López Lozano J J, Moreno Cano R
Departamento de Neurología, Clínica Puerta de Hierro, Madrid.
Neurologia. 1995 Apr;10(4):155-8.
Levodopa/inhibitor improves motor function in parkinsonian patients. In its usual tablet form, however, its efficacy is reduced after several years, partially due to absorption deficiencies and changes in plasma kinetics; thus, other therapeutic strategies to provide a stable, easy to prepare formula are being sought. One such approach could be to dissolve L-dopa/carbidopa in ascorbic acid. This report describes the preparation method and demonstrates the stability of the sample using High pressure liquid cromatography (HPLC) with electrochemical detection. Regardless of the number of tablets the patient takes, the concentration of L-dopa/carbidopa/ascorbic acid remains constant (1/0.25/2 mg/ml). Thus, a patient taking 5 tablets of Sinemet Plus a day, would pulverize them in a glass, ceramic or marble mortar and add them to a measuring cup containing a 1 gram tablet of vitamin C (Redoxon) dissolved in 500 cc of cold water. This would be shaken or stirred until the Sinemet powder had dissolved. A few particles remaining in suspension after this process would be of no concern. The liquid would be stored in the refrigerator in an opaque or aluminum foil-covered glass bottle or, if possible, in several small dose-size vials. Using a measuring cup, a test tube and a syringe, the correct volume can be drawn out of the bottle and shaken well before drinking. The solution would be taken at regular intervals throughout the day (which vary from one patient to another) to maintain stable plasma L-dopa levels.
左旋多巴/抑制剂可改善帕金森病患者的运动功能。然而,以其常用片剂形式服用时,几年后其疗效会降低,部分原因是吸收不足和血浆动力学变化;因此,人们正在寻求其他治疗策略来提供一种稳定、易于制备的配方。一种方法可能是将左旋多巴/卡比多巴溶解在抗坏血酸中。本报告描述了制备方法,并使用带电化学检测的高压液相色谱法(HPLC)证明了样品的稳定性。无论患者服用多少片药,左旋多巴/卡比多巴/抗坏血酸的浓度都保持恒定(1/0.25/2毫克/毫升)。因此,一名每天服用5片息宁控释片的患者,可将药片在玻璃、陶瓷或大理石研钵中研碎,然后加入一个量杯中,量杯中有一片1克的维生素C(力度伸)溶解在500毫升冷水中。搅拌或摇动直至息宁粉末溶解。此过程后仍有一些颗粒悬浮并不影响。液体应储存在冰箱中,装在不透明或用铝箔覆盖的玻璃瓶中,或者如果可能的话,装在几个小剂量的小瓶中。使用量杯、试管和注射器,从瓶中取出正确体积的溶液,饮用前充分摇匀。该溶液应在一天中定期服用(不同患者服用时间不同)以维持稳定的血浆左旋多巴水平。