Irie T, Uekama K
J Pharmacobiodyn. 1985 Sep;8(9):788-91. doi: 10.1248/bpb1978.8.788.
The efficacy of three types of cyclodextrins (CyDs) to reduce skin irritation in guinea pigs caused by photoirradiated chlorpromazine (CPZ) was in the order of beta-greater than gamma-much greater than alpha-CyD, depending upon the magnitude of the stability constant of the CPZ-CyD complexes. The inhibitory effects of CyDs may be attributable to the alteration in the photochemical reactivity of CPZ through inclusion complexation. By the photoirradiation of CPZ in the presence of CyDs, promazine, which is less toxic than CPZ, was produced and the yield decreased in the order of beta-greater than gamma-much greater than alpha-CyD. These results clearly indicate that beta-CyD complexation is particularly useful to reduce the CPZ-photosensitized damage to skin.
三种环糊精(CyDs)减轻豚鼠因光照射氯丙嗪(CPZ)引起的皮肤刺激的功效顺序为β-环糊精>γ-环糊精>α-环糊精,这取决于CPZ-CyD复合物稳定常数的大小。环糊精的抑制作用可能归因于通过包合络合作用改变了CPZ的光化学反应性。在环糊精存在下对CPZ进行光照射时,会产生毒性比CPZ小的丙嗪,其产率顺序为β-环糊精>γ-环糊精>α-环糊精。这些结果清楚地表明,β-环糊精络合对于减少CPZ对皮肤的光致敏损伤特别有用。