Jones R C, Datko L J
Agents Actions. 1977 Dec;7(5-6):555-62. doi: 10.1007/BF02111129.
Eleven compounds, within hollow capsules of polydimethylsiloxane (Silastic), have been studied with regard to their rate of release and anti-inflammatory activity in the Adjuvant Arthritic (AA) rat. All of the compounds diffused through the capsule wall to some extent with cortisone acetate exhibiting the slowest and ibuprofen the fastest release rate. Of the eleven encapsulated compounds, only phenylbutazone, indomethacin, ibuprofen and naproxen significantly reduced right and left paw volume below that of control value. Silastic encapsulation increases efficacy of phenylbutazone and indomethacin two to three times over subcutaneous or oral administration. Based on potency and duration of constant release, indomethacin and naproxen should exhibit anti-inflammatory activity in excess of 12 months.
研究了聚二甲基硅氧烷（硅橡胶）空心胶囊内的11种化合物在佐剂性关节炎（AA）大鼠中的释放速率和抗炎活性。所有化合物都能在一定程度上透过胶囊壁扩散，其中醋酸可的松的释放速率最慢，布洛芬的释放速率最快。在这11种包封化合物中，只有保泰松、吲哚美辛、布洛芬和萘普生能使左右爪体积显著低于对照值。与皮下或口服给药相比，硅橡胶包封使保泰松和吲哚美辛的疗效提高了两到三倍。基于恒定释放的效力和持续时间，吲哚美辛和萘普生的抗炎活性应超过12个月。
