Parasetamol ile modifiye edilmiş vinil propiyonat-ko-maleik anhidrit polimerinden kontrollü ilaç salımının incelenmesi
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Dosyalar
Tarih
2021
Yazarlar
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Yayıncı
Selçuk Üniversitesi Fen Bilimleri Enstitüsü
Erişim Hakkı
info:eu-repo/semantics/openAccess
Özet
Bu tez çalışmasında, polimerik ilaç taşıyıcı sistem olarak önceden başka bir çalışmada sentezlenen vinilpropiyonat-maleik anhidrit (VPR-MA) kopolimerine parasetamol (VPR-MA-Parasetamol) ilaç etken maddesi bağlanmasıyla oluşturulan sistemlerde kontrollü ilaç salınımları florimetrik yöntemle incelenmiştir. Kontrollü ilaç salınım sistemlerinin temel hedefi, kan plazma konsantrasyonundaki etkin madde miktarını sabitlemektir. Kontrollü ilaç salınım sistemleri pH, iyonik kuvvetler, motilite hızı ve enzim gibi fizyolojik koşulları oluşturan faktörlerden etkilenmektedir. Çevre-duyarlı sistemler, sıcaklık, pH gibi dış ortam koşulları değiştirildiğinde cevap olarak ilaç salımını gerçekleştirirler. pH-duyarlı polimerlerse mide için zararlı ilaçların bağırsakta salınması amacıyla kullanılmaktadır. Mide pH'ında (pH<2.0) büzüşen jeller, bağırsaklarda (pH>7.0) şişerek ilacı salarlar. Ağzın nötral pH'ında (pH=7.0) polimer düşük şişme derecesine sahiptir ve içerisindeki ilaç salınmaz. Kontrollü ilaç salım sistemlerinin incelenmesi kapsamında, öncelikle Parasetamol ile modifiye edilmiş polimerden (VPR-Ko-MA-Parasetamol) in vitro olarak fizyolojik ortamlarda ilaç salım deneyleri yapılmıştır. Bilindiği üzere ester grupları asidik ve bazik ortamlarda hidroliz olurlar. Bu özellikten faydalanarak ester grupları taşıyan modifiye polimerlerin, değişik pH'larda hidrolizi gerçekleştirilmiştir. Parasetamol ile modifiye edilmiş VPR-MA kopolimerinden çözelti ortamına hidroliz olan ilaç miktarının tespit edilebilmesi için, öncelikle VPR-Ko-MA'in, parasetamolün ve parasetamol ile modifiye edilmiş VPR-MA kopolimerinin spektroflorimetrik özellikleri incelenmiştir. Daha sonra, 100 ppm'lik parasetamol stok çözeltisinden hazırlanan farklı derişimlerdeki çözeltilerle belirlenen en uygun spektral şartlarda kalibrasyon grafikleri oluşturulmuştur. Parasetamol modifiyeli kopolimerin, farklı fizyolojik pH'larda (pH=2.0, 4.5, 7.4 ve 9.0) fosfat tamponlarıyla hazırlanan 200 ppm'lik çözeltilerinden, sabit karışma hızında ve 37˚C'da belirli zaman aralıklarında alınan numunelerin, daha önce tespit edilen en uygun absorpsiyon ve florimetrik dalga boylarında spektrumları alınarak, maksimum floresans şiddeti değerleri ölçülmüştür. Her bir pH'da çözeltiye geçen parasetamol miktarları kalibrasyon grafiklerinden yararlanarak belirlenmiştir.
In this thesis, controlled drug release was investigated by fluorimetric method in the system formed by binding paracetamol (VPR-MA-Paracetamol) drug active ingredient to vinyl propionate-maleic anhydride (VPR-MA) copolymer synthesized as a polymeric drug delivery system previously in another study. The main objective of controlled release systems is to stabilize the amount of active substance in the blood plasma concentration. Controlled drug release systems are affected by factors that make up physiological conditions such as pH, ionic forces, motility rate and enzyme. Environmentally sensitive systems deliver drug release in response to changing external ambient conditions such as temperature and pH. The pH-sensitive polymers are used for the release of drugs in the intestine which are harmful to the stomach. The gels shrink at the pH of the stomach (pH <2.0) and release the drug by swelling in the intestines (pH> 7.0). At the neutral pH of the mouth (pH = 7.0) the polymer has a low degree of swelling and the drug is not released. In the scope of the investigation of controlled drug delivery systems, drug release experiments will be carried out in physiological environments in vitro from the paracetamol modified polymer (VPR-Co-MA-Paracetamol). As known, ester groups hydrolyze in acidic and basic environments. By utilizing this feature, hydrolysis of modified polymers bearing ester groups at different pHs were performed. In order to determine the amount of drug hydrolyzed from the paracetamol modified VPR-MA copolymer to the solution medium, the spectrophotometric and spectrofluorometric properties of VPR-Co-MA, paracetamol and paracetamol modified VPR-MA copolymers were studied. Then, calibration graphs were generated by both methods under optimal spectral conditions determined with solutions of different concentrations prepared from 100 ppm paracetamol stock solution. The maximum fluorescence intensities were measured using the most suitable predetermined absorption and fluorimetric wavelengths of the samples of paracetamol modified copolymer which was prepared with 200 ppm solutions prepared with phosphate buffers at different physiological pH (pH: 2.0, 4.5, 7.4 and 9.0), at constant mixing rate at 37°C. The amounts of paracetamol that are introduced into the solution at each pH were determined using calibration graphs.
In this thesis, controlled drug release was investigated by fluorimetric method in the system formed by binding paracetamol (VPR-MA-Paracetamol) drug active ingredient to vinyl propionate-maleic anhydride (VPR-MA) copolymer synthesized as a polymeric drug delivery system previously in another study. The main objective of controlled release systems is to stabilize the amount of active substance in the blood plasma concentration. Controlled drug release systems are affected by factors that make up physiological conditions such as pH, ionic forces, motility rate and enzyme. Environmentally sensitive systems deliver drug release in response to changing external ambient conditions such as temperature and pH. The pH-sensitive polymers are used for the release of drugs in the intestine which are harmful to the stomach. The gels shrink at the pH of the stomach (pH <2.0) and release the drug by swelling in the intestines (pH> 7.0). At the neutral pH of the mouth (pH = 7.0) the polymer has a low degree of swelling and the drug is not released. In the scope of the investigation of controlled drug delivery systems, drug release experiments will be carried out in physiological environments in vitro from the paracetamol modified polymer (VPR-Co-MA-Paracetamol). As known, ester groups hydrolyze in acidic and basic environments. By utilizing this feature, hydrolysis of modified polymers bearing ester groups at different pHs were performed. In order to determine the amount of drug hydrolyzed from the paracetamol modified VPR-MA copolymer to the solution medium, the spectrophotometric and spectrofluorometric properties of VPR-Co-MA, paracetamol and paracetamol modified VPR-MA copolymers were studied. Then, calibration graphs were generated by both methods under optimal spectral conditions determined with solutions of different concentrations prepared from 100 ppm paracetamol stock solution. The maximum fluorescence intensities were measured using the most suitable predetermined absorption and fluorimetric wavelengths of the samples of paracetamol modified copolymer which was prepared with 200 ppm solutions prepared with phosphate buffers at different physiological pH (pH: 2.0, 4.5, 7.4 and 9.0), at constant mixing rate at 37°C. The amounts of paracetamol that are introduced into the solution at each pH were determined using calibration graphs.
Açıklama
Anahtar Kelimeler
Kopolimer, Copolymer, Kontrollü ilaç salımı, Vinilpropiyonat-maleik anhidrit, Parasetamol, Florimetrik metot, Floresans, Controlled drug release, Vinyl propionate-maleic anhydride, Paracetamol, Fluorimetric method, Fluorescence
Kaynak
WoS Q Değeri
Scopus Q Değeri
Cilt
Sayı
Künye
Memiş, Y. (2021). Parasetamol ile modifiye edilmiş vinil propiyonat-ko-maleik anhidrit polimerinden kontrollü ilaç salımının incelenmesi. (Yüksek Lisans Tezi). Selçuk Üniversitesi, Fen Bilimleri Enstitüsü, Konya.
