Partial molal volumes and solubilities of physostigmine in isopropanol:isopropyl myristate solvents in relation to skin penetrability.

Abstract:

:Partial molal volumes (Vi infinity) of physostigmine, ranging from 232.9 to 239.8 cm3.mol-1, and its mole fraction solubilities (Xi), ranging from 0.051 to 0.009, were determined at 25 degrees C in solutions of isopropanol (IPA), isopropyl myristate (IPM), and their mixtures. An inverse relation was found between Vi infinity and Xi. At solubility----0, Vi infinity----240.6 (by extrapolation). The experimentally derived liquid molal volume in the standard state, Vi degrees (231.1), of physostigmine was lower than its lowest Vi infinity (value 232.9) in the series tested. Virtual cohesion parameters (lambda i) and excess free energies (delta EGi) of physostigmine in the various solutions were estimated from the partial molal volumes, assuming regular solution behavior. For each solution, the free energy (-RT In Xi) of the drug was estimated from its solubility. An increase in the virtual cohesion parameter and a decrease in the excess free energy and the free energy was found with an increase in volume fraction of IPA in the mixed solvent. The increase in lambda i over the invariant cohesion parameter, delta i (10.2), reflects a compensation effect needed to maintain the geometric mean assumption of Regular Solution Theory. Deviation from the theoretically expected linearity between -RT In Xi and delta EGi of physostigmine is ascribed to the existence of solvated molecules distinct from unsolvated molecules of physostigmine. The highest permeability coefficient of the delivery of physostigmine through excised human skin from IPA:IPM mixtures was seen from the mixture exhibiting the highest solvation effect, giving additional evidence that physostigmine penetrates through the skin, possibly in combination with IPA.

journal_name

J Pharm Sci

authors

Pardo A,Shiri Y,Cohen S

doi

10.1002/jps.2600800615

subject

Has Abstract

pub_date

1991-06-01 00:00:00

pages

567-72

issue

6

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(15)48574-0

journal_volume

80

pub_type

杂志文章
  • The biologic effects of growth factor-toxin conjugates in models of vascular injury depend on dose, mode of delivery, and animal species.

    abstract::Toxin-conjugates, complexes designed from the fusion of tissue toxins and pathology-specific ligands, offer the potential for targeted cytotoxic therapy. Some have postulated that the recurrent failure of these conjugates to exhibit benefit in animal models of vascular injury arose because the timing and frequency of ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js980086i

    authors: Yu C,Cunningham M,Rogers C,Dinbergs ID,Edelman ER

    更新日期:1998-11-01 00:00:00

  • Use of pharmacological data for bioavailability and pharmacokinetic analyses.

    abstract::The use of pharmacological responses such as pupil diameter for dosage individualization, bioavailability, and pharmacokinetic analyses is becoming more widespread. Attempts to use pupil diameter to assess morphine bioavailability illuminate the fact that multiple responses, nonlinearities, and the condition of the su...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600660431

    authors: Kramer PA

    更新日期:1977-04-01 00:00:00

  • Intraamniotic prostaglandin F2-alpha dose--twenty-four-hour abortifacient response.

    abstract::Prostaglandin F2 alpha was administered intraamniotically to 132 mid-first trimester gravidas to determine the dose-24-hour abortifacient response relationship. Single doses between 15-50 mg and multiple doses between 15-25 mg were administered to 3 groups each, the latter regimen at 6-hour intervals. Trials were de...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600620809

    authors: Brenner WE,Hendricks CH,Fishburne JI Jr,Staurovsky L,Braaksma J,Taft R

    更新日期:1973-08-01 00:00:00

  • Dissolution profiles and specifications for dihydroergotoxine sublingual tablets using a new in vitro method.

    abstract::A dissolution method (paddle method) for determining the dissolution rate profile for 0.5- and 1.0-mg dihydroergotoxine methanesulfonate sublingual tablets was developed. A fluorometric method was used for measuring drug concentration in the dissolution medium, distilled water. It was essential to filter the dissoluti...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600700722

    authors: Hunt JP,Shah VP,Prasad VK,Schuirmann DJ,Cabana BE

    更新日期:1981-07-01 00:00:00

  • Correlation of drug absorption with molecular surface properties.

    abstract::The correlation between dynamic surface properties of drug molecules and drug absorption in two common in vitro models of the intestinal wall (Caco-2 monolayers and rat intestinal segments) has been investigated. A homologous series of beta-adrenoreceptor antagonists were used as model compounds. Dynamic molecular sur...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js950285r

    authors: Palm K,Luthman K,Ungell AL,Strandlund G,Artursson P

    更新日期:1996-01-01 00:00:00

  • Comparison of In Vivo Transportability of Anti-Methicillin-Resistant Staphylococcus aureus (MRSA) Agents Into Intracellular and Extracellular Tissue Spaces in Rats.

    abstract::The pathogenic bacterium Staphylococcus aureus can penetrate host cells. However, intracellular S. aureus is not considered during antimicrobial agent selection in clinical chemotherapy because of the lack of information about drug transportability into cells in vivo. We focused on agents used to treat methicillin-res...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2020.09.045

    authors: Kobuchi S,Kita Y,Hiramatsu Y,Sasaki K,Uno T,Ito Y,Sakaeda T

    更新日期:2021-02-01 00:00:00

  • New method for characterizing dissolution properties of drug powders.

    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

    pub_type: 杂志文章

    doi:10.1002/jps.2600660603

    authors: Pedersen PV

    更新日期:1977-06-01 00:00:00

  • Meropenem exists in equilibrium with a carbon dioxide adduct in bicarbonate solution.

    abstract::Evidence is provided for the existence of a second discrete chemical form of meropenem at clinically relevant concentrations prepared from the marketed formulation of the drug. Proton and carbon-13 NMR spectra in D2O, coupled with tandem mass spectroscopy (MS/MS) and cross polarization/magic angle spinning (CP-MAS) NM...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js970370u

    authors: Almarsson O,Kaufman MJ,Stong JD,Wu Y,Mayr SM,Petrich MA,Williams JM

    更新日期:1998-05-01 00:00:00

  • Development of a Novel Amorphous Agomelatine Formulation With Improved Storage Stability and Enhanced Bioavailability.

    abstract::The present work describes the development of a novel formulation of amorphous agomelatine (AGM) that exhibits enhanced in vitro dissolution rate and bioavailability, as well as improved storage stability. AGM was loaded on a mixture of microcrystalline cellulose with a high specific surface area excipient, namely col...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1016/j.xphs.2017.09.017

    authors: Barmpalexis P,Grypioti A,Vardaka E,Karagianni A,Kachrimanis K

    更新日期:2018-01-01 00:00:00

  • Establishment of a Drug-Induced, Bile Acid-Dependent Hepatotoxicity Model Using HepaRG Cells.

    abstract::Bile acid (BA) retention within hepatocytes is an underlying mechanism of cholestatic drug-induced liver injury (DILI). We previously developed an assay using sandwich-cultured human hepatocytes (SCHHs) to evaluate drug-induced hepatocyte toxicity accompanying intracellular BA accumulation. However, due to shortcoming...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2016.01.013

    authors: Susukida T,Sekine S,Nozaki M,Tokizono M,Oizumi K,Horie T,Ito K

    更新日期:2016-04-01 00:00:00

  • Slow-release characteristics of diltiazem from ethylated beta-cyclodextrin complexes.

    abstract::Release characteristics of two ethylated beta-cyclodextrins [heptakis(2,6-di-O-ethyl)-beta-cyclodextrin (diethyl-beta-cyclodextrin) and heptakis(2,3,6-tri-O-ethyl)-beta-cyclodextrin (triethyl-beta-cyclodextrin)] as sustained-release drug carriers were evaluated using diltiazem hydrochloride, a water-soluble calcium an...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600790211

    authors: Horiuchi Y,Hirayama F,Uekama K

    更新日期:1990-02-01 00:00:00

  • Efficacy of the injectable calcium phosphate ceramics suspensions containing magnesium, zinc and fluoride on the bone mineral deficiency in ovariectomized rats.

    abstract::The purpose of this study was to evaluate the therapeutic efficacy of a new calcium phosphate (CaP)-based formulation in improving the bone mineral deficiency in ovariectomized (OVX) rats. The ions release experiments for CaP preparations (G2: 0.46% Mg, 5.78% Zn, and 2.5% F; G3:3.1% Mg, 0.03% Zn, and 3.01% F; G4: 1.25...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21131

    authors: Otsuka M,Oshinbe A,Legeros RZ,Tokudome Y,Ito A,Otsuka K,Higuchi WI

    更新日期:2008-01-01 00:00:00

  • GLC determination of methenamine in tablets.

    abstract::A rapid and sensitive GLC method was developed for the quantitative determination of methenamine in tablets. The method was shown to possess several advantages over the official NF assay. After dissolution of the whole tablet in absolute ethanol and addition of an internal standard (pentylenetetrazol), an aliquot was ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600660435

    authors: Strom JG Jr,Jun HW

    更新日期:1977-04-01 00:00:00

  • Extraction and analysis by high-performance liquid chromatography of antibiotics in a drug delivery system for farmed fish.

    abstract::Simple assays for extraction and determination of the concentrations of the antibiotics oxytetracycline, oxolinic acid, and flumequine in a drug dosage form for farmed fish are described. HPLC with UV detection was used in the analyses. The recovery of all three drugs was approximately 100%, and the precision varied f...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600820517

    authors: Rogstad A,Weng B

    更新日期:1993-05-01 00:00:00

  • Prediction of the adsorption of diazepam by activated carbon in aqueous media.

    abstract::Adsorption isotherms for the diazepam-activated carbon system in simulated intestinal fluid (SIF), without pancreatin, and in SIF with different percentages of ethanol were determined as were the solubilities of diazepam in SIF and in SIF with different percentages of ethanol. The surface area of the activated carbon ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.10454

    authors: Wurster DE,Alkhamis KA,Matheson LE

    更新日期:2003-10-01 00:00:00

  • Novel pH-sensitive physical hydrogels of carboxymethyl scleroglucan.

    abstract::A carboxymethyl derivative of scleroglucan (Scl-CM) with derivatization degree 300 ± 10 was synthesized and characterized by Fourier transform infrared spectroscopy, potentiometer titration, mucus adhesion studies, and rheological measurements. Rheological measurements showed the ability of the polymer to undergo sol-...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22766

    authors: Corrente F,Paolicelli P,Matricardi P,Tita B,Vitali F,Casadei MA

    更新日期:2012-01-01 00:00:00

  • Myocardial effect compartment modeling of metoprolol and sotalol: importance of myocardial subsite drug concentration.

    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

    pub_type: 临床试验,杂志文章

    doi:10.1021/js9702776

    authors: Ritchie RH,Morgan DJ,Horowitz JD

    更新日期:1998-02-01 00:00:00

  • Very rapid dissolution is not needed to guarantee bioequivalence for biopharmaceutics classification system (BCS) I drugs.

    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

    pub_type: 杂志文章

    doi:10.1002/jps.21879

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

    更新日期:2010-02-01 00:00:00

  • Prediction of distribution coefficient from structure. 1. Estimation method.

    abstract::A method has been developed for the estimation of the distribution coefficient (D), which considers the microspecies of a compound. D is calculated from the microscopic dissociation constants (microconstants), the partition coefficients of the microspecies, and the counterion concentration. A general equation for the ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js960177k

    authors: Csizmadia F,Tsantili-Kakoulidou A,Panderi I,Darvas F

    更新日期:1997-07-01 00:00:00

  • Current Inhalers Deliver Very Small Doses to the Lower Tracheobronchial Airways: Assessment of Healthy and Constricted Lungs.

    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

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2015.11.027

    authors: Walenga RL,Longest PW

    更新日期:2016-01-01 00:00:00

  • Cerebral kinetics of oxycodone in conscious sheep.

    abstract::Oxycodone is an opioid analgesic that is administered orally or parenterally. The time-course of opioid action is a function of the systemic kinetics of the opioid, and the rate and extent of its entry into the brain and central nervous system. The latter is incompletely understood for oxycodone. Therefore, the cerebr...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20632

    authors: Villesen HH,Foster DJ,Upton RN,Somogyi AA,Martinez A,Grant C

    更新日期:2006-08-01 00:00:00

  • Regulation of Tight-Junction Integrity by Insulin in an In Vitro Model of Human Blood-Brain Barrier.

    abstract::Although insulin receptor is expressed at the human blood-brain barrier (BBB), the physiological and pathologic roles of insulin signaling in biologic responses at the BBB remain unclear. Here, we investigate insulin signaling at the human BBB using human cerebral microvascular endothelial cell line (hCMEC/D3) as a we...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2017.04.036

    authors: Ito S,Yanai M,Yamaguchi S,Couraud PO,Ohtsuki S

    更新日期:2017-09-01 00:00:00

  • Mechanism of action of retinyl compounds on wound healing IV: effect of desmethylretinoic acid and its vinylogs on granuloma formation.

    abstract::The effect of side-chain length of desmethylretinoic acid on granuloma formation induced by implantation of cotton pellets was studied. As in the homologous series of retinoic acid studies, compounds with side chains shorter than retinoic acid were not active while compounds with side chains as long or longer than ret...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600650425

    authors: Lee KH,Fu CC,Jung M

    更新日期:1976-04-01 00:00:00

  • Application of Physiologically Based Pharmacokinetic Modeling to Predict the Effects of FcRn Inhibitors in Mice, Rats, and Monkeys.

    abstract::There is a growing interest in developing inhibitors of the neonatal Fc-receptor, FcRn, for use in the treatment for humoral autoimmune conditions. We have developed a new physiologically based pharmacokinetic model that is capable of characterizing the pharmacokinetics and pharmacodynamics of anti-FcRn monoclonal ant...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2018.10.065

    authors: Li T,Balthasar JP

    更新日期:2019-01-01 00:00:00

  • Anticonvulsant activity and selective inhibition of nicotinamide adenine dinucleotide-dependent oxidations by 10-(2-arylimino-3-acetylamino-4-thiazolidonyl) phenothiazines.

    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

    pub_type: 杂志文章

    doi:10.1002/jps.2600650319

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

    更新日期:1976-03-01 00:00:00

  • Simultaneous determination of unlabeled and carbon-13-labeled etoricoxib, a new cyclooxygenase-2 inhibitor, in human plasma using HPLC-MS/MS.

    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

    pub_type: 杂志文章

    doi:10.1002/jps.10038

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

    更新日期:2002-02-01 00:00:00

  • Development and Evaluation of a Novel Drug Delivery: Pluronics/SDS Mixed Micelle Loaded With Myricetin In Vitro and In Vivo.

    abstract::This study is to prepare and evaluate Pluronics-modified mixed micelle (MM) to deliver polyphenolic myricetin (MYR) across the blood-brain barrier. MYR has been proven to be an effective anticancer agent against glioblastoma cells in our previous studies. However, the poor solubility of MYR limits its access to the br...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2016.01.016

    authors: Wang G,Wang JJ,Li F,To SS

    更新日期:2016-04-01 00:00:00

  • A lamellar liquid crystal with fosinopril sodium.

    abstract::The location and conformation of fosinopril sodium (FS) in a lamellar liquid crystal of water, sodium dodecyl sulfate, and decanol was studied by low-angle X-ray diffraction. The result showed the FS molecule to be located within the amphiphilic part of the liquid crystalline structure with the polar parts anchored at...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600830517

    authors: Friberg SE,Moaddel T,Morris KR,Abramowitz R,Amsberry KL

    更新日期:1994-05-01 00:00:00

  • Convenient synthesis of alkyl esters of urocanic acid.

    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

    pub_type: 杂志文章

    doi:10.1002/jps.2600700123

    authors: Honda K,Nishijima Y

    更新日期:1981-01-01 00:00:00

  • Validation of washing procedures for maintaining a microbiologically clean gel filtration column.

    abstract::Chromatographic gel filtration matrixes used in various separation techniques are subject to microbial contamination. The need for a microbe-free column is critical when preparing materials that require a low or zero microbial count. This report proposes two alternative washing systems: 0.02 N HCl containing 0.81% NaC...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600690205

    authors: Wen LF,Bohannon T,Crabb A,Mamaril F

    更新日期:1980-02-01 00:00:00