Facile synthesis of glycol metabolites of phenethylamine drugs.

abstract：:The in vitro release of physostigmine salicylate (PS) from a submicron emulsion and an aqueous solution was studied using the dialysis bag method. These formulations were then perfused to various locations along the rat small intestine (proximal, mid, and distal jejunum), and two lengths (10 and 55 cm). The disappeara...

journal_title：Journal of pharmaceutical sciences

authors： Rubinstein A,Pathak YV,Kleinstern J,Reches A,Benita S

更新日期：1991-07-01 00:00:00

abstract：:Health authorities require that suitable stability of the drug substance be shown in relevant materials of construction. ICH Q1A(R2) explicitly states that "stability studies should be conducted on drug substance packaged in a container closure system that is the same as or simulates the packaging proposed for storage...

journal_title：Journal of pharmaceutical sciences

authors： Klair N,Kim MT,Lee A,Xiao NJ,Patel AR

更新日期：2020-10-07 00:00:00

abstract：:Sucrose is a common cryoprotectant and lyoprotectant to stabilize labile biopharmaceuticals during freeze-drying and storage. Sucrose-based formulations require low primary drying temperatures to avoid collapse and monoclonal antibody (mAb) containing products need to be stored refrigerated. The objective of this stud...

journal_title：Journal of pharmaceutical sciences

authors： Haeuser C,Goldbach P,Huwyler J,Friess W,Allmendinger A

更新日期：2020-01-01 00:00:00

abstract：:The aim of this study is to evaluate the effect of peptide cyclization on the blood-brain barrier (BBB) modulatory activity and plasma stability of His-Ala-Val peptides, which are derived from the extracellular 1 domain of human E-cadherin. The activities to modulate the intercellular junctions by linear HAV4 (Ac-SHAV...

journal_title：Journal of pharmaceutical sciences

authors： Alaofi A,On N,Kiptoo P,Williams TD,Miller DW,Siahaan TJ

更新日期：2016-02-01 00:00:00

abstract：:A GLC determination of cyclobenzaprine in human plasma and urine is described. After extraction from alkalinized samples with heptane-isopentyl alcohol (97:3), the drug and internal standard were back-extracted into 0.1 N HCl and then reextracted into ether. Use of a lower homolog of the drug as an internal standard w...

journal_title：Journal of pharmaceutical sciences

authors： Hucker HB,Stauffer SC

更新日期：1976-08-01 00:00:00

abstract：:Apparent acidity constants obtained for various benzothiadiazine diuretics by semiaqueous potentiometric titrations gave satisfactory agreement with many values obtained by aqueous potentiometry. One suitable method for determining the acidity constants of sparingly soluble drugs, the solubility variation with pH tech...

journal_title：Journal of pharmaceutical sciences

authors： Hennig UG,Moskalyk RE,Chatten LG,Chan SF

更新日期：1981-03-01 00:00:00

abstract：:The combined clearance of endogenous 6β-hydroxycortisol and 6β-hydroxycortisone is suggested biomarker for in vivo cytochrome P450 3A (CYP3A) activity. We aimed to determine whether the combined clearance of these two markers together with information of biopharmaceutics classification system (BCS) of drugs could be u...

journal_title：Journal of pharmaceutical sciences

authors： Luo X,Zheng L,Cai N,Liu Q,Yang S,He X,Cheng Z

更新日期：2015-10-01 00:00:00

abstract：:In this study, injectable microspheres were developed for the local treatment of joint degeneration in rheumatoid arthritis (RA). Microspheres loaded with triamcinolone (TA), a corticosteroid drug, and/or raloxifene (Ral), a cartilage regenerative drug, were prepared with a biodegradable and biocompatible polymer, pol...

journal_title：Journal of pharmaceutical sciences

authors： Ocal Y,Kurum B,Karahan S,Tezcaner A,Ozen S,Keskin D

更新日期：2014-08-01 00:00:00

abstract：:Aerosolized medicine is one of the fastest growing areas in the pharmaceutical industry. Dry powder aerosols of pharmaceutical compounds are particularly attractive for the prevention and treatment of respiratory diseases but are also emerging as a treatment option for systemic diseases. Engineering particles in dry p...

journal_title：Journal of pharmaceutical sciences

authors： El-Gendy N,Selvam P,Soni P,Berkland C

更新日期：2012-09-01 00:00:00

abstract：:The hydrogen-bonded interactions of chloral hydrate and halide ions have been investigated conductometrically at 25.00 degrees C in aqueous solutions. In spite of the strong competing effect of water, the 1:1 associates have relatively high stability constants, in the order of chloride greater than bromide greater tha...

journal_title：Journal of pharmaceutical sciences

authors： Barcza L,Lenner L

更新日期：1988-07-01 00:00:00

abstract：:Upon exposure to shaking stress, an IgG1 mAb formulation in both the liquid and lyophilized state formed subvisible particles. Because freeze-drying was expected to minimize protein physical instability under these conditions, the extent and nature of aggregate formation in the lyophilized preparation were examined us...

journal_title：Journal of pharmaceutical sciences

authors： Telikepalli S,Kumru OS,Kim JH,Joshi SB,O'Berry KB,Blake-Haskins AW,Perkins MD,Middaugh CR,Volkin DB

更新日期：2015-02-01 00:00:00

abstract：:Determination of the kinetics of water-soluble degradation products inside poly(lactide-co-glycolide) (PLGA) delivery systems during polymer degradation is important to evaluate the polymer microclimate conditions, particularly microclimate pH changes for optimization of encapsulated drug stability. A pre-derivatizati...

journal_title：Journal of pharmaceutical sciences

authors： Ding AG,Schwendeman SP

更新日期：2004-02-01 00:00:00

abstract：:A difference spectrophotometric analytical method was developed for the selective determination of p-hydroxybenzoic acid in the presence of its alkyl esters without prior separation. Based on the spectral shift to a shorter wavelength accompanyint carboxyl dissociation, the procedure measures as little as 2% of this a...

journal_title：Journal of pharmaceutical sciences

authors： Fink DW,Fink HC,Tolan JW,Blodinger J

更新日期：1978-06-01 00:00:00

abstract：:To evaluate the regional delivery of conventional aerosol medications, a new whole-lung computational fluid dynamics modeling approach was applied for metered dose inhaler (MDI) and dry powder inhaler (DPI) aerosols delivered to healthy and constricted airways. The computational fluid dynamics approach included comple...

journal_title：Journal of pharmaceutical sciences

authors： Walenga RL,Longest PW

更新日期：2016-01-01 00:00:00

abstract：:A series of 3-substituted indeno[1,2-c]pyrazol-4(1H)-one-2-acetic acids (3a-e) and 3-substituted indeno[1,2-c]pyrazol-4(1H)-one-1-acetic acids (4a-e) were synthesized as semirigid analogues of tolmetin (1). These compounds were evaluated for their anti-inflammatory action by investigating their ability to block arachi...

journal_title：Journal of pharmaceutical sciences

authors： Lemke TL,Abebe E,Moore PF,Carty TJ

更新日期：1989-04-01 00:00:00

abstract：:3-N-(1',8'-Naphthalimido)propionic acid was synthesized and shown to effectively lower both serum cholesterol and triglyceride levels in rats and mice. In hyperlipidemic mice, serum lipid levels were lowered significantly, approaching normal levels of cholesterol and below normal levels of triglyceride. The serum lipi...

journal_title：Journal of pharmaceutical sciences

authors： Hall IH,Chapman JM Jr,Voorstad PJ,Cocolas GH

更新日期：1984-07-01 00:00:00

abstract：:Cisplatin (CDDP) is an effective anticancer agent for many solid tumors but has significant systemic toxicity limiting its use in many patients. We have designed a loco-regional delivery system to increase platinum levels in the lymphatics, where early metastasis is most likely to occur, while reducing systemic toxici...

journal_title：Journal of pharmaceutical sciences

authors： Cai S,Xie Y,Davies NM,Cohen MS,Forrest ML

更新日期：2010-06-01 00:00:00

abstract：:A fully automated system for dissolution rate analysis of potassium in slow release tablets is described. Aliquots are removed after 1, 2, and 4 hr from six samples, and potassium is analyzed in a flame photometer at 768 nm. A complete study of six samples takes 5.5 hr. The system may be run overnight. During the time...

journal_title：Journal of pharmaceutical sciences

authors： Engdahl A,Karlberg B,Thelander S

更新日期：1976-03-01 00:00:00

abstract：:Azo compounds are commonly used to study radical-mediated degradation of pharmaceutical compounds. The favorable chemical and physical properties of 2,2'-azobis(2-methylpropanenitrile) (AIBN) have made it one of the most widely used compound for these type of studies. This article describes the characterization of a s...

journal_title：Journal of pharmaceutical sciences

authors： Wells-Knecht KJ,Dunn D

更新日期：2019-09-01 00:00:00

abstract：:Reported estrone pKa and solubility data show wide variation. Improved experimental procedures were designed and used to obtain reproducible results. The pKa values for several estrogens and related compounds also were determined to assess the effects of structural differences on ionization. No evidence was obtained f...

journal_title：Journal of pharmaceutical sciences

authors： Hurwitz AR,Liu ST

更新日期：1977-05-01 00:00:00

abstract：:The objective of the current study was to evaluate the performance of Raman and near-infrared (NIR) techniques combined with chemometrics in characterizing the critical quality attributes of brompheniramine (BP)-tannate complexes. Seven complexes were prepared and evaluated for chemical interactions, solubilities, dis...

journal_title：Journal of pharmaceutical sciences

authors： Zidan AS,Rahman Z,Khan MA

更新日期：2012-04-01 00:00:00

abstract：:Baclofen immediate release mode of administration exhibit sharp plasma peaking that results in the emergence of side effects like hypotension. This research employs preformulation studies to design an optimum dosage form for baclofen to enhance therapeutic outcomes. These studies include partition coefficient and ex-v...

journal_title：Journal of pharmaceutical sciences

authors： Ibrahim M,Naguib YW,Sarhan HA,Abdelkader H

更新日期：2020-10-15 00:00:00

abstract：:In vitro iontophoretic administration of drugs through a microporous polyolefin membrane with hydrophilic urethane polymerfilled pores was done for the ionized drugs dexamethasone sodium phosphate, hydrocortisone sodium phosphate, and prednisolone sodium succinate, and for a nonionizable drug cortisone acetate. Curren...

journal_title：Journal of pharmaceutical sciences

authors： Tu YH,Allen LV Jr

更新日期：1989-03-01 00:00:00

abstract：:A stability-indicating analytical method is described for the simultaneous determination of nitrate, and if present, its reductive degradation product, nitrite, in toothpastes. Nitrate and nitrite were extracted from the toothpaste using distilled water and separated from other water-soluble excipients by two RP-8 col...

journal_title：Journal of pharmaceutical sciences

authors： Lulla H,Chen SS,Sena FJ

更新日期：1984-07-01 00:00:00

abstract：:The dielectric constant of a solid substance in the dissolved state may be found by using a solvent with a dielectric constant that remains invariable when the solid substance is dissolved. The slope values obtained from dielectric constant versus concentration plots of the solid substance in two solvents with differe...

journal_title：Journal of pharmaceutical sciences

authors： Cavé G,Puisieux F,Carstensen JT

更新日期：1979-04-01 00:00:00

abstract：:Male fertility has reportedly been regulated by the long-term, continuous administration of testosterone. To deliver the testosterone at a controlled rate for a month or longer, a bandage-type, testosterone-releasing, disk-shaped device was developed. In vitro drug elution studies demonstrated that a constant release ...

journal_title：Journal of pharmaceutical sciences

authors： Chien YW

更新日期：1984-08-01 00:00:00

abstract：:The growing interest of pharmaceutical companies toward the crystal morphology prediction of active pharmaceutical ingredients is a consequence of the dramatic effect of the crystal habit on the tableting behavior of drugs. In order to help the optimization of the industrial process, molecular mechanics calculations t...

journal_title：Journal of pharmaceutical sciences

authors： Li Destri G,Marrazzo A,Rescifina A,Punzo F

更新日期：2013-01-01 00:00:00

abstract：:Previous studies from this laboratory suggested that a solution model (Flory-Huggins equation) modified by a free volume model (Vrentas equation) could satisfactorily describe water absorption into an amorphous solid composed of a sugar or a polymer. This paper has extended the studies of single solutes to binary mixt...

journal_title：Journal of pharmaceutical sciences

authors： Zhang J,Zografi G

更新日期：2001-09-01 00:00:00

abstract：:The standard free energy change (delta G0) for equilibrium dissolution in binary solvent mixtures is written as a sum of effects arising from solvent-solvent interactions (the general medium effect), solvent-solute interactions (the solvation effect), and solute-solute interactions (the intersolute effect). The genera...

journal_title：Journal of pharmaceutical sciences

authors： Khossravi D,Connors KA

更新日期：1992-04-01 00:00:00

abstract：:To relate the reported positive effect of food on the oral bioavailability of abiraterone to the intraluminal behavior of abiraterone acetate, an in vivo experiment was performed, in which duodenal fluids and plasma samples were collected from healthy volunteers after the administration of abiraterone acetate in faste...

journal_title：Journal of pharmaceutical sciences

authors： Geboers S,Stappaerts J,Mols R,Snoeys J,Tack J,Annaert P,Augustijns P

更新日期：2016-09-01 00:00:00