Controlled delivery of basal insulin from phase-sensitive polymeric systems after subcutaneous administration: in vitro release, stability, biocompatibility, in vivo absorption, and bioactivity of insulin.


:The purpose of this study was to investigate the phase-sensitive delivery systems (D,L-polylactide in triacetin) for controlled delivery of insulin at basal level. The effect of varying concentration of zinc, polymer, and insulin on the in vitro release of insulin was evaluated. Stability of released insulin was investigated by differential scanning calorimetry, circular dichroism, and matrix-assisted laser desorption/ionization time of flight mass spectrometry. In Vivo insulin absorption and bioactivity were studied in diabetic rats. In vitro and In Vivo biocompatibility of delivery systems were evaluated by 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide assay and skin histology, respectively. Extended release profiles of insulin for 2, 4, and 8 weeks from delivery systems containing 20%, 30%, and 40% (w/v) polymer concentration was observed. A ratio of 1:5 insulin hexamer to zinc was shown to be optimum. Physical and chemical stability of released insulin was greatly conserved. In Vivo studies demonstrated controlled release of insulin with reduction in blood glucose for approximately 1 month. In vitro and In Vivo studies demonstrated that the delivery system was biocompatible and controlled the delivery of insulin for longer durations after single subcutaneous injection.


J Pharm Sci


Al-Tahami K,Oak M,Singh J




Has Abstract


2011-06-01 00:00:00














  • Pharmacokinetics of ketoconazole administered intravenously to dogs and orally as tablet and solution to humans and dogs.

    abstract::The single-dose pharmacokinetics and bioavailability of three ketoconazole formulations were evaluated using HPLC in five healthy human volunteers and six male mongrel dogs. The human volunteers received 400 mg po of ketoconazole as tablet (Ktab) and solution (Ksol) formulations. The dogs received 400 mg po of Ktab an...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Baxter JG,Brass C,Schentag JJ,Slaughter RL

    更新日期:1986-05-01 00:00:00

  • Stability of batanopride hydrochloride in aqueous solutions.

    abstract::The degradation of batanopride hydrochloride, an investigational antiemetic drug, was studied in aqueous buffer solutions (pH 2-10; ionic strength, 0.5; 56 degrees C) in an attempt to improve drug stability for parenteral administration. Degradation occurs by two different mechanisms depending on the pH of the solutio...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Nassar MN,House CA,Agharkar SN

    更新日期:1992-11-01 00:00:00

  • Tocainide conjugation in humans: novel biotransformation pathway for a primary amine.

    abstract::The metabolism of tocainide, an experimental antiarrhythmic drug, was studied in humans. Urinary excretion of unchanged drug was 28-55% in 24 hr after oral dosing. Urine hydrolysis with hydrochloric acid or beta-glucuronidase increased tocainide recovery to 55-79%. Saccharo-1,4-lactone inhibited the beta-glucuronidase...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Elvin AT,Keenaghan JB,Byrnes EW,Tenthorey PA,McMaster PD,Takman BH,Lalka D,Manion CV,Baer DT,Wolshin EM,Meyer MB,Ronfeld RA

    更新日期:1980-01-01 00:00:00

  • Preparation, identification, and quantitative NMR determination of silyl derivatives of 6-aminopenicillanic acid, 7-amino-3-methyl-delta3-cephem-4-carboxylic acid, and 7-amino-3-acetoxymethyl-delta3-cephem-4-carboxylic acid.

    abstract::A rapid and accurate method for the quantitative determination of the extent and ratio of amino and carboxyl group trimethylsilylation of 6-aminopenicillanic acid, 7-amino-3-methyl-delta3-cephem-4-carboxylic acid, and 7-amino-3-acetoxymethyl-delta3-cephem-4-carboxylic acid is presented. The method utilizes NMR spectro...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Bortesi F,Cavalli S,Mangia A

    更新日期:1977-12-01 00:00:00

  • Using Image Attributes to Assure Accurate Particle Size and Count Using Nanoparticle Tracking Analysis.

    abstract::Nanoparticle tracking analysis (NTA) obtains particle size by analysis of particle diffusion through a time series of micrographs and particle count by a count of imaged particles. The number of observed particles imaged is controlled by the scattering cross-section of the particles and by camera settings such as sens...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Defante AP,Vreeland WN,Benkstein KD,Ripple DC

    更新日期:2018-05-01 00:00:00

  • Development of polyethylene glycol-conjugated alendronate, a novel nitrogen-containing bisphosphonate derivative: evaluation of absorption, safety, and effects after intrapulmonary administration in rats.

    abstract::Bisphosphonates are widely used for the treatment of bone diseases, including hypercalcemia and osteoporosis. However, the bioavailability (BA) of orally administered bisphosphonates is low, at approximately 0.9%-1.8%. In addition, the oral administration of bisphosphonates is associated with mucosal damage, including...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Katsumi H,Takashima M,Sano J,Nishiyama K,Kitamura N,Sakane T,Hibi T,Yamamoto A

    更新日期:2011-09-01 00:00:00

  • Formulation and evaluation of quercetin polycaprolactone microspheres for the treatment of rheumatoid arthritis.

    abstract::Quercetin had been shown to be effective in the management of arthritis. However, bioavailability of quercetin is a concern for such treatment. This work aims at the development of intra-articular drug delivery system by controlled release of quercetin (loaded in microspheres) for the management of rheumatoid arthriti...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Natarajan V,Krithica N,Madhan B,Sehgal PK

    更新日期:2011-01-01 00:00:00

  • In vitro evaluation of the permeation-enhancing effect of thiolated polycarbophil.

    abstract::The objective of this study was to investigate the permeation-enhancing effect of thiolated polycarbophil (PCP) on peptide drugs. Mediated by a carbodiimide, increasing amounts of cysteine (Cys) were covalently bound to sodium neutralized PCP (NaPCP). The extent of covalently attached Cys was determined by quantifying...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Clausen AE,Bernkop-Schnürch A

    更新日期:2000-10-01 00:00:00

  • Potential antineoplastics I: substituted 3,5-dioxo-and 3-thioxo-5-oxo-2,3,4,5-tetrahydro-1,2,4-triazines.

    abstract::The synthesis of some 6-substituted 3,5-dioxo- and 3-thioxo-5-oxo-2,3,4,5-tetrahydro-1,2,4-triazines for possible antineoplastic activity is reported. The assigned structures were substantiated by IR, NMR, and mass spectral studies of representative members of the series. Four compounds were tested against P-388 lymph...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ibrahim el-SA,Shams el-Dine SA,Soliman FS,Labouta IM

    更新日期:1979-02-01 00:00:00

  • Linear drug release from laminated hydroxypropyl cellulose-polyvinyl acetate films.

    abstract::Release of drug from a single-layer film containing dispersed drug follows a diffusion-controlled matrix model, where the quantity released per unit area is proportional to the square root of time. The kinetics may be made linear with time (zero order) by laminating a second film without drug to the releasing side of ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Borodkin S,Tucker FE

    更新日期:1975-08-01 00:00:00

  • Derivative and graphical procedures for correction of irrelevant UV spectrophotometric absorption in changeable matrixes.

    abstract::The application of direct zero-order UV spectrophotometric and graphical or derivative background correction methods to selected pharmaceutical preparations shows their relative advantages in different situations. The assay of the active components in a changeable matrix is a problem with formulations having a limited...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Traveset J,Such V,Gonzalo R,Gelpi E

    更新日期:1980-06-01 00:00:00

  • The formation of oxytocin dimers is suppressed by the zinc-aspartate-oxytocin complex.

    abstract::The aim of this study was to investigate the effect of divalent metal ions (Ca, Mg(2+) , and Zn(2+) ) on the stability of oxytocin in aspartate buffer (pH 4.5) and to determine their interaction with the peptide in aqueous solution. Reversed-phase high-performance liquid chromatography and high-performance size-exclus...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Avanti C,Hinrichs WLJ,Casini A,Eissens AC,Van Dam A,Kedrov A,Driessen AJM,Frijlink HW,Permentier HP

    更新日期:2013-06-01 00:00:00

  • Determination of coumarin and umbelliferone mixtures in whole blood by spectrophotofluorometry.

    abstract::A spectrophotofluorometric method is described for the quantitative analysis of coumarin, umbelliferone, and mixtures thereof in whole blood. The two drugs were selectively isolated from blood by solvent extraction. Analysis of the isolated coumarin was based on the measurement of the fluorophore at activation and emi...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Tan HS,Ritschel WA,Sanders PR

    更新日期:1976-01-01 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


    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

  • Pharmacokinetics and tissue distribution after intravenous administration of a single dose of amphotericin B cochleates, a new lipid-based delivery system.

    abstract::Model independent pharmacokinetic analysis of intravenous (iv) amphotericin B cochleates (CAMB), a new lipid-based drug delivery system, in mice (0.625 mg/kg) shows a two-phase disposition profile in blood [area under the curve of concentration versus time from time zero to infinity (AUC(0-infinity)) = 1.01 microg. h/...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Segarra I,Movshin DA,Zarif L

    更新日期:2002-08-01 00:00:00

  • Application of 13C CPMAS NMR for qualitative and quantitative characterization of carvedilol and its commercial formulations.

    abstract::(13) C cross-polarization magic-angle spinning nuclear magnetic resonance (CPMAS NMR) spectroscopy was applied to the identification and characterization of carvedilol (1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)-ethylamino]-propan-2-ol) in pharmaceutical preparations. Solid-state spectra (standard linewidth and l...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Zielińska-Pisklak M,Pisklak DM,Wawer I

    更新日期:2012-05-01 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

  • High-throughput determination of the free fraction of drugs strongly bound to plasma proteins.

    abstract::Quantification of protein binding of new chemical entities is an important early screening step during drug discovery and is of fundamental interest for the estimation of safety margins during drug development. In this publication, we describe the development of a new high-throughput assay for the determination of the...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Schuhmacher J,Kohlsdorfer C,Bühner K,Brandenburger T,Kruk R

    更新日期:2004-04-01 00:00:00

  • Pharmacokinetic model for simultaneous determination of drug levels in organs and tissues.

    abstract::An extension of the Bischoff-Dedrick pharmacokinetic model is presented. This model is derived from basic considerations of drug distrubition with physiological and anatomical meaning. The Bischoff-Dedrick model can simultaneously predict drug distribution with time in blood, organs, and tissues of pharmacological int...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Chen CN,Andrade JD

    更新日期:1976-05-01 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


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

    更新日期:1973-08-01 00:00:00

  • Interactions of cephalosporins and penicillins with nonpolar octadecylsilyl stationary phase.

    abstract::The capacity factors of several penicillins and cephalosporins, as well as those of 7-aminocephalosporanic acid, 6-aminopenicillanic acid, and 7-aminodeacetoxycephalosporanic acid, were determined at pH 2.5-7.5 with different methanol concentrations in the mobile phase. The influence of ionic strength on activity fact...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Salto F,Prieto JG,Alemany MT

    更新日期:1980-05-01 00:00:00

  • Quantitative determination of the stabilizers octanoic acid and N-acetyl-DL-tryptophan in human albumin products.

    abstract::Methods were developed for the determination of octanoic acid and N-acetyl-DL-tryptophan, which are used as stabilizers in the human blood-derived therapeutic products normal serum albumin and plasma protein fraction. The method for octanoic acid uses GC; quantitation is achieved using heptanoic acid as the internal s...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Yu MW,Finlayson JS

    更新日期:1984-01-01 00:00:00

  • Moisture sorption kinetics for water-soluble substances. I: Theoretical considerations of heat transport control.

    abstract::A model based on heat transport control was developed to describe the uptake of water on a deliquescent solid in an atmosphere of pure water vapor. The model assumes the presence of a saturated liquid film on the surface of the solid. The decrease in the vapor pressure of water over the surface, brought about by the c...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Van Campen L,Amidon GL,Zografi G

    更新日期:1983-12-01 00:00:00

  • The granule porosity controls the loss of compactibility for both dry- and wet-processed cellulose granules but at different rate.

    abstract::The aim of this study was to investigate the role of porosity on the compression behavior and tablet tensile strength for granules produced by a dry granulation procedure. Microcrystalline cellulose was used as a typical pharmaceutical excipient and a comparison was made with the effect of granule porosity on the comp...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Nordström J,Alderborn G

    更新日期:2015-06-01 00:00:00

  • Experimental evaluation of three single-particle dissolution models.

    abstract::The dissolution of the 60-85-mesh fraction os recording, flow-through dissolution apparatus equipped with a dissolution cell; it was particularly suitable for kinetic analysis of multiparticulate systems. By using a time-scaling approach, experimental data are compared with theoretical calculations to evaluate, quanti...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Pedersen PV,Brown KF

    更新日期:1976-10-01 00:00:00

  • Understanding the Increased Aggregation Propensity of a Light-Exposed IgG1 Monoclonal Antibody Using Hydrogen Exchange Mass Spectrometry, Biophysical Characterization, and Structural Analysis.

    abstract::This work compares the conformational stability, backbone flexibility, and aggregation propensity of monomer and dimer fractions of an IgG1 monoclonal antibody (mAb) generated on UVA light exposure for up to 72 h collected by preparative size-exclusion chromatography, compared with unstressed control. UVA light exposu...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Bommana R,Chai Q,Schöneich C,Weiss WF 4th,Majumdar R

    更新日期:2018-06-01 00:00:00

  • Distribution and elimination of poly(methyl methacrylate) nanoparticles after subcutaneous administration to rats.

    abstract::Poly(methyl [1-14C]methacrylate) nanoparticles were injected subcutaneously into rats. Almost all of the radioactivity stayed at the injection site. After an initial urinary and fecal excretion of approximately 1% of the administered dose per day, the rate of elimination dropped to a low level (approximately 0.005%/da...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Kreuter J,Nefzger M,Liehl E,Czok R,Voges R

    更新日期:1983-10-01 00:00:00

  • Hot Melt Extrusion as Solvent-Free Technique for a Continuous Manufacturing of Drug-Loaded Mesoporous Silica.

    abstract::The aim of this study is to explore hot melt extrusion (HME) as a solvent-free drug loading technique for preparation of stable amorphous solid dispersions using mesoporous silica (PSi). Ibuprofen and carvedilol were used as poorly soluble active pharmaceutical ingredients (APIs). Due to the high friction of an API:PS...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Genina N,Hadi B,Löbmann K

    更新日期:2018-01-01 00:00:00

  • Adsorption of local anesthetics on activated carbon: Freundlich adsorption isotherms.

    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


    authors: Abe I,Kamaya H,Ueda I

    更新日期:1990-04-01 00:00:00

  • VLDL-resembling phospholipid-submicron emulsion for cholesterol-based drug targeting.

    abstract::The objective of the current study was to develop and evaluate VLDL-resembling phospholipid-submicron emulsion (PSME) as a carrier system for new cholesterol-based compounds for targeted delivery to cancer cells. BCH, a boronated cholesterol compound, was originally developed in our laboratory to mimic the cholesterol...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Shawer M,Greenspan P,ØIe S,Lu DR

    更新日期:2002-06-01 00:00:00