The pharmacological response of an antibiotic depends on the optimum concentration of homogenous solution of the drug and deviation from this may result in major problems with generic and formulation developments of new chemical entities (NCE’s). Further, the introduction of additional new drugs with greater pharmacokinetic activity is limited because of their poor aqueous solubility. In the present work, an attempt has been made to explore the enhancement of solubility and hence the bioavailability or antimicrobial activity of a pharmaceutically significant drug Cefpodoxime acid (CA), a metabolite of third generation cephalosporin antibiotic cefpodoxime proxetil (CP), by the addition of aqueous paracetamol (PA) solution. Ultrasonic investigation has been carried out on the aqueous solutions of PA containing different concentration of CA at ambient and physiological temperatures and at pressure 101.3 kPa. The measured values of ultrasonic velocity, density and dynamic viscosity and the computed acoustical parameters at 303.15 K, 310.15 K and 313.15 K reveal significant intermolecular interactions between unlike drug molecules. The polarizable continuum model (PCM) study for the two drugs in four different solvents is applied in the calculation of free energy of solution (ΔG) which provide valid information regarding the mutual solubility of the two drugs and possible enhancement of bioavailability of CA in presence of PA. Antimicrobial activity of CA in the presence of PA in aqueous medium confirms the improvisation of solubility of CA drug. The data obtained through antimicrobial activity studies support the increased pharmacokinetic activity of CA in the presence of PA in aqueous environment.

中文翻译：

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通过声学、可极化连续介质模型和抗菌活性研究对乙酰氨基酚水溶液增强头孢泊肟酸的溶解度

抗生素的药理反应取决于药物均质溶液的最佳浓度，偏离此浓度可能会导致新化学实体（NCE）的仿制药和制剂开发出现重大问题。此外，由于其水溶性差，具有更大药代动力学活性的其他新药物的引入受到限制。在目前的工作中，我们尝试探索药物重要药物头孢泊肟酸（CA）的溶解度的增强，从而提高其生物利用度或抗菌活性，头孢泊肟酸是第三代头孢菌素抗生素头孢泊肟酯（CP）的代谢物，通过添加对乙酰氨基酚 (PA) 水溶液。在环境温度和生理温度以及101.3 kPa压力下对含有不同浓度CA的PA水溶液进行了超声研究。超声速度、密度和动力粘度的测量值以及在 303.15 K、310.15 K 和 313.15 K 处计算的声学参数揭示了不同药物分子之间显着的分子间相互作用。两种药物在四种不同溶剂中的可极化连续介质模型 (PCM) 研究应用于溶液自由能 (ΔG) 的计算，这提供了有关两种药物相互溶解度的有效信息以及 CA 存在时可能增强的生物利用度宾夕法尼亚州。在水性介质中存在 PA 的情况下，CA 的抗菌活性证实了 CA 药物溶解度的即兴发挥。通过抗菌活性研究获得的数据支持在水环境中存在 PA 的情况下 CA 的药代动力学活性增加。