Muhammad SAMİE, Sajid BASHİR, Jabbar ABBAS, Samiullah KHAN, Nargis AMAN, Habibullah JAN, Naveed MUHAMMAD

Design, Formulation and In Vitro Evaluation of Sustained-release Tablet Formulations of Levosulpiride

Objectives: Levosulpiride is a widely used gastroprokinetic agent in the treatment of various gastric disorders; however, its short half-life andincreased dosage frequency leads to non-compliance and possible adverse effects. The prime objective of the current study was to develop asustained-release formulation of Levosulpiride incorporating bioresorbable cellulose derivatives.Materials and Methods: Sustained-release formulations of Levosulpiride were prepared through direct compression using various cellulosederivatives such as CMC sodium, HPC, and HPMC in different polymer-to-drug weight ratios as release-modifying polymers. The powder blendsand compressed tablets were then subjected to pre-compressional and post-compressional evaluation, as well as FTIR analysis. In vitro releasestudies were performed for all formulations of the model drug in buffer solution of pH 6.8 at a wave length of 214 nm by a UV-visible lightspectrophotometer.Results: The FTIR results confirmed that the interaction between components was physical, and from the different kinetic models data, the releaseprofile was best expressed by the Higuchi model because the results showed high linearity. The results also showed formulation F9 to be the idealone among the developed formulations, exhibiting sustained- release behavior.Conclusion: Levosulpiride sustained-release matrices were prepared successfully using CMC sodium, HPC, and HPMC as the release-retardingpolymer/carrier

Levosulpirid Sürekli Salım Tablet Formülasyonlarının Tasarımı, Formülasyonu ve İn Vitro Değerlendirilmesi

Amaç: Levosulpirid, çeşitli gastrik bozuklukların tedavisinde yaygın olarak kullanılan bir gastroprokinetik ajandır; bununla birlikte, kısa yarı ömrü ve artan dozlama sıklığı, uyumsuzluk ve olası yan etkilere yol açar. Bu çalışmanın asıl amacı, biyolojik olarak resorbe olabilen selüloz türevlerini içeren Levosulpiridin sürekli salımlı bir formülasyonunu geliştirmektir. Gereç ve Yöntemler: Levosulpiridinin sürekli salım formülasyonları, salım modifiye eden polimerler olarak CMC sodyum, HPC ve HPMC gibi çeşitli selüloz türevlerinin farklı polimer-etkin madde ağırlık oranlarında kullanımıyla direkt basım yoluyla hazırlandı. Daha sonra, toz karışımları ve basılmış tabletler basım öncesi ve basım sonrası değerlendirmeye ve aynı zamanda FTIR analizlerine tabi tutuldu. UV/görünür ışık spektrofotometresi ile 214 nm dalga boyunda pH 6.8 tampon çözeltisinde model etkin maddenin tüm formülasyonları için in vitro salım çalışmaları gerçekleştirildi. Bulgular: FTIR sonuçları, bileşenler arasındaki etkileşimin fiziksel olduğunu ve farklı kinetik model verilerinden, salım profilinin Higuchi modeline en iyi şekilde uyum gösterdiğini doğruladı, çünkü sonuçlar yüksek doğrusallık gösterdi. Sonuçlar ayrıca, geliştirilmiş sürekli salım formülasyonları arasında F9 formülasyonunun ideal olduğunu gösterdi. Sonuç: Salım geciktirici polimer/taşıyıcı olarak CMC sodyum, HPC ve HPMC kullanılarak levosulpirid sürekli salımlı matrisler, başarıyla hazırlandı.

Tam Metin

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