Nifedipin-Yüklü Partiküler İlaç Tașıyıcı Sistemlere Genel Bir Bakıș

Year 2014, Issue: 2, 73 - 95, 01.06.2014

Emrah Özakar Evren Alğın Yapar Meltem Çetin

Abstract

Dihidropridin grubuna ait bir kalsiyum kanal blokeri olan nifedipin NF başlıca antianjinal ve antihipertansif etkilere sahiptir. NF’nin sudaki çözünürlüğü oldukça düşüktür ve yüksek oranda fotooksidasyona uğrar. NF’nin hemen salım yapan dozaj şekillerinin çeşitli sakıncaları ilk-geçiş etkisinden dolayı düşük oral biyoyararlanım, çoklu dozlama, plazma NF konsantrasyonunda dalgalanmalar ve hipotansiyon, taşikardi gibi yan etkiler mevcuttur. Bu derlemede, NFnin fizikokimyasal ve farmakolojik özelliklerinden kısaca bahsedildikten sonra NF’nin stabilitesi ve farmakolojik etkileri açısından sakıncalarını gidermek/iyileştirmek üzere geliştirilen partiküler ilaç taşıyıcı sistemlerle ilgili çalışmalar ele alınarak sunulmuştur.

Keywords

Mikropartikül, Nanopartikül, Nifedipin, Partiküler ilaç taşıyıcı sistemler

Overview on nifedipine loaded particulate drug delivery systems

Abstract

Nifedipine NF , a dihydropyridine calcium-channel blocker, has primarily antianginal and antihypertensive effects. It is a poorly water-soluble drug and highly sensitive to photo-oxidation. The immediate release NF dosage forms have several disadvantages such as low oral bioavailability due to first-pass effect, multiple dosing fluctuations in the plasma NF concentration and adverse effects such as hypotension, tachycardia . In this review, after briefly mentioned the physicochemical and pharmacological properties of NF, the studies with regard to the particulate drug delivery systems developed to eliminate/improve the drawbacks in terms of the stability and pharmacological effect of NF were presented.

Keywords

Microparticle, Nanoparticle, Nifedipine, Particulate drug delivery systems

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