In vitro and in vivo evaluation of flax seed polymer and chitosan combination as a carrier

RAGHAVAN, Vijaya; JANAKI, G.; RAMAKRISHNAN, A.

In vitro and in vivo evaluation of flax seed polymer and chitosan combination as a carrier

Vijaya RAGHAVAN, (Sri Ramakrishna Inst. of Paramedical Sciences, Pharmaceutics, Coimbatore., Hindistan)

G. JANAKI, (Sri Ramakrishna Inst. of Paramedical Sciences, Pharmaceutics, Coimbatore., Hindistan)

A. RAMAKRISHNAN (Sri Ramakrishna Inst. of Paramedical Sciences, Pharmaceutics, Coimbatore., Hindistan)

Erciyes Tıp Dergisi

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Yıl: 2007 Cilt: 29 Sayı: 3 Sayfa Aralığı: 175 - 183 Metin Dili: Türkçe İndeks Tarihi: 29-07-2022

In vitro and in vivo evaluation of flax seed polymer and chitosan combination as a carrier

Öz:

Amaç: Sunulan çalışma, ucuz ve toksik olmayan keten tohumu ve sitozan kombinasyonunu kolon spesifik taşıyıcı olarak kullanarak, formülasyonun serbestleme özellikleri üzerine sitozanın etkisini araştırmayı amaçlamaktadır.Gereç ve Yöntem: Meselazin tablet özleri nişasta hamurlu ıslak granül olarak hazırlandı ve ağırlıklarına göre 2:3, 3:2 ve 4:1 oranlarında keten tohumu polimeri ve sitozan içeren formülasyonları sıkıştırılarak kaplandı. In vitro serbestleme çalışmalarında bu tabletler kolonik ortamı taklit eden bir sıvıda (Rat çökal içeriğinin ağırlık/hacim olarak %4’ü) ve in vivo deneylerde 6 sağlıklı gönüllüde çalışıldı.Bulgular: Sıkıştırılarak kaplanmış keten tohumu polimeri ve sitozan tabletlerinin 26 saatin sonunda kolon ortamına benzer sıvıda rat çökal içeriğin kolonik bakterileri tarafından parçalandığı bulunması, formülasyonun rat çökal içeriğine duyarlılığına işaret etmektedir. Ağırlık/hacim oranı %4 olan rat çökal içeriği bulunduran fosfat tamponu (pH:6,8) ile yapılan in vitro çalışmalar, 26 saat sonar mesalazinin kümülatif yüzdelerinin 2:3, 3:2, ve 4:1 oranlarında keten tohumu ve sitozan içeren tabletler için sırasıyla 52,16±0,06; 64,10±0,08 ve 98,00±0,19 (ortalama ± standart sapma) olduğunu gösterdi. Altı gönüllüde yapılan in vivo çalışmalar ilaç serbestlenmesinin 5 saatlik ince bağırsak geçiş zamanından hemen sonra başladığını ve ilacın biyoyararlanımının 2:3, 3:2 ve 4:1 oranlarında keten tohumu polimeri ve sitozan içeren tabletler için sırasıyla 196,97±3,02; 245,8±5,10 ve 910,51±9,61 (ortalama ± standart sapma) olduğunu ortaya çıkardı. Yüz on mg sitozan içeren C6 formülasyonu 330 ve 220 mg sitozan içeren C4 ve C5 formülasyonları ile karşılaştırıldığı zaman daha iyi ilaç salımı ve bu nedenle daha yüksek biyoyararlanıma sahip olan elverişli oran olarak bulundu. Sonuç: Çalışmamızın sonuçları 4:1 oranında keten tohumu polimeri ve sitozan içeren sıkıştırılarak kaplanmış tabletlerin daha iyi çözünme profiline, daha yüksek biyoyararlanıma ve bu nedenle kolona hedeflenen ilaçlar için potansiyel bir taşıyıcı olma özelliğine sahip olduğunu göstermektedir.

Anahtar Kelime: İlaç dağıtım sistemleri Çitosan Mesalamin Keten Kolon In vitro

Konular: Genel ve Dahili Tıp

Keten tohumu polimeri ve sitozan kombinasyonun kolon spesifik ilaç dağıtım taşıyıcısı olarak in vivo ve in vitro değerlendirilmesi

Öz:

Purpose: The present investigation is aimed to use an inexpensive, nontoxic naturally available flax seed polymer and chitosan combination as colon-specific drug carriers and to study the influence of chitosan on the release characteristics of the formulation. Materials and Methods: Core tablets of mesalazine were prepared by wet granulation with starch paste and were compression coated with coating formulations containing different weight ratios of flax seed polymer and chitosan 2:3, 3:2 and 4:1. The tablets were subjected to in vitro drug release studies in simulated colonic fluids (4% w/v of rat cecal contents). In vivo evaluation was performed in six healthy human volunteers. Results: The compression coated flax seed polymer and chitosan tablets were found degraded by colonic bacteria of rat cecal contents in simulated colonic fluids at the end of 26 h indicating the susceptibility of the formulation to the rat cecal contents. In vitro studies in pH 6.8 phosphate buffer containing 4% w/v rat cecal contents showed that the cumulative percentage of mesalazine after 26 h were 52.16±0.06, 64.10±0.08 and 98.00±0.19 (mean ± s.d) respectively for tablets containing different weight ratios of flax seed polymer and chitosan 2:3, 3:2 and 4:1. In vivo studies conducted in six healthy male human volunteers for the various formulations revealed that the drug released was intiated only after 5h (i.e) transit time of small intestine and the bioavailability (AUC 0-t*)of the drug was found to be 196.97±3.02, 245.8±5.10 and 910.51±9.61 (mean s.d) respectively for tablets containing different weight ratios of flax seed polymer and chitosan 2:3, 3:2 and 4:1. Formulation C6 which contains 110mg of chitosan when compared to formulation C4 and C5 containg 330mg and 220mg of chitosan is the suitable ratio for the better release of the drug which in turn having higher bioavailability. Conculusion: The results of the present study indicates that compression coated tablets containing 4:1 ratio of flax seed polymer and chitosan held a better dissolution profile, higher bioavailability and hence a potential carrier for drug targeting to colon.

Anahtar Kelime: Flax Colon In Vitro Drug Delivery Systems Chitosan Mesalamine

Konular: Genel ve Dahili Tıp

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

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APA	RAGHAVAN V, JANAKI G, RAMAKRISHNAN A (2007). In vitro and in vivo evaluation of flax seed polymer and chitosan combination as a carrier. , 175 - 183.
Chicago	RAGHAVAN Vijaya,JANAKI G.,RAMAKRISHNAN A. In vitro and in vivo evaluation of flax seed polymer and chitosan combination as a carrier. (2007): 175 - 183.
MLA	RAGHAVAN Vijaya,JANAKI G.,RAMAKRISHNAN A. In vitro and in vivo evaluation of flax seed polymer and chitosan combination as a carrier. , 2007, ss.175 - 183.
AMA	RAGHAVAN V,JANAKI G,RAMAKRISHNAN A In vitro and in vivo evaluation of flax seed polymer and chitosan combination as a carrier. . 2007; 175 - 183.
Vancouver	RAGHAVAN V,JANAKI G,RAMAKRISHNAN A In vitro and in vivo evaluation of flax seed polymer and chitosan combination as a carrier. . 2007; 175 - 183.
IEEE	RAGHAVAN V,JANAKI G,RAMAKRISHNAN A "In vitro and in vivo evaluation of flax seed polymer and chitosan combination as a carrier." , ss.175 - 183, 2007.
ISNAD	RAGHAVAN, Vijaya vd. "In vitro and in vivo evaluation of flax seed polymer and chitosan combination as a carrier". (2007), 175-183.

APA	RAGHAVAN V, JANAKI G, RAMAKRISHNAN A (2007). In vitro and in vivo evaluation of flax seed polymer and chitosan combination as a carrier. Erciyes Tıp Dergisi, 29(3), 175 - 183.
Chicago	RAGHAVAN Vijaya,JANAKI G.,RAMAKRISHNAN A. In vitro and in vivo evaluation of flax seed polymer and chitosan combination as a carrier. Erciyes Tıp Dergisi 29, no.3 (2007): 175 - 183.
MLA	RAGHAVAN Vijaya,JANAKI G.,RAMAKRISHNAN A. In vitro and in vivo evaluation of flax seed polymer and chitosan combination as a carrier. Erciyes Tıp Dergisi, vol.29, no.3, 2007, ss.175 - 183.
AMA	RAGHAVAN V,JANAKI G,RAMAKRISHNAN A In vitro and in vivo evaluation of flax seed polymer and chitosan combination as a carrier. Erciyes Tıp Dergisi. 2007; 29(3): 175 - 183.
Vancouver	RAGHAVAN V,JANAKI G,RAMAKRISHNAN A In vitro and in vivo evaluation of flax seed polymer and chitosan combination as a carrier. Erciyes Tıp Dergisi. 2007; 29(3): 175 - 183.
IEEE	RAGHAVAN V,JANAKI G,RAMAKRISHNAN A "In vitro and in vivo evaluation of flax seed polymer and chitosan combination as a carrier." Erciyes Tıp Dergisi, 29, ss.175 - 183, 2007.
ISNAD	RAGHAVAN, Vijaya vd. "In vitro and in vivo evaluation of flax seed polymer and chitosan combination as a carrier". Erciyes Tıp Dergisi 29/3 (2007), 175-183.