Microstructure of calcium stearate matrix pellets: a function of the drying process.


: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 and spheronization. Subsequent drying was performed by either desiccation, fluid-bed drying, or lyophilization, and the final pellets were compared with respect to their microstructure. To minimize the effect of solute ibuprofen molecules on the shrinking behavior of the CaSt, low ibuprofen loadings were used, as ibuprofen is soluble in the granulation liquid. Pellet porosity and specific surface area increased during desiccation, fluid-bed drying, and lyophilization. The inlet-air temperature during fluid-bed drying affected the specific surface area, which increased at lower inlet-air temperatures rather than the pellet porosity. The in vitro dissolution profiles were found to be a nonlinear function of the specific surface area. Overall, the microstructure, including porosity, pore size, and specific surface area, of CaSt pellets was a strong function of the drying conditions.


J Pharm Sci


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




Has Abstract


2013-11-01 00:00:00














  • Synthesis and biological investigations of some 5H-1,3,4-oxadiazolo[3,2-a]pyrimidin-5-ones.

    abstract::The synthesis of some substituted 7-hydroxy-5H-1,3,4-oxadiazolo [3,2-a]pyrimidin-5-ones, a class of bicyclics with unexplored pharmacotoxicological properties, is described. Reacting the 2-phenyl derivative with bis(2,4,5-trichlorophenyl)benzylmalonate afforded a linear pyrano-oxadiazolopyrimidinedione. The assigned s...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Soliman FS,Shafik RM,Darwish M

    更新日期:1982-02-01 00:00:00

  • Development of a Novel Lung Slice Methodology for Profiling of Inhaled Compounds.

    abstract::The challenge of defining the concentration of unbound drug at the lung target site after inhalation limits the possibility to optimize target exposure by compound design. In this study, a novel rat lung slice methodology has been developed and applied to study drug uptake in lung tissue, and the mechanisms by which t...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Bäckström E,Lundqvist A,Boger E,Svanberg P,Ewing P,Hammarlund-Udenaes M,Fridén M

    更新日期:2016-02-01 00:00:00

  • Micellar aggregation of poloxamer 213 and its interaction with cholesterol derivatives.

    abstract::The micellar properties of Poloxamer 213 (1), a Pluronic copolymer shown to affect lipid absorption and serum cholesterol level in experimental animals, are investigated by surface tension measurements, photon correlation spectroscopy (PCS), Reichardt's dye solubilization technique, differential scanning calorimetry (...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Cheng HY,Holl WW

    更新日期:1990-10-01 00:00:00

  • Identification of degradation products in a phenylbutazone tablet formulation.

    abstract::Two previously reported but unidentified phenylburazone degradation products were isolated from a tablet that was stored at 60 degrees for 203 days. The compounds, alpha-(N-phenylcarbamoyl)-N-caproylhydrazobenzene and alpha-hydroxy-alpha-(N-phenylcarbamoyl)-N-caproylhydrazobenzene, were isolated by chromatography, ide...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Matsui F,Robertson DL,Poirier MA,Lovering EG

    更新日期:1980-04-01 00:00:00

  • Transdermal delivery of nonsteroidal anti-inflammatory drugs mediated by polyamidoamine (PAMAM) dendrimers.

    abstract::Nonsteroidal anti-inflammatory drugs (NSAIDs) are among the most frequently used drugs in the world, primarily for symptoms associated with osteoarthritis and other chronic musculoskeletal conditions. However, adverse effects caused by oral administration, such as local or systemic disturbance in the gastrointestinal ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Cheng Y,Man N,Xu T,Fu R,Wang X,Wang X,Wen L

    更新日期:2007-03-01 00:00:00

  • Determination of diphenoxylate hydrochloride and atropine sulfate in solutions and tablets.

    abstract::Methods for the determination of diphenoxylate hydrochloride and atropine sulfate combinations in solutions and powdered tablet composites are presented. A semiautomated assay for diphenoxylate hydrochloride in individual tablets (content uniformity) also is presented. The USP XIX assays for these products are cumbers...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ballbach RL,Brown DJ,Walters SM

    更新日期:1977-11-01 00:00:00

  • Theoretical description of transdermal transport of hydrophilic permeants: application to low-frequency sonophoresis.

    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


    authors: Tang H,Mitragotri S,Blankschtein D,Langer R

    更新日期:2001-05-01 00:00:00

  • Determination of a cephalosporin antibiotic, ceftibuten, in human plasma with column-switching high-performance liquid chromatography with ultraviolet detection.

    abstract::A column-switching high-performance liquid chromatographic assay combined with a heart-cutting technique and UV detection (LC/LC/UV) was developed to determine ceftibuten, a new oral cephalosporin, in human plasma. Plasma samples were directly injected into the first chromatographic column for sample cleanup and extra...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Pan HT,Kumari P,Lim J,Lin CC

    更新日期:1992-07-01 00:00:00

  • Container Surfaces Control Initiation of Cavitation and Resulting Particle Formation in Protein Formulations After Application of Mechanical Shock.

    abstract::Mechanical shock may cause cavitation in vials containing liquid formulations of therapeutic proteins and generate protein aggregates and other particulates. To test whether common formulation components such as protein molecules, air bubbles, or polysorbate 20 (PS20) micelles might nucleate cavitation, a high-speed v...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Wu H,Chisholm CF,Puryear M,Movafaghi S,Smith SD,Pokhilchuk Y,Lengsfeld CS,Randolph TW

    更新日期:2020-03-01 00:00:00

  • Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Proguanil Hydrochloride.

    abstract::Literature data relevant to the decision to waive in vivo bioequivalence testing for the approval of generic immediate release solid oral dosage forms of proguanil hydrochloride are reviewed. To elucidate the Biopharmaceutics Classification System (BCS) classification, experimental solubility and dissolution studies w...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审


    authors: Plöger GF,Abrahamsson B,Cristofoletti R,Groot DW,Langguth P,Mehta MU,Parr A,Polli JE,Shah VP,Tajiri T,Dressman JB

    更新日期:2018-07-01 00:00:00

  • Estimating the relative stability of polymorphs and hydrates from heats of solution and solubility data.

    abstract::The transition temperature, T(t), of polymorphs is estimated from both their heats of solution and solubilities (or intrinsic dissolution rates) determined at any one temperature (e.g., ambient). At a given temperature, T, the enthalpy difference, DeltaH, between polymorphs, I and II, is equal to the difference betwee...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Gu CH,Grant DJ

    更新日期:2001-09-01 00:00:00

  • Increased tumor cisplatin levels in heated tumors in mice after administration of thermosensitive, large unilamellar vesicles encapsulating cisplatin.

    abstract::Hyperthermia (HT)-dependent cisplatin (CDDP) release and tumor CDDP level increase after the administration of thermosensitive, large unilamellar vesicles (LUVs: LUV-1 and LUV-2) and a thermosensitive, small unilamellar vesicle (SUV: SUV-1) were examined in comparison with those following administration of a non-therm...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Iga K,Hamaguchi N,Igari Y,Ogawa Y,Toguchi H,Shimamoto T

    更新日期:1991-06-01 00:00:00

  • Gentamicin-loaded hydraulic calcium phosphate bone cement as antibiotic delivery system.

    abstract::A hydraulic calcium phosphate cement made of beta-tricalcium phosphate [beta-Ca3(PO4)2], monocalcium phosphate monohydrate [Ca(H2PO4)2-H2O], and water was used as a delivery system for the antibiotic gentamicin sulfate (GS). GS, added as powder or as aqueous solution, was very beneficial to the physicochemical propert...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Bohner M,Lemaître J,Van Landuyt P,Zambelli PY,Merkle HP,Gander B

    更新日期:1997-05-01 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


    authors: Horiuchi Y,Hirayama F,Uekama K

    更新日期:1990-02-01 00:00:00

  • Hydrazine levels in formulations of hydralazine, isoniazid, and phenelzine over a 2-year period.

    abstract::Hydrazine levels in formulations of hydralazine, isoniazid, and phenelzine have been measured over a 2-year period under ambient conditions and under temperature and humidity stress. Hydralazine tablets are stable under ambient conditions, but the hydrazine level in an injectable formulation increased from 4.5 to 10 m...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Lovering EG,Matsui F,Curran NM,Robertson DL,Sears RW

    更新日期:1983-08-01 00:00:00

  • Antitumor agents. XXXIV: Mechanism of action of bruceoside A and brusatol on nucleic acid metabolism of P-388 lymphocytic leukemia cells.

    abstract::The quassinoids bruceantin, brucein D, brucein E, bruceoside A, and brusatol significantly inhibited P-388 lymphocytic leukemic cell RNA and protein synthesis in tissue culture. However, DNA synthesis inhibition seemed to correlate more directly with the anti-neoplastic activity of these compounds in the in vivo P-338...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Hall IH,Lee KH,Eigebaly SA,Imakura Y,Sumida Y,Wu RY

    更新日期:1979-07-01 00:00:00

  • Synthesis of N,N'-bis(3-substituted benzylideneaminopropyl)-piperazines and their anti-inflammatory, antiproteolytic, and anticonvulsant properties.

    abstract::Some N,N'-bis(3-substituted benzylideneaminopropyl) piperazines were synthesized and characterized by their sharp melting points and elemental analyses. These substituted piperazines possessed anti-inflammatory activity, and the protection afforded by these compounds against carrageenan-induced edema ranged from 23 to...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Chaturvedi AK,Sastry BV,Chaudhari A,Parmar SS

    更新日期:1976-03-01 00:00:00

  • Plasma levels following single and repeated doses of erythromycin estolate and erythromycin stearate.

    abstract::The pharmacokinetics of erythromycin and erythromycin 2'-propanoate were studied in healthy male volunteers following single and repeated doses of erythromycin stearate tablets, erythromycin estolate capsules, and a suspension. Estolate dosages gave rise to higher plasma levels of total drug than the stearate. However...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Welling PG,Elliott RL,Pitterle ME,Corrick-West HP,Lyons LL

    更新日期:1979-02-01 00:00:00

  • Suppository formulations as a potential treatment for nephropathic cystinosis.

    abstract::Nephropathic cystinosis is a rare autosomal recessive disease characterised by raised lysosomal levels of cystine in the cells of all the organs. It is treated by the 6-h oral administration of the aminothiol, cysteamine, which has an offensive taste and smell. In an attempt to reduce this frequency and improve the tr...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Buchan B,Kay G,Matthews KH,Cairns D

    更新日期:2012-10-01 00:00:00

  • Determination of safrole, dihydrosafrole, and chloromethyldihydrosafrole in piperonyl butoxide by high-performance liquid chromatography.

    abstract::An HPLC method for the simultaneous determination of safrole (S), dihydrosafrole (DHS), and chloromethyldihydrosafrole (CM-DHS) in piperonyl butoxide, with fluorimetric detection and elution gradient, is described. Samples with internal standard (piperonyl isobutyrate) are adsorbed on silica cartridges, then eluted wi...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Schreiber-Deturmeny EM,Pauli AM,Pastor JL

    更新日期:1993-08-01 00:00:00

  • Solvent effects on chemical processes. I: Solubility of aromatic and heterocyclic compounds in binary aqueous-organic solvents.

    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

    pub_type: 杂志文章


    authors: Khossravi D,Connors KA

    更新日期:1992-04-01 00:00:00

  • Modified silicone elastomer vaginal gels for sustained release of antiretroviral HIV microbicides.

    abstract::We previously reported nonaqueous silicone elastomer gels (SEGs) for sustained vaginal administration of the CCR5-targeted entry inhibitor maraviroc (MVC). Here, we describe chemically modified SEGs (h-SEGs) in which the hydrophobic cyclomethicone component was partially replaced with relatively hydrophilic silanol-te...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Forbes CJ,McCoy CF,Murphy DJ,Woolfson AD,Moore JP,Evans A,Shattock RJ,Malcolm RK

    更新日期:2014-05-01 00:00:00

  • Benefits of methylated cyclodextrins in the development of midazolam pharmaceutical formulations.

    abstract::Midazolam (MDZ) is a benzodiazepine commonly administered in preanesthesia of children by oral or by sublingual routes. To mask its bitter taste and enhance its aqueous solubility, we already developed a 0.2% (w/v) MDZ oral solution containing γ-cyclodextrin (γ-CD), which proves to be better accepted by children in pe...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Mathiron D,Marçon F,Dubaele JM,Cailleu D,Pilard S,Djedaïni-Pilard F

    更新日期:2013-07-01 00:00:00

  • A procedure to optimize scale-up for the primary drying phase of lyophilization.

    abstract::This article describes a procedure to facilitate scale-up for the primary drying phase of lyophilization using a combination of empirical testing and numerical modeling. Freeze dry microscopy is used to determine the temperature at which lyophile collapse occurs. A laboratory scale freeze-dryer equipped with manometri...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Kramer T,Kremer DM,Pikal MJ,Petre WJ,Shalaev EY,Gatlin LA

    更新日期:2009-01-01 00:00:00

  • Novel methodology for predicting photogenotoxic risk of pharmaceutical substances based on reactive oxygen species (ROS) and DNA-binding assay.

    abstract::Drug-induced phototoxic skin responses involves photoirritation, photoallergy, and photogenotoxicity. In the present study, we attempted to develop effective analytical tools to predict the photogenotoxic potential of pharmaceutical substances on the basis of their photobiological and DNA-binding properties. Photoclea...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Onoue S,Seto Y,Oishi A,Yamada S

    更新日期:2009-10-01 00:00:00

  • On the hydrolytic behavior of tinidazole, metronidazole, and ornidazole.

    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

    pub_type: 杂志文章


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

    更新日期:2003-04-01 00:00:00

  • Quantitative determination of hexamidine isethionate in pharmaceutical preparations by high-performance liquid chromatography.

    abstract::Hexamidine isethionate in various pharmaceutical formulations was analyzed quantitatively by high-performance liquid chromatography. The method is rapid, accurate, and precise. Excellent results were obtained from four commercial bases. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Taylor P,Braddock PD,Ross S

    更新日期:1983-12-01 00:00:00

  • Direct nose-brain transport of benzoylecgonine following intranasal administration in rats.

    abstract::In our previous research, cocaine applied intranasally in rats diffused or was transported directly from the nasal cavity to the brain. However, the direct nose-brain cocaine transport only contributes to an initial increase in the relative cocaine brain exposure. In this study, we have determined the nose-brain trans...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Chow HH,Anavy N,Villalobos A

    更新日期:2001-11-01 00:00:00

  • Automated spectrophotometric assay of cefazolin.

    abstract::An automated, stability-indicating, UV spectrophotometric assay for cefazolin is presented. The method employs a reaction with hydroxylamine and derives its stability-indicating power through comparison of reacted and unreacted aliquots of the sample. A double-probe sampling procedure is used. Good agreement with micr...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Holl WW,O'Brien M,Filan J,Mazeika TR,Post A,Pitkin D,Actor P

    更新日期:1975-07-01 00:00:00

  • Enhanced transdermal delivery of sex hormones in swine with a novel topical aerosol.

    abstract::This study investigated the enhanced transdermal delivery of testosterone (Tes) and estradiol (E2) in swine in vivo with novel metered-dose topical aerosols containing the penetration enhancer padimate O (PadO) and predicted the dose deliverable in humans from the calculated drug flux across the skin. Weanling swine w...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Morgan TM,Parr RA,Reed BL,Finnin BC

    更新日期:1998-10-01 00:00:00