The Preparation Of Tadalafil Oral Fast Dissolving Films And Pharmacokinetic Study In Beagle Dogs

Oral fast dissolving films is a new type of oral solid quick-released preparation.It is accurate and convenient to take.The drug in the OFDF is absorbed into the body through the oral mucosa,which can take effect quickly,avoid the first pass effect and improve the bioavailability.It is because of these advantages,it get more and more attention from pharmaceutical researchers.Objective To prepare a new oral Fast Dissolving films Preparation of Tadalafil and to evaluate its disintegration time,dissolution and solubility and other related properties.The pharmacokinetic studies were carried out in the Beagle dogs,analysed the dynamic changes of drugs in the body and studied the relevant parameters.Through the comparison of the self-made membrane and the listed products,to evaluate whether the self-made membrane can improve the bioavailability and quick effect.Method Tadalafil was prepared with suitable film-forming material,the disintegration time,appearance,taste and thickness of the film agent were used as the evaluation indexes,to select the best plasticizers,disintegrating agents and their dosages.Preparation of each film contains 5 mg of tadalafil.The blood concentration of tadalafil in beagle dogs was detected by LC-MS/MS.Study on pharmacokinetics of self-made Tadalafil oral Fast Dissolving films and listed products in Beagle Dogs.Results After the study of the physical and chemical properties of the raw materials,the quality standard of oral instant membrane was studied.Finally,the HPMC E5 was selected as the film-forming material;Propylene glycol as the plasticizer;CCMC-NA as the disintegranting agent;mannitol as the sweetener.Successfully established a method for determination of dissolution of tadalafil and content.The result of animal experiment of the self-made membrane and the listed products : T_max were（2.375 + 0.791）h and（1.875 + 0.443）h;C_max were（77.757 + 35.061）ug/L and（76.119 + 30.536）ug/L;AUC_（0-52）were（728.107 + 467.316）ug/L*h and（714.734 + 692.435）ug/L* h.Conclusion This study has successfully prepared a new type of tadalafil oral Fast Dissolving films Preparation,and its quality evaluation index is established.Compared with the the pharmacokinetic parameters of the listed products in beagle dogs,although not to improve the bioavailability and rapid onset,but it provides a scientific basis for the study of tadalafil dosage form,the research is of great significance,for further research.