109 - Intranasal morphine  pp. 437-439


By Denis V. Snegovskikh

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Generic Name: intranasal morphine (morphine mesylate/chitosan)

Trade Name: Rylomine™

Drug Class: opioid analgesic

Manufacturer: Javelin Pharmaceuticals, 125 Cambridge Park Drive Cambridge, MA 02140; Javelin was recently acquired by Hospira, Lake Forest, IL

Chemical Structure: see Figure 109.1

Chemical Name: (5α,6α)-7,8-didehydro-4,5-epoxy-17-methyl morphinian-3,6-diol

Chemical Formula: C17H19NO3; molecular wt 285.34

Introduction

Intranasal (IN) morphine (Rylomine™) is a patient-controlled nasal spray that delivers a single, metered dose of Morphine. Rylomine™ is currently in phase 3 clinical development and may have use as a rapid-acting analgesic in both acute and chronic pain settings.

Description

Intranasal morphine provides rapid analgesic onset (comparable to IV) together with a simple and non-invasive way to control moderate to severe pain. It consists of a combination of active ingredient morphine mesylate and ChiSys delivery system. ChiSys is based on the use of chitosan to evenly disperse and improve morphine absorption through the nasal mucosa.

Chitosan is a cationic linear polysaccharide, composed of two monosaccharides: N-acetyl-d-glucosamine and d-glucosamine linked together by glucosidic bonds. Chitosan is obtained from partial deacetylation of chitin, which originates from shells of crustaceans (e.g. crabs and prawns) and forms positively charged salts when dissolved in inorganic and organic acids. Glutamate salt of chitosan with a mean molecular weight of around 200 kDa and a degree of deacetylation of 80–90% is used for nasal delivery of drugs.

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