Intranasal Delivery of Morphine
| Autor: | H. Norbury, Inderjit Jabbal-Gill, Stanley Stewart Davis, Lisbeth Illum, M Hinchcliffe, R. Nankervis, Watts Peter, A. N. Fisher |
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| Rok vydání: | 2002 |
| Předmět: |
Adult
Male Adolescent Metabolite Pain relief Chitin Absorption (skin) Pharmacology Absorption Excipients chemistry.chemical_compound Oral administration Adhesives medicine Animals Humans Administration Intranasal Chitosan Sheep Morphine business.industry Starch Microspheres Bioavailability Analgesics Opioid Solutions Nasal Mucosa chemistry Area Under Curve Anesthesia Injections Intravenous Molecular Medicine Female Nasal administration Powders business Intravenous route medicine.drug |
| Zdroj: | Journal of Pharmacology and Experimental Therapeutics. 301:391-400 |
| ISSN: | 1521-0103 0022-3565 |
| DOI: | 10.1124/jpet.301.1.391 |
| Popis: | Morphine administered nasally to humans as a simple solution is only absorbed to a limited degree, with a bioavailability of the order of 10% compared with intravenous administration. This article describes the development of novel nasal morphine formulations based on chitosan, which, in the sheep model, provide a highly increased absorption with a 5- to 6-fold increase in bioavailability over simple morphine solutions. The chitosan-morphine nasal formulations have been tested in healthy volunteers in comparison with a slow i.v. infusion (over 30 min) of morphine. The results show that the nasal formulation was rapidly absorbed with a T(max) of 15 min or less and a bioavailability of nearly 60%. The shape of the plasma profile for nasal delivery of the chitosan-morphine formulation was similar to the one obtained for the slow i.v. administration of morphine. Furthermore, the metabolite profile obtained after the nasal administration of the chitosan-morphine nasal formulation was essentially identical to the one obtained for morphine administered by the intravenous route. The levels of both morphine-6-glucuronide and morphine-3-glucuronide were only about 25% of that found after oral administration of morphine. It is concluded that a properly designed nasal morphine formulation (such as one with chitosan) can result in a non-injectable opioid product capable of offering patients rapid and efficient pain relief. |
| Databáze: | OpenAIRE |
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