Ev. Kokurina et al., ASCOLONG - A NEW BUCCAL DOSAGE FORM OF AC ETYLSALICYLIC-ACID TO BE USED AS ANTIAGGREGANT, Terapevticeskij arhiv, 70(1), 1998, pp. 32
Aim. Study of the tolerance and pharmacodynamic and pharmacokinetic ch
aracteristics of ascolong, a new buccal dosage form of aspirin contain
ing a very low dose of acetylsalicylic acid (ASA): 12.5 mg. Materials
and Methods. The study was carried out in 43 healthy men (assessment o
f the drug tolerance) and 19 male patients with coronary disease or ce
rebrovascular disorders. In 10 patients the antiaggregant efficacy of
ascolong administered once or regularly (for 2 weeks) in a dose of 12.
5 mg was compared with placebo, in 9 patients a random cross study of
2-week courses of ascolong and Russian aspirin tablets in a dose of 10
0 mg was carried out. Platelet aggregation was assessed on days 1 and
14 of each course before and 2, 4, and 24 h after the drug intake. Res
ults. Ascolong containing a very low dose of ASA exerts a reliable ant
iaggregant effect after a single and regular intake, although this eff
ect is less manifest than after aspirin tablets. Profiles of ASA conce
ntrations in the blood were studied. Transbuccal entry of ASA in syste
mic circulation decelerated its metabolism into a less active metaboli
te, salicylic acid, due to which fact the ASA microdose had an express
ed antiaggregant effect. The drug was sufficiently well tolerated. Con
clusion. The new buccal film form of aspirin containing a very low clo
se of ASA possesses a good antiaggregant effect and is promising in su
bjects with contraindications to oral intake of aspirin.