| [OBJECTIVE] To prepare and evaluate budesonide pulsatile release tablets for colon-specific delivery. [METHODS] First, diclofenac sodium was used as model drug, the core tablet was prepared by powder-pressed technique and an outer shell was prepared by the method of spraying-coated. The effects of the amount of disintegrants and drug loaded, core tablet hardness, the composition of the outer shell, the coating weight and the manipulation on the drug release were studied by dissolution test in vitro using lag-time (Tlag) as index, the formulation and preparation process was optimized by the method of Orthogonal design. Then, based on the preliminary experiment above, budesonide pulsatile controllec-release tablets for colon-specific delivery was prepared and a spectrophotometric method for the determination of this preparation was also established. The quality of the preparation was evaluated by means of assay, dissolution test as well as stability test. [RESULTS] It showed that Tlag had a tendency of prolonging while pore-former decreased and the thickness of coating materials increased. The budesonide pulsatile controiled-release tablets for colon-specific delivery with lag time about 5-7 hours could be attained and the aim of targeted-release was satisfied as followings: CMS-Na was used as a preferable disintegrate with a content of 10%, Eudragit L as pore-former with 70% and DPT as plasticizer with 15%, outer coating weight on a range of 6-8% and heat at 40C for 2 hours after coated. This preparation conformed to the quality requirements under Tablets of Appendix I A of Pharmacopoeia of P.R .China (part II ,Edi 2000), that the preparation was unstable to light and heat as well as humidity was also indicated. [CONCLUSIONS] The preparation process of budesonide pulsatile controiled-release tablets for colon-specific delivery was practicable and the drugcould be released in colon as expected. At the same time, the method of qualitycontrol is accurate and credible. |
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