Pharmaceutical Sciences Graduate Program, College of Pharmacy, Federal University of Rio Grande do Sul (UFRGS), Av. Ipiranga, 2752. Laboratory 402, Santana, Porto Alegre, RS, 90610-000, Brazil.
College of Pharmacy, Federal University of Rio Grande do Sul (UFRGS), Av. Ipiranga 2752, Porto Alegre, RS, Brazil.
AAPS PharmSciTech. 2020 Jul 29;21(6):210. doi: 10.1208/s12249-020-01751-8.
Tizanidine hydrochloride is a centrally acting skeletal muscle relaxant used in the treatment of spasticity. This drug is sold only as tablets or capsules, which highlights the need to develop oral liquid formulations that allow administration to children and adults with impaired swallowing. This study aim was to develop and improve tizanidine hydrochloride liquid formulations from raw material and to evaluate their stability. A stability-indicating high performance liquid chromatography method was validated for two formulations developed. Fifteen formulations were developed containing syrup and fifteen containing sodium carboxymethyl cellulose as vehicles, to select the two most suitable for stability testing. The formulations were prepared in triplicate and placed in amber polyethylene terephthalate and glass bottles, which were stored under three different conditions: at room temperature (15-30°C), under refrigeration (2-8°C), and at 40°C. The physicochemical and microbiological stability of formulations were evaluated, applying high performance liquid chromatography and microbiological count. The studied formulations at 15-30°C, 2-8°C, and 40°C can be used for a period of 70 days, and all parameters are inside of recommended specifications, enough to allow its use in the context for which it was developed, the application in hospital. The formulations developed in this work have simple components to avoid adverse reactions in vulnerable populations. Results of this study could be applied as a reference for hospital use; once it demonstrated the reliability of storage time interval and proper conditions for use.
盐酸替扎尼定是一种中枢作用的骨骼肌松弛剂，用于治疗痉挛。这种药物仅以片剂或胶囊形式销售，这突出表明需要开发口服液体制剂，以便为吞咽功能受损的儿童和成人提供给药途径。本研究旨在开发和改进盐酸替扎尼定的原料药液体制剂，并对其稳定性进行评估。为两种已开发的制剂验证了一种稳定指示的高效液相色谱法。开发了十五种含有糖浆的制剂和十五种含有羧甲基纤维素钠的制剂作为载体，以选择最适合稳定性测试的两种制剂。制剂以三倍量制备，并分别置于琥珀色聚对苯二甲酸乙二醇酯和玻璃瓶中，在三种不同条件下储存：室温（15-30°C）、冷藏（2-8°C）和 40°C。通过高效液相色谱法和微生物计数评估制剂的理化和微生物稳定性。在 15-30°C、2-8°C 和 40°C 下研究的制剂可使用 70 天，所有参数均在推荐规格内，足以允许其在开发的背景下使用，即医院应用。本工作中开发的制剂具有简单的成分，可避免在脆弱人群中发生不良反应。这项研究的结果可作为医院使用的参考；一旦证明了储存时间间隔和使用条件的可靠性。
