Aman W, Thoma K
Department of Pharmaceutical Technology, Ludwig-Maximilians-University Munich, Germany.
Pharmazie. 2003 Sep;58(9):645-50.
Nifedipine and molsidomine tablets are extremely photolabile drug preparations, even at cool room light. Compared to solutions the light spectrum responsible for photodegradation is moved towards the long-wavelength range corresponding to the bathochromic shift of light absorption in the solid state. In the case of nifedipine tablets light up to 500 nm, especially the range between 400-420 nm, is degrading. Molsidomine tablets are affected only by ultraviolet light, but not by visible light. In both cases light penetrates less than 1 mm into the tablets. For nifedipine tablets the exact penetration depth could be determined due to the discolouration of the drug substance upon irradiation. It varied from 360 microm to 880 microm depending on the drug content. Since the decomposition products of nifedipine act as photostabilizers by spectral overlay, light penetration and photodegradation in nifedipine tablets are limited. The formation of gaseous and liquid decomposition products in molsidomine tablets enhances photodegradation. Changes of the tablet structure as well as dissolution and migration processes are discussed. Furthermore the degradation products donot photostabilize the drug substance due to the missing light absorption above 300 nm.
硝苯地平和莫索尼定片是极易发生光降解的药物制剂,即使在室内凉爽的光线条件下也是如此。与溶液相比,导致光降解的光谱向长波长范围移动,这与固态下光吸收的红移相对应。就硝苯地平片而言,波长高达500nm的光,尤其是400 - 420nm之间的范围,会导致其降解。莫索尼定片仅受紫外光影响,不受可见光影响。在这两种情况下,光线穿透片剂的深度均小于1mm。对于硝苯地平片,由于药物在光照下变色,因此可以确定其确切的穿透深度。根据药物含量不同,穿透深度在360微米至880微米之间变化。由于硝苯地平的分解产物通过光谱叠加起到光稳定剂的作用,因此硝苯地平片中的光穿透和光降解受到限制。莫索尼定片中气态和液态分解产物的形成会增强光降解。文中还讨论了片剂结构的变化以及溶解和迁移过程。此外,由于在300nm以上没有光吸收,降解产物不会使药物物质光稳定。