İlaç Ko-Kristallerinin Fiziksel Özelliklerinin Çözünme Konsantrasyonuna Etkisinin Analizi

Sedef hastalığı bulaşıcı olmayan bir deri hastalığıdır. Hastalığın tedavi yöntemi şiddetine göre değişmektedir. Şiddetli evrelerde ağız yolu ile yapılan tedavilerde, çözünme davranışı, ko-kristali değerlendirmek, çözünme mekanizmasını anlamak ve ilacın biyoyararlanımını tahmin etmek için önemli bir karakterizasyon aşamasıdır. Bu çalışmada sedef hastalığının ağız yoluyla tedavisinde kullanılan kokristallerin (i) farklı şekil, (ii) boyutlarının ve (iii) öğütme işleminin çözünme davranışı üzerindeki etkisi ultraviyole-görünür (UV/Vis) spektroskopisi ile analiz edilmiştir. Çözünme konsantrasyonunun değişen fiziksel özellikler ve öğütme işlemi ile birlikte arttığı kanıtlanmıştır.

ANALYSIS OF THE EFFECT OF PHYSICAL PROPERTIES OF DRUG CO-CRYSTALS ON DISSOLUTION CONCENTRATION

Psoriasis is an itchy and non-contagious skin disease. Its treatment method varies according to the severity of the disease. In oral treatments used in heavy stages, dissolution behavior is a vital characterization parameter for evaluating cocrystal, understanding dissolution mechanism, and predicting bioavailability of the drug. In this study, dissolution of cocrystals used in psoriasis was investigated. Effect of (i) different shapes, (ii) sizes, and (iii) grinding of cocrystals on the dissolution were considered with ultraviolet-visible (UV/Vis) spectroscopy. Results show that different physical properties and grinding can significantly increase the dissolution of cocrystals.

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Aakeröy, C. B., & Salmon, D. J. (2005). Building co-crystals with molecular sense and supramolecular sensibility. CrystEngComm, 7(72), 439–448. https://doi.org/10.1039/b505883j
Adhiyaman, R., & Basu, S. K. (2006). Crystal modification of dipyridamole using different solvents and crystallization conditions. International Journal of Pharmaceutics, 321(1–2), 27–34. https://doi.org/10.1016/j.ijpharm.2006.04.021
Blagden, N., de Matas, M., Gavan, P. T., & York, P. (2007). Crystal engineering of active pharmaceutical ingredients to improve solubility and dissolution rates. In Advanced Drug Delivery Reviews. https://doi.org/10.1016/j.addr.2007.05.011
Bolourtchian, N., Nokhodchl, A., & Dinarvand, R. (2001). The effect of solvent and crystallization conditions on habit modification of carbamazepine. DARU Journal of Pharmaceutical Sciences 9(1), 12-22.
Bukovec, P., Meden, A., Smrkolj, M., & Vrečer, F. (2015). Influence of crystal habit on the dissolution of simvastatin single crystals. Acta Chimica Slovenica, 62(4), 958–966. https://doi.org/10.17344/acsi.2015.1849
Chan, E. J., Gao, Q., & Dabros, M. (2014). Understanding the structure details when drying hydrate crystals of pharmaceuticals - Interpretations from diffuse scattering and inter-modulation satellites of a partially dehydrated crystal. Acta Crystallographica Section B: Structural Science, Crystal Engineering and Materials, 70(3), 555–567. https://doi.org/10.1107/S2052520614005125
Değim, Z. (2009). Öğütme. In Modern Farmasötik Teknoloji (1st ed., pp. 3–8). TEB Eczacılık Akademisi. http://e-kutuphane.teb.org.tr/pdf/tebakademi/modern_farmasotk/3.pdf
Dizaj, S. M., Vazifehasl, Z., Salatin, S., Adibkia, K., & Javadzadeh, Y. (2015). Recrystallization of drugs: Effect on dissolution rate. In V. Glebovsky (Ed.), Research in Pharmaceutical Sciences (pp. 191– 211). https://www.intechopen.com/books/recrystallization-in-materials processing/recrystallization-of-drugs-effect-on-dissolution-rate
Gadade, D. D., Pekamwar, S. S., Lahoti, S. R., Patni, S. D., & Sarode, M. C. (2017). Etodolak’ın kokristalizasyonu: Ko-kristalizasyon tahmini, ko-kristal sentezi, katı faz yapı aydınlatma Çalışmaları ve in vitro İlaç salımı. Marmara Pharmaceutical Journal, 21(1), 78–88. https://doi.org/10.12991/marupj.259884
Nokhodchi, A., Bolourtchian, N., & Dinarvand, R. (2003). Crystal modification of phenytoin using different solvents and crystallization conditions. International Journal of Pharmaceutics, 250(1), 85–97. https://doi.org/10.1016/S0378-5173(02)00488-X
Qiao, N., Li, M., Schlindwein, W., Malek, N., Davies, A., & Trappitt, G. (2011). Pharmaceutical cocrystals: An overview. International Journal of Pharmaceutics, 419(1–2), 1–11. https://doi.org/10.1016/j.ijpharm.2011.07.037
Ren, S., Liu, M., Hong, C., Li, G., Sun, J., Wang, J., Zhang, L., & Xie, Y. (2019). The effects of pH, surfactant, ion concentration, coformer, and molecular arrangement on the solubility behavior of myricetin cocrystals. Acta Pharmaceutica Sinica B, 9(1), 59–73. https://doi.org/10.1016/j.apsb.2018.09.008
Renkoğlu, P., Çelebier, M., & Arica, B. (2015). HPLC determination of olanzapine and carbamazepine in their nicotinamide cocrystals and investigation of the dissolution profiles of cocrystal tablet formulations. Pharmaceutical Development and Technology, 20(3), 380–384. https://doi.org/10.3109/10837450.2014.882937
Ross, S. A., Lamprou, D. A., & Douroumis, D. (2016). Engineering and manufacturing of pharmaceutical co-crystals: A review of solvent-free manufacturing technologies. Chemical Communications, 52(57), 8772–8786. https://doi.org/10.1039/c6cc01289b
Schultheiss, N., & Newman, A. (2009). Pharmaceutical cocrystals and their physicochemical properties. Crystal Growth and Design, 9(6), 2950–2967. https://doi.org/10.1021/cg900129f
Serrano, D. R., O’Connell, P., Paluch, K. J., Walsh, D., & Healy, A. M. (2016). Cocrystal habit engineering to improve drug dissolution and alter derived powder properties. Journal of Pharmacy and Pharmacology, 68(5), 665–677. https://doi.org/10.1111/jphp.12476
Shiraki, K., Takata, N., Takano, R., Hayashi, Y., & Terada, K. (2008). Dissolution improvement and the mechanism of the improvement from cocrystallization of poorly water-soluble compounds. Pharmaceutical Research, 25(11), 2581–2592. https://doi.org/10.1007/s11095-008-9676-2
Sun, C., & Grant, D. J. W. (2001). Influence of crystal structure on the tableting properties of sulfamerazine polySun, C., & Grant, D. J. W. (2001). Influence of crystal structure on the tableting properties of sulfamerazine polymorphs. Pharmaceutical Research, 18(3), 274–280. doi:10.1023. Pharmaceutical Research, 18(3), 274–280. https://doi.org/10.1023/A:1011038526805
Thakuria, R., Delori, A., Jones, W., Lipert, M. P., Roy, L., & Rodríguez-Hornedo, N. (2013). Pharmaceutical cocrystals and poorly soluble drugs. International Journal of Pharmaceutics, 453(1), 101–125. https://doi.org/10.1016/j.ijpharm.2012.10.043