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Sustained release subcutaneous delivery of BMS-686117, a GLP-1 receptor peptide agonist, via a zinc adduct by Feng Qian; Nina Ni; Lori S. Burton; Yue Fen Wang; Sridhar Desikan; Munir Hussain; Ronald L. Smith is a Pharmacology, Toxicology and Pharmaceutics article available to read on EtoBox.

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BMS-686117 is an 11-mer GLP-1 receptor agonist with a short intrinsic pharmacokinetic half-life (t(1/2)) of approximately 2h. In order to develop an extended release formulation for once-daily (QD) subcutaneous administration, a non-covalently bonded Zn/BMS-686117 adduct with very low aqueous solubility was prepared through mixing zinc acetate and BMS-686117 solutions, followed by filtration or spray drying. At pH 6.8, free BMS-686117 concentration decreased continuously with the increase of Zn:BMS-686117 ratio. Furthermore, free BMS-686117 concentration increases in the presence of ethylenediaminetetraacetic acid (EDTA), indicating the reversibility of the zinc-peptide association. As solids, the glass transition temperature of Zn/BMS-686117 adduct increases with the increase of Zn:BMS-686117 ratio. A Zn/BMS-686117 adduct suspension, with a molar ratio of zinc:BMS-686117 of 3:1, was dosed subcutaneously to dogs along with two other solution formulations. The Zn/BMS-686117 adduct showed a prolonged BMS-686117 terminal t(1/2) of 8.5h, a mean residence time (MRT) of 16h, and a C(max) value 6-8 times lower than the solution formulations. Additionally, the Zn/BMS-686117 was encapsulate

Who reads Sustained release subcutaneous delivery of BMS-686117, a GLP-1 receptor peptide agonist, via a zinc adduct?

Author

Feng Qian; Nina Ni; Lori S. Burton; Yue Fen Wang; Sridhar Desikan; Munir Hussain; Ronald L. Smith

Publisher

Elsevier Science; Elsevier ; Elsevier BV (ISSN 0378-5173)

Published

2009

Language

EN

Field

Pharmacology, Toxicology and Pharmaceutics (Life Sciences)