Chem. Pharm. Bull., 53(7),811-815, July 2005

Regular Articles

Evaluation of Titanium Dioxide as a Pharmaceutical Excipient for Preformulation of a Photo-Labile Drug: Effect of Physicochemical Properties on the Photostability of Solid-State Nisoldipine


Koichi KAKINOKI,a Kenji YAMANE,a Miho IGARASHI,b Manami YAMAMOTO,b Reiko TERAOKA,b and Yoshihisa MATSUDAb

a Formulation & Industrial Technology Lab., Taiho Pharmaceutical Co., Ltd.; Tokushima 771-0194, Japan: and b Department of Pharmaceutical Technology, Kobe Pharmaceutical University; Higashinada-ku, Kobe 658-8558, Japan. * To whom correspondence should be addressed. e-mail: k-kakinoki@taiho.co.jp

To characterize the photocatalytic activity of TiO2 via solid-state reaction, the relationship between the physicochemical properties and photocatalytic activity of TiO2 was investigated and estimated from the results of photodegradation of nisoldipine. The photodegradation of nisoldipine was significantly enhanced by addition of TiO2. Two degradation products, nitroso-phenylpyridine derivative and nitro-phenylpyridine derivative, were formed. The degree of photocatalytic activity of TiO2 was quite different between the various types of TiO2 investigated, even when the crystalline phase was the same. As a result of the investigations into the relationship between the photocatalytic activity and physicochemical properties of TiO2, it was found that for the rutile form the photocatalytic activity has good correlation with specific surface area of TiO2, but poor correlation with water loss on drying of TiO2. However, for the anatase form, the photocatalytic activity has good correlation with water loss on drying of TiO2, but poor correlation with specific surface area. Moreover, it was found that the crystallinity of TiO2 has a moderate correlation with the photocatalytic activity of both crystal forms of TiO2. These results suggest that a degree of photocatalytic activity of TiO2 depends on the various physicochemical properties of each type of TiO2 investigated.

Key words preformulation; solid-state stability; photostability; titanium dioxide; photocatalytic activity