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Co-amorphous Form of Curcumin–Folic Acid Dihydrate with Increased Dissolution Rate
Crystal Growth & Design ( IF 3.2 ) Pub Date : 2017-10-26 00:00:00 , DOI: 10.1021/acs.cgd.7b00947 Jenna Marie Skieneh 1 , Indumathi Sathisaran , Sameer Vishvanath Dalvi , Sohrab Rohani 1
Crystal Growth & Design ( IF 3.2 ) Pub Date : 2017-10-26 00:00:00 , DOI: 10.1021/acs.cgd.7b00947 Jenna Marie Skieneh 1 , Indumathi Sathisaran , Sameer Vishvanath Dalvi , Sohrab Rohani 1
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Curcumin is a naturally occurring compound derived from turmeric. Despite its many medicinal properties, such as being an antioxidant, anti-inflammatory, tumor reducer, etc., applications of curcumin are restricted due to its low aqueous solubility and consequently its poor bioavailability. By converting the solid state of poorly water-soluble active pharmaceutical ingredients to coamorphous mixtures, solvates, cocrystals, and eutectics, the solubility can be significantly improved. In this study, U. S. Food and Drug Administration approved excipients were screened for their ability to form novel solid states with curcumin to increase its aqueous solubility. Excipients were screened based on their molecular complementarity with curcumin, using Mercury software. Folic acid dihydrate (FAD), suberic acid, and dextrose are the three coformers that are investigated in this study. It was found that a coamorphous mixture can be formed between curcumin and FAD. FAD has potential as a prenatal or a women’s health drug due to its use in pre-eclampsia and ovarian cancer treatments. This mixture was found to have an increased dissolution rate when compared with curcumin. After 1 h, 175 mg/L of curcumin was dissolved from the coamorphous mixture, while only 45 mg/L was dissolved from curcumin Form I. The coamorphous mixture is stable as it was shown to keep its amorphous behavior after 24 h in solution at elevated temperatures. Curcumin formed a eutectic with suberic acid at a mole fraction of 0.2, whereas it remained as a physical mixture with dextrose. Also, solution crystallization of curcumin with dextrose at a mole fraction of 0.5 resulted into a form II curcumin polymorph.
中文翻译：
姜黄素-叶酸二水合物的共非晶形式，溶解速率增加
姜黄素是衍生自姜黄的天然化合物。尽管姜黄素具有许多医学特性，例如是抗氧化剂，消炎药，肿瘤减少剂等，但姜黄素的水溶性低，因此其生物利用度差，限制了姜黄素的应用。通过将水溶性差的活性药物成分的固态转变为共晶混合物，溶剂化物，共晶体和低共熔混合物，可以显着提高溶解度。在这项研究中，筛选了美国食品和药物管理局批准的赋形剂，其与姜黄素形成新型固态以增加其水溶性的能力。使用Mercury软件根据与姜黄素的分子互补性筛选赋形剂。叶酸二水合物（FAD），辛二酸，右旋糖和右旋糖是本研究中研究的三种共形成物。发现在姜黄素和FAD之间可以形成共晶混合物。由于FAD可用于先兆子痫和卵巢癌治疗，因此具有产前或妇女保健药的潜力。与姜黄素相比，发现该混合物具有增加的溶出速率。1小时后，从无定形混合物中溶解了175 mg / L姜黄素，而从形式I的姜黄素中仅溶解了45 mg / L。该无定形混合物是稳定的，因为它在24 h的溶液中保持其无定形行为。高温。姜黄素与辛二酸以0.2的摩尔分数形成低共熔物，而与葡萄糖形成物理混合物。同样，姜黄素与葡萄糖以0的摩尔分数进行溶液结晶。
更新日期：2017-10-27
中文翻译：
姜黄素-叶酸二水合物的共非晶形式，溶解速率增加
姜黄素是衍生自姜黄的天然化合物。尽管姜黄素具有许多医学特性，例如是抗氧化剂，消炎药，肿瘤减少剂等，但姜黄素的水溶性低，因此其生物利用度差，限制了姜黄素的应用。通过将水溶性差的活性药物成分的固态转变为共晶混合物，溶剂化物，共晶体和低共熔混合物，可以显着提高溶解度。在这项研究中，筛选了美国食品和药物管理局批准的赋形剂，其与姜黄素形成新型固态以增加其水溶性的能力。使用Mercury软件根据与姜黄素的分子互补性筛选赋形剂。叶酸二水合物（FAD），辛二酸，右旋糖和右旋糖是本研究中研究的三种共形成物。发现在姜黄素和FAD之间可以形成共晶混合物。由于FAD可用于先兆子痫和卵巢癌治疗，因此具有产前或妇女保健药的潜力。与姜黄素相比，发现该混合物具有增加的溶出速率。1小时后，从无定形混合物中溶解了175 mg / L姜黄素，而从形式I的姜黄素中仅溶解了45 mg / L。该无定形混合物是稳定的，因为它在24 h的溶液中保持其无定形行为。高温。姜黄素与辛二酸以0.2的摩尔分数形成低共熔物，而与葡萄糖形成物理混合物。同样，姜黄素与葡萄糖以0的摩尔分数进行溶液结晶。
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