Development, Characterization and In-vitro Evaluation of Solid Self-Emulsifying Drug Delivery Systems (S-SEDDS) Containing Valsartan

Year 2023, Volume: 16 Issue: 3, 672 - 686, 31.12.2023

Mine Diril , Gülbeyaz Yıldız Türkyılmaz , Eda Gülmezoğlu , Yesim Karasulu

https://doi.org/10.18185/erzifbed.1332052

Cited By: 1

Abstract

Hipertansiyon, kardiyovasküler hastalık için ana risk faktörüdür. Valsartan, anjiyotensin II'nin anjiyotensin Tip 1 reseptörü üzerindeki etkisini spesifik olarak bloke ederek yaygın olarak kullanılan, etkili ve iyi tolere edilen antihipertansif ajandır. Ancak gastrointestinal sistemin üst kısmından emilir ve buranın asidik ortamı nedeniyle bu bölgede az çözünür ve oral biyoyararlanımı sadece %25'tir. Bu çalışmanın amacı, Valsartan'ın (VST) ticari formülasyonuna alternatif olarak yeni bir dozaj formu geliştirmektir. Bu amaçla, VST’ın çözünürlüğünü artırmak ve pH'tan bağımsız bir çözünürlüğe sahip olan katı kendiliğinden emülsifiye olabilen ilaç taşıyıcı sistem (S-SEDDS) formülasyonu geliştirmek hedeflenmiştir. VST'ın en yüksek çözünürlük gösterdiği SEDDS bileşenlerini belirlemek için çözünürlük çalışmaları yapılmıştır. Çözünürlük çalışmalarına göre; yağ fazı olarak izopropil miristat (3.5 mg/mL), yüzey etkin maddeler olarak Capyrol 90 (19.8 mg/mL) ve Tween 20 (32.5 mg/mL), yardımcı yüzey etkin madde olarak ise Transcutol HP (168.9 mg/mL) kullanılmıştır. Çözünürlük çalışmaları ile belirlenen yardımcı maddeler ile üçgen faz diyagramları çizilmiştir. VST içeren SEDDS formülasyonları Avicel pH101 ve Hidroksipropil metil selüloz’a (HPMC) ayrı ayrı yaş granülasyon tekniği ile adsorbe edilmiş ve karakterizasyon çalışmaları yapılmıştır. Geliştirilen VST-SEDDS, VST-SEDDS-Avicel ve VST-SEDDS-HPMC formülasyonları pH 1.2 ortamında ticari ürüne göre VST salınımı arttırmıştır. Ayrıca VST-SEDDS-Avicel formülasyonunun açlık, tokluk durumlarından ve pH değişiminden etkilenmediği gözlenmiştir. Bu nedenle VST-SEDDS-Avicel formülasyonunun, pH'tan bağımsız çözünürlüğü arttırdığı ve antihipertansif tedavi için potansiyel bir formülasyon adayı olabileceği söylenebilmektedir.

Keywords

Valsartan, Solid Self-Emulsifying Drug Delivery Systems, SEDDS, Antihypertensive

Supporting Institution

TUBİTAK

Project Number

117S821

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