Rehman Attaur, Bushra Rabia, Beg Anwar Ejaz, Ali Huma, Zafar Farya, Ashfaq Maria, Alam Shazia, Mustapha Omer, Shafique Shumaila
Department of Pharmaceutics, Faculty of Pharmacy, Ziauddin University, Karachi, Pakistan.
Department of Pharmaceutics, Dow College of Pharmacy, Dow University of Health Sciences, Karachi, Pakistan.
Pak J Pharm Sci. 2018 Mar;31(2(Suppl.)):643-650.
The initiation of newer techniques and development of mouth dissolving (MD) products has created new avenues of higher patients' compliance. MD formulations are actually lessen the difficulties associated with solid swallowing with better bioavailability of especially poorly soluble drugs. In the current study mouth dissolving tablet (MDT) formulations of cinitapride (1 mg) were prepared by direct compression method using various proportion and combination of superdisintegrants. Nine formulations in three batches were compressed by incorporating low (2%), intermediate (6%) and higher (10%) levels of crospovidone, croscarmellose sodium, sodium starch glycolate. Micromeritic assessment of the powder blends were carried out and were found within the acceptable official limits. All newly developed trial formulations were exposed to different pharmacopoeial and non-pharmacopoeial testing. It was found that FC2 trial tablets containing polyplasdone XL® (crospovidone) at level of 6% (4.5 mg) presented the best physico-chemical attributes deemed to be desirable for the ODT products. Disintegration and wetting time of optimized FC2 was computed between 15-17 and 12-15 seconds respectively. The assay and content uniformity of FC2 were estimated to be 100.02±0.36 and 99.66±1.70 percent correspondingly. On the basis of the findings it was concluded that MDT could be successfully developed by incorporating appropriate concentration of superdisintegrant and their combinations.
更新技术的引入以及口腔崩解（MD）产品的开发为提高患者依从性开辟了新途径。MD制剂实际上减少了与固体吞咽相关的困难，尤其是对于难溶性药物具有更好的生物利用度。在本研究中，使用各种比例和组合的超级崩解剂通过直接压片法制备了西沙必利（1毫克）口腔崩解片（MDT）制剂。通过加入低（2%）、中（6%）和高（10%）水平的交联聚维酮、交联羧甲基纤维素钠、淀粉乙醇酸钠，分三批压制了九种制剂。对粉末混合物进行了粉体学评估，发现其在可接受的官方限度内。所有新开发的试验制剂都进行了不同的药典和非药典测试。结果发现，含有6%（4.5毫克）水平的聚维酮XL®（交联聚维酮）的FC2试验片具有ODT产品所需的最佳理化特性。优化后的FC2的崩解时间和湿润时间分别计算为15 - 17秒和12 - 15秒。FC2的含量测定和含量均匀度估计分别为100.02±0.36%和99.66±1.70%。基于这些发现得出结论，通过加入适当浓度的超级崩解剂及其组合可以成功开发MDT。
