Chemical Properties
White or almost white, crystalline powder.
Uses
Salicylate; non-selective cyclo-oxygenase inhibitor; antipyretic; analgesic; antiinflammatory.
Description
Carbasalate calcium is a calcium-urea chelate of aspirin (Item No.
70260) that has analgesic, anti-inflammatory, and antipyretic effects.
1,2 It reduces carrageenan-induced paw edema in rats.
2
Originator
Calurin,Dorsey,US,1959
Manufacturing Process
500 g of finely powdered acetylsalicylic acid and 160 g of calcium carbonate
(precipitated chalk), are intimately mixed and 3,000 cc of water are added.
The mixture is stirred for 15 minutes or until the reaction is completed, which
is indicated by the cessation of the liberation of carbon dioxide. The
temperature is desirably maintained below 20°C by any suitable means. The
mass is allowed to settle until the supernatant liquor is almost clear; this
usually takes about 5 minutes, and the mixture is then filtered to remove
unreacted material. This part of the process is carried out as quickly as
possible so as to minimize any tendency of the calcium aspirin to hydrolyze in
the solution. The filtrate is cooled to about 10°C and 1 to 1.5 volumes of 97% methanol, or pure wood alcohol is added. This causes the calcium aspirin to
precipitate and the mass is then filtered to remove as thoroughly as possible
the mother liquor. The residue of calcium aspirin is then suspended in a
quantity of methanol equivalent to the volume previously used as a
precipitant, and it is allowed to stand there for one hour or more with
occasional or continuous agitation. The mass is again filtered, the filtrate
being employed for the precipitation of calcium aspirin in a later batch. After
the filtering of the first wash liquor, the calcium aspirin is again suspended in
another quantity of methanol of an equivalent volume. This constitutes the
second wash and it is carried out in the same way as the first wash. The
filtrate is employed as a first wash in a later batch and this filtrate in turn is
used, as is the filtrate of the first wash, for the precipitation of more calcium
aspirin. Fresh alcohol is used as a new wash in a later batch and the washes
are carried out in series. After the second wash the calcium aspirin is dried in
a suitable manner, as by passing dry warm air over it, the temperature not
being allowed to rise to such an extent as to decompose the aspirin;
preferably the temperature is not permitted to rise above 50°C, but should be
high enough to avoid deposition of water vapor, and the drying is completed
when there is no longer an odor of methanol.
Therapeutic Function
Analgesic, Antipyretic, Antirheumatic
Mechanism of action
Carbasalate calcium is a non-steroidal anti-inflammatory drug. In addition to their anti-inflammatory effects, they are analgesic, antipyretic and platelet inhibitory. They block prostaglandin synthesis by inhibiting the enzyme cyclooxygenase, which converts arachidonic acid into cyclic endoperoxide, the precursor of prostaglandins. Inhibition of prostaglandin synthesis is responsible for their analgesic, antipyretic, and platelet-inhibitory effects; other mechanisms may contribute to their anti-inflammatory effects.
