Experimental Elucidation of Templated Crystallization and Secondary Processing of Peptides.

Experimental Elucidation of Templated Crystallization and Secondary Processing of Peptides.
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DOI:
10.3390/pharmaceutics15041288
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发表时间:
2023-04-20
期刊:
影响因子:
5.4
通讯作者:
Heng JYY
Heng JYY
中科院分区:
医学2区
文献类型:
--
作者:
Verma V;Bade I;Karde V;Heng JYY

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多肽的结晶为提纯过程提供了一种可持续且廉价的替代方法。在本研究中,二甘氨酸在多孔二氧化硅中结晶,显示了多孔模板的积极但区分作用。在孔径分别为6 nm和10 nm的二氧化硅存在下,二甘氨酸的诱导时间分别减少了5倍和3倍。二甘氨酸诱导时间与二氧化硅孔径大小有直接关系。在多孔二氧化硅的存在下,二甘氨酸的稳定形式(α形式)被结晶,得到的二甘氨酸晶体与二氧化硅颗粒相结合。此外,我们还研究了双甘氨酸片的机械性能,包括可压性、可成型性和可压性。即使片剂中存在二甘氨酸晶体,其力学性能也与纯MCC相似。透析膜对片剂的扩散研究表明,双甘氨酸在透析膜中有较长时间的释放,证实了多肽晶体可用于口服制剂。因此,多肽的结晶保留了它们的机械和药理性质。更多关于不同多肽的数据可以帮助我们比平时更快地生产口服配方多肽。
The crystallization of peptides offers a sustainable and inexpensive alternative to the purification process. In this study, diglycine was crystallised in porous silica, showing the porous templates’ positive yet discriminating effect. The diglycine induction time was reduced by five-fold and three-fold upon crystallising in the presence of silica with pore sizes of 6 nm and 10 nm, respectively. The diglycine induction time had a direct relationship with the silica pore size. The stable form (α-form) of diglycine was crystallised in the presence of porous silica, with the diglycine crystals obtained associated with the silica particles. Further, we studied the mechanical properties of diglycine tablets for their tabletability, compactability, and compressibility. The mechanical properties of the diglycine tablets were similar to those of pure MCC, even with the presence of diglycine crystals in the tablets. The diffusion studies of the tablets using the dialysis membrane presented an extended release of diglycine through the dialysis membrane, confirming that the peptide crystal can be used for oral formulation. Hence, the crystallization of peptides preserved their mechanical and pharmacological properties. More data on different peptides can help us produce oral formulation peptides faster than usual.
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