In-vivo Meloksikam Miktar Tayininin Validasyonu ve Tavşanlarda Meloksikam İçeren Mikropartiküller ile Biyoeşdeğerlik Çalışması

Yıl 2009, Sayı: 2, 115 - 130, 01.06.2009

Hakan Eroğlu Nihan Burul-bozkurt Serdar Uma Levent Öner

Öz

Meloksikam, analjezik ve antipiretik etkileri olan ve steroidal olmayan anti-inflamatuvar ilaçlar grubuna dahil bir etkin maddedir. Düşük çözünürlük ve yüksek permeabilite özellikleri ile Biyofarmasötik Sınıflandırma Sitemine gore Sınıf II grubuna dahildir. Bu çalışmada meloksikam içeren mikropartikül formülasyonlarının oral olarak tavşanlara uygulanmasından sonra miktar tayininin yapılabilmesine yönelik olarak hızlı ve basit bir HPLC yöntemi valide edilmiştir. AUC0- ∞, tmaks, t1/2, and Cmaks değerleri üzerinden farmakokinetik parametreler değerlendirilmiştir. AUC0-∞ and Cmaks değerlerinin gerekli logaritmik dönüşümleri sonrasında güven aralığı değerleri sırasıyla %68.38-147.87 ve %78.85-161.49 olarak bulunmuştur. Bu sonuçlar doğrultusunda, biyoeşdeğer olarak kabul edilme sınırları olan %80-125 aralığının dışında kalmalarından dolayı bu iki mikropartikül formülasyonlarının biyoeşdeğer olmadıkları gösterilmiştir.

Anahtar Kelimeler

Meloksikam, Biyoeşdeğerlik, Mikropartikül

Validation of the Analytical Method for In-Vivo Determination of Meloxicam and Bioequivalence Study from Meloxicam Containing Microparticle Formulations in Rabbits

Öz

Meloxicam is a member of non-steroidal anti-inflammatory drugs having analgesic and anti-pyretic effects. It belongs to the Biopharmaceutics Classification System Class II with its low solubility and high permeability profile. In this study, we have validated a rapid and simple HPLC method for the in-vivo determination of meloxicam from rabbit plasma after oral administration of microparticle formulations containing meloxicam. The pharmacokinetic parameters of AUC0-∞ , tmax, t1/2, and Cmax were determined for the microparticle formulations. After necessary logarithmic transformation of the AUC0-∞ and Cmax values, the confidence interval limits for both AUC0-∞ and Cmax values were calculated as 68.38-147.87% and 78.85-161.49%, respectively. These results indicated that these two microparticle formulations were not bioequivalent, since they were both out of the range for the establishment of bioequivalence which is 80-125%.

Anahtar Kelimeler

Meloxicam, Bioequivalence, Microparticle

Kaynakça

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