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"How are medicines transported intact through the body to their specific target sites without triggering side effects? The answer is "Drug targeting".This thoroughly application-oriented book gives comprehensive answers to this and many other questions that confront scientists daily in chemical, pharmaceutical and medical research. A concise overview of the most important basic theories, modern forms of therapy and molecular biological tools, it represents a comprehensible introduction to the topic. The book then goes on to deal with strategies for target applications, divided according to target site, for example brain, lungs, liver, blood vessels and tumor cells. The third part is devoted to special, modern techniques, from phage display methods, via the use of tissue slices right up to pharmacokinetic modeling. Throughout, the focus remains on the practical aspect and successful application of the method in question, although a glance at what the future holds is also included. "

"With its particular emphasis on the constitutive activity of G-protein-coupled receptors (GPCRs)s, this book comprehensively discusses an important biological process that has not yet been covered in such depth in any other existing books on GPCRs. The international team of highly distinguished authors addresses in detail current models and concepts, to introduce medicinal chemists, physiologists, pharmacologists, and medical researchers into the advances in the understanding of GPCR activation and constitutive activity. In addition, the book provides an overview on methods of investigating constitutive GPCR activity. The text is well illustrated by selected experimental data and schemes.The chapters are all cross-referenced with each other and cover general mechanisms, methodological approaches and cover selected important GPCR systems, the consequences for drug action, including, side effects, and rational drug design for GPCR targets. The text is backed by abundant case studies and methodological advice for analysing GPCRs, covering selected pharmacologically relevant GPCR systems, the consequences for drug action, including unwanted side effects, and rational drug design for GPCR targets. It is a highly practical reference for researchers in academia and industry."

"The book covers a broad spectrum of topics, ranging from pioneering research in the field of classical steroid hormones to very recently discovered orphan receptors and their modulators. State of the art technologies are also discussed in the individual chapters that help to develop a deeper insight into the biochemical and pharmacological principles underlying the biological function of nuclear receptors.Edited by two experts working at the pioneering pharmaceutical company and major global player in hormone-derived drugs, this handbook and reference systematically treats the drug development aspects of all human nuclear receptors, including recently characterized receptors such as PPAR, FXR and LXR. Authors from leading pharmaceutical companies around the world present examples and real-life data from their own work."

"Sediaan kolon tertarget digunakan untuk penghantaran spesifik terapi penyakit yang berada di kolon, diharapkan obat tidak terlepas di dalam gastrointestinal bagian atas. Beberapa sediaan dapat digunakan sebagai sediaan kolon tertarget, salah satunya adalah Beads. Tujuan dari penelitian ini adalah optimasi dari formulasi beads tetrandrine, sebagai antifibrosis dengan aktifitas lokal pada kolon, dengan alginat dan hidroksi propil metil selulosa dalam berbagai konsentrasi sebagai polimer. Beads dikarakterisasi dengan SEM, DSC, XRD, kadar air, indeks daya mengembang, dan uji in vitro. Beads yang terbuat dari alginat 2 ,b/v dan konsentrasi Hidroksi propil metil selulosa HPMC yang tertinggi 2 , b/v menghasilkan beads dengan efisiensi penjerapan yang tinggi sebesar 49,83 0,46 dan ukuran partikel yang paling besar dalam kisaran ukuran 888 ndash; 914. Beads dengan konsentrasi HPMC tertinggi dapat mengembang dengan indeks mengembang hingga 1116,53 . Pengujian in-vitro menunjukan ketidak mampuan beads dalam menahan pelepasan tetrandrine di dalam medium HCl pH 1,2, tetrandrine yang terlepas sebesar 51,86 0,007 . Bertambahnya konsentrasi HPMC menyebabkan peningkatan di dalam distribusi ukuran, index daya mengembang dan efisiensi penjerapan. HPMC dapat dibuktikan menahan pelepasan tetrandrine.

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Colon targeted drug delivery system is addressing specific needs in the therapy of colon based diseases, with this drug delivery system less drug expected to be released in the upper gastrointestinal. One of pharmaceutical dosage can be used for colon targeted drug delivery system is beads. The objective of the current study was to optimize the formulation of antifibrotic tetrandrine beads with alginate and various concentrations of HPMC as polymers. Beads were characterized by SEM, DSC, XRD, moisture content, swelling measurements, and in vitro release studies. Alginate 2 , w v and highest HPMC concentration 2 , w v produced beads with higher entrapment efficiency of 49.83 0.46 , and had a particle size in the range of 888 ndash 914. Beads with highest HPMC concentration reached 1116.53 of its swelling index. In vitro release studies showed that beads inadequate to retain tetrandrine in stomach condition, it release 51.86 0.007 . Increase in the concentration of HPMC lead to increases in size distribution, swelling index, and entrapment efficiency. Formulation with highest concentration of HPMC perform a slower drug release than the rest formula."

"Sistem penghantaran ke kolon banyak digunakan untuk pengobatan penyakit yang terdapat pada kolon secara lokal. Sehingga, diperlukan suatu sistem penghantaran obat yang mampu mempertahankan kondisi obat hingga mencapai kolon dan melindungi obat dari berbagai macam kondisi pada saluran gastrointestinal. Salah satu obat yang memerlukan sistem penghantaran ini adalah tetrandrine. Pada penelitian ini, dilakukan pembuatan beads dengan menggunakan campuran polimer natrium alginat dan kitosan. Beads dibuat dalam tiga perbandingan alginat:kitosan, yaitu 2:0,25; 2:0,5 dan 2:0,75. Masing-masing formulasi akan dilakukan karakterisasi meliputi bentuk dan morfologi beads, ukuran partikel, efisiensi proses, kadar air, efisiensi penjerapan dan kandungan obat, uji termal, analisis difraksi sinar x, uji indeks mengembang, spektroskopi FTIR dan uji pelepasan obat secara in vitro. Hasil karakterisasi menunjukkan beads dengan perbandingan alginat:kitosan 2:0,75 menghasilkan karakterisasi beads yang paling baik. Hal ini dilihat dari hasil uji efisiensi penjerapan yang dilakukan beads perbandingan alginat:kitosan 2:0,75 menghasilkan nilai sebesar 50,71 0,31 dengan nilai kandungan obat 16,90 0,10 , kemudian pada hasil uji pelepasan secara in-vitro memiliki kemampuan menahan pelepasan obat paling baik dengan nilai pelepasan kumulatif pada medium HCl pH 1,2 41,63 0,87 , medium dapar fosfat pH 7,4 Tween 80 2 52,54 1,22 dan medium dapar fosfat pH 6,8 Tween 80 2 66,68 4,33.

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Colon drug delivery widely used for the treatment local colonic diseases. Therefore, a drug delivery system must be able to maintain the condition of the drug active substance to reach the colon and protect the drug from various conditions in the gastrointestinal tract. The aim of this research was to prepare beads using a mixture of sodium alginate and chitosan polymers. One of the drugs that required this delivery system is tetrandrine. Beads were made in three different formulations with ratio alginat chitosan are 2 0.25 2 0.5 and 2 0.75. Each Formulation would be characterized including morphology of beads, particle size, process efficiency, moisture content, entrapment efficiency and drug loading, thermal analysis, x ray diffraction analysis, swelling analysis, spectroscopy FTIR and in vitro drug release. Ratio alginate chitosan 2 0.75 produced the best characterization of beads. The result of entrapment efficiency from alginate chitosan 2 0.75 50.71 0.31 with the percentage of drug loading 16.90 0.10 , then the result in vitro drug release of alginate chitosan 2 0.75 had the best ability to withstand drug with cumulative release value on HCl medium pH 1,2 41.63 0.87 , phosphate buffer saline pH 7,4 Tween 80 2 52.54 1.22 and phosphate buffer saline pH 6,8 Tween 80 2 66.68 4.33."

"Sistem penghantaran obat ke kolon harus mampu menunda pelepasan obat hingga sistem mencapai tempat targetnya, yaitu kolon. Pada penelitian ini dipilih bentuk sediaan beads menggunakan gabungan dua polimer alginat dan Polivinil Alkohol PVA sebagai sistem pembawa Tetrandrine menuju kolon. Beads diformulasikan ke dalam tiga formula dengan perbandingan konsentrasi alginat:PVA yang berbeda-beda yaitu 2:0,5, 2:0,75 dan 2:1. Kemudian dilakukan karakterisasi meliputi morfologi, distribusi ukuran partikel, efisiensi proses, efisiensi penjerapan, penentuan kadar air, uji termal DSC, Difraksi Sinar X XRD , Spektroskopi FTIR, index mengembang, dan uji pelepasan obat secara in vitro. Formula 3 dengan perbandingan alginat dan PVA 2:1 merupakan formula terbaik dengan diameter rata-rata beads 790,87 75,64 ?m dan efisiensi penjerapan 32,12 0,84 . Uji pelepasan obat dilakukan dalam medium HCl pH 1,2 2jam , dapar fosfat pH 7,4 Tween80 2 3 jam dan dapar fosfat pH 6,8 Tween80 2 3 jam. Profil pelepasan obat in vitro dalam medium HCl pH 1,2 Formula 1, Formula 2, dan Formula 3 secara berurutan adalah 84,13 0,60, 73,12 1,64 , dan 66,57 1,56. Hasil ini menunjukan semua formula belum mampu menghasilkan sediaan kolon tertarget yang ideal.

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Colon drug delivery system should be able to maintain drug release until the system reaches its target. In this research, beads was selected as drug carrier system to deliver tetrandrine to colon using combination of two polymers, alginate and Polyvinyl Alcohol PVA . Beads were formulated into three formulas with different alginate PVA concentration 2 0.5, 2 0.75, and 2 1. Each formula were characterized based on morphology beads, particle size distribution, process efficiency, entrapment efficiency, drug loading percentage, moisture content, thermal test DSC , X ray Diffraction XRD , FTIR, swelling analysis and in vitro drug release test. Formula 3 with concentration alginate PVA 2 1 was the best formula with size of beads 790,87 75.64 m and an entrapment efficiency 32.12 0.84 . Drug release test was perform in HCl pH 1,2 2 hours , phosphate buffer pH 7,4 Tween80 2 3 hours , and phosphate buffer pH 6,8 Tween80 2 3 hours . Cumulative drug release of three formulas beads in hydrochloric acid medium was 84.13 0,60 , 73.12 1,64 , and 66.57 1,56 , respectively. Based on those result, all formulas beads are not ideal to be colon targeted dosage form, yet."