PILOT-STUDY OF CONTROLLED-RELEASE PILOCARPINE IN NORMAL SUBJECTS

Objectives. Current systemic treatments with sialogogues for patients with xerostomia are limited because of minimal efficacy, short duratio n of activity, or problems with side effects. The purpose of this pilo t study wag an initial assessment of safety, efficacy, duration of act ion, multiple dose tolerance, and side effects of a controlled-release formulation of pilocarpine hydrochloride. Study design. Eight healthy hospitalized subjects were given 15 mg of a controlled-release piloca rpine formulation every 12 hours for three doses. Saliva and blood sam ples were collected at assigned intervals. Repeated measures analysis and paired tests were used for statistical analyses. Results. A signif icant (p < 0.05) increase in both parotid and whole saliva output foll owed all three doses beginning within 1 hour of dosing and lasting ove r 10 hours. Mean plasma pilocarpine concentration reached a maximum of 8.2 ng/ml at approximately 1 hour after the first dose, 11.5 ng/ml af ter the third dose, and declined to near baseline (0.06 ng/ml) 24 hour s after the final dose. None of the participants showed evidence of ad verse effects including complaints of sweating or gastrointestinal dis comfort Conclusions. A controlled-release formulation of pilocarpine m ay overcome the therapeutic weaknesses of current pilocarpine preparat ions by prolonging salivary secretion and reducing undesirable side ef fects.