Study on Drug Release from 25 Products of NSAIDs for External Use (4 Components) Using the Franz Diffusion Cell / 医薬品情報学

Objective: An evaluation index for drug release was measured in 25 currently used non‐steroidal anti‐inflammatory drugs (NSAIDs) for external use (4 components: indomethacin, diclofenac sodium, ketoprofen, and suprofen).Methods: All release tests were performed using the Franz diffusion cell with phosphate buffered saline (PBS) as the receptor phase and an artificial membrane to maintain uniform measurement conditions.　The receptor phase was collected over time and measured using high performance liquid chromatography (HPLC) to calculate the release rate.　The measurement time points were set over 0-4 h based on clinical use.　Furthermore, the additives were compared among the products.Results: The release profile of diclofenac sodium was similar among all 8 products.　On the other hand, the release rate of IN‐E (15.0% after 4 h) from indomethacin was higher than that from the other 6 products (6.2-9.1% after 4 h).　The release rate of KE‐D (39.2% after 4 h) from ketoprofen was higher than that from the cream, KE‐C (30.6 % after 4 h).　For suprofen, the release rate of SU‐E from the cream (18.1% after 4 h) was 1.6-1.7‐times higher than that of the other 2 products (10.9-11.3 %).　No release was detected from 3 suprofen ointments.Conclusion: Differences in the additives may have been a cause of the observed differences in release over 0-4 h.　This study may serve as a useful index for pharmacists to propose and select appropriate drugs.

The Role of Prostaglandins in Surgically Induced Miosis

In cataract surgery, the surgically induced miosis complicate the removal of lens materials and implantation of a posterior chamber intraocular lens, which increase the risk of ocular trauma and its associated complication. The refore maintenance of mydriasis during cataract syrgery makes the operation easier and brings a good results. This study was performed in rabbit and human eyes to assess the role of the prostaglandins in surgically induced miosis by observing the reduction of pupillary constriction and by measuring the amount of prostaglandins in aqueous humor when the 1.0% suprofen, cyclo-oxygenase inhibitor, was used, and to assess the effect of suprofen in intraocular pressure. In the results, suprofen inhibits syrgically induced miosis (p value: <0.01, human <0.01) without intraocular pressure change, and for this miosis, prostaglans and for this miosis, prostaglandins are at least partially responsible.

Inhibition of the Apraclonidine induced Reduction of Intraocular Presure by Topical Suprofen in Normal Human Eyes

We studied the effect of prostaglandin synthesis inhibitor on the ocular hypotensive action of apraclonidine in a prospective, double-masked study. Twenty normal volunteers were studied. Suprofen, cyclooxygenase;nhibitor and apraclonidine were applied to one eye, and normal saline and apraclonidine to the other eye. Intraocular pressure(IOP) was then measured hourly in both eyes for 7 hours. The results showed significant reduction in mean IOP of both eyes one hour after apraclonidine application. The differences of IOP between the suprofen-treated eyes and control eyes were significant at 2 hours following treatment(p<0.05), reached maximum at 3 to 4 hours(p<0.01) and lasted until 7 hours(p<0.05). In suprofentreated eyes, there was less reduction of mean IOP than in control eyes. These results suggest that this reduction of IOP is at least in part mediated by prostaglandins or other cyclooxygenase products, since suprofen inhibits the ocular hypotensive effect of topically applied apraclonidine.