熔融造粒法制备拉莫三嗪消味咀嚼分散片的设计与评价

P. P. Amrutkar, S. Patil, Abhijeet N. Todarwal, M. Wagh, P. D. Kothawade, R. K. Surawase
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引用次数: 30

摘要

拉莫三嗪是苯三嗪类抗癫痫药物(AED),与现有的抗癫痫药物在化学上无关。拉莫三嗪也用于治疗抑郁症和双相情感障碍。但它是一种苦味的药物,微溶于水。因此,在进行的工作中,试图掩盖味道,并通过与普瑞罗尔ATO-05络合成咀嚼分散片剂,普瑞罗尔ATO-05也起到掩盖味道的作用。因为,这些片剂可以分散的形式吞下;适合儿科和老年患者的剂型。药物-普瑞罗尔ATO-05分别在药物与普瑞罗尔ATO-05的比例为1:2、1:1.5、1:1、1:0.5的条件下制备。对制备的片剂进行了总体外观、含量均匀性、硬度、脆性、口感评价、口感、体外崩解时间、体外溶出度等评价。普瑞罗尔ATO-05片具有良好的崩解特性,分散体无苦味,说明普瑞罗尔ATO-05具有作为味掩蔽剂的能力。几乎90%以上的药物在1小时内从配方中释放出来。进一步的配方在25±5oC/60±5%RH的温度下进行了3个月的稳定性测试;30±5oC/65±5%RH和40±5oC/75±5%RH。片剂在味道、崩解和溶出度方面没有明显的变化。关键词:拉莫三嗪;熔体造粒;Precirol;味道掩盖;咀嚼分散片。
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Design and evaluation of taste masked chewable dispersible tablet of lamotrigine by melt granulation
Lamotrigine, an antiepileptic drug (AED) of the phenyltriazine class, is chemically unrelated to existing antiepileptic drugs. Lamotrigine is also used in the treatment of depression and bipolar disorder. But it is a bitter drug and slightly soluble in water. Thus, in the work under taken, an attempt was made to mask the taste and to formulate into a chewable dispersible tablet by complexation with Precirol ATO-05, which also acts as taste masking agent. Since, these tablets can be swallowed in the form of dispersion; it is suitable dosage form for paediatric and geriatric patients. Drug-Precirol ATO-05 was prepared in drug to Precirol ATO-05 ratio of 1:2, 1:1.5, 1:1, 1:0.5. The prepared tablets were evaluated for general appearance, content uniformity, hardness, friability, taste evaluation, mouth feel, in vitro disintegration time, and in vitro dissolution studies. Tablets with Precirol ATO-05 have shown good disintegrating features, also, the dispersion not showing any bitter taste, indicate the capability of Precirol ATO-05 used, both as taste masking agents. Almost more than 90 percent of drug was released from the formulation within 1 h. Further formulations were subjected to stability testing for 3 months at temperatures 25±5oC/60±5%RH; 30±5oC/65±5%RH and 40±5oC/75±5%RH. Tablets have shown no appreciable changes with respect to taste, disintegration, and dissolution profiles. Keywords: Lamotrigine; Melt granulation; Precirol; Taste masking; Chewable dispersible tablets.
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