[Ascolong: a new buccal dosage form of acetylsalicylic acid to be used and antiaggregant].
OBJECTIVE
Study of the tolerance and pharmacodynamic and pharmacokinetic characteristics of ascolong, a new buccal dosage form of aspirin containing a very low dose of acetylsalicylic acid (ASA): 12.5 mg.


METHODS
The study was carried out in 43 healthy men (assessment of the drug tolerance) and 19 male patients with coronary disease or cerebrovascular 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 100 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.


RESULTS
Ascolong containing a very low dose of ASA exerts a reliable antiaggregant effect after a single and regular intake, although this effect is less manifest than after aspirin tablets. Profiles of ASA concentrations in the blood were studied. Transbuccal entry of ASA in systemic circulation decelerated its metabolism into a less active metabolite, salicylic acid, due to which fact the ASA microdose had an expressed antiaggregant effect. The drug was sufficiently well tolerated.


CONCLUSIONS
The new buccal film form of aspirin containing a very low dose of ASA possesses a good antiaggregant effect and is promising in subjects with contraindications to oral intake of aspirin.
Kokurina
E V
EV
Suslina
Z A
ZA
Khromov
G L
GL
Davydo
A B
AB
Metelitsa
V I
VI
Ionova
V G
VG
Tanashian
M M
MM
Demina
E G
EG
Bochkareva
E V
EV
Belolipetskaia
V G
VG
Deev
A D
AD
Kucheriaeva
N G
NG
Zidra
S I
SI
Gorin
N N
NN
Rumiantsev
D O
DO
D000278:Administration, Buccal; D001241:Aspirin / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D002561:Cerebrovascular Disorders / Q000188:drug therapy / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D003327:Coronary Disease / Q000188:drug therapy / Q000378:metabolism; D018592:Cross-Over Studies; D004304:Dosage Forms; D005500:Follow-Up Studies; D006801:Humans; D008297:Male; D008875:Middle Aged; D010975:Platelet Aggregation Inhibitors / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D012449:Safety; D016896:Treatment Outcome
D004304:Dosage Forms; D010975:Platelet Aggregation Inhibitors; D001241:Aspirin
Aksolong: novaia bukkal'naia forma atsetilsalitsilovoĭ kisloty dlia primeneniia v kachestve antiagreganta.