Explication of Definitional Description and Empirical Use of Fraction of Orally Administered Drugs Absorbed From the Intestine (Fa) and Intestinal Availability (Fg): Effect of P-glycoprotein and CYP3A on Fa and Fg.

abstract：:Using two UV-spectrophotometric methods, the hydrolysis of tinidazole was studied at pH 1.00-8.45 at 80 degrees C. The reaction followed apparent first-order kinetics throughout the studied range. No kinetic salt effect was detected, indicating that at least one of the reacting partners forming the transition state ha...

journal_title：Journal of pharmaceutical sciences

authors： Salo JP,Yli-Kauhaluoma J,Salomies H

更新日期：2003-04-01 00:00:00

abstract：:A GLC method was developed for the determination of ethylene oxide and its two reaction products, ethylene chlorohydrin and ethylene glycol, in ophthalmic solutions at the levels recently proposed by the Food and Drug Administration. The method requires no extractions, sample preparations, or elaborate trapping and co...

journal_title：Journal of pharmaceutical sciences

authors： Manius GJ

更新日期：1979-12-01 00:00:00

abstract：:Various multiparticulate dissolution models that assume a log-normal particle-size distribution are fitted by nonlinear least-squares regression to data from the dissolution of micronized glyburide. Estimates of parameters describing the effective initial particle-size distribution are obtained, together with estimate...

journal_title：Journal of pharmaceutical sciences

authors： Pedersen PV

更新日期：1977-06-01 00:00:00

abstract：:Pelrinone HCl is essentially nonhygroscopic. The pH-solubility profile exhibits a U-shaped curve, while the octanol-water partition coefficient-pH profile shows a bell-shaped curve. Two ionizable functions, with a pKa1 value of 4.71 and a pKa2 value of 8.94, produce the cationic and anionic forms, respectively. A weak...

journal_title：Journal of pharmaceutical sciences

authors： Hajdu J,Adams G,Lee HK

更新日期：1988-11-01 00:00:00

abstract：:A α-helical GALA peptide (WEAALAEALAEALAEHLAEALAEALEALAA) has been found to possess dual functions: a pH-dependent inducer of endosomal escape, and a ligand that targets lung endothelium. In the present study, the flexibility of GALA was improved by modifying the edge with polyethylene glycol linker, to increase lung-...

journal_title：Journal of pharmaceutical sciences

authors： Santiwarangkool S,Akita H,Nakatani T,Kusumoto K,Kimura H,Suzuki M,Nishimura M,Sato Y,Harashima H

更新日期：2017-09-01 00:00:00

abstract：:A crossover experiment was utilized to compare the pharmacokinetics of a 1-g dose of cephalexin tablets, cephalexin capsules, or cephradine capsules in nine normal human volunteers. These antibiotics were administered as three formulations: two 500-mg capsulin every 6 hr for five doses, and one 1000-mg tablet of cepha...

journal_title：Journal of pharmaceutical sciences

authors： Finkelstein E,Quintiliani R,Lee R,Bracci A,Nightingale CH

更新日期：1978-10-01 00:00:00

abstract：:A revised classification system for oral drugs was developed using the biopharmaceutics classification system (BCS) as a starting point. The revised system is designed to have a greater focus on drug developability. Intestinal solubility, the compensatory nature of solubility and permeability in the small intestine an...

journal_title：Journal of pharmaceutical sciences

authors： Butler JM,Dressman JB

更新日期：2010-12-01 00:00:00

abstract：:A continuous nonisothermal-isothermal method for stability prediction was developed. The approach yields all necessary parameters for prediction, including reaction order. The experimental procedure involves changing the temperature of the samples being studied until degradation is rapid enough to proceed at a conveni...

journal_title：Journal of pharmaceutical sciences

authors： Zoglio MA,Maulding HV,Streng WH,Vincek WC

更新日期：1975-08-01 00:00:00

abstract：:The geometry and structural features of the inclusion complexes of beta-cyclodextrin (beta-CD) with the chiral antiamnesic drugs (+/-)-1-benzyl-4-hydroxymethylpyrrolidin-2-one (WEB-1868). (+/-)-1-benzenesulfonyl-5-ethoxypyrrolidin-2-one (RU-35929), and (+/-)-1-(3-pyridinlysulfonyl)-5-ethoxypyrrolidin-2-one (RU-47010) ...

journal_title：Journal of pharmaceutical sciences

authors： Amato ME,Djedaïni F,Pappalardo GC,Perly B,Scarlata G

更新日期：1992-12-01 00:00:00

abstract：:The highly lipid soluble, free-base form of halofantrine (Hf base; approximately 50 mg/mL in triglyceride lipids), a highly lipophilic (calculated log P approximately 8.5) antimalarial, has recently been shown to undergo significant intestinal lymphatic transport (54% of administered dose) after postprandial administr...

journal_title：Journal of pharmaceutical sciences

authors： Khoo SM,Prankerd RJ,Edwards GA,Porter CJ,Charman WN

更新日期：2002-03-01 00:00:00

abstract：:Compact strength and the particle-size distribution of milled roller compacted compacts were correlated to the slope of the best-fit line through near-infrared spectra for samples prepared under different roll speeds and feed rates. The above correlations were found to hold for compacts prepared from microcrystalline ...

journal_title：Journal of pharmaceutical sciences

authors： Gupta A,Peck GE,Miller RW,Morris KR

更新日期：2004-04-01 00:00:00

abstract：:The progress in continuous downstream manufacturing of oral solid doses demands effective real-time process management, with monitoring at its core. This study evaluates the feasibility of using a commercial sensor to measure the mass flow rate of the particulates, a critical process variable in continuous manufacturi...

journal_title：Journal of pharmaceutical sciences

authors： Ganesh S,Troscinski R,Schmall N,Lim J,Nagy Z,Reklaitis G

更新日期：2017-12-01 00:00:00

abstract：:Solid dispersion (SD) of indomethacin with crospovidone (CrosPVP) shows useful characteristics for preparation of dosage forms. This study aimed to determine the types of drugs that could adopt a stable amorphous form in SD. Twenty compounds with various melting points (70-218 degrees C), molecular weights (135-504) a...

journal_title：Journal of pharmaceutical sciences

authors： Shibata Y,Fujii M,Kokudai M,Noda S,Okada H,Kondoh M,Watanabe Y

更新日期：2007-06-01 00:00:00

abstract：:Circular dichroism (CD) spectroscopy is routinely used in the biopharmaceutical industry to study the effects of manufacturing, formulation, and storage conditions on protein conformation and stability, and these results are often included in regulatory filings. In this context, the purpose of CD spectroscopy is often...

journal_title：Journal of pharmaceutical sciences

authors： Li CH,Nguyen X,Narhi L,Chemmalil L,Towers E,Muzammil S,Gabrielson J,Jiang Y

更新日期：2011-11-01 00:00:00

abstract：:Antisense phosphorodiamidate Morpholino oligomers (PMO) are resistant to degradation by cellular hydrolases, DNases, RNases, and phosphodiesterases, but remain sensitive to prolonged exposure to low pH. The present studies evaluate the oral fractional bioavailability, stability, and efficacy of two distinct PMO sequen...

journal_title：Journal of pharmaceutical sciences

authors： Arora V,Knapp DC,Reddy MT,Weller DD,Iversen PL

更新日期：2002-04-01 00:00:00

abstract：:Die filling is a critical process step during tablet production as it defines the tablet weight. Achieving die fill consistency during production of mini-tablets, tablets with diameters ≤6 mm, is considerably more challenging. Although die filling in rotary presses had been studied in relation to the feed paddle desig...

journal_title：Journal of pharmaceutical sciences

authors： Goh HP,Sia Heng PW,Liew CV

更新日期：2019-03-01 00:00:00

abstract：:Specifically tailored amino acid-based formulations were previously shown to have a high potential to avoid stress-mediated degradation of complex molecules such as monoclonal antibodies and viral vectors. By using adenovirus 5 (Ad5) as a model, we studied whether such formulations may also efficiently protect viral v...

journal_title：Journal of pharmaceutical sciences

authors： Reinauer EB,Grosso SS,Henz SR,Rabas JA,Rodenstein C,Altrichter J,Scholz M,Kemter KF

更新日期：2020-01-01 00:00:00

abstract：:A computational approach which concomitantly determines the capacity-limited rate constants of parent drug elimination and metabolite formation is presented. The approach applies both the presently derived total excretory recovery versus dose relationships of the metabolite and the AUC versus dose relationships of the...

journal_title：Journal of pharmaceutical sciences

authors： Chow AT,Jusko WJ

更新日期：1990-10-01 00:00:00

abstract：:Eight analogs of the fentanyl-type analgesics, in which the piperidine ring is restricted into a boat conformation, were evaluated for analgesic activity. All analogs were less active than fentanyl, but interesting conformational and structural relationships were observed. Results of the study are discussed. ...

journal_title：Journal of pharmaceutical sciences

authors： Borne RF,Law SJ,Kapeghian JC,Masten LW

更新日期：1980-09-01 00:00:00

abstract：:Targeted echogenic liposome dispersions for ultrasonic enhancement of vasoactive and pathological components of endothelium and atherosclerosis have recently been developed. The component lipids required for acoustic and targeting properties include phosphatidylcholine, phosphatidylethanolamine phosphatidylglycerol (P...

journal_title：Journal of pharmaceutical sciences

authors： Huang SL,Hamilton AJ,Nagaraj A,Tiukinhoy SD,Klegerman ME,McPherson DD,Macdonald RC

更新日期：2001-12-01 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：:A method of depicting dimensional illustrations of molecules in vacuo that are sensitive to small electronic perturbations was attempted. This method would be useful in determining the effects of either perturbing groups from other molecules or changes produced by the addition or modification of an existing atom or ch...

journal_title：Journal of pharmaceutical sciences

authors： Breon TL,Petersen H Jr,Paruta AN

更新日期：1978-01-01 00:00:00

abstract：:Cephalosporins are among the most frequently used broad-spectrum antimicrobial agents. Ceftazidime is a semisynthetic β-lactam antibiotic for parenteral administration widely used in the clinical practice, which has been categorized as a third-generation cephalosporin antibiotic. This drug crystallizes as a pentahydra...

journal_title：Journal of pharmaceutical sciences

authors： Alves de Santana MS,Santiago de Oliveira Y,de Castro Fonseca J,Ferreira WC,Neto VS,Ayala AP

更新日期：2020-03-01 00:00:00

abstract：:A representative series of hydroxy-5 beta-cholanyl-24-amines were tested both in vitro and in vivo with respect to their activity against the intestinal bacteria responsible for bile acid metabolism. For the in vitro studies, radiolabeled [14C]cholic acid was incubated with human stools both in aerobic and anaerobic c...

journal_title：Journal of pharmaceutical sciences

authors： Roda A,Bellini AM,Mencini E,Minutello A,Fini A,Guarneri M

更新日期：1992-03-01 00:00:00

abstract：:A new indole based chalcone molecule MOMIPP induced methuosis mediated cell death in gliobastoma and other cancer cell lines. But the drug was insoluble in water and had a very short plasma half-life. The purpose of this work was to develop a formulation that can provide sustained levels of MOMIPP in vivo. Initial stu...

journal_title：Journal of pharmaceutical sciences

authors： Oppong F,Li Z,Fakhrabadi EA,Raorane T,Giri PM,Liberatore MW,Sarver JG,Trabbic CJ,Hosier CE,Erhardt PW,Maltese WA,Nesamony J

更新日期：2020-09-01 00:00:00

abstract：:In an attempt to explain the triamterene stone diathesis, we studied the excretion and solubility of triamterene, 1, and its metabolite, the sulfate ester of the hydroxy derivative of triamterene, 3. The urinary excretion pattern and metabolism in stone formers was the same as in other chronic users of triamterene or ...

journal_title：Journal of pharmaceutical sciences

authors： Sörgel F,Ettinger B,Benet LZ

更新日期：1986-02-01 00:00:00

abstract：:The solubility of ergotamine tartrate in aqueous solutions of tartaric acid, citric acid, hydrochloric acid, and caffeine and the dissolution rate of ergotamine tartrate in aqueous mixtures containing hydrochloric acid, caffeine, citric acid, or sodium acetate were studied. The Noyes-Whitney model of dissolution is us...

journal_title：Journal of pharmaceutical sciences

authors： Anderson JR,Pitman IH

更新日期：1980-07-01 00:00:00

abstract：:Griseofulvin/cyclodextrin interactions were investigated in aqueous environment and in solid state. Two cyclodextrin derivatives (beta-cyclodextrin and 2-hydroxypropyl beta-cyclodextrin) were used to prepare different physical mixtures and kneaded systems, and the drug/cyclodextrin ratios were 1:1 and 1:2 mol/mol. Sca...

journal_title：Journal of pharmaceutical sciences

authors： Veiga MD,Díaz PJ,Ahsan F

更新日期：1998-07-01 00:00:00

abstract：:Nanocrystals have emerged as a potential formulation strategy to eliminate the bioavailability-related problems by enhancing the initial dissolution rate and moderately super-saturating the thermodynamic solubility. This review contains an in-depth knowledge of, the processing method for formulation, an accurate quant...

journal_title：Journal of pharmaceutical sciences

authors： Shah DA,Murdande SB,Dave RH

更新日期：2016-01-01 00:00:00

abstract：:3D cultures of primary human hepatocytes (PHH) are emerging as a more in vivo-like culture system than previously available hepatic models. This work describes the characterisation of drug metabolism in 3D PHH spheroids. Spheroids were formed from three different donors of PHH and the expression and activities of impo...

journal_title：Journal of pharmaceutical sciences

authors： Kanebratt KP,Janefeldt A,Vilén L,Vildhede A,Samuelsson K,Milton L,Björkbom A,Persson M,Leandersson C,Andersson TB,Hilgendorf C

更新日期：2021-01-01 00:00:00