T. Vanlaar et al., A NEW SUBLINGUAL FORMULATION OF APOMORPHINE IN THE TREATMENT OF PATIENTS WITH PARKINSONS-DISEASE, Movement disorders, 11(6), 1996, pp. 633-638
A new formulation of a sublingual tablet with 10 mg apomorphine was ex
amined in 13 patients with Parkinson's disease. Vitamin C (250 mg) was
added sublingually to lower the salivary pH. Four patients received s
ublingual apomorphine and nine received sublingual apomorphine as well
as vitamin C. Subcutaneous apomorphine was given to all patients. The
study was de signed as a randomized three-way cross-over study. T-max
, C and bioavailability (F) were determined. Clinical efficacy was ass
essed by hand-tapping during 30 s, walking time over 25 m, and a 4-poi
nt tremor score. The mean T-max, after subcutaneous apomorphine was 14
.5 +/- 1.9 min with a mean C-max, of 19.2 +/- 3.8 ng/ml. The mean clea
rance of all patients was 3.8 +/- 0.6 L/min. The mean T-max, after sub
lingual apomorphine was 61.1 +/- 6.9 min vs. 61.7 +/- 8.2 min with vit
amin C. The mean C was 7.4 +/- 1.0 ng/ml (- vitamin C) vs. 4.3 +/- 1.3
ng/ml (+ vitamin C). These data resulted consequently in a not signif
icantly different mean bioavailability, varying from 17.6% (- vitamin
C) to 6.1% (+ vitamin C), The latency of onset of clinical efficacy va
ried between 25.0 +/- 8.5 min (- vitamin C) and 26.0 +/- 5.3 min (+ vi
tamin C). The duration of effect was lower (not significantly) when vi
tamin C was added: 88.0 +/- 12.5 min (- vitamin C) vs. 61.0 +/- 11.9 m
in (+ vitamin C). These data show that 10 mg apomorphine sublingually
was effective in 56% of the patients, The combination with vitamin C d
id not significantly change the latency of onset or duration of clinic
al efficacy. Sublingual apomorphine should be considered as an alterna
tive in the treatment of ''off''-periods in Parkinson's disease, in pa
rticular when patients have the capacity to anticipate their off-perio
ds.