An Extrusion Spheronization Approach to Enable a High Drug Load Formulation of a Poorly Soluble Drug with a Low Melting Surfactant.

abstract：:There is a recognized need for new approaches to understand unit operations with pharmaceutical relevance. A method for analyzing complex interactions in experimental data is introduced. Higher-order interactions do exist between process parameters, which complicate the interpretation of experimental results. In this ...

journal_title：Journal of pharmaceutical sciences

authors： Naelapää K,Allesø M,Kristensen HG,Bro R,Rantanen J,Bertelsen P

更新日期：2009-05-01 00:00:00

abstract：:In our previous research, cocaine applied intranasally in rats diffused or was transported directly from the nasal cavity to the brain. However, the direct nose-brain cocaine transport only contributes to an initial increase in the relative cocaine brain exposure. In this study, we have determined the nose-brain trans...

journal_title：Journal of pharmaceutical sciences

authors： Chow HH,Anavy N,Villalobos A

更新日期：2001-11-01 00:00:00

abstract：:Selected synthetic luteinizing hormone releasing hormone preparations were assayed, and their potencies were determined relative to one sample utilizing primary cultures of enzymatically dispersed rat anterior pituitary cells. Preliminary cell culture experiments indicated that luteinizing hormone releasing hormone ha...

journal_title：Journal of pharmaceutical sciences

authors： Dermody WC,Pastushok CA,Sakowski R,Vaitkus JW,Reel JR

更新日期：1977-03-01 00:00:00

abstract：:15-Lipoxygenase (15-LOX) is one of the key enzymes responsible for the formation of oxidized low-density lipoprotein, a major causal factor for atherosclerosis. Δ(9)-Tetrahydrocannabinol (Δ(9)-THC), a major component of marijuana, has suggested to suppress atherosclerosis. Although Δ(9)-THC seems to be attractive for ...

journal_title：Journal of pharmaceutical sciences

authors： Takeda S,Jiang R,Aramaki H,Imoto M,Toda A,Eyanagi R,Amamoto T,Yamamoto I,Watanabe K

更新日期：2011-03-01 00:00:00

abstract：:This work establishes a predictive model that explicitly recognizes microstructural parameters in the description of the overall mass uptake and local gradients of moisture into tablets. Model equations were formulated based on local tablet geometry to describe the transient uptake of moisture. An analytical solution ...

journal_title：Journal of pharmaceutical sciences

authors： Klinzing GR,Zavaliangos A

更新日期：2016-08-01 00:00:00

abstract：:In adult patients, nilotinib is indicated for chronic myeloid leukemia at an approved oral dose of 300 or 400 mg BID. Physiologically based pharmacokinetic (PBPK) model was developed to describe and supplement limited PK data in the pediatric population ranging from 2 to less than 6 years of age and ultimately inform ...

journal_title：Journal of pharmaceutical sciences

authors： Heimbach T,Lin W,Hourcade-Potelleret F,Tian X,Combes FP,Horvath N,He H

更新日期：2019-06-01 00:00:00

abstract：:Currently, the EMEA, FDA, and WHO as regulatory authorities accept rapidly dissolving (>85% dissolved in 30 min) biopharmaceutics classification system (BCS) I drug products for biowaiver candidates. In the draft EMEA guideline the requirement has been set tighter, that is, the drug product should be very rapidly diss...

journal_title：Journal of pharmaceutical sciences

authors： Kortejärvi H,Shawahna R,Koski A,Malkki J,Ojala K,Yliperttula M

更新日期：2010-02-01 00:00:00

abstract：:Capillary gas chromatography using an open tubular fused silica column and NP-FID was applied to the simultaneous analysis of the antihistamine, carbinoxamine, and the antitussive, hydrocodone, in human serum. Carbinoxamine and hydrocodone were extracted into methylene chloride-2-propanol (9:1) under alkaline conditio...

journal_title：Journal of pharmaceutical sciences

authors： Hoffman DJ,Leveque MJ,Thomson T

更新日期：1983-11-01 00:00:00

abstract：:The polymorphism of rac-5,6-diisobutyryloxy-2-methylamino-1,2,3,4-tetrahydro-naphthalene hydrochloride (CHF 1035) was investigated. Three different crystal forms (Form I, Form II, and Form III) were obtained by recrystallization procedures from common organic solvents. The polymorphs were characterized by Raman and ca...

journal_title：Journal of pharmaceutical sciences

authors： Giordano F,Rossi A,Moyano JR,Gazzaniga A,Massarotti V,Bini M,Capsoni D,Peveri T,Redenti E,Carima L,Dagli Alberi M,Zanol M

更新日期：2001-08-01 00:00:00

abstract：:The advisability of a progressive curtailment of organic solvent film coating offers an incentive to develop latex systems. Here, the use of aqueous colloidal dispersions of cellulose acetate, plasticized with water-soluble additives, is proposed as an alternative way to obtain cellulose acetate membranes either by ca...

journal_title：Journal of pharmaceutical sciences

authors： Bindschaedler C,Gurny R,Doelker E

更新日期：1987-06-01 00:00:00

abstract：:The neuroprotective blood-brain barrier (BBB) keeps many drug candidates below therapeutic levels in the central nervous system. Glutathione PEGylated liposomal doxorubicin (2B3-101) has been developed to safely enhance the delivery of doxorubicin to brain tumors. However, doxorubicin concentration in extracellular br...

journal_title：Journal of pharmaceutical sciences

authors： Birngruber T,Raml R,Gladdines W,Gatschelhofer C,Gander E,Ghosh A,Kroath T,Gaillard PJ,Pieber TR,Sinner F

更新日期：2014-07-01 00:00:00

abstract：:Acitretin, a retinoid for the treatment of severe psoriasis, exhibits extremely low aqueous solubility and high photosensitivity. This study investigated the effects of the complexation of acitretin with the respective hydroxypropyl-beta-cyclodextrin (HPBCD) and randomly substituted methyl-beta-cyclodextrin (RMBCD) on...

journal_title：Journal of pharmaceutical sciences

authors： Liu X,Lin HS,Thenmozhiyal JC,Chan SY,Ho PC

更新日期：2003-12-01 00:00:00

abstract：:A confocal Raman microscopic technique was optimized to more efficiently detect amorphous-amorphous phase separation in freeze-dried protein formulations. A Renishaw Raman inVia confocal microscope was used to collect 100-200 μm line maps (2 μm step size) of freeze-dried protein-excipient formulations. At each point a...

journal_title：Journal of pharmaceutical sciences

authors： Forney-Stevens KM,Pelletier MJ,Shalaev EY,Pikal MJ,Bogner RH

更新日期：2014-09-01 00:00:00

abstract：:Responses from the second Product Quality Research Institute (PQRI) Blend Uniformity Working Group (BUWG) survey of industry have been reanalyzed to identify potential links between formulation and processing variables and the measured uniformity of blends and unit dosage forms. As expected, the variability of the ble...

journal_title：Journal of pharmaceutical sciences

authors： Hancock BC,Garcia-Munoz S

更新日期：2013-03-01 00:00:00

abstract：:Here, we report the structural characterization of several amorphous drugs made using the method of quenching molten droplets suspended in an acoustic levitator. (13) C NMR, X-ray, and neutron diffraction results are discussed for glassy cinnarizine, carbamazepine, miconazole nitrate, probucol, and clotrimazole. The (...

journal_title：Journal of pharmaceutical sciences

authors： Benmore CJ,Weber JK,Tailor AN,Cherry BR,Yarger JL,Mou Q,Weber W,Neuefeind J,Byrn SR

更新日期：2013-04-01 00:00:00

abstract：:A single method for the quantitative determinations of three active ingredients, phenylephrine hydrochloride, phenylpropanolamine hydrochloride, and brompheniramine maleate, and one inactive ingredient (sodium benzoate) in a commercial product for colds is reported. The method is based on paired ion high-pressure liqu...

journal_title：Journal of pharmaceutical sciences

authors： Ghanekar AG,Das Gupta V

更新日期：1978-06-01 00:00:00

abstract：:A simulation study was done to determine if 72 h is the most informative sampling duration for bioequivalence (BE) determination in parallel-designed BE studies with drugs that have half-lives of at least 30 h. The impact of absorption and elimination half-lives on informative sampling was evaluated. Two-treatment par...

journal_title：Journal of pharmaceutical sciences

authors： El-Tahtawy A,Harrison F,Zirkelbach JF,Jackson AJ

更新日期：2012-11-01 00:00:00

abstract：:The comparative pharmacokinetics of free MTP-PE (muramyl tripeptide phosphatidyl ethanolamine) and MTP-PE entrapped in negatively charged multilamellar liposomes (liposomal MPT-PE) was evaluated in rats at a bolus intravenous (i.v.) dose of 0.2 mg/kg and in dogs at a bolus i.v. dose of 0.1 mg/kg. Additional studies we...

journal_title：Journal of pharmaceutical sciences

authors： Gay B,Cardot JM,Schnell C,van Hoogevest P,Gygax D

更新日期：1993-10-01 00:00:00

abstract：:Quality-by-design (QbD) is a systematic approach to drug development, which begins with predefined objectives, and uses science and risk management approaches to gain product and process understanding and ultimately process control. The concept of QbD can be extended to analytical methods. QbD mandates the definition ...

journal_title：Journal of pharmaceutical sciences

authors： Vogt FG,Kord AS

更新日期：2011-03-01 00:00:00

abstract：:A consistent account of the assumptions of the well-stirred perfusion limited model leads to the equation for the organ tissue that does not coincide with that often presented in books and papers. The difference in pharmacokinetic profiles calculated by the valid and the commonly used equations could be quite signific...

journal_title：Journal of pharmaceutical sciences

authors： Berezhkovskiy LM

更新日期：2010-01-01 00:00:00

abstract：:Phenytoin-loaded alkyd nanoemulsions were prepared spontaneously using the phase inversion method from a mixture of novel biosourced alkyds and Tween 80 surfactant. Exposure of human adult keratinocytes (HaCaT cells) for 48 h to alkyd nanoemulsions producing phenytoin concentrations of 3.125-200 μg/mL resulted in rela...

journal_title：Journal of pharmaceutical sciences

authors： Teo SY,Yew MY,Lee SY,Rathbone MJ,Gan SN,Coombes AGA

更新日期：2017-01-01 00:00:00

abstract：:The synthesis of the diethyl analog of neostigmine, its preliminary pharmacology, and its use as an internal standard for the GLC assay of neostigmine are described. Both the diethyl analog and neostigmine undergo thermal demethylation in the injection port. The column selected produced satisfactory resolution and sho...

journal_title：Journal of pharmaceutical sciences

authors： Ward HE Jr,Freeman JJ,Sowell JW,Kosh JW

更新日期：1981-04-01 00:00:00

abstract：:A method for the simultaneous determination of etoricoxib and its carbon-13 analog ((13)C(6)-etoricoxib) from human plasma has been developed and used to support bioavailability studies. Plasma samples (0.5 mL) were extracted by using a 3M Empore 96-well plate (C(8)) and the resulting extracts were analyzed by using a...

journal_title：Journal of pharmaceutical sciences

authors： Rose MJ,Agrawal N,Woolf EJ,Matuszewski BK

更新日期：2002-02-01 00:00:00

abstract：:To reduce the risk of immunogenicity that may be caused by therapeutic protein products, it is important to properly characterize subvisible particles and to develop strategies to reduce the levels of particles delivered to patients. In the present study, by using state-of-the-art methods to quantify particle levels, ...

journal_title：Journal of pharmaceutical sciences

authors： Ueda T,Nakamura K,Abe Y,Carpenter JF

更新日期：2019-01-01 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：:The entropy of fusion of 84 disubstituted benzenes was essentially constant and independent of the participation of the compounds in intramolecular or intermolecular hydrogen bonding. It was also independent of the shapes, sizes, and dipole moments of the rigid molecules studied. While the entropy of fusion was indepe...

journal_title：Journal of pharmaceutical sciences

authors： Martin E,Yalkowsky SH,Wells JE

更新日期：1979-05-01 00:00:00

abstract：:6-Chloro-9-[2-(6-methyl-3-pyridyl)ethyl]-1,2,3,4-tetrahydrocarbazole-2-carboxylic acid hydrochloride lowered serum cholesterol, triglyceride, phospholipid, and free fatty acid levels in normal rats. The compound appeared to have a low toxicity and to be well tolerated in mice, adult and neonatal rats, and rabbits. At ...

journal_title：Journal of pharmaceutical sciences

authors： Dalton C,Pool WR

更新日期：1977-03-01 00:00:00

abstract：:Eighteen healthy adult volunteers completed an open-label, four-way crossover study designed to determine the bioequivalency of 160-mg cibenzoline [2-(2,2-diphenylcyclopropyl)-4,5-dihydro-1H-imidazole] capsules and tablets, their relative bioavailability compared with an oral solution of the drug, as well as the absol...

journal_title：Journal of pharmaceutical sciences

authors： Massarella J,Silvestri T,Lin A

更新日期：1986-09-01 00:00:00

abstract：:The aims of the present study were to formulate stable onion phases of the biodegradable surfactant PEG-8 Distearate (PEG8DS) and evaluate application of the onion phases in encapsulating sumatriptan succinate, a BCS class III potent antimigraine drug. Drug loaded and placebo onion phases were prepared by shearing lyo...

journal_title：Journal of pharmaceutical sciences

authors： Redkar M,Hassan PA,Aswal V,Devarajan P

更新日期：2007-09-01 00:00:00

abstract：:We have recently reported the time course of acute myocardial drug uptake and simultaneous pharmacodynamic effects for metoprolol (4 mg; n = 12) and sotalol (20 mg; n = 10) in patients with ischemic heart disease. The acute pharmacodynamic effects of the two drugs included reductions in both spontaneous heart rate and...

journal_title：Journal of pharmaceutical sciences

authors： Ritchie RH,Morgan DJ,Horowitz JD

更新日期：1998-02-01 00:00:00