Dipak D. GADEDE, Sanjay S. PEKAMWAR, Swaroop R. LAHOTI, Mahesh C. SARODE, Santosh D. PATNI

Etodolak’ın Ko-kristalizasyonu: Ko-kristalizasyon Tahmini, Ko-kristal Sentezi, Katı Faz Yapı Aydınlatma Çalışmaları ve In Vitro İlaç Salımı

Bu araştırma kapsamında, etodolak ko-kristallerinin sentezi ve farklı koformerlerin yapılarının aydınlatılması ile hansen çözünürlük paratmetrelerinin tayini çalışılmıştır. etodolak’ın çözünürlüğünün arttırılması ve dissolüsyon özelliğinin iyileştirilmesi amacıyla hazırlanan etodolak ko-kristallerinin farklı koformerleri izlenmiştir. ko-kristallerin yapısı; Fourier dönüşümlü infrared spektroskopisi (FtIR), diferansiyal taramalı kalorimetri (DSC) tayini, X-ışını kırınım (PXRD) tayini ile aydınlatılmış, ayrıca çözünürlük ve çözelti doygunluğu çalışmaları, in vitro dissolüsyon ve stabilite çalışmaları yapılmıştır. Çalışma sonucunda etodolak’ın, p-amino benzoik asit, ferrulik asit ve salisilik asit ile kokristalleri hazırlandığında çözünürlüğünün arttığı tespit edilmiştir. etodolak:Salisilik ait 1:1M kokristalinin hızlı ilaç salımı için formüle edilen tablet içeriğinde kullanılması öngörülmüştür. etodolak kokristallerinin yeterli farmasötik stabiliteye sahip oldukları ve etodolak’ın çözünürlük ve dissolüsyon özelliğini arttırdıkları sonucuna ulaşılmıştır.

Cocrystallization of Etodolac: Prediction of Cocrystallization, Synthesis, Solid State Characterization and In Vitro Drug Release

The present investigation deals with determination of hansen solubility parameters, synthesis and characterization of etodolac co-crystals with various coformers. Various coformers were screened under the study to prepare cocrystals of etodolac for improving its solubility and dissolution. The prepared cocrystals were characterized by saturation solubility study, Fourier transform infrared spectroscopy (FtIR), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), in vitro dissolution studies and stability study. The outcome of study show that the significant improvement in solubility with p-aminobenzoic acid, ferulic acid and salicylic acid. etodolac:Salicylic acid cocrystal 1:1M were formulated as immediate release tablets. The results reveal that solubility and dissolution of etodolac was improved by cocrystallization and it possesses adequate pharmaceutical stability.

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