The aim of the present study was to develop oral sublingual tablets of ticagrelor to give quick onset of action by rapidly disintegrating in a few seconds without the need of water with better patient compliance. In such cases, bioavailability of drug is significantly greater and adverse event is reduced than those observed from conventional tablet dosage form.
The work done is summarized as follows:
Ticagrelor is very slightly soluble in water; so the study plan was done, to improve the solubility of ticagrelor by solid dispersion, and then was to formulate sublingual tablets.
Solid dispersion was prepared by melting method using water soluble carrier polyethylene glycol 6000 showed better in vitro release studies in phosphate buffer pH6.8 using USP Type II apparatus.
The results revealed that the increase in the carrier concentration increased the dissolution rate (1:4 ratios).
The in vitro release studies revealed that the solid dispersion formulations showed a faster drug release when compared to the physical mixture and pure drug.
By performing Drug - Excipients compatibility studies by IR
spectrophotometry, no interaction drug-excipients was confirmed. Oral disintegrating tablets were formulated by direct compression method and suitable analytical method based on UV-Visible spectrophotometer was developed for the model drug.
Standard calibration curve prepared to determine the drug content in the prepared tablets and UV analysis was performed to determine the drug during in vitro release studies.
Prior to compression, the blend of drug and excipients were evaluated for flow properties such as Angle of repose, loose bulk density, Tapped density, % Compressibility, and Hausner’s ratio. All the formulations showed good flow properties.
Sublingual tablets were prepared by direct compression technique using 12-Station D/B Tooling Compression Machine, equipped with concave round punch of 8 mm diameter.
Post compression evaluation of prepared sublingual tablets were carried out with the help of different pharmacopoeial tests.
The shape and colour of all the formulations were found to be circular and white in colour.
The thickness was found to be uniform in specific formulations. The hardness, weight variation, diameter are also within the permitted limits.
The friability of all the tablets was found to be ˂ 1%, which indicates the good mechanical resistance.
The wetting time of sublingual tablets containing crosspovidone (7.5%) was found to be 54 seconds.
CONCLUSION:
The study conclusively demonstrated significant results for ticagrelor sublingual tablets. The sublingual tablets of ticagrelor was more palatable, and it is mostly helpful to the patients for the treatment of acute coronary
syndrome, cardiac angina. The sublingual tablets of ticagrelor can be successfully prepared by direct compression method using selected superdisintegrants with Crosscarmellose sodium 1.5%, 3%, 4.5%, 6%, 7.5%,
Crosspovidone 1.5%, 3%, 4.5%, 6%, 7.5% and Sodium starch glycolate 1.5%, 3%, 4.5%, 6%, 7.5% for the better patient compliance and effective therapy the relative efficiency to improve the disintegration and dissolution rate of tablets were found. The disintegration time of F10 with 7.5%
Crosspovidone formulation to be as 55.8 seconds respectively and is almost better than other formulations. Invitro dissolution studies were performed for all formulations. The formulation F10 showed 98.21% release within the 30 minutes. Crosspovidone shows good result as compare to other
superdisintegrants.
Crosspovidone > crosscarmellose sodium > sodium starch glycolate
