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

Abstract

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 Para Amino Benzoic 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 possess adequate pharmaceutical stability.

Keywords

• Etodolac,Cocrystal,Solubility,Dissolution,Hansen Solubility Parameter

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

Abstract

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.  

Keywords

• Etodolak,Ko-Kristal,Çözünürlük,Dissolüsyon,Hansen Çözünürlük Parametresi

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