Abdullahu Bedri, Lajci Azem, Shehu Vehbi, Krasniqi Shaip, Islami Hilmi
Department of Pharmacy, Faculty of Medicine, University of Prishtina, Clinical Centre, Prishtina, Kosovo.
Med Arh. 2010;64(4):196-9.
It is a well-known fact that tablets are the most ordinary medicines in daily practice, which along with capsules represents about 70% of pharmaceutical preparations. Experimenting with paracetamol tablets of 500 mg dose was scope of this study. Study of formulation, preparation, quality control, and follow-up of the paracetamol stability in tablets was conducted. Carefully analyzing the physical--chemical properties of the paracetamol, in particular to the high number of excipients utilized in the preparation of tablets (diluting, connective, analyzing, and lubricant excipients), and by researching an considerable number of bibliographic sources, we have conceived four different formulations of the paracetamol tablets 500 mg. Preparation of tablets was realized by the humid method of granulation. Quality control of the paracetamol tablets was performed by implementing a series of trials and analyses forecasted in latest editions of most recognized pharmacopoeias. From these trials and analyses, we can mention as follows: reactions of identification, diameter, and average mass, time of analysis, velocity of dissolution and determination of 4-aminophenol. Requirements deriving from the abovementioned trials and analyses were accomplished, excluding the velocity of dissolution that was not accomplished in two of the last formulation (3 and 4). Since this trial is very important in regard to the quality of solid pharmaceutical forms, two of the abovementioned formulations are considered as inappropriate to be used in practice. From the four formulations of paracetamol tablets, results shows that 1st and 2nd are most appropriate formulations due to its simplicity in preparation and practice to be produced industrially. Defining of the timely depending content of the paracetamol in tablet was performed by the implementing of two contemporary methods of spectrophotometry in UV zone and chromatography in the liquid phase with high pressure (HPLC). Just as it was expected, results of these analyses showed that acting substance did not incur any alteration during the period of storage and that alterations of the analyses results in between these two methods are almost inconsiderable ones.
片剂是日常医疗实践中最常见的药物，这是一个众所周知的事实，片剂与胶囊剂一起约占药物制剂的70%。本研究的范围是对500毫克剂量的扑热息痛片剂进行试验。开展了扑热息痛片剂的配方、制备、质量控制及稳定性跟踪研究。通过仔细分析扑热息痛的物理化学性质，特别是制备片剂时使用的大量辅料（稀释剂、黏合剂、分析剂和润滑剂辅料），并研究大量文献资料，我们构思了四种不同的500毫克扑热息痛片剂配方。片剂制备采用湿法制粒。扑热息痛片剂的质量控制是通过实施最权威药典最新版本中规定的一系列试验和分析来进行的。从这些试验和分析中，我们可以列举如下：鉴别反应、直径、平均质量、分析时间、溶出速度以及对4-氨基酚的测定。上述试验和分析得出的要求均已达成，但最后两种配方（3号和4号）的溶出速度未达标。由于该试验对固体药物剂型的质量非常重要，上述两种配方被认为不适用于实际应用。从四种扑热息痛片剂配方来看，结果表明1号和2号配方是最合适的，因为它们制备简单且适合工业化生产。通过采用紫外区分光光度法和高压液相色谱法这两种现代方法来测定片剂中扑热息痛随时间变化的含量。正如预期的那样，这些分析结果表明活性物质在储存期间未发生任何变化，并且这两种方法之间分析结果的差异几乎可以忽略不计。
