Yardımcı Maddelerin İlaç Formülasyonundaki Etkilerini Araştırmak İçin In vitro Testler

Öz

İlaçların formülasyonu, farmakolojik olarak aktif kabul edilmeyen ve bir ilaç formülasyonunda farklı rollere sahip olabilecek bazı eksipiyanlarla birleştirilebilen aktif farmasötik bileşenler (API) gerektirir. Bir biguanid antidiyabetik olarak jenerik bir isim olan Glukofen, diyet yönetimi ve egzersiz yeterli glisemik kontrole yardımcı olmadığında, özellikle aşırı kilolu hastalarda tip 2 Diabetes Mellitus tedavisinde kullanılır. Glukofen formülasyonunda, bir API olarak metformin-HCl ve povidon, magnezyum stearat, hipromelloz ve titanyum dioksit gibi bazı yardımcı maddeler birleştirilir. Bu çalışmanın amacı, Glukofen ve metformin-HCl'nin insan bronşiyal epitel hücre dizisi (Beas-2b) üzerindeki etkilerinin in vitro araştırılmasıdır. Toksik etkilerini ve hücrelere alımlarını gözlemlemek ve karşılaştırmak için sitotoksisite testi ve akış sitometrisi deneyleri yapıldı. Bu çalışmadan elde edilen sonuçlar, hem Glukofen hem de metformin-HCl'nin Beas-2b hücreleri üzerinde herhangi bir toksik etkisinin elde edilmediğini göstermiştir. Ayrıca Glukofen'in hücrelere alımı, metformin-HCl'den daha fazla gözlendi. Yardımcı maddelerin metformin-HCl'ye dahil edilmesinin, hücre çoğalmasında ve hücrelere alınmasında önemli bir artışa yol açtığı açıktır.

Anahtar Kelimeler

• Glukofen
• metformin
• in vitro
• Beas-2b
• yardımcı maddeler
• toksisite

In vitro Testing to Investigate Effects of Excipients in Drug Formulation

Öz

The formulation of drugs requires active pharmaceutical ingredients (API), which can be combined with some excipients, which are not considered pharmacologically active and could have different roles in a drug formulation. Glukofen, a generic name as a biguanide antidiabetic, is used for treating type 2 Diabetes Mellitus, mainly in overweight patients when dietary management and exercise do not help in adequate glycemic control. In Glukofen formulation, metformin-HCl as an API and some excipients such as povidone, magnesium stearate, hypromellose, and titanium dioxide are combined. The goal of this study is in vitro investigation of the effects of Glukofen and metformin-HCl on the human bronchial epithelial cell line (Beas-2b). To observe and compare their toxic effects and uptake into cells, cytotoxicity assay and flow cytometry experiments were carried out. The obtained results from this study showed that any toxic effects of both Glukofen and metformin-HCl on Beas-2b cells were not obtained. In addition, uptake of Glukofen into cells was observed more than metformin-HCl. It is evident that the incorporation of excipients to metformin-HCl results in a significant rise in cell proliferation and uptaking into cells.

Anahtar Kelimeler

• Glukofen
• metformin
• in vitro
• Beas-2b
• excipients
• toxicity

Kaynakça

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