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In vitro and in vivo studies on lidocaine formulated in an o/w cream and in a polyethylene glycol ointment

In vitro and in vivo studies on lidocaine formulated in an o/w cream and in a polyethylene glycol ointment

Acta Pharmaceutica Suecica 19(3): 229-240

Silicone membrane and isopropyl myristate (ISM) sink methods were used to study the release of lidocaine from an o/w [oil/water] cream and a polyethylene glycol (PEG) ointment base. For creams of different lidocaine concentrations, the rate of release was faster with the ISM method but slower for the PEG base. Diffusion coefficients independent of the initial concentation were calculated by using free unsolubilized lidocaine in the external aqueous phase as the saturation concentration in an equation designed for suspended drug. For the PEG base, independent values were obtained by assuming complete solubility of the drug. The local anesthetic effect of the formulations was measured by pin-pricking on guinea pig skin. Good correlations to both the in vitro methods were found. When comparing cream and ointment bases, the silicone membrane method appears to be more suitable. The topical efficacy of the 1% lidocaine cream is equal to that of the 5% ointment.

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Accession: 068651775

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PMID: 7113730

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