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  1. Article ; Online: Aggregation Behavior of Structurally Similar Therapeutic Peptides Investigated by

    Hjalte, Johanna / Hossain, Shakhawath / Hugerth, Andreas / Sjögren, Helen / Wahlgren, Marie / Larsson, Per / Lundberg, Dan

    Molecular pharmaceutics

    2022  Volume 19, Issue 3, Page(s) 904–917

    Abstract: Understanding of peptide aggregation propensity is an important aspect in pharmaceutical development of peptide drugs. In this work, methodologies based on all-atom molecular dynamics (AA-MD) simulations ... ...

    Abstract Understanding of peptide aggregation propensity is an important aspect in pharmaceutical development of peptide drugs. In this work, methodologies based on all-atom molecular dynamics (AA-MD) simulations and
    MeSH term(s) Magnetic Resonance Spectroscopy ; Molecular Dynamics Simulation ; Proton Magnetic Resonance Spectroscopy
    Language English
    Publishing date 2022-02-01
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2138405-8
    ISSN 1543-8392 ; 1543-8384
    ISSN (online) 1543-8392
    ISSN 1543-8384
    DOI 10.1021/acs.molpharmaceut.1c00883
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Intestinal Absorption of FITC-Dextrans and Macromolecular Model Drugs in the Rat Intestinal Instillation Model.

    Berg, Staffan / Suljovic, Denny / Kärrberg, Lillevi / Englund, Maria / Bönisch, Heiko / Karlberg, Ida / Van Zuydam, Natalie / Abrahamsson, Bertil / Hugerth, Andreas Martin / Davies, Nigel / Bergström, Christel A S

    Molecular pharmaceutics

    2022  Volume 19, Issue 7, Page(s) 2564–2572

    Abstract: In this work, we studied the intestinal absorption of a peptide with a molecular weight of 4353 Da (MEDI7219) and a protein having a molecular weight of 11 740 Da (PEP12210) in the rat intestinal instillation model and compared their absorption to ... ...

    Abstract In this work, we studied the intestinal absorption of a peptide with a molecular weight of 4353 Da (MEDI7219) and a protein having a molecular weight of 11 740 Da (PEP12210) in the rat intestinal instillation model and compared their absorption to fluorescein isothiocyanate (FITC)-labeled dextrans of similar molecular weights (4 and 10 kDa). To increase the absorption of the compounds, the permeation enhancer sodium caprate (C10) was included in the liquid formulations at concentrations of 50 and 300 mM. All studied compounds displayed an increased absorption rate and extent when delivered together with 50 mM C10 as compared to control formulations not containing C10. The time period during which the macromolecules maintained an increased permeability through the intestinal epithelium was approximately 20 min for all studied compounds at 50 mM C10. For the formulations containing 300 mM C10, it was noted that the dextrans displayed an increased absorption rate (compared to 50 mM C10), and their absorption continued for at least 60 min. The absorption rate of MEDI7219, on the other hand, was similar at both studied C10 concentrations, but the duration of absorption was extended at the higher enhancer concentration, leading to an increase in the overall extent of absorption. The absorption of PEP12210 was similar in terms of the rate and duration at both studied C10 concentrations. This is likely caused by the instability of this molecule in the intestinal lumen. The degradation decreases the luminal concentrations over time, which in turn limits absorption at time points beyond 20 min. The results from this study show that permeation enhancement effects cannot be extrapolated between different types of macromolecules. Furthermore, to maximize the absorption of a macromolecule delivered together with C10, prolonging the duration of absorption appears to be important. In addition, the macromolecule needs to be stable enough in the intestinal lumen to take advantage of the prolonged absorption time window enabled by the permeation enhancer.
    MeSH term(s) Animals ; Dextrans ; Fluorescein-5-isothiocyanate ; Intestinal Absorption ; Intestinal Mucosa/metabolism ; Permeability ; Rats
    Chemical Substances Dextrans ; Fluorescein-5-isothiocyanate (I223NX31W9)
    Language English
    Publishing date 2022-06-01
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2138405-8
    ISSN 1543-8392 ; 1543-8384
    ISSN (online) 1543-8392
    ISSN 1543-8384
    DOI 10.1021/acs.molpharmaceut.2c00261
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: Impact of Intestinal Concentration and Colloidal Structure on the Permeation-Enhancing Efficiency of Sodium Caprate in the Rat.

    Berg, Staffan / Kärrberg, Lillevi / Suljovic, Denny / Seeliger, Frank / Söderberg, Magnus / Perez-Alcazar, Marta / Van Zuydam, Natalie / Abrahamsson, Bertil / Hugerth, Andreas M / Davies, Nigel / Bergström, Christel A S

    Molecular pharmaceutics

    2021  Volume 19, Issue 1, Page(s) 200–212

    Abstract: In this work, we set out to better understand how the permeation enhancer sodium caprate (C10) influences the intestinal absorption of macromolecules. FITC-dextran 4000 (FD4) was selected as a model compound and formulated with 50-300 mM C10. Absorption ... ...

    Abstract In this work, we set out to better understand how the permeation enhancer sodium caprate (C10) influences the intestinal absorption of macromolecules. FITC-dextran 4000 (FD4) was selected as a model compound and formulated with 50-300 mM C10. Absorption was studied after bolus instillation of liquid formulation to the duodenum of anesthetized rats and intravenously as a reference, whereafter plasma samples were taken and analyzed for FD4 content. It was found that the AUC and
    MeSH term(s) Animals ; Colloids/chemistry ; Cryoelectron Microscopy ; Decanoic Acids/analysis ; Decanoic Acids/chemistry ; Decanoic Acids/pharmacology ; Dextrans/pharmacology ; Drug Synergism ; Fluorescein-5-isothiocyanate/analogs & derivatives ; Fluorescein-5-isothiocyanate/pharmacology ; Intestinal Absorption/drug effects ; Intestinal Mucosa/chemistry ; Intestinal Mucosa/drug effects ; Male ; Rats ; Rats, Wistar
    Chemical Substances Colloids ; Decanoic Acids ; Dextrans ; fluorescein isothiocyanate dextran ; decanoic acid (4G9EDB6V73) ; Fluorescein-5-isothiocyanate (I223NX31W9)
    Language English
    Publishing date 2021-12-20
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2138405-8
    ISSN 1543-8392 ; 1543-8384
    ISSN (online) 1543-8392
    ISSN 1543-8384
    DOI 10.1021/acs.molpharmaceut.1c00724
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: Evaluation in pig of an intestinal administration device for oral peptide delivery.

    Berg, Staffan / Uggla, Teresia / Antonsson, Malin / Nunes, Sandro Filipe / Englund, Maria / Rosengren, Louise / Fahraj, Masoud / Wu, Xiaoqiu / Govender, Rydvikha / Söderberg, Magnus / Janzén, David / Van Zuydam, Natalie / Hugerth, Andreas / Larsson, Anette / Abrahmsén-Alami, Susanna / Abrahamsson, Bertil / Davies, Nigel / Bergström, Christel A S

    Journal of controlled release : official journal of the Controlled Release Society

    2022  Volume 353, Page(s) 792–801

    Abstract: The bioavailability of peptides co-delivered with permeation enhancers following oral administration remains low and highly variable. Two factors that may contribute to this are the dilution of the permeation enhancer in the intestinal fluid, as well as ... ...

    Abstract The bioavailability of peptides co-delivered with permeation enhancers following oral administration remains low and highly variable. Two factors that may contribute to this are the dilution of the permeation enhancer in the intestinal fluid, as well as spreading of the released permeation enhancer and peptide in the lumen by intestinal motility. In this work we evaluated an Intestinal Administration Device (IAD) designed to reduce the luminal dilution of drug and permeation enhancer, and to minimize movement of the dosage form in the intestinal lumen. To achieve this, the IAD utilizes an expanding design that holds immediate release mini tablets and places these in contact with the intestinal epithelium, where unidirectional drug release can occur. The expanding conformation limits movement of the IAD in the intestinal tract, thereby enabling drug release at a single focal point in the intestine. A pig model was selected to study the ability of the IAD to promote intestinal absorption of the peptide MEDI7219 formulated together with the permeation enhancer sodium caprate. We compared the IAD to intestinally administered enteric coated capsules and an intestinally administered solution. The IAD restricted movement of the immediate release tablets in the small intestine and histological evaluation of the mucosa indicated that high concentrations of sodium caprate were achieved. Despite significant effect of the permeation enhancer on the integrity of the intestinal epithelium, the bioavailability of MEDI7219 was of the same order of magnitude as that achieved with the solution and enteric coated capsule formulations (2.5-3.8%). The variability in plasma concentrations of MEDI7219 were however lower when delivered using the IAD as compared to the solution and enteric coated capsule formulations. This suggests that dosage forms that can limit intestinal dilution and control the position of drug release can be a way to reduce the absorptive variability of peptides delivered with permeation enhancers but do not offer significant benefits in terms of increasing bioavailability.
    MeSH term(s) Animals ; Swine ; Intestines ; Intestinal Mucosa/metabolism ; Peptides/chemistry ; Intestinal Absorption ; Administration, Oral ; Tablets ; Biological Availability
    Chemical Substances MEDI7219 ; Peptides ; Tablets
    Language English
    Publishing date 2022-12-16
    Publishing country Netherlands
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 632533-6
    ISSN 1873-4995 ; 0168-3659
    ISSN (online) 1873-4995
    ISSN 0168-3659
    DOI 10.1016/j.jconrel.2022.12.011
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article ; Online: In Vitro and In Vivo Evaluation of 3D Printed Capsules with Pressure Triggered Release Mechanism for Oral Peptide Delivery.

    Berg, Staffan / Krause, Julius / Björkbom, Anders / Walter, Katrin / Harun, Said / Granfeldt, Andreas / Janzén, David / Nunes, Sandro Filipe / Antonsson, Malin / Van Zuydam, Natalie / Skrtic, Stanko / Hugerth, Andreas / Weitschies, Werner / Davies, Nigel / Abrahamsson, Bertil / Bergström, Christel A S

    Journal of pharmaceutical sciences

    2020  Volume 110, Issue 1, Page(s) 228–238

    Abstract: In this study a 3D printed capsule designed to break from the physiological pressures in the antropyloric region was evaluated for its ability to deliver the synthetic octapeptide octreotide in beagle dogs when co-formulated with the permeation enhancer ... ...

    Abstract In this study a 3D printed capsule designed to break from the physiological pressures in the antropyloric region was evaluated for its ability to deliver the synthetic octapeptide octreotide in beagle dogs when co-formulated with the permeation enhancer sodium caprate. The pressure sensitive capsules were compared to traditional enteric coated hard gelatin capsules and enteric coated tablets. Paracetamol, which is completely absorbed in dogs, was included in the formulations and used as an absorption marker to give information about the in vivo performance of the dosage forms. The pressure sensitive capsules released drug in 50% of the dogs. In the cases where drug was released, there was no difference in octreotide bioavailability or C
    MeSH term(s) Administration, Oral ; Animals ; Biological Availability ; Capsules ; Dogs ; Peptides ; Printing, Three-Dimensional ; Tablets, Enteric-Coated
    Chemical Substances Capsules ; Peptides ; Tablets, Enteric-Coated
    Language English
    Publishing date 2020-11-17
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 3151-3
    ISSN 1520-6017 ; 0022-3549
    ISSN (online) 1520-6017
    ISSN 0022-3549
    DOI 10.1016/j.xphs.2020.10.066
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. Article: Physical characterization of anhydrous and hydrous forms of the hydrochloride salt of BVT.5182 a novel 5-HT(6) receptor antagonist.

    Hugerth, Andreas / Brisander, Magnus / Wrange, Ulla / Kritikos, Mikael / Norrlind, Björn / Svensson, Marianne / Bisrat, Mikael / Ostelius, Jan

    Drug development and industrial pharmacy

    2006  Volume 32, Issue 2, Page(s) 185–196

    Abstract: The physicochemical properties of 1-benzenesulfonyl-4-(piperazin-1-yl)-indole hydrochloride, a novel 5-HT(6) receptor antagonist for the treatment of obesity were characterized. Two solid state forms were identified at ambient conditions (23 degrees C): ... ...

    Abstract The physicochemical properties of 1-benzenesulfonyl-4-(piperazin-1-yl)-indole hydrochloride, a novel 5-HT(6) receptor antagonist for the treatment of obesity were characterized. Two solid state forms were identified at ambient conditions (23 degrees C): an anhydrate form (1) and a hydrate form (2), with 1.5 moles of H(2)O. The latter easily dehydrates and rehydrates without affecting the crystal morphology. Investigations of the propensity for interconversion between the two forms reveal that a) conversion of 2-->1 takes place above 145 degrees C and that b) conversion of 1-->2 only occurs after crystallization from supersaturated aqueous solutions at a water activity >or=0.94 or in the presence of comparable amounts of crystals of 2 in water at ambient conditions. However, in an equimolar suspension of 1 and 2 at 37 degrees C no phase transformation was observed. Thus, the difference in chemical potential between the two forms is small. Form 1 was shown to have overall favorable solid state properties and, hence, considered the preferred form for continued pharmaceutical development. The characterization was performed by means of light microscopy, scanning electron microscopy, powder X-ray diffraction, FTIR/NIR-spectroscopy, differential scanning calorimetry, hot stage microscopy, thermogravimetry, dynamic vapor sorption, Karl Fischer water content determination, phase stability studies of suspensions, solubility, and intrinsic dissolution rate measurements.
    MeSH term(s) Anti-Obesity Agents/chemistry ; Chemistry Techniques, Analytical ; Drug Stability ; Indoles/chemistry ; Piperazines/chemistry ; Serotonin 5-HT1 Receptor Antagonists ; Solubility ; Water/chemistry
    Chemical Substances Anti-Obesity Agents ; BVT.5182 ; Indoles ; Piperazines ; Serotonin 5-HT1 Receptor Antagonists ; Water (059QF0KO0R)
    Language English
    Publishing date 2006-02-10
    Publishing country England
    Document type Journal Article
    ZDB-ID 751874-2
    ISSN 1520-5762 ; 0363-9045
    ISSN (online) 1520-5762
    ISSN 0363-9045
    DOI 10.1080/03639040500466122
    Database MEDical Literature Analysis and Retrieval System OnLINE

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