FORMULATION DEVELOPMENT AND EVALUATION OF SUBLINGUAL DRUG DELIVERY SYSTEM OF BILASTINE FOR ALLERGIC RHINOCONJUNCTIVITIS

Allergic rhinitis (AR) is very common clinical condition and affects 10–40% of individuals worldwide. It has a substantial negative effect on patient’s quality of life (QoL), sleep and daily activities. Various therapeutic classes are used for the management of allergic rhinitis. Among all the classes, H₁ receptor antagonist is used as first line treatment. Many molecules belong to antihistamine class and on the basis of selectivity and its adverse effect it can be classified as first generation, second generation and novel second-generation antihistamine. Among all the molecules, Bilastine is a novel new second generation with selective peripheral, non – sedating, H₁ antihistamine. Its affinity is also higher than the other antihistamine. It belongs to BCS class II drug which has less solubility and high permeability. So, for enhancement of solubility complexation technique is used and inclusion complex of Drug: HP-β-CD (1:2) was prepared by microwave irradiation method. Here great need arises to alter the route of administration of Bilastine for improving absorption and drug release pattern. As per the literature study, it can be concluded that Sublingual route offer immediate drug release directly into systemic circulation, results in rapid on-set of action. In present study sublingual tablet of Bilastine is prepared by direct compression method. The effect of different superdisintegrants (SSG, CCS, Kyron T-314, Indion 414) in two different concentrations are examined for selection of best superdisintegrant. Result of check point batch F 10 suggested that tablet disintegrated within 50 sec. Similarly, in-vitro dissolution study showed 97.68 % drug release in 10 min.

Keywords: Allergic rhinoconjunctivitis, Quality of life, H₁ receptor antagonist, Bilastine, Sublingual tablet.