OBJECTIVE: To prepare the inclusion compound of diclofenac sodium (DFS)-β-cyclodextrin (β-CD) and investigate its properties. METHOD: The inclusion compound of DFS-β-CD was prepared by the co-precipitation method. RESULTS: The inclusion compound of DFS-β-CD was confirmed by UV absorption spectrum, IR absorption spectroscopy, differential scanning calorimetry (DSC) and phase solubility diagram. Meanwhile, the content analysis of the inclusion compound showed that the molecular ratio of DFS to β-CD was 1∶1. CONCLUSION: The soluability and dissolution rate of DFS were increased and its irritation to stomach was reduced when the drug was included by β-CD.

The pharmacodynamics of prostaglandin E1 (PGE1) administered by different routes to rats was investigated in this paper. The hypotensive effect of PGE1 was used as an index of drug efficacy, pharmacodynamic parameters such as time to reach peak effect (Tmax), maximal percentage of blood pressure decrease (Emax, %), duration of effect (Td), and the area determined after PGE1 given to rats intranasally, sublingually, intraperitoneally (ip),and intramuscularly (im), separately, and compared with those obtained from intravenous (iv) administration. Similar to iv route, the pharmacodynamic parameters of PGE1 from the other administration routes, Emax, Td and in particular AUC values were all increased with increasing doses, showing dose-efficacy relationship. Tmax was found to be approximately 3-4 min for nasal route, 3-8 min for im, 6-8 min for ip and 12-30 min for sublingual route, separately. Thus, the order of magnitude of absorption rate of the drug was as follows: nasal≈im＞ip＞sublingual. If the pharmacological bioavailability (PF) for each administration route was used as a tentative measure of drug absorption extent, the order of magnitude of absolute bioavailability appeared as follows: nasal＞im≈ip＞sublingual. Furthermore, the interindividual difference was found to be larger for im and ip route than that for nasal and sublingual route. These results indicate nasal and sublingual routes are two promising routes for the systemic delivery of PGE1 in clinical applications.