Design and Development of Crystallo-coagglomerates of Ritonavir for the Improvement of Physicochemical Properties

Objectives: The aim of the present study was to obtain CCA of ritonavir to improve the solubility, dissolution rate, and other physicochemicalproperties.Materials and Methods: Ritonavir agglomerates were prepared using the CCA technique. Acetone-water containing HPMC K-15, PEG-6000, PVPK-30 was used as the crystallization medium. The agglomerates were evaluated for saturation solubility, micromeritic properties, yield, and drugcontent. The agglomerates were also characterized using FTIR, DSC, XRPD and SEM.Results: The growth of particle size and the spherical form of the agglomerates resulted in the formation of products with good flow and packingproperties. The improved compaction properties of the agglomerated crystals were due to the fragmentation that occurred during compression.DSC and XRD studies showed that ritonavir particles crystallized in the presence of HPMC, PEG-6000, PVP K-30 and diluents did not undergostructural modifications. The solubility and dissolution rate of ritonavir agglomerates were improve compare to pure ritonavir.Conclusion: CCA was successfully applied to improve the physicochemical properties of ritonavir.

Fizikokimyasal Özelliklerin İyileştirilmesi için Ritonavirin KristaloKoaglomeratlarının Tasarımı ve Geliştirilmesi

Amaç: Bu çalışmanın amacı, çözünürlük, çözünme hızı ve diğer fizikokimyasal özelliklerini iyileştirmek için ritonavirin CCA’larını elde etmektir. Gereç ve Yöntemler: Ritonavir aglomeraları, CCA tekniği kullanılarak hazırlandı. Kristalizasyon ortamı olarak HPMC K-15, PEG-6000, PVP K-30 içeren aseton-su kullanıldı. Aglomeratlar, doygunluk çözünürlüğü, mikromeritik özellikler, verim ve etkin madde içeriği açısından değerlendirildi. Aglomeratlar ayrıca FTIR, DSC, XRPD ve SEM kullanılarak karakterize edildi. Bulgular: Aglomeratların partikül büyüklüğünün ve küresel formunun büyümesi, iyi akış ve paketleme özelliklerine sahip ürünlerin oluşumu ile sonuçlandı. Aglomere olmuş kristallerin iyileşmiş sıkıştırma özellikleri, sıkıştırma sırasında meydana gelen parçalanmadan kaynaklanmıştır. DSC ve XRD çalışmaları, HPMC, PEG-6000, PVP K-30 ve seyrelticilerin varlığında kristalleşen ritonavir partiküllerinin yapısal modifikasyonlara maruz kalmadığını gösterdi. Ritonavir aglomeratlarının çözünürlüğü ve çözünme hızı, saf ritonavir ile karşılaştırılır derecede gelişti. Sonuç: Ritonavirin fizikokimyasal özelliklerini iyileştirmek için kristalo-koaglomerasyonu başarıyla uygulanmıştır

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Turkish Journal of Pharmaceutical Sciences
  • ISSN: 1304-530X
  • Yayın Aralığı: Yılda 6 Sayı
  • Başlangıç: 2000

6.6b293

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