期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICAL INVESTIGATION
卷 3, 期 4, 页码 194-202出版社
WOLTERS KLUWER MEDKNOW PUBLICATIONS
DOI: 10.4103/2230-973X.121292
关键词
Atenolol; hydroxylamine derivatives; metal-polymer cross-linked beads; pulsatile release; sodium alginate
Introduction: Alginates can be tailored chemically to improve solubility, physicochemical, and biological properties and its complexation with metal ion is useful for controlling the drug release. Materials And Methods: Synthesized N, Odimethyl, N-methyl, or N-Benzyl hydroxylamine derivatives of sodium alginate were subsequently complexed with zinc to form beads. Hydroxamation of sodium alginate was confirmed by Fourier transform infra-red spectroscopy (FTIR) and differential scanning calorimetry (DSC). Results: The synthesized polymeric material exhibited reduced aqueous, HCl and NaOH solubility. The hydroxamated derivatives demonstrated pulsed release where change in pH of the dissolution medium stimulated the atenolol release. Conclusion: Atenolol loaded Zn cross-linked polymeric beads demonstrated the sustained the plasma drug levels with increased half-life. Although the synthesized derivatives greatly altered the aqueous solubility of sodium alginate, no significant differences in in vitro and in vivo atenolol release behavior amongst the N, O-dimethyl, N-methyl, or N-Benzyl hydroxylamine derivatives of sodium alginate were observed.
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