Optimal Solubility of Diclofenac β-Cyclodextrin in Combination with Local Anaesthetics for Mesotherapy Applications

Because of low injection volume, the recently marketed injectable solution of diclofenac in complex with β-cyclodextrin (Akis®, IBSA Farmaceutici Italia) is an ideal candidate for mesotherapy applications. In this study, we investigated the solubility of Akis, 25 and 50 mg/kg, in combination with va...

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Bibliographic Details
Main Authors: Giuseppe Tringali, Pierluigi Navarra
Format: Article
Language:English
Published: Hindawi Limited 2017-01-01
Series:Evidence-Based Complementary and Alternative Medicine
Online Access:http://dx.doi.org/10.1155/2017/8321325
Description
Summary:Because of low injection volume, the recently marketed injectable solution of diclofenac in complex with β-cyclodextrin (Akis®, IBSA Farmaceutici Italia) is an ideal candidate for mesotherapy applications. In this study, we investigated the solubility of Akis, 25 and 50 mg/kg, in combination with various local anaesthetics (lidocaine, mepivacaine, bupivacaine, levobupivacaine, and ropivacaine) at different concentrations in aqueous vehicles (normal saline, sterile water, or bicarbonate). Final injection mixtures were classified as limpid, turbid, or milky at visual analysis under standardized conditions. We found that (i) the use of sterile water for injections or normal saline as vehicles to dilute Akis in combination with whatever local anaesthetic normally results in milky solutions and therefore is not recommended; (ii) using bicarbonate, optimal solubility was obtained combining Akis with lidocaine, both 1 and 2%, or mepivacaine, both 1 and 2%, whereas solutions were turbid in combination with bupivacaine, levobupivacaine, or ropivacaine. Thus, we recommend that Akis is used in combination with lidocaine or mepivacaine in a bicarbonate vehicle.
ISSN:1741-427X
1741-4288