SEDEM DİYAGRAM SİSTEMİ KULLANILARAK KAPTOPRİL İÇEREN AĞIZDA DAĞILAN TABLET FORMÜLASYONUNUN GELİŞTİRİLMESİ

Öz

Amaç: Bu çalışma ile sistematik bir yaklaşım olan SeDeM diagram sistemi kullanılarak, doğrudan basım ile hazırlanan kaptopril içeren ağızda dağılan tabletlerin formülasyon geliştirme sürecinin kolaylaştırılması ve hızlandırılması amaçlanmaktadır. Gereç ve Yöntem: Kaptopril ve ağızda dağılan tablet formülasyonlarında kullanılan olası yardımcı maddeler; sıkıştırılabilirlik, akışkanlık, kohezyon, higroskopiklik, partikül boyutu ve homojenlik gibi toz özellikleri açısından incelenmiştir. Tozların bu mikromeritik özelliklerine ait değerler kullanılarak SeDeM diyagramları oluşturulmuştur. Ardından, doğrudan basım yöntemiyle tablet üretimine uygunluklarını değerlendirmek amacıyla her bir tozun insidans faktörleri ve kapsamlı indeksleri hesaplanmıştır. SeDeM analizi temel alınarak seçilen yardımcı maddeler kullanılarak kaptopril içeren ağızda dağılan tabletleri formüle edilmiştir. Karakterizasyon çalışmaları kapsamında ağırlık sapması tayini, tablet çapı ve kalınlığı tayini, kırılma dayanıklılığı, tablet sertliği ve dağılma süresi testleri yapılmıştır. Sonuç ve Tartışma: SeDeM analizi; dolgu maddesi olarak olarak kullanılan mikrokristal selülozun, 5’in üzerinde iyi bir sıkıştırma indeksine sahip olduğunu ve kaptopril için kritik olan sıkıştırılabilirlik faktörü de dahil olmak üzere çok sayıda uygun insidans faktörleri gösterdiğini ortaya koymuştur. Dağıtıcı madde olarak sodyum nişasta glikolat ve bağlayıcı madde olarak polivinil pirolidon K30 limit değeri altında bazı insidans faktörü değerleri göstermelerine rağmen, mikrokristal selülozun basılabilirlik özelliğinin yüksek olması nedeniyle bu eksikliklerin telafi edeceği düşünülerek formülasyona dahil edilmişlerdir. Mikrokristal selüloz, sodyum nişasta glikolat ve polivinil pirolidon K30 ile formüle edilen kaptopril içeren ağızda dağılan tabletler ise ağırlık sapması, çap, kalınlık, kırılma dayanaklılığı, tablet sertliği ve dağılma süresi açısından farmakope standartlarının kabul limitlerini karşılamıştır. Sonuç olarak, doğrudan basım yöntemi ile hazırlanan kaptopril içeren ağızda dağılan tablet formülasyonu az sayıda formülasyon denemesi ile kısa sürede SeDeM diyagram sistemi kullanılarak geliştirilmiştir.

Anahtar Kelimeler

• Ağızda dağılan tabletler
• doğrudan basım yöntemi
• kaptopril
• SeDeM diyagram sistemi

FORMULATION DEVELOPMENT OF CAPTOPRIL ORODISPERSIBLE TABLETS USING SEDEM EXPERT DIAGRAM SYSTEM

Öz

Objective: This study aimed to streamline the formulation development process of captopril orodispersible tablets for direct compression by utilizing SeDeM Expert Diagram System as a systematic approach. Material and Method: Captopril and potential excipients for the formulation of orodispersible tablets were individually analysed in terms of powder characteristics including compressibility, flowability, cohesion, hygroscopicity, particle size, and homogeneity. The SeDeM Diagrams were constructed using these micromeritic values of the powders. Subsequently, incidence factors and comprehensive indexes for each powder were calculated to assess the suitability of them for direct compression process. Based on SeDeM analysis, captopril orodispersible tablets were formulated by direct compression using the selected excipients, and characterized in terms of weight variation, diameter, thickness, friability, hardness, disintegration time and dissolution. Result and Discussion: SeDeM analysis indicated that microcrystalline cellulose as a diluent had an index of good compression over 5, with the greatest number of suitable incidence factors, including compressibility which was a critical limitation for captopril. Although sodium starch glycolate (as a disintegrant) and polyvinyl pyrrolidone K30 (as a binder) exhibited some suboptimal incidence factor values, they were incorporated into the formulation with the thought of that microcrystalline cellulose would compensate for their deficiencies, as well as those of captopril. Captopril orodispersible tablets formulated with the aforementioned excipients complied with the pharmacopoeial standards for weight variation, diameter, thickness, friability, hardness, disintegration time and dissolution. In conclusion, the formulation of captopril orodispersible tablets by direct compression was developed to minimize extensive time and experimentation, utilizing SeDeM Expert Diagram System.

Anahtar Kelimeler

• Captopril
• direct compression
• orodispersible tablets
• SeDeM expert diagram system

Kaynakça

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