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用噻吗洛尔滴眼治疗青光眼时,药物的眼吸收量仅为给药剂量的4％左右,全身吸收量却高达70％以上,因此常可引起严重的不良反应,甚至有致死的报告。作者设想用调节噻吗洛尔眼药水的 pH 值,或预先给予肾上腺素滴眼,来达到减少噻吗洛尔的全身吸收量并改善其眼/体吸收比的目的。试验用体重为1.6～3.4kg 的家兔,不拘性别,允许其自由取食和饮水,但饲养条件包括光照、温度、湿度须标准化。试验用肾上腺素滴眼液浓度为20mg/ml,在给予噻吗洛尔滴眼前5min,每次给予50μl 滴眼。噻吗洛尔眼药水含 L-噻吗洛尔顺丁烯二酸盐6.84mg/ml(相当于游离碱5mg/ml),已预先用磷酸盐缓冲剂调 pH 为6.2,6.9或7.5,并加入示踪物(~3H)噻吗洛尔使眼药水的放射活性相当于0.14μCi/μl,每次滴眼剂量25μl。试验用液相闪烁计数器测定各个组织标本的放射活性。结果:随着噻吗洛尔眼药水 pH的增高,噻吗洛尔的眼吸收量和全身吸收量均增高,但眼/体吸收比不变。预先给予肾上腺
Eye drops with timolol treatment of glaucoma, the drug eye absorption is only about 4% of the dose, systemic absorption is as high as 70% or more, it can often cause serious adverse reactions, and even fatal reports. The authors envisaged the goal of reducing the systemic absorption of timolol and improving its ophthalmic / body absorption ratio by adjusting the pH of timolol eye drops or pre-adrenalin eye drops. The rabbits weighing 1.6-3.4 kg were tested for gender and allowed to eat and drink freely. However, breeding conditions including light, temperature and humidity should be standardized. The test epinephrine eye drops concentration of 20mg / ml, given timolol eye drops 5min, each give 50l drops. Timolol Eye Drops contains L-timolol maleate 6.84 mg / ml (equivalent to 5 mg / ml of free base) and has been previously adjusted to pH 6.2, 6.9, or 7.5 with phosphate buffer and The addition of tracer (~ 3H) timolol resulted in an equivalent of 0.14 μCi / μl radioactivity to eyedrops, with 25 μl per eye drop. Test liquid scintillation counter determination of the radioactivity of each tissue sample. RESULTS: With the increase of pH of timolol eyedrops, both eye absorption and systemic absorption of timolol increased, but the ratio of eye / body absorption remained unchanged. Adrenal gland