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首页> 外文期刊>Crystal growth & design >Influence of Excipients on Cocrystal Stability and Formation
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Influence of Excipients on Cocrystal Stability and Formation

机译：赋形剂对COCRYSTAL稳定性和形成的影响

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摘要

Cocrystal formation is widely used to modify and optimize the physicochemical properties of an active pharmaceutical ingredient (API). However, the stability of cocrystals toward formulation with excipients is little investigated. In this work, the effect of grinding in the presence of the common excipients polyvinylpyrrolidone (PVP) and microcrystalline cellulose (MCC) on 11 cocrystals and a salt of the sulfonamide diuretic chlorothiazide (ctz) was studied (ctz-bipy, ctz-ebipy, ctz-pbipy, ctz-pyr, ctzhyp, ctz-hma, ctz-bza, ctz-nia, ctz-ina, ctz-cbz, ctz-aca, ctz-ppa, (bzamH(+))(ctz(-)); bipy = 4,4'-bipyridine, ebipy = 1,2-di(4-pyridyl)ethylene, pbipy = 1,3-di(4-pyridyl)propane, pyr = pyrazine, hyp = 2-hydroxypyridine, hma = hexamethylenetetramine, bza = benzamide, nia = nicotinamide, ina = isonicotinamide, cbz = carbamazepine, aca = acetamide, ppa = propionamide, bzamH+ = benzamidinium). Except for ctz-ppa and ctz-aca, all cocrystals were stable toward milling with 1 weight equiv PVP or MCC. It was also shown that the cocrystals ctz-bipy, ctz-ebipy, ctz-pbipy, ctz-pyr, ctz-hma, ctz-bza, ctz-ina, ctz-cbz, and the salt (bzamH+)(ctz-) formed in situ, when ctz was milled with the respective coformer in the presence of PVP or MCC. The stability and formation of ctz-cbz, ctz-nia, and htz-nia (htz = hydrochlorothiazide) toward grinding with a wider range of excipients (HPC, alpha-lactose, deoxycholic acid, and sodium taurocholate) was also investigated, and the results are discussed with regard to the heterosynthons of the ctz cocrystals and competing H bonding with the excipients.
机译：共晶体形成广泛用于改变和优化活性药物成分（API）的物理化学性质。然而，与赋形剂的配方朝向制剂的稳定性很少被研究。在这项工作中，研究了在11个酰胺和微晶纤维素（MCC）的常见赋形剂聚乙烯吡咯烷酮（PVP）和微晶纤维素（MCC）的存在下研磨的影响（CTZ-Bipy，CTZ-Ebipy， CTZ-PBIPY，CTZ-PYR，CTZHYP，CTZ-HMA，CTZ-BZA，CTZ-NIA，CTZ-INA，CTZ-CBZ，CTZ-ACA，CTZ-PPA，（BZAMH（+））（CTZ（ - ）） ; Bipy = 4,4'-Bi0赖丁，EBIPY = 1,2-DI（4-吡啶基）乙烯，PBIPY = 1,3-二（4-吡啶基）丙烷，Pyr =吡嗪，Hyp = 2-羟基吡啶，HMA =六亚甲基丁胺，BZA =苯甲酰胺，NIA =烟酰胺，INA = inICOTINAMIDE，CBZ = CARBAMAZEPINE，ACA =乙酰胺，PPA =丙酰胺，BZAMH + =苯甲酰胺）。除了CTZ-PPA和CTZ-ACA外，所有的COCrystals均稳定，朝向1重量等方面的PVP或MCC磨削。还表明，Cocrystals CTZ-Bipy，CTZ-EBIPY，CTZ-PBIPY，CTZ-PYR，CTZ-HMA，CTZ-BZA，CTZ-INA，CTZ-CBZ和盐（BZAMH +）（CTZ-）形成原位，当CTZ在PVP或MCC的存在下用相应的COFormer铣削时。 CTZ-CBZ，CTZ-NIA和HTZ-NIA（HTZ =氢氯噻嗪）对用更广泛的赋形剂（HPC，α-乳糖，脱氧胆酸和牛磺酸钠）进行研磨的稳定性和形成，并进行了研究，关于CTZ COCRYSTALAL的异质酶和与赋形剂键合的结果讨论了结果。

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