Preparation, Identification And Evaluation Of Retinamidoester/HP-β-CD Inclusion Complex

Retinamidoester chemical name: N-4-ethoxycarbonylphenyl retinamideis, Yellow crystalline powder, is an usual medicine for acne and related dermatoses, also have some role in prevention and treatment of cancer,but its solubility and stability are not favourable for clinical use. In this work, Retinamidoester/hydroxypropyl-β-cyclodextrin inclusion complex and its inclusion capsules have been prepared and the character of inclusion capsules and normal market capsules was also compared.(1)Study on retinamidoester/HP-β-CD inclusion:kneaded and ultrasonic systems were applied for the preparation of retinamidoester/HP-β-CD complexes, and the latter resulted in more suitable for our experiment. The orthogonalexperimental design was adopted in the determination of inclusion procedure, and prepared inclusion under the best parameters.(2)Analysis of retinamidoester/HP-β-CD inclusion complex: FT-IR ,X-raydiffraction analysis and Differential Scanning Calorimetry were used to analysis the retinamidoester/HP-β-CD inclusion complex. Ultraviolet spectra were used to determine whether the retinamidoester was in retinamidoester/HP-β-CD inclusion complex and the stability of the complex. The results are as follows: retinamidoester/HP-β-CD was a new substance different from retinamidoester and HP-β-CD. The encapsulation of retinamidoester was about 70.18% and the load of retinamidoester in the inclusion complex was about 9.66%, which approximated to thetheoretical values and the calculated values by XRD quantificational analysis. Compared to the material drug of etinamidoester, the stability and dissolution of retinamidoester/HP-β-CD inclusion complex were both improved, and they meet the requirements of new drugs in pharmacopeias quite well.(3)Preparation of inclusion capsules:As the referenced prescription design discribed, inclusion capsules were prepared; compared with normal market capsules,the solubility of inclusion capsules is increased about 20% to that drugs.In our study, orthogonal design was applied for optimizing preparition process: change of the ingredients of Retinamidoester before and after included by hydroxypropyl-β-cyclodextrin were also investigated. In conclusion, HP-β-CD is an ideal solubilizer for poorly water soluble drugs.The solubility and dissolution of retinamidoester were greatly improved by HP-β-CD.