Kaur Amanpreet, Parmar Prashantkumar Khodabhai, Bansal Arvind Kumar
Solid State Pharmaceutics Lab, Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Sector-67, S.A.S Nagar, Mohali, Punjab-160062, India.
Pharmaceutics. 2019 Oct 7;11(10):516. doi: 10.3390/pharmaceutics11100516.
Celecoxib (CEL) Nanocrystalline Solid Dispersion (CEL_NCSD) was generated by spray drying CEL, mannitol (MAN) and sodium lauryl sulfate (SLS) from a solvent mixture of methanol, acetone and water. The purpose of the work was to determine the size of CEL nanocrystals, investigate agglomeration and inspect dissolution of CEL_NCSD. Size determination was challenging as CEL nanocrystals are embedded in the matrix of MAN. Firstly, neat CEL_NCSD was analyzed using Scherrer equation. Secondly, MAN was dissolved in an aqueous stabilizer medium to selectively measure the size of CEL nanocrystals. Raman Spectra captured in Morphologi G3-ID confirmed the presence of CEL-only particles in the media. This dispersion gave D values of 882 ± 170.34 nm in Zetasizer. Discriminatory dissolution studies confirmed total release of 34.61 ± 1.59%, 47.42 ± 0.24%, and 44.61 ± 1.11% at 120 min from a microsuspension (size 3 µm), a nanosuspension (media milled; size 660 nm) and CEL_NCSD, respectively. The dissolution profile of CEL_NCSD was similar to that of a nanosuspension (f2 72.24) instead of a coarse microsuspension. Thus, the present study revealed that optimized sample preparation is critical for the size determination of embedded drug nanocrystals in NCSD. Further, a discriminatory dissolution study substantiated that the size of CEL nanocrystals in CEL_NCSD is well below 1000 nm, thus showing a size-dependent improved dissolution profile.
塞来昔布（CEL）纳米晶固体分散体（CEL_NCSD）是通过将CEL、甘露醇（MAN）和十二烷基硫酸钠（SLS）从甲醇、丙酮和水的混合溶剂中喷雾干燥而制得。该研究的目的是确定CEL纳米晶体的尺寸，研究团聚情况并考察CEL_NCSD的溶出度。由于CEL纳米晶体嵌入在MAN基质中，因此尺寸测定具有挑战性。首先，使用谢乐方程分析纯CEL_NCSD。其次，将MAN溶解在水性稳定剂介质中以选择性地测量CEL纳米晶体的尺寸。在Morphologi G3-ID中采集的拉曼光谱证实了介质中仅存在CEL颗粒。该分散体在Zetasizer中的D值为882±170.34 nm。鉴别溶出度研究证实，在120分钟时，微悬浮液（粒径3 µm）、纳米悬浮液（介质研磨；粒径660 nm）和CEL_NCSD的总释放率分别为34.61±1.59%、47.42±0.24%和44.61±1.11%。CEL_NCSD的溶出曲线与纳米悬浮液的相似（f2 72.24），而不是粗微悬浮液的。因此，本研究表明，优化的样品制备对于确定NCSD中嵌入药物纳米晶体的尺寸至关重要。此外，鉴别溶出度研究证实，CEL_NCSD中CEL纳米晶体的尺寸远低于1000 nm，因此显示出与尺寸相关的改善的溶出曲线。
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