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In-vitro and in-vivo evaluation of formulated lidocaine dental gels and ointments



In-vitro and in-vivo evaluation of formulated lidocaine dental gels and ointments



Egyptian Journal of Pharmaceutical Sciences 38(4-6): 471-486



IN THIS research, lidocaine Hcl and lidocaine were fromulated in different gel and ointment bases. Eight fromulations of lidocaine and lidocaine Hcl ointment and gel (four as 2% gel, one as 5% gel and three as 5% ointment) were prepared and tested for their release in sorensen's phosphate buffer pH7.4 using U.S.P. dissolution test apparatus at 37degree +- 0.5degree and compared with four commercially available products namely xylocaine 2% jelly (Astra - Sweden), xylonor 5% gel (Septodont - England) xylocaine 5% ointment (Astra - Sweden and Astra Cid). In vitro results showed that: Formulae I (Lidocaine Hcl 2.0 g in carbopol gel base) and formula IV (Lidocaine Hcl 2.0g in carboxymethyl cellulose gel base) gave the highest extent of release of the prepared gel formulae. Formula VII (Lidocaine 5g in emulsifying ointment base containing liquid paraffin and bees wax) gave the highest extent of release among all the prepared ointment formulae. The local anesthetic effect of the prepared lidocaine gel and ointment was evaluated in vivo using albino mice. The mean duration of action for each of the tested preparation was obtained using the corneal reflex for the bioassay of the topical anesthetic effect. Results of this study showed that: Formula IV and Formula V of the gels were the best formulae regarding the mean duration of anesthetic effect. Formula VI of the ointments gave the highest duration of action followed by formula VII. Correlation of the in vitro release studies to the in vivo studies showed that there is a moderate correlation in case of lidocaine Hcl gels, while in case of ointments, there was no correlation.

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