INVESTIGATING THE EFFECT OF pH AND ION STRENGTH ON LOADING AND RELEASE PROPERTIES OF DIFFERENT ION EXCHANGERS

Öz

Objective: Ion-exchangers are inert, water-insoluble polymers with ionizable functional groups on their surface. They can be used for purposes such as disintegrating or taste masking in orally disintegrating dosage forms, or they can provide a pH-dependent controlled release. Material and Method: The loading and release properties of different cation exchangers were investigated by loading Atenolol to Amberlite CG50, Dowex 50W-X2 and Smopex 101 as weak or strong resin and strong fiber, respectively. The effect of the ionic strength of the medium on the loading capacities of these materials were investigated in water and pH 7.4 HEPES buffer using batch method and loading was monitored by pH, zeta potential, FTIR and SEM analysis. Loading capacity was calculated UV spectrophotometrically. The effect of pH and ionic strength on the atenolol release was investigated by the dialysis bag method in pH 1.2 HCl, pH 6.8 PBS and pH 6.8 HEPES media. Result and Discussion: Due to its low molecular weight and high pKa atenolol was successfully loaded with a capacity over 93%. As the pH could be balanced a higher loading capacity was achieved in HEPES buffer. The decrease in zeta potential values proved that the complexes were successfully obtained and the ionic complex formation was also monitored with FTIR and SEM micrographs. Atenolol did not get released in pH 1.2 medium, contrarily to pH 6.8 in which the functional groups are ionized. The higher amount of counter ions in PBS buffer also affected the release. The highest release rate was obtained with Amberlite. All ion-exchangers provided a pH-dependent release fitting to Higuchi or Zero order kinetics that shows diffusion. Boyd equation results also showed that diffusion mechanism was particle controlled.

Anahtar Kelimeler

• Amberlite CG50
• atenolol
• cation-exchange materials
• Dowex 50W
• Smopex 101

pH VE İYON KUVVETİNİN İYON DEĞİŞTİRİCİLERİN YÜKLEME VE SALIM ÖZELLİKLERİ ÜZERİNE ETKİSİNİN İNCELENMESİ

Öz

Amaç: İyon değiştiriciler, yüzeylerinde iyonize olabilen fonksiyonel gruplar bulunan suda çözünmeyen inert polimerlerdir. Ağızda dağılan dozaj formlarında dağıtıcı veya tat maskeleyici gibi amaçlar için kullanılabilirler veya pH'ya bağlı kontrollü salım sağlayabilirler. Gereç ve Yöntem: Atenolol kullanılarak üç farklı katyon değiştiricinin yükleme ve salım özellikleri araştırılmıştır. Kullanılan katyon değiştiriciler zayıf veya kuvvetli reçine ve kuvvetli fiber olarak sırasıyla Amberlite CG50, Dowex 50W-X2 ve Smopex 101 olarak seçilmiştir. Ortamın iyonik kuvvetinin bu malzemelerin yükleme kapasitelerine etkisi, beç yöntemi kullanılarak su ve pH 7.4 HEPES tamponunda araştırılmış ve yükleme pH, zeta potansiyeli, FTIR ve SEM analizi ile izlenmiştir. Yükleme kapasitesi UV spektrofotometrik yöntemle hesaplanmıştır. Ortam pH değeri ve iyonik kuvvetinin salım üzerindeki etkisi diyaliz torba kullanılarak pH 1.2 HCl, pH 6.8 PBS ve pH 6.8 HEPES ortamlarında incelenmiştir. Sonuç ve Tartışma: Atenolol düşük molekül ağırlığı ve yüksek pKa değeri nedeniyle % 93'ün üzerinde bir kapasite ile başarıyla yüklenmiştir. pH dengelenebildiğinden, HEPES tamponunda daha yüksek bir yükleme kapasitesi elde edilmiştir. Zeta potansiyel değerlerindeki düşüş, iyon değiştirici-etken madde komplekslerinin başarılı bir şekilde elde edildiğini kanıtlamıştır. İyonik kompleks oluşumu FTIR ve SEM mikrografları ile de görüntülenmiştir. Atenolol, fonksiyonel grupların iyonize olduğu pH 6.8'in aksine pH 1.2 ortamında salınmamıştır. İçerdiği karşıt iyonlar nedeniyle PBS tamponunda daha yüksek miktarda salım sağlanmıştır. En hızlı salım Amberlite ile elde edilmiştir. Tüm iyon değiştiriciler, difüzyonu gösteren Higuchi veya Sıfır derece kinetikle pH'a bağlı bir salım göstermiştir. Boyd eşitlik sonucuna göre salım aynı zamanda partikülden kontrolle gerçekleşmiştir.

Anahtar Kelimeler

• Amberlite CG50
• atenolol
• Dowex 50W
• katyon değiştiriciler
• Smopex 101

Kaynakça

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