Al Hujran Tayel A, Magharbeh Mousa K, Al-Gharabli Samer, Haddadin Rula R, Al Soub Manal N, Tawfeek Hesham M
The Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Mutah University, Al-Karak 61710, Jordan.
Pharmaceutical and Chemical Engineering Department, School of Applied Medical Sciences, German Jordanian University, Amman 11118, Jordan.
Pharmaceutics. 2021 Jun 30;13(7):994. doi: 10.3390/pharmaceutics13070994.
The interaction between meloxicam and sulfonatocalix [4] naphthalene was investigated to improve the meloxicam solubility and its dissolution performance. Solubility behavior was investigated in distilled water (DW) and at different pH conditions. Besides, solid systems were prepared in a 1:1 molar ratio using coevaporate, kneading, and simple physical mixture techniques. Further, they were characterized by PXRD, FT-IR, DCS, and TGA. In vitro dissolution rate for coevaporate, kneaded, and physical mixture powders were also investigated. Solubility study revealed that meloxicam solubility significantly increased about 23.99 folds at phosphate buffer of pH 7.4 in the presence of sulfonatocalix [4] naphthalene. The solubility phase diagram was classified as A type, indicating the formation of 1:1 stoichiometric inclusion complex. PXRD, FT-IR, DCS, and TGA pointed out the formation of an inclusion complex between meloxicam and sulfonatocalix [4] naphthalene solid powders prepared using coevaporate technique. In addition, in vitro meloxicam dissolution studies revealed an improvement of the drug dissolution rate. Furthermore, a significantly higher drug release ( ≤ 0.05) and a complete dissolution was achieved during the first 10 min compared with the other solid powders and commercial meloxicam product. The coevaporate product has the highest increasing dissolution fold and RDR in the investigated media, with average values ranging from 5.4-65.28 folds and 7.3-90.7, respectively. In conclusion, sulfonatocalix [4] naphthalene is a promising host carrier for enhancing the solubility and dissolution performance of meloxicam with an anticipated enhanced bioavailability and fast action for acute and chronic pain disorders.
研究了美洛昔康与磺化杯[4]萘之间的相互作用，以提高美洛昔康的溶解度及其溶解性能。在蒸馏水（DW）和不同pH条件下研究了其溶解行为。此外，采用共蒸发、捏合和简单物理混合技术，以1:1的摩尔比制备了固体体系。此外，还通过粉末X射线衍射（PXRD）、傅里叶变换红外光谱（FT-IR）、差示扫描量热法（DCS）和热重分析法（TGA）对其进行了表征。还研究了共蒸发、捏合和物理混合粉末的体外溶出速率。溶解度研究表明，在pH 7.4的磷酸盐缓冲液中，存在磺化杯[4]萘时，美洛昔康的溶解度显著增加了约23.99倍。溶解度相图被归类为A型，表明形成了1:1化学计量比的包合物。PXRD、FT-IR、DCS和TGA表明，采用共蒸发技术制备的美洛昔康与磺化杯[4]萘固体粉末之间形成了包合物。此外，美洛昔康的体外溶出研究表明药物溶出速率有所提高。此外，与其他固体粉末和市售美洛昔康产品相比，在前10分钟内实现了显著更高的药物释放（≤0.05）和完全溶解。在所研究的介质中，共蒸发产物具有最高的溶出倍数增加和相对溶出度（RDR），平均值分别为5.4-65.28倍和7.3-90.7。总之，磺化杯[4]萘是一种很有前景的主体载体，可提高美洛昔康的溶解度和溶解性能，预期可提高生物利用度，并对急慢性疼痛疾病有快速作用。
