Isolation and characterization of the sesquiterpene lactones costunolide, parthenolide, costunolide diepoxide, santamarine, and reynosin from Magnolia grandiflora L.

abstract：:A rapid approach for estimating the pK(a) value of small organic molecules was developed using vacuum-assisted multiplexed capillary electrophoresis (VAMCE) with ultraviolet detection. The VAMCE method employed a 96-capillary array, arranged in a standard 8 x 12 microtiter plate configuration, with each row of capilla...

journal_title：Journal of pharmaceutical sciences

authors： Zhou C,Jin Y,Kenseth JR,Stella M,Wehmeyer KR,Heineman WR

更新日期：2005-03-01 00:00:00

abstract：:3-Fluoro-, 3-chloro-, and 3-bromocyclophosphamide were prepared from the reaction of trifluoromethylhypofluorite, sodium hypochlorite, and bromine with the anticancer drug cyclophosphamide. Treatment of cis- and trans-4-phenylcyclophosphamide and 5,6-benzocyclophosphamide with sodium hypochlorite afforded cis- and tra...

journal_title：Journal of pharmaceutical sciences

authors： Zon G,Ludeman SM,Ozkan G,Chandrasegaran S,Hammer CF,Dickerson R,Mizuta K,Egan W

更新日期：1983-06-01 00:00:00

abstract：:The organic extract of the whole plant Xanthorhiza simplicissima was found to exhibit good activity against the AIDS-related opportunistic pathogens Candida albicans, Cryptococcus neoformans, and Mycobacterium intracellularae. Bioassay-directed fractionation of the extract led to the isolation of the known alkaloid be...

journal_title：Journal of pharmaceutical sciences

authors： Okunade AL,Hufford CD,Richardson MD,Peterson JR,Clark AM

更新日期：1994-03-01 00:00:00

abstract：:The aim of the present work was to prepare and characterize chitosan-stearic acid conjugate nanomicelles for encapsulation of amphotericin B (AmB) and to evaluate the in vitro nebulization of the formulations. Water soluble chitosan was grafted to stearic acid (SA) chains via 1-ethyl-3-(3-dimethylaminopropyl)carbodiim...

journal_title：Journal of pharmaceutical sciences

authors： Gilani K,Moazeni E,Ramezanli T,Amini M,Fazeli MR,Jamalifar H

更新日期：2011-01-01 00:00:00

abstract：:The degradation kinetics of gonadorelin were investigated systematically with reversed-phase high-performance liquid chromatography. The stability-indicating properties of this system were checked with photodiode array detection and by comparison with capillary zone electrophoretic analysis. Influences of gonadorelin ...

journal_title：Journal of pharmaceutical sciences

authors： Hoitink MA,Beijnen JH,Bult A,van der Houwen OA,Nijholt J,Underberg WJ

更新日期：1996-10-01 00:00:00

abstract：:Hydrazine levels in formulations of hydralazine, isoniazid, and phenelzine have been measured over a 2-year period under ambient conditions and under temperature and humidity stress. Hydralazine tablets are stable under ambient conditions, but the hydrazine level in an injectable formulation increased from 4.5 to 10 m...

journal_title：Journal of pharmaceutical sciences

authors： Lovering EG,Matsui F,Curran NM,Robertson DL,Sears RW

更新日期：1983-08-01 00:00:00

abstract：:The aim of this study is to explore hot melt extrusion (HME) as a solvent-free drug loading technique for preparation of stable amorphous solid dispersions using mesoporous silica (PSi). Ibuprofen and carvedilol were used as poorly soluble active pharmaceutical ingredients (APIs). Due to the high friction of an API:PS...

journal_title：Journal of pharmaceutical sciences

authors： Genina N,Hadi B,Löbmann K

更新日期：2018-01-01 00:00:00

abstract：:The aim of this study was to utilize high-speed video imaging for understanding the disintegrability of compacts and disintegrant action upon wetting. High-speed video imaging was used to visualize the disintegration of compacts and effect of wetting on free disintegrant particles. Acquired images were processed using...

journal_title：Journal of pharmaceutical sciences

authors： Desai PM,Liew CV,Heng PW

更新日期：2012-06-01 00:00:00

abstract：:The synthesis, characterization, and therapeutic evaluation of a series of partially esterified derivatives of pentetic (diethylenetriaminepentaacetic) acid are reported. These compounds were prepared in an attempt to promote increased decorporation of insoluble colloidal forms of plutonium, which are removed by pente...

journal_title：Journal of pharmaceutical sciences

authors： Guilmette RA,Parks JE,Lindenbaum A

更新日期：1979-02-01 00:00:00

abstract：:The diterpene esters, genkwadaphnin and yuanhuacine, have been shown to possess significant antileukemic activity in the P-388 screen. The major metabolic effects of the diterpene esters were on DNA and protein synthesis. The effects on DNA synthesis in vitro were evoked at a lower concentration than that required for...

journal_title：Journal of pharmaceutical sciences

authors： Hall IH,Kasai R,Wu RY,Tagahara K,Lee KH

更新日期：1982-11-01 00:00:00

abstract：:The metabolic fate of aprophen hydrochloride (2-diethylaminoethyl 2,2-diphenylpropionate) was studied in rats after intravenous administration. Both 14C-labeled and unlabeled aprophen were used in these studies. Blood samples were collected and analyzed to determine the identities of the metabolites formed. Utilizing ...

journal_title：Journal of pharmaceutical sciences

authors： Brown ND,Smejkal RM,Breuer E,Doctor BP,Chiang PK

更新日期：1988-02-01 00:00:00

abstract：:The fungal microorganism Cunninghamella echinulata was utilized to para-hydroxylate the synthetic substrate (+/-)-1-isopropylamino-3-phenoxy-propan-2-ol (1). The resulting product, (+/-)-1-(4-hydroxyphenoxy)-3-isopropylamino-propan-2-ol, or (+/-)-prenalterol, (2) was formed in greater than 85% yield. Extracts from inc...

journal_title：Journal of pharmaceutical sciences

authors： Pasutto FM,Singh NN,Jamali F,Coutts RT,Abuzar S

更新日期：1987-02-01 00:00:00

abstract：:A Bayesian approach was developed to determine an amikacin dosage regimen to achieve the desired plasma concentrations for each patient. Statistical characteristics of pharmacokinetic parameters were first evaluated in a group of patients (reference population), which when combined with three individual plasma concent...

journal_title：Journal of pharmaceutical sciences

authors： Garraffo R,Iliadis A,Cano JP,Dellamonica P,Lapalus P

更新日期：1989-09-01 00:00:00

abstract：:Molecular interactions between iodine and disulfiram, clomethiazole, and tolnaftate were investigated by electron spectroscopy. Iodine forms charge transfer complexes with these molecules, with 1:1 stoichiometry and of the n-sigma type. The formation constants were compared with those obtained with antithyroid molecul...

journal_title：Journal of pharmaceutical sciences

authors： Buxeraud J,Absil AC,Raby C

更新日期：1984-12-01 00:00:00

abstract：:Alkyl esters (C1--C4) of the four halofumaric acids were tested for antifungal activity against Candida albicans, Aspergillus niger, Mucor mucedo, and Trichophyton mentagrophytes at pH 5.6 and 7.0 in the absence and presence of 10% beef serum in Sabouraud dextrose agar. The most toxic compound to each organism was: C....

journal_title：Journal of pharmaceutical sciences

authors： Gershon H,Shanks L

更新日期：1978-04-01 00:00:00

abstract：:Numerous studies have demonstrated that the administration of nonsteroidal anti-inflammatory drugs (NSAIDs) increases small intestinal permeability, and this has been suggested to be a prerequisite to enteropathy. It is believed that the inhibitory effect of chiral NSAIDs on the synthesis of prostaglandins and hence t...

journal_title：Journal of pharmaceutical sciences

authors： Davies NM,Wright MR,Russell AS,Jamali F

更新日期：1996-11-01 00:00:00

abstract：:Stability testing of morphine sulfate formulated with nonpareil sugar seeds (consisting of sucrose and starch) and fumaric acid revealed the formation of the three impurities 5-(hydroxymethyl)-2-furfural, 10-hydroxymorphine and 10-oxomorphine. 5-(Hydroxymethyl)-2-furfural was isolated via semipreparative HPLC utilizin...

journal_title：Journal of pharmaceutical sciences

authors： Kelly SS,Glynn PM,Madden SJ,Grayson DH

更新日期：2003-03-01 00:00:00

abstract：:Two polymorphs of celastrol were discovered and fully characterized by X-ray powder diffraction, thermogravimetry analysis, and differential scanning calorimetry. The single-crystal structures of form I and the isostructural solvate of form II were disclosed by single-crystal X-ray diffraction. The apparent solubility...

journal_title：Journal of pharmaceutical sciences

authors： Zha J,Zhang Q,Li M,Wang JR,Mei X

更新日期：2018-11-01 00:00:00

abstract：:The effects of various types of substituted and nonsubstituted cyclodextrins (CDs) on the physical and colloidal stability of three different proteins were studied to further ascertain the mechanism by which cyclodextrins stabilize proteins. The three proteins examined in this study are the Clostridium difficile Toxoi...

journal_title：Journal of pharmaceutical sciences

authors： Samra HS,He F,Bhambhani A,Pipkin JD,Zimmerer R,Joshi SB,Middaugh CR

更新日期：2010-06-01 00:00:00

abstract：:Paclitaxel and other taxanes have complex structures including the presence of numerous hydrolytically sensitive ester groups and a chiral center that readily undergoes epimerization thus making their kinetics complex. The present study attempts to understand the mechanism of epimerization at the 7-position of paclita...

journal_title：Journal of pharmaceutical sciences

authors： Tian J,Stella VJ

更新日期：2008-03-01 00:00:00

abstract：:An aqueous solution of trimedoxime bromide, atropine, and benactyzine hydrochloride was formulated to have maximum stability as an antidote in organophosphorus poisoning. The stability of the mixture in glass and plastic cartridges was determined. Glass cartridges were more desirable than plastic; there was less vapor...

journal_title：Journal of pharmaceutical sciences

authors： Zvirblis P,Ellin RI

更新日期：1982-03-01 00:00:00

abstract：:Crystallization of polymorphs still has a touch of art, as even prior observations of polymorphs do not guarantee their crystallization. However, once crystals of various polymorphs have been obtained, their relative stabilities can be established with a straightforward thermodynamic approach even if the conclusion wi...

journal_title：Journal of pharmaceutical sciences

authors： Rietveld IB,Céolin R

更新日期：2015-12-01 00:00:00

abstract：:An immune response for a nasal ovalbumin (OVA) powder formulation with an applied nasal delivery platform technology, consisting of a powdery nasal carrier and a device, was evaluated in monkeys with similar upper respiratory tracts and immune systems to those of humans, in order to assess the applicability to a vacci...

journal_title：Journal of pharmaceutical sciences

authors： Torikai Y,Sasaki Y,Sasaki K,Kyuno A,Haruta S,Tanimoto A

更新日期：2020-12-03 00:00:00

abstract：:The blood-brain barrier permeation has been investigated by using a topological substructural molecular design approach (TOPS-MODE). A linear regression model was developed to predict the in vivo blood-brain partitioning coefficient on a data set of 119 compounds, treated as the logarithm of the blood-brain concentrat...

journal_title：Journal of pharmaceutical sciences

authors： Cabrera MA,Bermejo M,Pérez M,Ramos R

更新日期：2004-07-01 00:00:00

abstract：:A pharmacokinetic study was performed in plasma and cerebrospinal fluid (CSF) of patients suffering from brain tumors to describe the disposition of methotrexate. An open three-compartment model was developed to fit together the data obtained in plasma and CSF. The pharmacokinetic parameters obtained by the model agre...

journal_title：Journal of pharmaceutical sciences

authors： Chatelut E,Roche H,Plusquellec Y,Peyrille F,De Biasi J,Pujol A,Canal P,Houin G

更新日期：1991-08-01 00:00:00

abstract：:Thiamine hydrochloride (Vitamin B(1), THCl) can exist as a nonstoichiometric hydrate (NSH) and as a hemihydrate (HH). NSH can contain up to approximately 1 molar equivalent of water and be dehydrated to an isomorphic desolvate (ID) with minimal change in lattice structure. Crystallographic and spectroscopic techniques...

journal_title：Journal of pharmaceutical sciences

authors： Chakravarty P,Berendt RT,Munson EJ,Young VG Jr,Govindarajan R,Suryanarayanan R

更新日期：2010-02-01 00:00:00

abstract：:Role of water in chemical (in)stability is revisited, with focus on deamidation in freeze-dried amorphous proteins and peptides. Two distinct patterns for deamidation versus water have been reported, that is, a consistent increase in rate constant with water, and a "hockey stick"-type behavior. For the latter, deamida...

journal_title：Journal of pharmaceutical sciences

authors： Ohtake S,Feng S,Shalaev E

更新日期：2018-01-01 00:00:00

abstract：:Literature data relevant to the decision to waive in vivo bioequivalence testing for the approval of generic immediate release solid oral dosage forms of proguanil hydrochloride are reviewed. To elucidate the Biopharmaceutics Classification System (BCS) classification, experimental solubility and dissolution studies w...

journal_title：Journal of pharmaceutical sciences

authors： Plöger GF,Abrahamsson B,Cristofoletti R,Groot DW,Langguth P,Mehta MU,Parr A,Polli JE,Shah VP,Tajiri T,Dressman JB

更新日期：2018-07-01 00:00:00

abstract：:Spray-dried dispersions (SDDs) are an important technology for enhancing the oral bioavailability of poorly water-soluble drugs. To design an effective oral SDD formulation, the key rate-determining step(s) for oral drug absorption must be understood. This work combined in vivo and in vitro tests with in silico modeli...

journal_title：Journal of pharmaceutical sciences

authors： Stewart A,Yates I,Mudie D,Pivette P,Goodwin A,Sarmiento A,Winter M,Morgen M,Vodak D

更新日期：2019-01-01 00:00:00

abstract：:Bisphosphonates are widely used for the treatment of bone diseases, including hypercalcemia and osteoporosis. However, the bioavailability (BA) of orally administered bisphosphonates is low, at approximately 0.9%-1.8%. In addition, the oral administration of bisphosphonates is associated with mucosal damage, including...

journal_title：Journal of pharmaceutical sciences

authors： Katsumi H,Takashima M,Sano J,Nishiyama K,Kitamura N,Sakane T,Hibi T,Yamamoto A

更新日期：2011-09-01 00:00:00