Serdar TORT, Esra KODAN AKÇA, Seval OLĞAÇ, Sinem SAAR, Ayşegül YILDIZ, İlay Sema ÜNAL, Zeliha Duygu ÖZDAL, Fatmanur TUĞCU DEMİRÖZ

Venlafaksin Hidroklorürün Uzatılmış Salım Yapan Tablet Formülasyonlarının Geliştirilmesi ve Değerlendirilmesi

Amaç: Depresyon, 250 milyondan fazla insanı yaştan bağımsız olarak etkileyen mental bozukluktur. Venlafaksin, antidepresan bir ilaçtır ve eski antidepresan ilaçlara göre daha az yan etki ile panik atak ve anksiyete tedavisinde kullanılır. Bununla birlikte, venlafaksin hidroklorür (VH), yeterli plazma-ilaç konsantrasyonunu sağlamak için günde üç kez dozlama gerektiren kısa yarı ömre sahiptir. Bu çalışmanın amacı, günde bir kez verilecek uzun süreli salım yapan VH tabletleri geliştirmektir. Gereç ve Yöntemler: Kontrollü salım ajanı olarak polietilen oksit, sodyum aljinat, hidroksipropil metil selüloz, guar zamkı ve poliakrilik asit kullanıldı. Tabletler doğrudan basım yöntemi ile hazırlandı. Toz (yığın açısı, akış hızı, Carr indeksi ve Hausner oranı) ve tablet (ağırlık homojenliği, sertlik, friabilite) karakterizasyonları değerlendirildi. 24 saat boyunca in vitro salım çalışmaları yapıldı ve ilaç salım kinetikleri farklı modeller kullanılarak değerlendirildi. Bulgular: Guar zamkı ile hazırlanan formülasyon dışında tüm formülasyonlar uygun Carr indeksi ve Hausner oranı gösterdi. Doğrudan basım yöntemi ile üretilen tabletler, ticari tablet ile karşılaştırıldı. Tüm formülasyonlar için uzun süreli VH salımı gözlendi. In vitro salım hızı test sonuçlarına göre, HPMC ve Carbopol polimerlerini içeren F1 formülasyonundan ilaç salımı, ticari tabletlere kıyasla benzer bulunmuştur. Sonuç: Doğrudan basılmış VH tabletler, hasta uyumu ve diğer üretim yöntemlerine kıyasla daha az üretim aşaması ile ticari tabletlere tercih edilebilir bir alternatif olabilir.

Anahtar Kelimeler:

venlafaksin hidroklorür, uzatılmış salım, depresyon tedavisi, doğrudan basım, oral tablet

Development and Evaluation of Sustained Release Tablet Formulations of Venlafaxine Hydrochloride

Keywords:

Oral tablet, venlafaxine hydrocloride, sustained release, direct compression, depression treatment,

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