Design and Development of Crystallo-co-agglomerates of Ritonavir for the Improvement of Physicochemical Properties/Fizikokimyasal Ozelliklerin Iyilestirilmesi icin Ritonavirin Kristalo-Koaglomeratlarinin Tasarimi ve Gelistirilmesi

• Published in: Turkish Journal of Pharmaceutical Sciences Vol. 15; no. 3; p. 248
• Main Authors: Mahajan, Nilesh M, Malghade, Ashwini D, Dumore, Nitin G, Thenge, Raju R
• Format: Journal Article
• Language: English
• Published: Galenos Yayinevi Tic. Ltd 01.12.2018
• Subjects: Acetone; Antiretroviral agents; Bioavailability; Crystal structure; Pharmaceutical research; Ritonavir; Testing
• ISSN: 1304-530X
• DOI: 10.4274/tjps.44227

Objectives: The aim of the present study was to obtain CCA of ritonavir to improve the solubility, dissolution rate, and other physicochemical properties.Materials and Methods: Ritonavir agglomerates were prepared using the CCA technique. Acetone-water containing HPMC K-15, PEG-6000, PVP K-30 was used as the crystallization medium. The agglomerates were evaluated for saturation solubility, micromeritic properties, yield, and drug content. 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 packing properties. 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 undergo structural 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.Key words: Crystallo-co-agglomeration, solubility, dissolution, ritonavirAmac: Bu calismanin amaci, cozunurluk, cozunme hizi ve diger fizikokimyasal ozelliklerini iyilestirmek icin ritonavirin CCA'larini elde etmektir. Gerec ve Yontemler: Ritonavir aglomeralari, CCA teknigi kullanilarak hazirlandi. Kristalizasyon ortami olarak HPMC K-15, PEG-6000, PVP K-30 iceren aseton-su kullanildi. Aglomeratlar, doygunluk cozunurlugu, mikromeritik ozellikler, verim ve etkin madde icerigi acisindan degerlendirildi. Aglomeratlar ayrica FTIR, DSC, XRPD ve SEM kullanilarak karakterize edildi.Bulgular: Aglomeratlarin partikul buyuklugunun ve kuresel formunun buyumesi, iyi akis ve paketleme ozelliklerine sahip urunlerin olusumu ile sonuclandi. Aglomere olmus kristallerin iyilesmis sikistirma ozellikleri, sikistirma sirasinda meydana gelen parcalanmadan kaynaklanmistir. DSC ve XRD calismalari, HPMC, PEG-6000, PVP K-30 ve seyrelticilerin varliginda kristallesen ritonavir partikullerinin yapisal modifikasyonlara maruz kalmadigini gosterdi. Ritonavir aglomeratlarinin cozunurlugu ve cozunme hizi, saf ritonavir ile karsilastirilir derecede gelisti.Sonuc: Ritonavirin fizikokimyasal ozelliklerini iyilestirmek icin kristalo-koaglomerasyonu basariyla uygulanmistir.Anahtar kelimeler: Kristalo-koaglomerasyon, cozunurluk, cozunme, ritonavir