Preparation And Evaluation Of Loratidine Oral Fast Dissolving Films

Objectives: To achieve the pharmaceutical pre-formulation studies of loratidine,which performed as the active pharmaceutical ingredient.Optimize the formulation to prepare loratidine oral fast dissolving films and evaluate its thickness,weight,API content,disintegration time,in-vitro dissolution rate,etc.To achieve the success of rapid release and fast absorption of loratidine.Method:(1)the pharmaceutical pre-formulation studies of the API: The purity and maximum UV absorption wavelength was detected to establish an HPLC method for the analysis of loratidine.The precision,recovery and reproducibility of the analytical methodwere also evaluated.The stability of loratidine under high humidity,high temperature and light conditions after 5 and 10 days respectively were further studied.(2)Orthogonal experiment was designed to optimize the formulation and then the oral fast dissolving films of loratidine was prepared by solvent casting method.The film was evaluated by its appearance,thickness,weight,and disintegration time,etc.(3)The quality of the film was evaluated by its appearance,weight variation,thickness,disintegration time,dissolution rate,etc.The structure of the film after formulation was verified by X-RD and FI-IR.The stability of the film under high humidity,high temperature and light condition were also detected.Results:(1)The maximum absorption wavelength of loratidine measured by UV scanning was 247 nm.The analysis method established by HPLC showed good linear relationship between the ranges of 1-100 ?g/mL.The stability test of the prepared film demonstrated that it was stable under high humidity,high temperature,light condition,strong acid,strong base,and strong oxidant for extended period of time.(2)The optimal formulation was determined by the orthogonal experiment: Pullulan was used as water-soluble film-forming material and the ratio of film-forming material and API is 6.4:1.0.18 g PEG-400 and 0.2 g corn starch were added as plasticizer and disintegrant separately.The smooth appearance and weight variation of the prepared oral fast dissolving films were compliant with the 2015 edition of “Chinese pharmacopeia”.The average thickness and disintegrated time of the films were measured at 122 ± 28 ?m and 38 s respectively.(3)The X-RD and FT-IR results indicates that loratidine may be combined with other excipients during the formulation of the films.The cumulative release of the films in different pH media showed that loratidine oral fast dissolving films could be rapidly released,especially in the simulated oral cavity.Conclusion: A kind of loratidine oral fast disintegrating and releasing film was successfully prepared in this essay,which provided fundamental basis for future research and development.