MUCOADHESIVE ORODISPERSIBLE FILM FORMULATIONS OF RASAGILINE MESYLATE FOR PARKINSON TREATMENT

Abstract

Objective: The article is included formulation studies and in vitro evaluation of orally dispersible Rasagiline mesylate (RM) orodispersible films (ODFs) for non-oral treatment of Parkinson's Disease. RM undergoes extensive hepatic biotransformation and is a highly selective and irreversible MAO-B inhibitor. It is metabolized in the liver and has an oral bioavailability of approximately 36% and a half-life of 3 hours. These properties suggest that RM may be an excellent candidate for buccal drug delivery.

Material and Method: ODFs of RM were prepared using PEO by the solvent casting method. While evaluating these formulations, parameters such as appearance, weight homogeneity, thickness, surface pH, drug content, swelling ratio, tensile strength, mucoadhesion, in vitro drug release studies and also stability were considered.

Result and Discussion: Obtained results show that ODFs are an effective and viable approach for RM delivery and may be a new alternative to existing oral delivery systems for Parkinson's treatment.

Keywords

• Buccal delivery
• orodispersible film
• polyethylene oxide
• rasagiline mesylate

PARKİNSON TEDAVİSİ İÇİN RASAJİLİN MESİLAT MUKOADEZİF AĞIZDA DAĞILAN FİLM FORMÜLASYONLARI

Abstract

Amaç: Bu makale, Parkinson Hastalığının oral olmayan tedavisi için Rasagilin mesilat (RM) ağızda dağılan filmlerin (ODF'ler) formülasyon çalışmalarını ve in vitro değerlendirmesini içermektedir. RM, özellikle yoğun hepatik biyotransformasyona uğrayan geri döndürülemez ve yüksek seçiciliğe sahip bir MAO-B inhibitörüdür. Karaciğerde metabolize edilir ve oral biyoyararlanımı yaklaşık %36 ve yarılanma ömrü 3 saattir. Bu özellikler, RM'nin bukkal ilaç dağıtımı için mükemmel bir aday olabileceğini göstermektedir.

Yöntem: RM'nin ODF'leri, solvent döküm yöntemiyle PEO kullanılarak hazırlandı. Bu formülasyonlar değerlendirilirken görünüş, ağırlık homojenliği, kalınlık, yüzey pH’sı, ilaç içeriği, şişme oranı, gerilme mukavemeti, mukoadezyon, in vitro ilaç salım çalışmaları ve stabilite gibi parametreler göz önünde bulundurulmuştur.

Sonuç ve Tartışma: Elde edilen sonuçlar, ODF'lerin RM uygulaması için etkili ve uygulanabilir bir yaklaşım olduğunu ve Parkinson tedavisi için mevcut oral dağıtım sistemlerine yeni bir alternatif olabileceğini göstermektedir.

Keywords

• Ağızda dağılan film
• bukkal uygulama
• polietilen oksit
• rasajilin mesilat

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