title: Oral sustained-release suspension based on a novel taste-masked and mucoadhesive carrier-ion-exchange fiber.
abstract: The purpose of this study was to evaluate the feasibility of ion-exchange fiber ZB-1 as a novel carrier in oral taste-masked mucoadhesive sustained-release suspensions. Propranolol (PPN) hydrochloride was selected as a model drug with good water solubility, short half life and bitter taste. The PPN-fiber complexes (PF) were prepared by a batch process and coated with Eudragit(®) RS100. Gamma scintigraphy was performed on fasted volunteers revealed about 30% ZB-1 and more than 50% coated ZB-1 were still remaining in the stomach at 6h. In vitro results showed the releases of PF and coated PPN-fiber complexes (C-PF) were sustained. The release, drug content and particle size of C-PF were influenced by coat to core ratio, concentration of coating material and rotation rate. The suspension was stable after standing for 30 days in 0.5% Carbopol(®) with no release rate and taste changed. The administration of C-PF suspension to rats resulted a significant different (P<0.05) improvement of the plasma drug level and prolongation of the release. However, because of the burst effect, the Cmax values of PF suspension didn't differ from drug solution (P>0.05). Furthermore, a linear relationship between in vitro dissolution and in vivo absorption was observed.
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
authors.forename: Jing
authors.initials: J
authors.lastname: Yuan
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
authors.forename: Tiaotiao
authors.initials: T
authors.lastname: Liu
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
authors.forename: Heran
authors.initials: H
authors.lastname: Li
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
authors.forename: Tianyu
authors.initials: T
authors.lastname: Shi
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
authors.forename: Jie
authors.initials: J
authors.lastname: Xu
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
authors.forename: Hongzhuo
authors.initials: H
authors.lastname: Liu
authors.affiliation: Nuclear Medicine Department, The General Hospital of Shenyang Military Command, Shenyang 110016, PR China.
authors.forename: Zhiguo
authors.initials: Z
authors.lastname: Wang
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
authors.forename: Qifang
authors.initials: Q
authors.lastname: Wang
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
authors.forename: Lu
authors.initials: L
authors.lastname: Xu
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
authors.forename: Yan
authors.initials: Y
authors.lastname: Wang
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, PR China. Electronic address: li_sanming@126.com.
authors.forename: Sanming
authors.initials: S
authors.lastname: Li
mesh_terms: D000180:Acrylic Resins / Q000737:chemistry; D000268:Adhesiveness; D000284:Administration, Oral; D000328:Adult; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D004337:Drug Carriers / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D005215:Fasting / Q000378:metabolism; D005753:Gastric Mucosa / Q000378:metabolism; D006801:Humans; D007474:Ion Exchange; D008297:Male; D011433:Propranolol / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics; D011877:Radionuclide Imaging; D013535:Suspensions; D013649:Taste; D013667:Technetium; D055815:Young Adult
chemical_list: D000180:Acrylic Resins; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D013535:Suspensions; C050528:Eudragit RS; D013667:Technetium; D011433:Propranolol
keywords: Acetonitrile (PubChem CID: 6342); Dibutyl phthalate (PubChem CID: 3026); Ethanol (PubChem CID: 702); Ether (PubChem CID: 3283); Gamma scintigraphy; Ion-exchange fiber; Mucoadhension; Polyethylene glycol 400 (PubChem CID: 5327147); Propranolol hydrochloride; Span 80 (PubChem CID: 9920342); Sustained-release suspension; Taste masking; Technetium-99 m (as pertechnetate) (PubChem CID: 23689036)