PDF(Pubmed)
Abstract：
Poorly water-soluble drugs represent a challenge for the pharmaceutical industry because it is necessary to find properly tuned and efficient systems for their release. In this framework, organic-inorganic hybrid systems could represent a promising strategy. A largely diffused inorganic host is hydroxyapatite (HAP, Ca10(PO4)6(OH)2), which is easily synthesized with different external forms and can adsorb different kinds of molecules, thereby allowing rapid drug release. Hybrid nanocomposites of HAP nanorods, obtained through hydrothermal synthesis, were prepared with two model pharmaceutical molecules characterized by low and pH-dependent solubility: meloxicam, a non-steroidal anti-inflammatory drug, and bumetanide, a diuretic drug. Both hybrids were physically and chemically characterized through the combined use of X-ray powder diffraction, scanning electron microscopy with energy-dispersive spectroscopy, differential scanning calorimetry, and infrared spectroscopy measurements. Then, their dissolution profiles and hydrophilicity (contact angles) in different media as well as their solubility were determined and compared to the pure drugs. This hybrid system seems particularly suitable as a drug carrier for bumetanide, as it shows higher drug loading and good dissolution profiles, while is less suitable for meloxicam, an acid molecule.
摘要：
水溶性差的药物代表了制药工业的挑战,因为有必要找到适当调节和有效的释放系统。在这个框架中,有机-无机混合体系可以代表一种有前途的策略。大量扩散的无机主体是羟基磷灰石(HAP，Ca10(PO4)6(OH)2),很容易合成不同的外部形式，可以吸附不同种类的分子，从而允许药物快速释放。HAP纳米棒的杂化纳米复合材料,通过水热合成获得，用两种具有低和pH依赖性溶解度的模型药物分子制备：美洛昔康，一种非甾体抗炎药,和布美他尼,一种利尿药.通过结合使用X射线粉末衍射对两种杂种进行了物理和化学表征，扫描电子显微镜与能量色散谱，差示扫描量热法,和红外光谱测量。然后，测定了它们在不同介质中的溶出曲线和亲水性（接触角）以及它们的溶解度，并与纯药物进行了比较。这种混合系统似乎特别适合作为布美他尼的药物载体，因为它显示出较高的载药量和良好的溶出曲线，虽然不太适合美洛昔康，酸分子.
