Regulatory, design, and analysis aspects of complex stability studies. US Food & Drug Administration.

abstract：:Ethyl, n-dodecyl, and n-hexadecyl esters of urocanic acid (4-imidazoleacrylic acid) were prepared from 4-imidazolecarboxaldehyde in satisfactory yields via the Wittig reaction. ...

journal_title：Journal of pharmaceutical sciences

authors： Honda K,Nishijima Y

更新日期：1981-01-01 00:00:00

abstract：:The potential binding interaction(s) of the anti-thyroid drug methimazole (MMZ) with the protein bovine serum albumin (BSA) has been studied using isothermal titration calorimetry (ITC) and UV-Visible, fluorescence and circular dichroism (CD) spectroscopic techniques. The binding of MMZ to BSA has been studied in both...

journal_title：Journal of pharmaceutical sciences

authors： Singh SK,Kishore N

更新日期：2008-06-01 00:00:00

abstract：:Alginate-based polyelectrolyte complexes (PECs) and hydrogel were engineered as platforms for local bevacizumab (BVZ) therapy. This study provides deep comprehension on the microstructures of such systems, and their correlation with drug-release patterns. PECs and hydrogel were characterized using Fourier transform in...

journal_title：Journal of pharmaceutical sciences

authors： Ferreira NN,Caetano BL,Boni FI,Sousa F,Magnani M,Sarmento B,Ferreira Cury BS,Daflon Gremião MP

更新日期：2019-04-01 00:00:00

abstract：:Systematic structural modifications were performed on the natural sesquiterpene lactone tenulin to define those groupings essential to, or significant in, its in vivo antitumor activity. Accordingly, the following tenulin analogs were prepared: dihydrotenulin, 2,3-epoxytenulin, isotenulin, dihydroisotenulin, 2,3-epoxy...

journal_title：Journal of pharmaceutical sciences

authors： Waddell TG,Austin AM,Cochran JW,Gerhart KG,Hall IH,Lee KH

更新日期：1979-06-01 00:00:00

abstract：:The dissolution rates of a number of drug-urethan solid-state dispersion systems were studied. A marked enhancement of the initial dissolution rates of several poorly water-soluble drugs was found when they were incorporated into a urethan matrix by heat fusion. These differences were considerable when pure substances...

journal_title：Journal of pharmaceutical sciences

authors： Maulding HV

更新日期：1978-03-01 00:00:00

abstract：:Small particles of two steroids, cholesteryl acetate and beta-sitosterol, were prepared by the following technique. The steroid was dissolved in an organic solvent, which was emulsified in water in the presence of surfactant, thus giving a water-continuous emulsion. As the organic solvent was evaporated, the steroid p...

journal_title：Journal of pharmaceutical sciences

authors： Sjöström B,Bergenståhl B,Kronberg B

更新日期：1993-06-01 00:00:00

abstract：:A rapid, automated method for the determination of phenylbutazone in plasma and urine was developed. The method offers distinct advantages over earlier procedures and is particularly suitable for large-scale bioavailability studies. ...

journal_title：Journal of pharmaceutical sciences

authors： Lukas G,Borman CB,Zak SB

更新日期：1976-01-01 00:00:00

abstract：:The purpose of this work is to evaluate biodegradable drug carriers with defined size, hydrophobicity, and surface charge density for preferential lymphatic uptake and retention for sustained regional drug delivery. PLGA-PMA:PLA-PEG (PP) nanoparticles of defined size and relative hydrophobicity were prepared by nanopr...

journal_title：Journal of pharmaceutical sciences

authors： Rao DA,Forrest ML,Alani AW,Kwon GS,Robinson JR

更新日期：2010-04-01 00:00:00

abstract：:In this paper, we establish a mechanistic model for the prediction of amorphous solid dispersion (ASD) stability. The novel approach incorporates fundamental physical parameters, principally supersaturation, diffusivity, and interfacial energy, to model crystallization in ASDs accounting for both kinetic and thermodyn...

journal_title：Journal of pharmaceutical sciences

authors： Ojo AT,Lee PI

更新日期：2020-08-18 00:00:00

abstract：:Controlling residual solvent levels is a major concern in pharmaceutical freeze-drying from co-solvent systems. This review provides an overview of the factors influencing this process and estimates their potential to reduce residual solvents in freeze-dried products. Decreased solvent contents are potentially correla...

journal_title：Journal of pharmaceutical sciences

authors： Kunz C,Gieseler H

更新日期：2018-08-01 00:00:00

abstract：:A pharmacokinetic study of the dopamine D2 receptor agonist (S)-(-)-2-(N-propyl-N-(2-thienylethyl)amino)-5-hydroxytetralin+ ++-HCl (N-0923) infused in female cynomolgus monkeys over a 4-h period was carried out at International Research and Development Corporation. The purpose of this study was to estimate the elimina...

journal_title：Journal of pharmaceutical sciences

authors： Walters DR,McConnell WR,Cefali EA

更新日期：1994-05-01 00:00:00

abstract：:Aqueous solubilities for some guanine derivatives were estimated by semiempirical equations developed by Yalkowsky and Valvani1 using the data for partition coefficient and melting temperature. It was shown that in the case of guanine derivatives examined in this study, the solubility values could not be estimated ade...

journal_title：Journal of pharmaceutical sciences

authors： Kristl A

更新日期：1999-01-01 00:00:00

abstract：:Amorphous nifedipine (NFD), which has a smooth surface immediately after preparation, was shown to have structures resembling clusters of curling and branching fibers approximately 1 μm wide by atomic force microscopy (AFM) after storage at 25°C. The size of the cluster-like structures increased with storage over time...

journal_title：Journal of pharmaceutical sciences

authors： Miyazaki T,Aso Y,Kawanishi T

更新日期：2011-10-01 00:00:00

abstract：:(13) C cross-polarization magic-angle spinning nuclear magnetic resonance (CPMAS NMR) spectroscopy was applied to the identification and characterization of carvedilol (1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)-ethylamino]-propan-2-ol) in pharmaceutical preparations. Solid-state spectra (standard linewidth and l...

journal_title：Journal of pharmaceutical sciences

authors： Zielińska-Pisklak M,Pisklak DM,Wawer I

更新日期：2012-05-01 00:00:00

abstract：:The disposition kinetics of nicotine and cotinine enantiomers was determined in rabbits. The clearance of (R)-nicotine was similar to that of (S)-nicotine, but clearance of (R)-cotinine was twice that of (S)-cotinine. Fractional conversions of both enantiomers of nicotine to cotinine were approximately 50%. These resu...

journal_title：Journal of pharmaceutical sciences

authors： Jacob P 3rd,Benowitz NL,Copeland JR,Risner ME,Cone EJ

更新日期：1988-05-01 00:00:00

abstract：:In this study a 3D printed capsule designed to break from the physiological pressures in the antropyloric region was evaluated for its ability to deliver the synthetic octapeptide octreotide in beagle dogs when co-formulated with the permeation enhancer sodium caprate. The pressure sensitive capsules were compared to ...

journal_title：Journal of pharmaceutical sciences

authors： Berg S,Krause J,Björkbom A,Walter K,Harun S,Granfeldt A,Janzén D,Nunes SF,Antonsson M,Van Zuydam N,Skrtic S,Hugerth A,Weitschies W,Davies N,Abrahamsson B,Bergström CAS

更新日期：2021-01-01 00:00:00

abstract：:Conventionally, it is believed that the fraction of orally administered drugs absorbed from the intestine (Fa) and intestinal availability (Fg) are independently determined by the apical membrane permeation and intestinal metabolism, respectively. However, the validity of this belief has not been well discussed, and F...

journal_title：Journal of pharmaceutical sciences

authors： Tanaka Y,Kitamura Y,Maeda K,Sugiyama Y

更新日期：2016-02-01 00:00:00

abstract：:Profiles of the steady-state concentrations of haloperidol (HL) and its major metabolite, reduced haloperidol (RHL), in plasma versus time were determined in 10 Japanese patients whose schizophrenic symptoms were clinically controlled by fixed, oral maintenance doses (4-30 mg/day, three times a day) for greater than 4...

journal_title：Journal of pharmaceutical sciences

authors： Uematsu T,Matsuno H,Sato H,Hirayama H,Hasegawa K,Nakashima M

更新日期：1992-10-01 00:00:00

abstract：:A direct high-performance liquid chromatographic (HPLC) method was applied to monitor 2,5-diaziridinyl-3,6-bis(carboethoxyamino)-1,4-benzoquinone (I) and its degradation products in pharmaceutical vehicles at 25 +/- 0.1 degrees. At the optimal pH for stability of I, an increase in buffer concentration [phosphate and t...

journal_title：Journal of pharmaceutical sciences

authors： Poochikian GK,Kelley JA

更新日期：1981-02-01 00:00:00

abstract：:Progesterone release from monolithic devices prepared from various copolymers of poly(hydroxyethyl methacrylate) and poly(methoxyethoxyethyl methacrylate) or poly(methoxyethyl methacrylate) was examined. In general, plots of the fraction of drug released versus (time)1/2 were linear during the early stages of drug rel...

journal_title：Journal of pharmaceutical sciences

authors： Song SZ,Cardinal JR,Kim SH,Kim SW

更新日期：1981-02-01 00:00:00

abstract：:The dissolution rates of the two polymorphic forms of sulfathiazole containing polyethylene glycol 4000 were significantly different in water. The effect of agitation on the dissolution rates also was studied. At higher stirring speeds, the dissolution rates of the stable form were affected more than the metastable fo...

journal_title：Journal of pharmaceutical sciences

authors： Niazi S

更新日期：1976-02-01 00:00:00

abstract：:X-ray diffraction and infrared spectroscopy measurements for the N,N-dimethylformamide (DMF) and dimethyl sulfoxide (DMSO) solvatomorphs of betulonic acid (BA) were investigated. BA [3-oxolup-20(29)-en-28-oic acid, C(30)H(46)O(3)] exhibits a wide spectrum of biological activities and is considered to be a promising na...

journal_title：Journal of pharmaceutical sciences

authors： Boryczka S,Jastrzebska M,Bębenek E,Kusz J,Zubko M,Kadela M,Michalik E

更新日期：2012-12-01 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 dissolution characteristics of dicumarol were markedly enhanced by preparing dispersions of drug in polyethylene glycol 4000. Solid dispersions of varying weight fractions were formed by a melt method without measurable drug degradation or evaporation. There were no significant differences in dissolution rates amo...

journal_title：Journal of pharmaceutical sciences

authors： Ravis WR,Chen CY

更新日期：1981-12-01 00:00:00

abstract：:Several Several 10-(1-acetyl-4-arylthiosemicarbazido) phenothiazines and their corresponding cyclized 10-(2-arylimino-3-acetylamino-4-thiazolidonyl)phenothiazines were synthetized and characterized by their sharp melting points and elemental analyses. All compounds inhibited nicotinamide adenine dinucleotide (NAD)-dep...

journal_title：Journal of pharmaceutical sciences

authors： Singh SP,Ali B,Auyong TK,Parmar SS,De Boer B

更新日期：1976-03-01 00:00:00

abstract：:The aim of this study is to prepare novel pH-sensitive beads to obtain a gastric mucosa protective formulation and to ensure drug delivery into the intestine. Diclofenac sodium was used as a model drug. Bead formation was achieved by ionotropic gelation method using three-component gel system containing sodium alginat...

journal_title：Journal of pharmaceutical sciences

authors： Fenyvesi Z,Auner A,Schmalz D,Pásztor E,Csóka G,Gyires K,Marton S,Klebovich I,Antal I

更新日期：2009-11-01 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：:Drying is a common pharmaceutical process, whose potential to modify the final drug and/or dosage form properties is often underestimated. In the present study, pellets consisting of the matrix former calcium stearate (CaSt) incorporating the active pharmaceutical ingredient ibuprofen were prepared via wet extrusion a...

journal_title：Journal of pharmaceutical sciences

authors： Schrank S,Kann B,Windbergs M,Glasser BJ,Zimmer A,Khinast J,Roblegg E

更新日期：2013-11-01 00:00:00

abstract：:Foam granulation is a relatively newer wet granulation process whereby foamed binder solutions are added to powders in a mixer. It is essential to understand the effect of powder substrate on foam drainage and half-life, which are relevant to nucleation and agglomeration during foam granulation. Hydroxypropyl methylce...

journal_title：Journal of pharmaceutical sciences

authors： Koo OM,Ji J,Li J

更新日期：2012-04-01 00:00:00

abstract：:Aggregation of therapeutic monoclonal antibodies has a potential risk of immunogenicity, requiring minimization of aggregate formation. We have developed a fitting formula for antibody aggregation at 40°C based on physicochemical parameters, including colloidal and conformational stabilities. An IgG1 monoclonal antibo...

journal_title：Journal of pharmaceutical sciences

authors： Oyama H,Koga H,Tadokoro T,Maenaka K,Shiota A,Yokoyama M,Noda M,Torisu T,Uchiyama S

更新日期：2020-01-01 00:00:00