COMPOSITION AND BIOPHARMACEUTICAL PROPERTIES OF NASAL SPRAY WITH SYSTEMIC ACTION

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DOI: https://doi.org/None
Issue: 
7
Year: 
2015

E.P. Bezuglaya (1), PhD; E.A. Bariev (3); Professor N.A. Lyapunov (1), PhD; O.V. Timchenko (2); A.I. Bardakov (3), PhD 1 -State Scientific Institution «Institute for Single Crystals», National Academy of Sciences of Ukraine, Kharkov, Ukraine 2 -State Research Center of Medicines and Medical Products, Kharkov, Ukraine 3 -N.A. Semasko Moscow Production Chemopharmaceutical Association; 9, B. Kamenshchiki St., Moscow 115172

The composition of Naloxone nasal spray was designed using the results of an investigation of its physicochemical and biopharmaceutical properties. The agent’s properties (wettability, spreadability, hyperosmolarity, and a penetration intensifier, rapid and complete release of naloxone hydrochloride in moderate water absorption, and no respirable particle fraction in aerosol spray) are favorable to the accurate dosing and rapid absorption of intranasal naloxone hydrochloride into the rabbit systemic blood flow with the absolute bioavailability of about 30%. The results of the investigations make it possible to consider intranasal naloxone chloride spray as an alternative to the parenteral administration of solution for injection.
Keywords: 
naloxone hydrochloride
nasal spray
composition
release
bioavailability
pharmacokinetics
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