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Læknablaðið - 15.03.1993, Qupperneq 16

Læknablaðið - 15.03.1993, Qupperneq 16
104 LÆKNABLAÐIÐ molecule, or some part of it, into the cavity. Such encapsulation of a drug molecule will affect many of its physicochemical properties. Cyclodextrins are shown to have effect on the aqueous solubility of drugs and their delivery through biological mentbranes, e.g. transcorneal delivery of acetazolamide. Also, they can increase both solubility and chemical stability of many anticancer drugs. There are basically two methods which can be used to increase the transdermal delivery of drugs, i.e. by changing the barrier function of the skin and by increasing the availability of drugs at the skin surface. Penetration enhancers, such as oleic acid and lauroylcholine iodide, alter the skin barrier and thereby increase the permeability of drugs into and through the skin. Cyclodextrins do not penetrate the skin barrier. Drug-cyclodextrin complexes deliver drug molecules to the skin surface where they are released before they partition into the skin. HEIMILDIR 1. Korolkovas A. Essentials of Medicinal Chemistry, 2nd ed. New York: John Wily & Sons, 1988: 53-139. 2. Ariens EJ. A General Introduction to the Field of Drug Design. In: Ariéns EJ. ed. Drug Design, Vol. I. New York: Academic Press, 1971: 1-270. 3. Albert A. Selective Toxicity. New York: John Wily & Sons, 1964: 57-63. 4. Ellmer R. Acetylsalicylsaure. Chem Labor Betr 1978; 7: 82. 5. Loftsson T, Kaminski JJ, Bodor N. Improved Delivery through Biological Membranes VIII. Design, Synthesis and In Vivo Testing of True Prodrugs of Aspirin. J Pharm Sci 1981; 70: 743-9. 6. Loftsson T. Bodor N. Improved Delivery through Biological Membranes IX. The Kinetics and Mechanism of Hydrolysis of Methylsulfinylmethyl 2-Acetoxybenzoate and Related Aspirin Prodrugs. J Pharm Sci 1981; 70: 750-5. 7. Loftsson T, Bodor N. Improved Delivery through Biological Membranes VIII. Percutaneous absorption and Metabolism of the Methylsulfinylmethyl 2- Acetoxybenzoate and Related Aspirin Prodrugs. J Pharm Sci 1981; 70: 756-8. 8. Raghavan K, Loftsson T, Brewster ME, Bodor N. Improved Delivery Through Biological Membranes XLV. Synthesis, Physical-Chemical Evaluation, and Brain Uptake Studies of 2-Chloroethyl Nitrosourea Delivery System. Pharm Res 1992; 9: 743-9. 9. Pop E, Loftsson T, Bodor N. Novel Central Nervous System Targeted Semisynthetic Penicillins. Drug Design Del 1990; 5: 221-37. 10. Bodor N, Loftsson T. Novel Chemical Approaches for Sustained Drug Delivery. In: Robinson JR, Lee VHL, ed. Controlled Drug Delivery: Fundamentals and Applications, 2nd ed. New York: Marcel Dekker, 1987: 337-71. 11. Bodor N. The Application of Soft Dmg Approaches to the Design of Safer Corticosteroids. In: Christophers E, Kligman AM, Schopf E, Stoughton RB, cds. Topical Corticosteroid Therapy: A Novel Approach to Safer Drugs. New York: Raven Press, 1988: 13-25. 12. Bodor N, Loftsson T, Wu W. Metabolism, Distribution, and Transdermal Permeation of a Soft Corticosteroid, Loteprednol Etabonate. Pharm Res 1992; 9: 1275-8. 13. Bodor N, Oshiro Y, Loftsson T. Katovich M, Caldwell W. Soft Drugs VI. The Application of the Inactive Metabolite Approach for Design of Soft /3- Blockers. Pharm Res 1984; 1: 120-5. 14. Loftsson T, Brewster ME, Derendorf H, Bodor N. 2- Hydroxypropyl-/3-cyclodextrin: Properties and Usage in Pharmaceutical Formulations. Pharni Ztg Wiss 1991; 4/136: 5-10. 15. Loftsson T, Bodor N. Effects of 2-Hydroxypropyl- /3-cyclodestrin on Aqueous Solubility of Drugs and Transdermal Delivery of 17/3-Estradiol. Acta Pharm Nord 1989; 1: 185-94. 16. Loftsson T, Ólafsdóttir BJ, Friðriksdóttir H. Comparative Study on Inclusion Complexation of Acetylsalicylic Acid, Cholecalciferol and Melphalan with /3- and 7-Cyclodextrin and some of their Derivatives. Acta Pharm Nord 1990; 2: 303-12. 17. Brewster ME, Loftsson T, Baldvinsdóttir J, Bodor N. Stabilization of Aspartame by Cyclodextrins. Int J Pharm 1991; 75: R5-R8. 18. Loftsson T, Friðriksdóttir H, Ólafsdóttir BJ, Guðmundsson Ö. Solubilization and Stabilization of Drugs through Cyclodextrin Complexation. Acta Pharm Nord 1991; 3: 215-17. 19. Loftsson T. Stefánsdóttir Ó, Friðriksdóttir, Gupmundsson Ö. Interactions between Preservatives and 2-Hydroxypropyl-/3-cyclodextrin. Drug Dev Ind Pharm 1992; 18: 1477-84. 20. Kristmundsdóttir T, Loftsson T, Holbrook WP, Ingvarsdóttir K, Friðriksdóttir H. Hönnun og klínískt mat á hýdrókortisón lausn til meðhöndlunar á bólgusjúkdómum í munnholi. Læknablaðið 1992; 78/Fylgirit 22: 66. 21. Friðriksdóttir H, Þórisdóttir S, Sigurðardóttir AM, Loftsson T, Stefánsson E. Áhrif karbóanhýdrasablokkara á augnþrýsting í kanínum. Læknablaðið 1992; 78/ Fylgirit 22: 85. 22. Loftsson T, Björnsdóttir S, Pálsdóttir G, Bodor N. The Effects of 2-Hydroxypropyl-/3-cyclodextrin on the Solubility and Stability of Chlorambucil and Melphalan in Aqueous Solution. Int J Pharm 1989; 57: 63-72. 23. Loftsson T, Ólafsdóttir BJ. The Effect of 2- Hydroxypropyl-/3-cyclodextrin on the Simultaneous Dissolution and Degradation of Chlorambucil. Int J Pharm 1990; 66: 289-92. 24. Brewster ME, Loftsson T, Estes KS, Lin JL, Friðriksdóttir H, Bodor N. Effect of Various Cyclodextrins on Solution Stability and Dissolution Rate of Doxorubicin Hydrochloride. Int J Pharm 1992; 79: 289-99. 25. Loftsson T, Friðriksdóttir H. Degradation of Lomustine (CCNU) in Aqueous Solutions. Int J Pharm 1990; 62: 243-7. 26. Loftsson T, Ólafsdóttir BJ, Baldvinsdóttir J. Estramustine: Hydrolysis, Solubilization, and Stabilization in Aqueous Solutions. Int J Pharm 1992; 79: 107-12. 27. Loftsson T, Baldvinsdóttir J. Degradation of Tauromustine (TCNU) in Aqueous Solutions. Acta Pharm Nord 1992; 4: 129-32. 28. Loftsson T, Ólafsdóttir BJ. Cyclodextrin-accelerated Degradation of /3-Lactam Antibiotics in Aqueous Solutions. Int J Pharm 1991; 67: R5-R7. 29. Pop E, Loftsson T, Bodor N. Solubilization and

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