The aim of the present research work was to explore the impact of ibuprofen-captisol® (sulfobutylether sodium salt of β-CD) inclusion complexes on in vitro dissolution performance. Phase solubility studies of ibuprofen using the carrier captisol® had generated A_L-type profiles which indicated the formation of 1:1 stoichiometric inclusion complexes. The study revealed that more stable complexes of ibuprofen-captisol® were formed in double distilled water compared to phosphate buffer (pH 7.2) as more fraction of the drug is in un-ionized form. Ibuprofen-captisol® complexes were prepared by (i) kneading and (ii) freeze-drying technique with the various drug-carrier ratio (1:1, 1:3 and 1:5 w/w). Complex formation was explained on the basis of physical mixtures (PMs) of identical compositions. Fourier transform infrared spectroscopy (FT-IR), Differential scanning calorimetry (DSC), X-ray powder diffractometry (XRPD), Scanning electron microscope (SEM) and Molecular docking studies were carried out to establish the inclusion complexation. Molecular docking confirmed the possibility of forming a complex between drug and polymer, and it was evident from the energy-minimized structure of the drug-polymer complex. Minimization of energy suggested the formation of a stable drug-polymer complex with binding energy of (−) 3.6 kcal mol⁻¹. The negative docking energy of the complex formation justifies the reason of its solubility enhancement. The complexes prepared by freeze-drying technique were found to be superior in the enhancement of in vitro dissolution rate of ibuprofen when compared to that of complexes prepared by kneading technique.

本研究工作的目的是探讨布洛芬-captisol®（β-CD的磺丁基醚钠盐）包合物对体外溶出性能的影响。使用载体captisol®进行布洛芬的相溶性研究已产生A _L-型谱，其表明形成了1：1化学计量的包合物。该研究表明，与磷酸盐缓冲液（pH 7.2）相比，双倍蒸馏水中形成了更稳定的布洛芬-captisol®复合物，因为该药物的更多部分呈非电离形式。布洛芬-captisol®复合物是通过（i）捏合和（ii）冷冻干燥技术以各种药物-载体比（1：1、1：3和1：5 w / w）制备的。根据相同组成的物理混合物（PM）解释了复合物的形成。进行了傅里叶变换红外光谱（FT-IR），差示扫描量热法（DSC），X射线粉末衍射法（XRPD），扫描电子显微镜（SEM）和分子对接研究以建立夹杂物络合。分子对接证实了在药物和聚合物之间形成复合物的可能性，这从药物-聚合物复合物的能量最小化结构中可以明显看出。能量最小化表明形成稳定的药物-聚合物复合物，其结合能为（-）3.6 kcal mol^-1。配合物形成的负对接能证明了其溶解度提高的原因。与通过捏合技术制备的复合物相比，发现通过冷冻干燥技术制备的复合物在提高布洛芬的体外溶出速率方面具有优越性。