Formulation of Suppositories Containing Imipramine and Clomipramine Chlorhydrates

AbstractImipramine chlorhydrate and clomipramine chlorhydrate could be formulated into suppositories forms. Their ability to be administered by the rectal way was assessed by the measurement of their hydrophilic/lipophilic partition coefficient and their diffusion coefficient with the Strieker's apparatus. The suppositories were formulated with several halfglycerides excipients. The selection of the formulae was carried out by using the following physicochemical tests: rheological behaviour, melting point, liquefaction time with the Krowczynski's technique, disintegration time with the Munzel's method, spreading area, hardness, kinetic of release. The bioavailability of the suppositories evaluated on rabbits compared to an intravenous injection was 28% for Clomipramine and 25 % for Imipramine.A clinical assay was carried out with three inpatients, The plasmatic levels of the drugs and the clinical efficiency were in the same range as previous data reported in the literature for oral forms.