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Formation of Indomethacin-Saccharin Cocrystals during Wet Granulation: Role of Polymeric Excipients.
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2019-12-18 , DOI: 10.1021/acs.molpharmaceut.9b01004 Ryoma Tanaka 1 , Naga Kiran Duggirala 1 , Yusuke Hattori , Makoto Otsuka , Raj Suryanarayanan 1
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2019-12-18 , DOI: 10.1021/acs.molpharmaceut.9b01004 Ryoma Tanaka 1 , Naga Kiran Duggirala 1 , Yusuke Hattori , Makoto Otsuka , Raj Suryanarayanan 1
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Formulation of a cocrystal into a solid pharmaceutical dosage form entails numerous processing steps during which there is risk of dissociation. In an effort to reduce the number of unit operations, we have attempted the in situ formation of an indomethacin-saccharin (INDSAC) cocrystal during high-shear wet granulation (HSWG). HSWG of IND (poorly water-soluble drug) and SAC (coformer), with polymers (granulating agents), was carried out using ethanol as the granulation liquid and yielded INDSAC cocrystal granules. Therefore, cocrystal formation and granulation were simultaneously accomplished. Our objectives were to (i) evaluate the influence of polymers on cocrystal formation kinetics during wet granulation and (ii) mechanistically understand the role of polymers in facilitating the cocrystal formation. Polyvinylpyrrolidone (PVP), hydroxypropyl cellulose (HPC), and polyethylene oxide (PEO) were chosen to investigate the influence of soluble polymers. The cocrystal formation kinetics was influenced by the polymer (PVP < HPC < PEO) and its concentration. The interaction of the polymer with cocrystal components inhibited the cocrystal formation. Complete cocrystal formation was observed in the presence of PEO, a polymer which does not interact with IND and SAC.
中文翻译：
湿法制粒过程中消炎痛-糖精共晶体的形成：聚合物赋形剂的作用。
将共晶体配制成固体药物剂型需要许多处理步骤，在此期间存在解离的风险。为了减少单元操作的次数，我们尝试了在高剪切湿法制粒（HSWG）过程中原位形成吲哚美辛-糖精（INDSAC）共晶。使用乙醇作为制粒液，对IND（水溶性差的药物）和聚合物（制粒剂）的SAC进行HSWG，制得INDASC共结晶颗粒。因此，同时完成了共晶的形成和造粒。我们的目标是（i）在湿法制粒过程中评估聚合物对共晶形成动力学的影响，以及（ii）从机械上理解聚合物在促进共晶形成中的作用。聚乙烯吡咯烷酮（PVP），选择羟丙基纤维素（HPC）和聚环氧乙烷（PEO）来研究可溶性聚合物的影响。共晶形成动力学受聚合物（PVP <HPC <PEO）及其浓度影响。聚合物与共晶体组分的相互作用抑制了共晶体的形成。在PEO（一种不与IND和SAC相互作用的聚合物）的存在下，观察到完全共晶形成。
更新日期：2019-12-19
中文翻译：
湿法制粒过程中消炎痛-糖精共晶体的形成：聚合物赋形剂的作用。
将共晶体配制成固体药物剂型需要许多处理步骤，在此期间存在解离的风险。为了减少单元操作的次数，我们尝试了在高剪切湿法制粒（HSWG）过程中原位形成吲哚美辛-糖精（INDSAC）共晶。使用乙醇作为制粒液，对IND（水溶性差的药物）和聚合物（制粒剂）的SAC进行HSWG，制得INDASC共结晶颗粒。因此，同时完成了共晶的形成和造粒。我们的目标是（i）在湿法制粒过程中评估聚合物对共晶形成动力学的影响，以及（ii）从机械上理解聚合物在促进共晶形成中的作用。聚乙烯吡咯烷酮（PVP），选择羟丙基纤维素（HPC）和聚环氧乙烷（PEO）来研究可溶性聚合物的影响。共晶形成动力学受聚合物（PVP <HPC <PEO）及其浓度影响。聚合物与共晶体组分的相互作用抑制了共晶体的形成。在PEO（一种不与IND和SAC相互作用的聚合物）的存在下，观察到完全共晶形成。
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