İndomethacinin Geliştirilmiş Çözünürlük ve Sözlü İzolasyon ile Formülasyonunun Özel Emülsifilleştirilmesi

RAVOURU, Nagaraju; DAMINENI, Saritha; POREDDY, Srikanth Reddy; PENJURI, Subhash Chandra Bose

İndomethacinin Geliştirilmiş Çözünürlük ve Sözlü İzolasyon ile Formülasyonunun Özel Emülsifilleştirilmesi

Subhash Chandra Bose PENJURI, (Mnr College of Pharmacy, Department of Pharmaceutics, Telangana, India)

Saritha DAMINENI, (Sultan-ul-uloom College of Pharmacy, Department of Pharmaceutics, Telangana, India)

Nagaraju RAVOURU, (Sri Padmavathi Mahila Visvavidyalayam (Women's University), Institute of Pharmaceutical Technology, Andhra Pradesh, India)

Srikanth Reddy POREDDY (Mnr College of Pharmacy, Department of Pharmaceutics, Telangana, India)

Turkish Journal of Pharmaceutical Sciences

1 1

Yıl: 2017 Cilt: 14 Sayı: 2 Sayfa Aralığı: 108 - 119 Metin Dili: Türkçe İndeks Tarihi: 29-07-2022

İndomethacinin Geliştirilmiş Çözünürlük ve Sözlü İzolasyon ile Formülasyonunun Özel Emülsifilleştirilmesi

Öz:

Amaç: Bu çalışmanın amacı, kendiliğinden emülsifiye edici sistemlere formüle ederek, az çözünen ilaç indometazinin (IMN) çözünürlüğünü,çözünmesini ve dolayısıyla anti-inflamatuvar aktiviteyi arttırmaktır.Gereç ve Yöntemler: Kendi kendine emülsiyon haline getirici formülasyonlar yağ olarak capmul MCM, yüzey aktif madde olarak tween 80, kosürfaktantolarak transcutol P kullanılarak hazırlandı. İlaç ve eksipiyanlar arasındaki etkileşimi bilmek için fourier dönüşüm kızılötesi spektroskopisi vediferansiyel tarama kalorimetrisi çalışmaları yapılmıştır. Pseudo üçlü faz diyagramları, kendinden emülsiyonlaşmış bölgeyi bilmek için 1:1 ile 1:4 ve2:1 ile 4:1 arasında yüzey aktif madde ve kosürfaktant kullanılarak oluşturulmuştur. Formülasyonlar, parçacık büyüklüğü, zeta potansiyeli, kırılmaindisi, viskozite ve bulut noktası açısından değerlendirildi. İn vitro çözünme çalışmaları, pH 7.2 fosfat tamponun bir bölümünde ve dört kısım sudagerçekleştirildi. Farmakokinetik parametreler Win Nonlin yazılımı ile analiz edildi.Bulgular: Kendiliğinden emülsifikasyon 2:1, 3:1 ve 1:2 oranında surfaktan ve kosürfaktant oranlarına göre daha yüksekti ve IMN formülasyonlarıhazırlandı. Formülasyonlar, farklı pH ve seyreltmelerde kararlıydı. Küre boyutu, 184.1 nm ile 340.5 nm aralığındaydı, çünkü yağ, yüzey aktif maddeve ko-yüzey aktif madde karışımı oranı kürenin boyutuna farklı etkiler yapmıştır. Tüm formülasyonların globüllerinin üzerindeki negatif yük,kararlılıklarına atıfta bulunmaktadır. Optimize edilmiş formülasyon, pazarlanan ürüne kıyasla daha iyi salınım gösterdi. Optimize edilmiş KendiKendine Emülsifiye Edici İlaç Taşıma Sistemi'nin AUC'si pazarlanan ürüne göre önemli derecede yüksekti.Sonuç: Böylece, mevcut araştırmadan kendi kendine emülsifiye IMN sistemleri, çözünmeyi ve dolayısıyla anti-inflamatuvar aktiviteyi arttırmak içinyararlı bir alternatif sağlar.

Anahtar Kelime:

Konular: Farmakoloji ve Eczacılık

Self-Emulsifying Formulation of Indomethacin with Improved Dissolution and Oral Absorption

Öz:

Objectives: The objective of the present study was to enhance the solubility, dissolution and hence anti-inflammatory activity of poorly soluble drug indomethacin (IMN) by formulating into self emulsifying systems.Materials and Methods: Self emulsifying formulations were prepared using capmul MCM as oil, tween 80 as surfactant, transcutol P as cosurfactant. Fourier transform infrared spectroscopy and differential scanning calorimetry studies were conducted to know the interaction between drug and excipients. Pseudo ternary phase diagrams were constructed using surfactant and cosurfactant in 1:1 to 1:4 and 2:1 to 4:1 to know the efficient self emulsification region. The formulations were evaluated for their particle size, zeta potential, refractive index, viscosity and cloud point. In vitro dissolution studies were conducted in one part of pH 7.2 phosphate buffer and four parts of water. The pharmacokinetic parameters were analysed by Win Nonlin software. Results: The self emulsification was higher with the ratios 2:1, 3:1 and 1:2 of surfactant and co surfactant and the IMN formulations were prepared. The formulations were stable at different pH and dilutions. The globule size was in the range of 184.1 nm to 340.5 nm, as the ratio of oil, surfactant and cosurfactant mixture has varied effects on the size of globule. The negative charge on the globules of all formulations attributes their stability. The optimized formulation showed better release as compared to marketed product. The AUC of the optimised Self-Emulsifying Drug Delivery System was significantly higher than the marketed product.Conclusion: Thus, from the present research, self emulsifying systems of IMN provide a useful alternative to enhance dissolution and hence anti inflammatory activity.

Anahtar Kelime:

Konular: Farmakoloji ve Eczacılık

Belge Türü: Makale Makale Türü: Araştırma Makalesi Erişim Türü: Erişime Açık

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APA	PENJURI S, DAMINENI S, RAVOURU N, POREDDY S (2017). İndomethacinin Geliştirilmiş Çözünürlük ve Sözlü İzolasyon ile Formülasyonunun Özel Emülsifilleştirilmesi. , 108 - 119.
Chicago	PENJURI Subhash Chandra Bose,DAMINENI Saritha,RAVOURU Nagaraju,POREDDY Srikanth Reddy İndomethacinin Geliştirilmiş Çözünürlük ve Sözlü İzolasyon ile Formülasyonunun Özel Emülsifilleştirilmesi. (2017): 108 - 119.
MLA	PENJURI Subhash Chandra Bose,DAMINENI Saritha,RAVOURU Nagaraju,POREDDY Srikanth Reddy İndomethacinin Geliştirilmiş Çözünürlük ve Sözlü İzolasyon ile Formülasyonunun Özel Emülsifilleştirilmesi. , 2017, ss.108 - 119.
AMA	PENJURI S,DAMINENI S,RAVOURU N,POREDDY S İndomethacinin Geliştirilmiş Çözünürlük ve Sözlü İzolasyon ile Formülasyonunun Özel Emülsifilleştirilmesi. . 2017; 108 - 119.
Vancouver	PENJURI S,DAMINENI S,RAVOURU N,POREDDY S İndomethacinin Geliştirilmiş Çözünürlük ve Sözlü İzolasyon ile Formülasyonunun Özel Emülsifilleştirilmesi. . 2017; 108 - 119.
IEEE	PENJURI S,DAMINENI S,RAVOURU N,POREDDY S "İndomethacinin Geliştirilmiş Çözünürlük ve Sözlü İzolasyon ile Formülasyonunun Özel Emülsifilleştirilmesi." , ss.108 - 119, 2017.
ISNAD	PENJURI, Subhash Chandra Bose vd. "İndomethacinin Geliştirilmiş Çözünürlük ve Sözlü İzolasyon ile Formülasyonunun Özel Emülsifilleştirilmesi". (2017), 108-119.

APA	PENJURI S, DAMINENI S, RAVOURU N, POREDDY S (2017). İndomethacinin Geliştirilmiş Çözünürlük ve Sözlü İzolasyon ile Formülasyonunun Özel Emülsifilleştirilmesi. Turkish Journal of Pharmaceutical Sciences, 14(2), 108 - 119.
Chicago	PENJURI Subhash Chandra Bose,DAMINENI Saritha,RAVOURU Nagaraju,POREDDY Srikanth Reddy İndomethacinin Geliştirilmiş Çözünürlük ve Sözlü İzolasyon ile Formülasyonunun Özel Emülsifilleştirilmesi. Turkish Journal of Pharmaceutical Sciences 14, no.2 (2017): 108 - 119.
MLA	PENJURI Subhash Chandra Bose,DAMINENI Saritha,RAVOURU Nagaraju,POREDDY Srikanth Reddy İndomethacinin Geliştirilmiş Çözünürlük ve Sözlü İzolasyon ile Formülasyonunun Özel Emülsifilleştirilmesi. Turkish Journal of Pharmaceutical Sciences, vol.14, no.2, 2017, ss.108 - 119.
AMA	PENJURI S,DAMINENI S,RAVOURU N,POREDDY S İndomethacinin Geliştirilmiş Çözünürlük ve Sözlü İzolasyon ile Formülasyonunun Özel Emülsifilleştirilmesi. Turkish Journal of Pharmaceutical Sciences. 2017; 14(2): 108 - 119.
Vancouver	PENJURI S,DAMINENI S,RAVOURU N,POREDDY S İndomethacinin Geliştirilmiş Çözünürlük ve Sözlü İzolasyon ile Formülasyonunun Özel Emülsifilleştirilmesi. Turkish Journal of Pharmaceutical Sciences. 2017; 14(2): 108 - 119.
IEEE	PENJURI S,DAMINENI S,RAVOURU N,POREDDY S "İndomethacinin Geliştirilmiş Çözünürlük ve Sözlü İzolasyon ile Formülasyonunun Özel Emülsifilleştirilmesi." Turkish Journal of Pharmaceutical Sciences, 14, ss.108 - 119, 2017.
ISNAD	PENJURI, Subhash Chandra Bose vd. "İndomethacinin Geliştirilmiş Çözünürlük ve Sözlü İzolasyon ile Formülasyonunun Özel Emülsifilleştirilmesi". Turkish Journal of Pharmaceutical Sciences 14/2 (2017), 108-119.