L-lactide:glycolide(75:25), MW 90,000-126,000 Da] and Resomer...

journal_title：Pharmaceutical research

authors： Duvvuri S,Gaurav Janoria K,Mitra AK

更新日期：2006-01-01 00:00:00

abstract：PURPOSE:To study the miscibility of proteins and polymer excipients in frozen solutions and freeze-dried solids as protein formulation models. METHODS:Thermal profiles of frozen solutions and freeze-dried solids containing various proteins (lysozyme, ovalbumin, BSA), nonionic polymers (Ficoll, polyvinylpyrrolidone [PV...

journal_title：Pharmaceutical research

authors： Izutsu K,Kojima S

更新日期：2000-10-01 00:00:00

abstract：PURPOSE:The aim was to replace the traditional 21-day Caco-2 permeability protocol by a more high-throughput assay. METHODS:Caco-2 cells were seeded at high density in 96-well plates in novel cell culture boxes. After 7 days, drug permeability studies were performed. Samples were analyzed by a new UV detection method....

journal_title：Pharmaceutical research

authors： Alsenz J,Haenel E

更新日期：2003-12-01 00:00:00

abstract：PURPOSE:Solid dispersions (SDs) represent the most common formulation technique used to increase the dissolution rate of a drug. In this work, the three most common methods used to prepare SDs, namely spray-drying, solvent-casting and freeze-drying, have been compared in order to investigate their effect on increasing ...

journal_title：Pharmaceutical research

authors： De Mohac LM,Caruana R,Cavallaro G,Giammona G,Licciardi M

更新日期：2020-02-19 00:00:00

abstract：:The in situ rat gut technique was used to study the effects of hypothermia on the intestinal absorption of a 1 mg/ml solution of sodium pentobarbital in 0.01 M phosphate buffer (pH 6.0). Male Sprague-Dawley rats weighing between 300 and 370 g were exposed to an atmosphere of helox (helium:oxygen, 80:20) at 0-4 degrees...

journal_title：Pharmaceutical research

authors： Stavchansky S,Tung IL

更新日期：1987-06-01 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：: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: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 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：:Alpha- and beta-cyclodextrins and their hydroxypropyl derivatives were converted by the reaction with chlorosulfonic acid in pyridine to the corresponding sulfates. Cyclodextrin sulfates were shown by fast-atom bombardment mass spectrometry (negative ion mode, triethanolamine matrix) to be mixtures with nearly symmetr...

journal_title：Pharmaceutical research

authors： Pitha J,Mallis LM,Lamb DJ,Irie T,Uekama K

更新日期：1991-09-01 00:00:00

abstract：PURPOSE:Reverse micellar solutions of diclofenac sodium were encapsulated in soft gelatine capsules. On contact with aqueous media they exhibited an application induced transformation (AIT) into a semisolid system of liquid crystals (SSLC) which slows down drug release. The aim of the present paper was to study in vitr...

journal_title：Pharmaceutical research

authors： Schneeweis A,Müller-Goymann CC

更新日期：1997-12-01 00:00:00

abstract：PURPOSE:Phase II metabolism involves the conjugation of a polar moiety, such as sulfate or glucuronic acid, to a (relatively) nonpolar xenobiotic. Although it might be expected that such conjugates may exhibit amphiphilic character (e.g., surface activity and potential to form micelles), no detailed study of the micell...

journal_title：Pharmaceutical research

authors： Shackleford DM,Prankerd RJ,Scanlon MJ,Charman WN

更新日期：2003-03-01 00:00:00

abstract：:A new magnetic microsphere carrier has been formulated that may localize drugs by both biochemical and physical means. The microspheres, prepared from the polysaccharide chitosan, are designed to bind to anionic glycosaminoglycan receptors on the surface of capillary endothelial cells. The microspheres were formulated...

journal_title：Pharmaceutical research

authors： Gallo JM,Hassan EE

更新日期：1988-05-01 00:00:00

abstract：PURPOSE:The discovery of nano drug delivery system has rendered a great hope for improving cancer therapy. However, there are some inevitable obstacles that constrain its development, such as the physical and biological barriers, the toxicity of carrier materials and the physiological toxicity of drugs. Here, we report...

journal_title：Pharmaceutical research

authors： Zhang Z,Yu M,An T,Yang J,Zou M,Zhai Y,Sun W,Cheng G

更新日期：2019-12-10 00:00:00

abstract：PURPOSE:The aim of this study was to investigate the effect of hepatic or renal insufficiency on the pharmacokinetics of paclitaxel in rats. METHODS:Rats were treated with carbon tetrachloride (CCl4; 0.5 ml/kg) to induce hepatic failure or were subjected to 5/6 nephrectomy (5/6 Nx) to induce renal failure. Paclitaxel ...

journal_title：Pharmaceutical research

authors： Jiko M,Yano I,Okuda M,Inui K

更新日期：2005-02-01 00:00:00

abstract：:The effect of the penetration enhancers Azone, oleic acid, 1-dodecanol, dodecyl N,N-dimethylaminoacetate (DDAA), and dodecyl N,N-dimethylaminoisopropionate (DDAIP) on epithelial membrane lipids was examined using human buccal cell membranes as a model for epithelial lipid bilayer. Buccal epithelial cells (BEC) were la...

journal_title：Pharmaceutical research

authors： Turunen TM,Urtti A,Paronen P,Audus KL,Rytting JH

更新日期：1994-02-01 00:00:00

abstract：PURPOSE:To elucidate the key parameters affecting solute transport from semi-interpenetrating networks (sIPNs) comprised of poly(ethylene glycol) diacrylate (PEGdA) and gelatin that are partially crosslinked, water-swellable and biodegradable. Effects of material compositions, solute size, solubility, and loading densi...

journal_title：Pharmaceutical research

authors： Fu Y,Kao WJ

更新日期：2009-09-01 00:00:00

abstract：PURPOSE:To develop an efficient tumor vasculature-targeted polymeric micelle delivery system for combretastatin A4 (CA4), a novel antivascular agent. METHODS:CA4-loaded micelles were prepared from poly (ethylene glycol)-b-poly (d, l-lactide) copolymers. RGD peptides that target integrins alphavbeta3 and alphavbeta5, m...

journal_title：Pharmaceutical research

authors： Wang Y,Yang T,Wang X,Wang J,Zhang X,Zhang Q

更新日期：2010-09-01 00:00:00

abstract：PURPOSE:This study uses high drug content solid dispersions for dose window extension beyond current demonstrations using fused deposition modelling (FDM) to; i) accommodate pharmaceutically relevant doses of drugs of varying potencies at acceptable dosage form sizes and ii) enable enhanced dose flexibility via modular...

journal_title：Pharmaceutical research

authors： Govender R,Abrahmsén-Alami S,Folestad S,Larsson A

更新日期：2019-12-17 00:00:00

abstract：:The limitations of traditional gas adsorption models for describing water vapor sorption by amorphous pharmaceutical solids are described and an alternative approach based on polymer solution theories is proposed. The approach is tested by comparing a priori predicted isotherms with literature data for the poly(vinylp...

journal_title：Pharmaceutical research

authors： Hancock BC,Zografi G

更新日期：1993-09-01 00:00:00

abstract：PURPOSE:Synthetic hydrogels fabricated from photopolymerization are attractive for tissue engineering for their controlled macroscopic properties, the ability to incorporate biological functionalities, and cell encapsulation. The goal of the present study was to exploit the attractive features of synthetic hydrogels to...

journal_title：Pharmaceutical research

authors： Bryant SJ,Nicodemus GD,Villanueva I

更新日期：2008-10-01 00:00:00

abstract：PURPOSE:To characterize the pharmacokinetics of simvastatin (SV) and simvastatin acid (SVA), a lactone-acid pair known to undergo reversible metabolism, and to better understand mechanisms underlying pharmacokinetic interactions observed between SV and gemfibrozil. METHODS:Pharmacokinetic studies were conducted after ...

journal_title：Pharmaceutical research

authors： Prueksaritanont T,Qiu Y,Mu L,Michel K,Brunner J,Richards KM,Lin JH

更新日期：2005-07-01 00:00:00

abstract：PURPOSE:To investigate the ability of various polymers to inhibit the crystallization of amorphous felodipine from amorphous molecular dispersions in the presence of absorbed moisture. METHODS:Spin coated films of felodipine with poly(vinylpyrrolidone) (PVP), hydroxypropylmethylcellulose acetate succinate (HPMCAS) and...

journal_title：Pharmaceutical research

authors： Konno H,Taylor LS

更新日期：2008-04-01 00:00:00

abstract：PURPOSE:To investigate the relationship between mean dissolution time (MDT) and dose/solubility ratio (q) using the diffusion layer model. METHODS:Using the classic Noyes-Whitney equation and considering a finite dose, we derived an expression for MDT as a function of q under various conditions. q was expressed as a d...

journal_title：Pharmaceutical research

authors： Rinaki E,Dokoumetzidis A,Macheras P

更新日期：2003-03-01 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