Enhanced potency of human calcitonin when fibrillation is avoided.


:The peptide hormone calcitonin (CT) is a potent drug for the therapy of different bone diseases. Salmon CT (sCT) is reported to be more active than human CT (hCT). Human CT, but not sCT, has a strong tendency to aggregate and fibrillate in aqueous solutions. Recent investigations of the fibrillation mechanisms contributed to the development of hCT solutions in which fibrillation is inhibited. Taking into consideration these new findings, we tested the relative activities of hCT handled so as to avoid aggregation/fibrillation, sCT handled in exactly the same way, and hCT handled carefully but without regard to possible fibrillation (denoted R-hCT). The effect of the CTs on bone resorption by isolated osteoclasts was measured. This assay measures the activity of interest (bone resorption) by the cell (the osteoclast) at which therapy is directed. The concentration that inhibits 50% of resorption (EC50) for hCT is 10(-5)-10(-4) pg/mL, compared with 10(-2)-1 pg/mL for R-hCT and 10(-3)-10(-1) pg/mL for sCT. The results show that when aggregation and fibrillation are avoided, hCT at the EC50 is 2-4 orders of magnitude more active than R-hCT. Thus, earlier reports of lower potency of hCT compared with sCT may have been based on inadvertent use of partially aggregated/fibrillated samples of hCT. This finding may have implications for the dose and dosage forms advised for human therapy.


J Pharm Sci


Cudd A,Arvinte T,Das RE,Chinni C,MacIntyre I




Has Abstract


1995-06-01 00:00:00














  • Polyamidoamine dendrimers can improve the pulmonary absorption of insulin and calcitonin in rats.

    abstract::The absorption-enhancing effects of polyamidoamine (PAMAM) dendrimers with various generations (G0-G3) and concentrations [0.1%-1.0% (w/v)] on the pulmonary absorption of peptide and protein drugs were studied in rats. Insulin and calcitonin were chosen as models of peptide and protein drugs, and their pulmonary absor...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Dong Z,Hamid KA,Gao Y,Lin Y,Katsumi H,Sakane T,Yamamoto A

    更新日期:2011-05-01 00:00:00

  • Effect of lipophilicity on the bioavailability of drugs after percutaneous administration by dissolving microneedles.

    abstract::To elucidate drug lipophilicity effects on the bioavailability (BA) of drugs from skin after administration by dissolving microneedles, nine compounds with different lipophilicity indexes (log p value) were formulated into two-layered dissolving microneedles and administered percutaneously to rat skin: desmopressin (D...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ito Y,Yoshimura M,Tanaka T,Takada K

    更新日期:2012-03-01 00:00:00

  • Preparation and analysis of deuterium-labeled aspirin: application to pharmacokinetic studies.

    abstract::Inhibition of endogenous prostacyclin and thromboxane biosynthesis by aspirin is critically dose-dependent in humans. Gastrointestinal and hepatic hydrolysis may limit systemic availability of aspirin, especially in low doses, perhaps contributing to the biochemical selectivity of aspirin. Existing analytical methods ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Pedersen AK,FitzGerald GA

    更新日期:1985-02-01 00:00:00

  • Determination of norethindrone stability on red delicious apples.

    abstract::A stability-indicating assay procedure for the determination of norethindrone on the surface of Red Delicious apple slices was developed. The apple slice is homogenized in pH 10 borate buffer solution and norethindrone is then partitioned into chloroform using a diffusion chamber that has a membrane that is permeable ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Mayberry DO,Kowblansky M,Lane PA,Wray PE

    更新日期:1990-08-01 00:00:00

  • Sarin transport across excised human skin II: Effect of solvent pretreatment on permeability.

    abstract::The effect of pretreating callus membranes with dimethyl sulfoxide, dimethylacetamide, dimethylformamide, formamide, dioxane, or methyl orthoformate on sarin permeability was studied at three temperatures to determine the activation energy for transport. In addition, the effect of membrane pretreatment on permeability...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Matheson LE,Wurster DE,Ostrenga JA

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  • Enhancement of solubility of drug salts by hydrophilic counterions: properties of organic salts of an antimalarial drug.

    abstract::Judicious choice of the salt form of a drug can greatly affect the aqueous solubility and formulation of the compound. The objective of this work was to demonstrate the effect of various counteranions on the aqueous solubility of the antimalarial agent alpha-(2-piperidyl)-3, 6-bis(trifluoromethyl)-9-phenanthrenemethan...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Agharkar S,Lindenbaum S,Higuchi T

    更新日期:1976-05-01 00:00:00

  • Mechanisms of potassium chloride release from compressed, hydrophilic, polymeric matrices: effect of entrapped air.

    abstract::The release of potassium chloride from hydroxypropyl methylcellulose matrices was investigated for tablets prepared with several different compression forces. It was determined that the release kinetics for these systems deviates significantly from the classical t1/2 dependence. This behavior was attributed to air ent...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Korsmeyer RW,Gurny R,Doelker E,Buri P,Peppas NA

    更新日期:1983-10-01 00:00:00

  • A novel calmodulin antagonist O-(4-ethoxyl-butyl)-berbamine overcomes multidrug resistance in drug-resistant MCF-7/ADR breast carcinoma cells.

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    journal_title:Journal of pharmaceutical sciences

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    authors: Liu R,Zhang Y,Chen Y,Qi J,Ren S,Xushi MY,Yang C,Zhu H,Xiong D

    更新日期:2010-07-01 00:00:00

  • Self-association of cromolyn sodium in aqueous solution characterized by nuclear magnetic resonance spectroscopy.

    abstract::The major objective of this study was to investigate and characterize the solution properties of cromolyn sodium (in D(2)O or D(2)O/H(2)O phosphate buffer at pH 7.5) using nuclear magnetic resonance (NMR) spectroscopy. The self-association of cromolyn molecules was examined primarily via one-dimensional (1)H and (13)C...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ding X,Stringfellow TC,Robinson JR

    更新日期:2004-05-01 00:00:00

  • High Sensitivity Detection of a Solubility Limiting Surface Transformation of Drug Particles by DNP SENS.

    abstract::We investigate the presence of a surface species for the active pharmaceutical ingredient (API) AZD9496 with dynamic nuclear polarization surface enhanced nuclear spectroscopy (DNP SENS). We show that using DNP we can elucidate the presence of an amorphous form of the API at the surface of crystalline particles of the...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Viger-Gravel J,Pinon AC,Björgvinsdóttir S,Skantze U,Svensk Ankarberg A,Von Corswant C,Schantz S,Emsley L

    更新日期:2021-01-05 00:00:00

  • Porous resins as a cavitation enhancer for low-frequency sonophoresis.

    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


    authors: Terahara T,Mitragotri S,Langer R

    更新日期:2002-03-01 00:00:00

  • Evaluation of 6β-Hydroxycortisol and 6β-Hydroxycortisone as Biomarkers for Cytochrome P450 3A Activity: Insight into Their Predictive Value for Estimating Oral Immunosuppressant Metabolism.

    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

    pub_type: 杂志文章


    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

  • Radiolytic degradation scheme for 60Co-irradiated corticosteroids.

    abstract::The cobalt 60 radiolytic degradation products have been identified in the following corticosteroids: cortisone, cortisone acetate, hydrocortisone, hydrocortisone acetate, hydrocortisone sodium succinate, isoflupredone acetate, methylprednisolone, methylprednisolone acetate, prednisolone, prednisolone acetate, and pred...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Kane MP,Tsuji K

    更新日期:1983-01-01 00:00:00

  • Verification and validation of computational models used in biopharmaceutical manufacturing: Potential application of the ASME Verification and Validation 40 standard and FDA proposed AI/ML model life cycle management framework.

    abstract::A wide variety of computational models covering statistical, mechanistic, and machine learning (locked and adaptive) methods are explored for use in biopharmaceutical manufacturing. Limited discussion exists on how to establish the credibility of a computational model for application in biopharmaceutical manufacturing...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Bideault G,Scaccia A,Zahel T,Forero RL,Daluwatte C

    更新日期:2021-01-22 00:00:00

  • Noninvasive identification of materials inside USP vials with Raman spectroscopy and a Raman spectral library.

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    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: McCreery RL,Horn AJ,Spencer J,Jefferson E

    更新日期:1998-01-01 00:00:00

  • Plasma levels of a novel antidysrhythmic agent, meobentine sulfate, in humans as determined by radioimmunoassay.

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    pub_type: 杂志文章


    authors: Warren JT,Coker GG,Welch RM,Fowle AS,Findlay JW

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  • Influence of asymmetric donor-receiver ion concentration upon transscleral iontophoretic transport.

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    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Li SK,Zhang Y,Zhu H,Higuchi WI,White HS

    更新日期:2005-04-01 00:00:00

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    abstract::Clinical lots of recombinant human platelet-activating factor acetylhydrolase (rhPAF-AH) were prepared in a lyophilized formulation. After reconstitution with sterile water for injection to form an aqueous solution (10 mM sodium citrate, 7.5 w/v% sucrose, and 0.1 w/v% Pluronic-F68, pH 6.5), a few visible, slowly growi...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Chi EY,Weickmann J,Carpenter JF,Manning MC,Randolph TW

    更新日期:2005-02-01 00:00:00

  • Structural studies of commercial fat emulsions used in parenteral nutrition.

    abstract::In this paper, we demonstrate that by employing a combination of sedimentation field-flow fractionation (sedFFF) and other characterization techniques, such as photon correlation spectroscopy (PCS) and freeze-fracture electron microscopy (EM), it is possible to show that commercial fat emulsions of similar overall che...

    journal_title:Journal of pharmaceutical sciences

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    authors: Li J,Caldwell KD

    更新日期:1994-11-01 00:00:00

  • Effect of food on the bioavailability of lisinopril, a nonsulfhydryl angiotensin-converting enzyme inhibitor.

    abstract::A randomized, two-way, crossover study was performed on 18 normal volunteers to assess the influence of food on the bioavailability of lisinopril, (1-[N2-[(S)-1-carboxy-3-phenylpropyl]-L-lysyl]-L-proline), a long-acting nonsulfhydryl angiotensin converting enzyme inhibitor. A single, 20-mg oral dose of lisinopril was ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 临床试验,杂志文章,随机对照试验


    authors: Mojaverian P,Rocci ML Jr,Vlasses PH,Hoholick C,Clementi RA,Ferguson RK

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  • Synthesis and antidiabetic activity of some sulfonylurea derivatives of 3,4,5-trisubstituted pyrazoles.

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    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Soliman R,Mokhtar H,Mohamed HF

    更新日期:1983-09-01 00:00:00

  • Factorial designs in pharmaceutical stability studies.

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    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Bolton S

    更新日期:1983-04-01 00:00:00

  • Protein Aggregation in Frozen Trehalose Formulations: Effects of Composition, Cooling Rate, and Storage Temperature.

    abstract::This study was designed to assess the effects of cooling rate, storage temperature, and formulation composition on trehalose phase distribution and protein stability in frozen solutions. The data demonstrate that faster cooling rates (>100°C/min) result in trehalose crystallization and protein aggregation as determine...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Connolly BD,Le L,Patapoff TW,Cromwell MEM,Moore JMR,Lam P

    更新日期:2015-12-01 00:00:00

  • Water vapor absorption into amorphous sucrose-poly(vinyl pyrrolidone) and trehalose-poly(vinyl pyrrolidone) mixtures.

    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

    pub_type: 杂志文章


    authors: Zhang J,Zografi G

    更新日期:2001-09-01 00:00:00

  • In vivo and in vitro evaluation of a microencapsulated narcotic antagonist.

    abstract::Injectable microcapsules containing 75% (w/w) cyclazocine, a narcotic antagonist, were prepared with dl-poly(lactic acid) as the coating material. Capsule fractions falling between 105 and 295 mum released about 90% of their cyclazocine in 8 days of rotating-bottle extraction at 37 degrees in pH 7.4 phosphate buffer. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Mason N,Thies C,Cicero TJ

    更新日期:1976-06-01 00:00:00

  • Characterization of polymorphism of gepirone hydrochloride.

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    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Behme RJ,Brooke D,Farney RF,Kensler TT

    更新日期:1985-10-01 00:00:00

  • Protection of bovine serum albumin from aggregation by Tween 80.

    abstract::In an attempt to explain the mechanism of protein stabilization conferred by detergents, we investigated the effect of Tween 80 on aggregation of bovine serum albumin (BSA) using circular dichroism (CD) and native gel electrophoresis. CD thermal scans showed that BSA denatures at about 54 degrees C in 20 mM Tris, pH 7...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Arakawa T,Kita Y

    更新日期:2000-05-01 00:00:00

  • Effect of low molecular weight chitosans on drug permeation through mouse skin: 1. Transdermal delivery of baicalin.

    abstract::The aim of this work was to evaluate the low molecular weight chitosans (LMWCs) as enhancers of transdermal administration of baicalin, an useful drug for the treatment of atopic dermatitis, viral hepatitis, and HIV infection. Permeation experiments were performed in vitro through mouse skin by using Franz cells. Impr...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Zhou X,Liu D,Liu H,Yang Q,Yao K,Wang X,Wang L,Yang X

    更新日期:2010-07-01 00:00:00

  • Mechanism of Drug Release From Temperature-Sensitive Formulations Composed of Low-Melting-Point Microcrystalline Wax.

    abstract::It was reported that wax matrix (WM) particles composed of low-melting-point microcrystalline wax showed unique release behaviors; the particles released only a small amount of the entrapped drug (non-diffusion-controlled release) at 37°C, whereas it showed comparatively fast drug release in a diffusion-controlled man...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Matsumoto K,Kimura SI,Noguchi S,Itai S,Kondo H,Iwao Y

    更新日期:2019-06-01 00:00:00

  • Antitumor agents LV: Effects of genkwadaphnin and yuanhuacine on nucleic acid synthesis of P-388 lymphocytic leukemia cells.

    abstract::The diterpene esters, genkwadaphnin and yuanhuacine, have been shown to possess significant antileukemic activity in the P-388 screen. The major metabolic effects of the diterpene esters were on DNA and protein synthesis. The effects on DNA synthesis in vitro were evoked at a lower concentration than that required for...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Hall IH,Kasai R,Wu RY,Tagahara K,Lee KH

    更新日期:1982-11-01 00:00:00