Abstract:
:Several factors affecting the dissolution rate of cholesterol in monooctanoin were investigated. This solvent is used clinically for dissolution of residual cholesterol gallstones in the bile duct after cholecystectomy. The effect of added water on dissolution rate, measured using the static- or rotating-disk methods, was not consistent with the previously measured solubility. The discrepancy was found to be due to the decreasing viscosity of the solvent as water was added. Addition of cholesterol, however, increased the viscosity of monooctanoin. The viscosity effect on dissolution rate was investigated further by addition of polymers (povidone and poloxamer 237) which increased solvent viscosity. Dissolution rate was proportional to viscosity to the -0.4 power with these polymers. An equation was derived which predicts that dissolution rate should be proportional to viscosity to the -2/3 power. The predicted exponent was very close to reported experimental values for benzoic acid, but the dissolution rate/viscosity relationship for cholesterol in aqueous monooctanoin was nonlinear with apparent exponents of -0.65 to -2.3. Although the Arrhenius activation energies for viscosity (3.79 kcal/mol) and dissolution rate constant (3.66 kcal/mol) were almost equal for benzoic acid, a nonlinear relationship was again observed for cholesterol in aqueous monooctanoin with approximate Ea values of 5.6-10 kcal/mol. The strong influence of viscosity on dissolution rate in this system is attributed to the viscosity-increasing effect of cholesterol in the diffusion layer. The increased viscosity at higher cholesterol concentrations reduces the diffusion coefficient of cholesterol and causes the dissolution rate to be slower even though solubility may have been higher.(ABSTRACT TRUNCATED AT 250 WORDS)
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Bogardus JBdoi
10.1002/jps.2600730711subject
Has Abstractpub_date
1984-07-01 00:00:00pages
906-10issue
7eissn
0022-3549issn
1520-6017pii
S0022-3549(15)46207-0journal_volume
73pub_type
杂志文章abstract::A major impediment of many QSAR-type analyses is that the data show a maximum or minimum and can no longer be adequately described by linear functions that provide unrivaled simplicity and usually give good description over more restricted ranges. Here, a general linearized biexponential (LinBiExp) model is proposed t...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.20438
更新日期:2005-11-01 00:00:00
abstract::Treatment of systemic diseases by means of the inhalation route is hampered by uncertainties of the drug dose applied by inhalation. In this study, the hypothesis was tested that by standardization of the breathing maneuver used for inhalation, the interindividual variability of the dose deposited intrathoracically ca...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/(SICI)1520-6017(200006)89:6<724::AID-JPS3>
更新日期:2000-06-01 00:00:00
abstract::Synthetic peptides corresponding to the variable tandem repeat domain of the cancer-associated antigen MUC1 mucin are candidates for cancer vaccines. In our investigation mice were immunized via subcutaneous injection with poly(d,l-lactic-co-glycolic acid) (PLGA) microspheres containing a MUC1 mucin peptide. It was hy...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1021/js980070s
更新日期:1998-11-01 00:00:00
abstract::N-linked glycosylation is an important post translational modification that occurs on Asparagine 297 residue or a homologous position on the Fc portion of monoclonal antibodies (mAbs). mAb Fc glycans play important roles in antibody structure, stability, and function including effector function and pharmacokinetics. T...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2020.09.056
更新日期:2021-02-01 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
pub_type: 杂志文章
doi:10.1002/jps.2600730724
更新日期:1984-07-01 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
pub_type: 杂志文章
doi:10.1002/jps.10088
更新日期:2002-04-01 00:00:00
abstract::Nonviral, plasmid-based therapeutics are a new class of pharmaceutical agents that offer the potential to cure many diseases that are currently considered untreatable. While nonviral vectors have shown promise in clinical trials, their physical instability in liquid formulations represents a major barrier to the devel...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章,评审
doi:10.1002/(SICI)1520-6017(200003)89:3<289::AID-JPS1>
更新日期:2000-03-01 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
pub_type: 杂志文章
doi:10.1002/jps.2600780308
更新日期:1989-03-01 00:00:00
abstract::The synthesis, hydrolysis rate, and bioavailability of 1-(p-acetaminophenoxy)-1-ethoxyethane, an acetaminophen prodrug, are described. The prodrug is less soluble than acetaminophen and stable at neutral pH. However, in an acidic environment, the compound cleaves rapidly, generating acetaminophen. When both the prodru...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600670426
更新日期:1978-04-01 00:00:00
abstract::To preserve the positive effect of collagen on tissue regeneration and to locally deliver low molecular weight compounds for an extended time period, a composite for parenteral application was devised based on a collagen sponge with gentamicin-loaded PLGA microparticles incorporated. Antibiotic liberation from the par...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.10460
更新日期:2003-11-01 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
pub_type: 杂志文章
doi:10.1016/j.xphs.2020.10.025
更新日期:2020-10-15 00:00:00
abstract::The crystal and molecular structures of 6-methylmercaptopurine trihydrate and of azathioprine dihydrate were determined by the use of three-dimensional, X-ray, diffractometer data and were refined by least squares. Both molecules crystallize in the N(9)-H tautomer form, in contrast to the N(7)-H tautomer form found in...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600640206
更新日期:1975-02-01 00:00:00
abstract::The objectives of this study were (i) to characterize the plasmid DNA encoding the chloramphenicol acetyltransferase reporter gene (pCAT) complexed with cationic liposomes (Lipofectin and LipofectACE) in terms of particle size and zeta potential, (ii) to compare pharmacokinetic characteristics, and (iii) to study the ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600841102
更新日期:1995-11-01 00:00:00
abstract::Because the ionized species is more polar than its un-ionized counterpart, it is often assumed that the ionized species of the drug does not make a meaningful contribution to solubilization by either cosolvents or surfactants. This report extends previous studies on solubilization of the ionic species by a combination...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1021/js980433o
更新日期:1999-05-01 00:00:00
abstract::We have shown that adsorbability of local anesthetics onto activated carbon, expressed by the partition coefficients at infinite dilution, correlated well with the pharmacological activity. However, there is no parameter that can singly express the tendency to be adsorbed. Adsorbability is a loosely defined term and i...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600790418
更新日期:1990-04-01 00:00:00
abstract::Papers and patents that deal with polymorphism (crystal systems for which a substance can exist in structures characterized by different unit cells, but where each of the forms has exactly the same elemental composition) and solvatomorphism (systems where the crystal structures of the substance are defined by differen...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章,评审
doi:10.1002/jps.21518
更新日期:2009-05-01 00:00:00
abstract::The phase diagram for the binary system nafcillin sodium-water, was determined using differential scanning calorimetry (DSC) and polarized light microscopy. In the temperature range of -20-30 degrees, three crystalline forms and an amphiphilic liquid crystalline phase were detected. The stable crystalline form of nafc...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600710125
更新日期:1982-01-01 00:00:00
abstract::Incorporation of starch USP or a modified cornstarch within the granules of several drug formulations was investigated. In general, the formulation containing the modified starch exhibited improved processing characteristics as well as improved tablet properties. A comparison of a granulated and a direct compression f...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600640231
更新日期:1975-02-01 00:00:00
abstract::The stability of therapeutic proteins formulated in prefilled syringes (PFS) may be negatively impacted by the exposure of protein molecules to silicone oil-water interfaces and air-water interfaces. In addition, agitation, such as that experienced during transportation, may increase the detrimental effects (i.e., pro...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.23973
更新日期:2014-06-01 00:00:00
abstract::Alkyl esters of ketorolac were synthesized as potential prodrugs for transdermal delivery and evaluated to determine the relationship between their skin permeation characteristics and their physicochemical properties. Solubility of the prodrugs in various vehicles was determined at room temperature while lipophilicity...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.10353
更新日期:2003-05-01 00:00:00
abstract::A sucrose-lactose-starch granulation was used to study particulate motion and attrition in a fluid bed dryer. There is some classification of material in the dryer as drying proceeds; fine particles are dried faster and become less dense, and the less dry but denser large particles show some (although not great) accum...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600641127
更新日期:1975-11-01 00:00:00
abstract::Cationic antimicrobial peptides are good candidates for new diagnostics and antimicrobial agents. They can rapidly kill a broad range of microbes and have additional activities that have impact on the quality and effectiveness of innate responses and inflammation. Furthermore, the challenge of bacterial resistance to ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章,评审
doi:10.1002/jps.21034
更新日期:2008-05-01 00:00:00
abstract::Intestinal transport of the type III phosphodiesterase inhibitor cilostazol was characterized to evaluate the influence of secretory transporter. Intestinal absorption of cilostazol measured by the in situ closed loop method, showed regional differences, with high permeability in the upper part of the small intestine....
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.10490
更新日期:2003-11-01 00:00:00
abstract::Diazepam (1), a hypnotic and anxiolytic drug in worldwide use, formed an intermediate product in a mixture of ethanol and sodium hydroxide ([NaOH] > or = 1 M). The intermediate product slowly decomposed to form 2-(methylamino)-5-chlorobenzophenone imine (2) and 2-(methylamino)-5-chlorobenzophenone (3). The amount of 2...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1021/js9504245
更新日期:1996-07-01 00:00:00
abstract::The application of low-frequency ultrasound enhances drug transport through the skin, a phenomenon referred to as low-frequency sonophoresis. This enhancement is mediated through cavitation, the formation and collapse of gaseous bubbles. We hypothesized that the efficacy of low-frequency sonophoresis can be significan...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.10080
更新日期:2002-03-01 00:00:00
abstract::Sustained release of ferrous sulfate (FeSO4) from gum arabica pellets has been achieved for 7 h. Release is further sustained for 12 to 600 h by coating the pellets with polyvinyl acetate and ethylene vinyl acetate, respectively. An increase in the amount of gum arabica in the pellets decreases the rate of release due...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600830507
更新日期:1994-05-01 00:00:00
abstract::Chitosan salts are being investigated as materials for bacterially triggered colonic drug delivery, via the oral route, based on the assumption that they will be degraded by the enzymes produced by the human colonic bacteria. The actual susceptibility of chitosan to these enzymes is, however, unclear. The digestion of...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.21271
更新日期:2008-09-01 00:00:00
abstract::Sucrose fatty acid esters are increasingly used as excipients in pharmaceutical products, but few data are available on their toxicity profile, mode of action, and efficacy on intestinal epithelial models. Three water-soluble sucrose esters, palmitate (P-1695), myristate (M-1695), laurate (D-1216), and two reference a...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.24085
更新日期:2014-10-01 00:00:00
abstract::Application of ultrasound enhances transdermal transport of drugs (sonophoresis). The enhancement may result from enhanced diffusion due to ultrasound-induced skin alteration and/or from forced convection. To understand the relative roles played by these two mechanisms in low-frequency sonophoresis (LFS, 20 kHz), a th...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/1520-6017(200105)90:5<545::aid-jps1012>3.0
更新日期:2001-05-01 00:00:00
abstract::The vaporization, fusion, and sublimation enthalpies of (R,S)- and (R)-flurbiprofen at T = 298.15 K are reported and compared with literature values when available. Correlation gas chromatography experiments were first performed to identify appropriate standards that could be used for materials containing a single flu...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.23094
更新日期:2012-06-01 00:00:00