Detail of "64019-93-8"

Reference

Studies on ocular penetration of dipivefrin hydrochloride in rabbit eyes

Studies on ocular penetration of dipivefrin hydrochloride in rabbit eyes. Kito, Hirokazu; Chiba, Takehisa; Hikida, Mitsushi (Res. Lab., Santen Pharm. Co., Ltd., Osaka 533, Japan). Nippon Ganka Kiyo, 37(4), 664-70 (Japanese) 1986. CODEN: NGKYA3. ISSN: 0015-5667. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 2 To clarify the metabolic fate in the eye of dipivefrin-HCl (I) [64019-93-8], a prodrug of epinephrine (EPI) [51-43-4], [7-14C]I and [carboxyl-14C]I were applied topically and their absorption and distribution were investigated in comparison with 14C-labeled epinephrine bitartrate (II) [51-42-3] in rabbits and mice. Radioactive concns. of ocular tissues after [7-14C]I treatment were much higher than those after [7-14C]II treatment (~40-fold in the aq. humor, 10-24-fold in the iris and ciliary body, ~35-fold in the cornea), indicating that I is a useful prodrug which penetrates into intraocular tissues more easily than does EPI. Some differences were noted in distribution of radioactivity between [7-14C]I- and [7-14C]II-treated eyes. [7-14C]I-treated eyes showed high radioactivity in the aq. humor, cornea, and iris-ciliary body, whereas [7-14C]II-treated eyes showed radioactivity in the conjunctiva, corneo-scleral junction, and anterior sclera. The above results suggest that I not only distributes better in anterior ocular tissues than does EPI; it also distributes in intraocular tissues, whereas most EPI distributes only in anterior ocular tissues. The results of TLC in ocular tissues after [7-14C]I treatment suggested that I was hydrolyzed in the ocular tissues to pivalic acid [75-98-9] and EPI. 75-98-9 and 51-42-3 which are cas registry numbers of substances are two of reagents here. The liberated EPI was long maintained in the ocular tissues, esp. in the cornea, iris, and ciliary body. The elimination of [carboxyl-14C]I from ocular tissues after treatment was faster than that of [7-14C]I, which suggests that pivalic acid liberated by the hydrolysis of I is eliminated by ocular tissues faster than is EPI. .