Keywords : Cinnarizine

Preparation of Cinnarizine Oral Lyophilizates

Rasha Dhahir; Myasar Al-Kotaji

Iraqi Journal of Pharmacy, 2021, Volume 18, Issue 1, Pages 33-43
DOI: 10.33899/iphr.2021.168800

Background: Orally disintegrating tablets (ODTs) have gained an increasing interest in the pharmaceutical industry for the last years. Several technologies have been sophisticated for ODTs to improve patient compliance. In the present work, an attempt has been made to formulate and evaluate cinnarizine, a drug for motion sickness, in an easy to administer, rapid disintegrated dosage form (oral lyophilizates with enhanced disintegration and dissolution profile and consequent potential improvement in bioavailability.
Materials and Methods: Cinnarizine oral lyophilizates were prepared by dispersing the drug in an aqueous solution of mannitol, hydroxypropyl methyl cellulose, and glycine. Different formulations were prepared by freeze-drying (lyophilisation) technique. The effect of concentration of mannitol, hydroxypropyl methyl cellulose, and freezing time on the lyophilizates characteristics was investigated. The drug-excipient interaction was investigated as well.
Results: The resulting cinnarizine oral lyophilizates showed an enhanced disintegration (27.5±3.53 sec to 56±12.73 sec) and enhanced dissolution profile (25.09% to 44.7% after two minutes). The infrared spectroscopic studies showed no drug-excipient interactions. Furthermore, increasing the concentration of mannitol, increasing the concentration of hydroxypropyl methyl cellulose and duplication of the duration of freezing time had a negative influence on the disintegration and dissolution properties of the resulting lyophilizates.
Conclusion: Cinnarizine oral lyophilizates were successfully prepared and resulted in a rapid disintegration, high dissolution profile, with stable characteristics and without noticeable drug-excipient interaction.