İkili Tadalafil Karışımlarında DSC, TGA ve FTIR Kullanılarak İlaç-Yardımcı Madde Geçimlilik Çalışmaları

Abstract

Amaç: İlaç ön formülasyon çalışmaları sırasında, formülasyondaki aktif bileşik ile yardımcı maddeler arasındaki fiziksel veya kimyasal geçimliliklerini tespit etmek ve nihai ürünün güvenilirliğini ve/veya etkinliğini göstermek için, uygun bir formülasyon eldesinde termal analiz ve spektroskopik teknikler kullanılır. Erektil disfonksiyonda, seçici bir siklik guanozin monofosfata özgü fosfodiesteraz tip 5 inhibitörlerinin geliştirilmesi ile devrim yaratmıştır. Tadalafil de bu inhibitörlerden bir tanesidir. Yardımcı maddeler, üretim, emilim veya uygulamaya yardımcı olmak için dozaj formlarına dahil edilmiştir. Farmakolojik olarak inert olduğu düşünülse de, ilaç aktif bileşiği etkinliği bozabilir. Gereç ve Yöntem: Çalışmada DSC, TGA ve FTIR sistemleri kullanılmıştır. Askorbik asit, butile hidroksianisol, kalsiyum fosfat dibazik, selüloz, magnezyum stearat, mannitol, sodyum karboksimetil selüloz, sukroz, talk, nişasta, primojel ve sitrik asidin Tadalafil ile etkileşimi incelenmiştir. İkili ilaç karışımları: eksipiyan analiz edilmiştir. Sonuçlar: Spektroskopik ve termal sonuçlara göre; Tadalafil magnezyum stearat, mannitol, sukroz ve askorbik asit ile geçimsizdir. Sonuç: İlaç-eksipiyan uyumluluğunu araştıran çalışmalar, ilaç geliştirme çalışmalarında önemli bir adımdır. Bu tür çalışmalarda termal ve spektroskopik teknikler yaygın olarak kullanılmaktadır.

Keywords

• Tadalafil
• Geçimlilik
• Yardımcı madde
• Fourier Dönüşümü Kızılötesi Spektroskopisi
• Diferansiyel tarama kalorimetrisi

Drug-Excipient Compatibility Studies In Binary Mixtures of Tadalafil by Using DSC, TGA and FTIR

Abstract

Objective: During drug preformulation studies, thermal analysis and spectroscopic techniques are used to detect physical or chemical incompatibilities between the active compound and the excipients in the formulation, and to demonstrate the safety and/or efficacy of the final product. It has revolutionized erectile dysfunction with the development of a selective cyclic guanosine monophosphate-specific PDE-5 inhibitors. Tadalafil is one of these inhibitors. Excipients are included in dosage forms to assist in manufacture, absorption or application. Although considered to be pharmacologically inert, the drug active compound may impair effectiveness. Material and Method: DSC, TGA, and FTIR, were used in the work. Ascorbic acid, butylated hydroxyanisole, calcium phosphate dibasic, cellulose, magnesium stearate, mannitol, sodium carboxymethyl cellulose, sucrose, talc, starch, primojel, and citric acid exhibit interaction with Tadalafil. Binary mixtures of drug:excipient have been analyzed. Results: Based on spectroscopic and thermal results; Tadalafil is incompatible with magnesium stearate, mannitol, sucrose, and ascorbic acid. Conclusion: Studies to investigate drug-excipient compatibility are an important step in drug development studies. Thermal and spectroscopic techniques are widely used in such studies.

Keywords

• Tadalafil
• Compatibility
• Excipient; Fourier Transform Infrared Spectroscopy
• Differential Scanning Calorimetry

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