Mide ülserasyonuna karşı yara iyileşmesini hızlandıran bir ilaç sistemi tasarımı
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Dosyalar
Tarih
2020
Yazarlar
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
Ege Üniversitesi, Fen Bilimleri Enstitüsü
Erişim Hakkı
info:eu-repo/semantics/openAccess
Özet
Gastrik kalış süresi, ilaç emilimini, dolayısıyla oral yoldan verilen ilaçların biyoyararlanımını etkileyen faktörlerden biridir. Gastroretentif sistemler, dozaj formlarının midede kalış süresini uzatan kontrollü ilaç salım sistemleridir. İlaçların gastrik kalış süresini uzatmak için; yüzen sistemler, yüksek yoğunluklu sistemler, mukoadhezif/biyoadhezif sistemler, genişletilebilir sistemler, manyetik sistemler, süper gözenekli hidrojel sistemleri, ikili çalışma sistemleri gibi farklı gastroretentif sistemler önerilmiştir. Yüzen sistemler; gastrointestinal hareketi etkilememeleri ve formülasyon geliştirmenin kısmen kolay olması nedeniyle en çok tercih edilen sistemlerden biridir. Yüzen sistemler, efervesan sistemler ve efervesan olmayan sistemler olarak ikiye ayrılabilir. Efervesan sistemler; gaz oluşumuna dayalı sistemler olduklarından, bu sistemler yüzme gecikme zamanına sahiptir. Bu nedenle, bu süre içerisinde dozaj formu, işlevini yerine getiremeden mideden boşaltılabilir. Düşük yoğunluklu malzemelerin dahil edilmesi yoluyla geliştirilen yüzen sistemler, yüzme gecikme zamanına sahip olmamalarından dolayı ilgi çekmektedir.
Bu çalışmada; hava bölmesi içeren boncuk tipi yüzen gastroretentif sistemlerin geliştirilmesi için yeni ve basit bir yöntem önerilmektedir. İlk kez iç kanaldan hava dış kanaldan aljinat çözeltisi verilerek yüzen hava içeren boncuk tipi gastroretentif sistemler üretilmiştir. Bu amaçla; ilk olarak hava içeren boş boncuklar üretmek için, farklı konsantrasyondaki polimer çözeltileri farklı iğne sistemleri ile denenmiş, polimer çözeltisinin akış hızı ve havanın akış hızı optimize edilmiştir. Yapılan çalışmalar sonucunda; ilaç yüklü hava içeren boncuk formülasyonları üretmek için 19G-27G iğne sistemi uygun bulunmuştur. Model ilaç olarak Helicobacter pilori tedavisinde kullanılan amoksisilin trihidrat kullanılmıştır. 19G-27G iğne sistemiyle üretilen ilaç yüklü hava içeren boncuklar elde etmek için uygun polimer-ilaç karışımı akış hızı ve hava akış hızı belirlenmiştir. İki farklı formülasyon için ilaç enkapsülasyonu %69,70±4,36 ve %67,29±6,44 olarak bulunmuştur. Geliştirilen yöntemle üretilen yüzen sistemlerin yüzme gecikme zamanı olmadan hemen yüzdüğü gözlemlenmiştir. İç kanaldan hava, dış kanaldan polimer ilaç karışımı verilerek hava bölmesi içeren yüzen sistemlerin başarılı bir şekilde üretilebileceği sonucuna varılmıştır. Geliştirilen yöntemle üretilen hava içeren yüzen formülasyonların H. pilori tedavisinde etkin, ekonomik ve güvenilir bir tedavi alternatifi olması beklenmektir. Geliştirilen yöntemin yüzen gastroretentif sistemlerin geliştirilmesi üzerine literatüre yenilik getirmesi, daha etkin ve güvenilir formülasyon geliştirilmesine yönelik çalışmalara katkı sağlaması ve yeni yaklaşımlara ışık tutması beklenmektedir.
Gastric residence time is one of the factors that affect drug absorption and therefore the bioavailability of orally administered drugs. Gastroretentive drug delivery systems are controlled drug delivery systems that extend the residence duration of dosage forms in the stomach. To prolong the gastric residence of medicines; different gastroretentive systems such as floating systems, high density systems, mucoadhesive/bioadhesive systems, expandable systems, magnetic systems, superporous hydrogel systems, dual working systems have been proposed. Floating systems are one of the most preferred systems due to the fact that they do not affect gastrointestinal motility and formulation development is partially easy. Floating systems can be divided into two as effervescent systems and non-effervescent systems. Effervescent systems; since they are systems based on gas formation, these systems have a floating lag time. Therefore, during this period, the dosage form can be emptied from the stomach without performing its function. Floating systems developed by the inclusion of low-density materials are of interest because they do not have a floating lag time. In this study; A new and simple method is proposed for the development of bead-type floating gastroretentive systems containing air compartment. For the first time, the technique has been developed to produce floating bead-type gastroretentive systems containing air by applying alginate solution from the outer channel and air from inner channel. For this purpose; initially, in order to produce blank beads containing air, polymer solutions of different concentrations were tried with different needle systems and the flow rate of the polymer solution and the flow rate of the air were optimized. As a result, the needle system 19G-27G was found suitable to produce drug loaded bead formulations containing air. Amoxicillin trihydrate used in the treatment of Helicobacter pylori has been chosen as a model drug. The appropriate polymer-drug mixture flow rate and air flow rate were determined to obtain drug loaded beads containing air produced with the 19G-27G needle system. Drug encapsulation for two different formulations were found %69,70±4,36 and %67,29±6,44. It has been observed that the floating systems produced by the developed method immediately float without floating lag time. It was concluded that floating systems including air compartment can be produced successfully by giving air from the inner channel and polymer-drug mixture from the outer channel. It is expected that air containing floating formulations produced by the developed method will be an effective, economical and reliable treatment alternative in H. pylori eradication treatment. It is expected that the developed method will bring innovation to the literature about the development of floating gastroretentive systems, contribute to studies for developing a more effective and reliable formulation, and shed light on new approaches.
Gastric residence time is one of the factors that affect drug absorption and therefore the bioavailability of orally administered drugs. Gastroretentive drug delivery systems are controlled drug delivery systems that extend the residence duration of dosage forms in the stomach. To prolong the gastric residence of medicines; different gastroretentive systems such as floating systems, high density systems, mucoadhesive/bioadhesive systems, expandable systems, magnetic systems, superporous hydrogel systems, dual working systems have been proposed. Floating systems are one of the most preferred systems due to the fact that they do not affect gastrointestinal motility and formulation development is partially easy. Floating systems can be divided into two as effervescent systems and non-effervescent systems. Effervescent systems; since they are systems based on gas formation, these systems have a floating lag time. Therefore, during this period, the dosage form can be emptied from the stomach without performing its function. Floating systems developed by the inclusion of low-density materials are of interest because they do not have a floating lag time. In this study; A new and simple method is proposed for the development of bead-type floating gastroretentive systems containing air compartment. For the first time, the technique has been developed to produce floating bead-type gastroretentive systems containing air by applying alginate solution from the outer channel and air from inner channel. For this purpose; initially, in order to produce blank beads containing air, polymer solutions of different concentrations were tried with different needle systems and the flow rate of the polymer solution and the flow rate of the air were optimized. As a result, the needle system 19G-27G was found suitable to produce drug loaded bead formulations containing air. Amoxicillin trihydrate used in the treatment of Helicobacter pylori has been chosen as a model drug. The appropriate polymer-drug mixture flow rate and air flow rate were determined to obtain drug loaded beads containing air produced with the 19G-27G needle system. Drug encapsulation for two different formulations were found %69,70±4,36 and %67,29±6,44. It has been observed that the floating systems produced by the developed method immediately float without floating lag time. It was concluded that floating systems including air compartment can be produced successfully by giving air from the inner channel and polymer-drug mixture from the outer channel. It is expected that air containing floating formulations produced by the developed method will be an effective, economical and reliable treatment alternative in H. pylori eradication treatment. It is expected that the developed method will bring innovation to the literature about the development of floating gastroretentive systems, contribute to studies for developing a more effective and reliable formulation, and shed light on new approaches.
Açıklama
Anahtar Kelimeler
Gastroretentif Sistemler, Yüzen Gastroretentif Sistemler, Hava İçeren Yüzen Sistem Üretimi İçin Yeni Bir Yöntem, Sodyum Aljinat, Helicobacter Pilori, Gastroretentive Drug Delivery Systems, Floating Drug Delivery Systems, A New Method For The Production of Air-Containing Floating Systems, Sodium Alginate, Helicobacter Pylori
