Expandable gastroretentive dosage forms

Journal of Controlled Release

Volumn 90, Issue 2, 2003, Pages 143-162

  Klausner, Eytan A ^a   Lavy, Eran ^b   Friedman, Michael ^a   Hoffman, Amnon ^a  

^a HEBREW UNIVERSITY OF JERUSALEM   (Israel)

^b HEBREW UNIVERSITY OF JERUSALEM   (Israel)

Author keywords

Controlled release; Expansion; Gastroretentive; Narrow absorption window drugs; Swelling; Unfolding

Indexed keywords

ABSORPTION; IMAGING TECHNIQUES; VETERINARY MEDICINE;

VETERINARY USES;

DRUG DOSAGE;

ACICLOVIR; ALENDRONIC ACID; ALPHA TOCOPHEROL; ATENOLOL; CAPTOPRIL; CINNARIZINE; CIPROFLOXACIN; CISAPRIDE; FUROSEMIDE; GANCICLOVIR; GLIPIZIDE; GRANULOCYTE COLONY STIMULATING FACTOR; KETOPROFEN; LEVODOPA; MELATONIN; METFORMIN; MINOCYCLINE; MISOPROSTOL; NICARDIPINE; RIBOFLAVIN; SOTALOL; TETRACYCLINE; VERAPAMIL;

DRUG ABSORPTION; DRUG DELIVERY SYSTEM; DRUG DOSAGE FORM; DRUG EFFECT; DRUG RELEASE; ECHOGRAPHY; GAMMA SCINTIGRAPHY; GASTROINTESTINAL TRACT; GASTROINTESTINAL TRACT FUNCTION; GASTROSCOPY; HUMAN; IN VIVO STUDY; NONHUMAN; NUCLEAR MAGNETIC RESONANCE IMAGING; PERISTALSIS; PRIORITY JOURNAL; REVIEW; STOMACH EMPTYING; STOMACH MOTILITY;

EID: 0037782350     PISSN: 01683659     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0168-3659(03)00203-7     Document Type: Review

References (143)

1. Hoffman A. Pharmacodynamic aspects of sustained release preparations. Adv. Drug Deliv. Rev. 33:1998;185-199.
2. Hwang S.-J., Park H., Park K. Gastric retentive drug-delivery systems. Crit. Rev. Ther. Drug Carrier Syst. 15:(3):1998;243-284.
3. Hoffman A., Stepensky D. Pharmacodynamic aspects of modes of drug administration for optimization of drug therapy. Crit. Rev. Ther. Drug Carrier Syst. 16:(6):1999;571-639.
4. Deshpande A.A., Rhodes C.T., Shah N.H., Malick A.W. Controlled-release drug delivery systems for prolonged gastric residence: an overview. Drug Dev. Ind. Pharm. 22:(6):1996;531-539.
5. Singh B.N., Kim K.H. Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention. J. Control. Release. 63:2000;235-259.
6. Moes A.J. Gastroretentive dosage forms. Crit. Rev. Ther. Drug Carrier Syst. 10:(2):1993;143-195.
7. Rubinstein A., Friend D.R. Domb A.J. Polymeric Site-Specific Pharmacotherapy. 1994;267-313 Wiley, Chichester.
8. Washington N., Washington C., Wilson C.G. Physiological Pharmaceutics. II. 2001;Taylor and Francis, New York.
9. Bannister L.H. Alimentary system. Williams P.L. Gray's Anatomy. XXXVIII. 1995;1683-1812 Churchill Livingstone, New York.
10. Rubinstein A., Li V.H.K., Gruber P., Robinson J.R. Yacobi A., Halperin-Walega E. Oral Sustained Release Formulations: Design and Evaluation. 1988;125-156 Pergamon Press, New York.
11. Thibodeau G.A., Patton K.T. Anatomy and Physiology. III. 1996;Mosby, St. Louis.
12. Hasler W.L. Yamada T. Textbook of Gastroenterology II. Vol. 1:1995;181-206 J.B. Lippincott, Philadelphia.
13. Dressman J.B., Berardi R.R., Dermentzoglou L.C., Russel T.L., Schmaltz S.P., Barnett J.L., Jarvenpaa K.M. Upper gastrointestinal (GI) pH in young, healthy men and women. Pharm. Res. 7:(7):1990;756-761.
14. Russell T.L., Berardi R.R., Barnett J.L., Dermentzoglou L.C., Jarvenpaa K.M., Schmaltz S.P., Dressman J.B. Upper gastrointestinal pH in seventy-nine healthy, elderly, north American men and women. Pharm. Res. 10:(2):1993;187-196.
15. Munk J., Gannaway R., Hoare M., Johnson A. Duthie H.L. Gastrointestinal Motility in Health and Disease. 1978;349-359 MTP Press, Lancaster.
16. Salessiotis N. Measurement of the diameter of the pylorus in man. I. Experimental project for clinical application. Am. J. Surg. 124:1972;331-333.
17. Ogihara H., Suzuki T., Nagamachi Y., Inui K., Takata K. Peptide transporter in the rat small intestine: ultrastructural localization and the effect of starvation and administration of amino acids. Histochem. J. 31:1999;169-174.
18. Barley N.F., Howard A., O'Callaghan D., Legon S., Walters J.R.F. Epithelial calcium transporter expression in human duodenum. Am. J. Physiol. Gastrointest. Liver Physiol. 280:2001;G285-G290.
19. Cousins R.J., McMahon R.J. Integrative aspects of zinc transporters. J. Nutr. 130:2000;1384s-1387s.
20. Read N.W., Sugden K. Gastrointestinal dynamics and pharmacology for the optimum design of controlled-release oral dosage forms. CRC Crit. Rev. Ther. Drug Carrier Syst. 4:(3):1987;221-263.
21. Kararli T.T. Comparison of the gastrointestinal anatomy, physiology, and biochemistry of humans and commonly used laboratory animals. Biopharm. Drug Dispos. 16:1995;351-380.
22. Davis S.S., Wilding E.A., Wilding I.R. Gastrointestinal transit of a matrix tablet formulation: comparison of canine and human data. Int. J. Pharm. 94:1993;235-238.
23. Rubinstein A. Approaches and opportunities in colon-specific drug delivery. Crit. Rev. Ther. Drug Carrier Syst. 12:(2-3):1995;101-149.
24. Rubinstein A., Tirosh B., Baluom M., Nassar T., David A., Radai R., Gliko-Kabir I., Friedman M. The rationale for peptide drug delivery to the colon and the potential of polymeric carries as effective tools. J. Control. Release. 46:1997;59-73.
25. Minami H., McCallum R.W. The physiology and pathophysiology of gastric emptying in humans. Gastroenterology. 86:1984;1592-1610.
26. Gruber P., Rubinstein A., Li V.H.K., Bass P., Robinson J.R. Gastric emptying of nondigestible solids in the fasted dog. J. Pharm. Sci. 76:(2):1987;117-122.
27. Ehrlein H.-J. Motility of the pyloric sphincter studied by the inductograph method in conscious dogs. Am. J. Physiol. 254:1988;G650-G657.
28. Wilding I. Site-specific drug delivery in the gastrointestinal tract. Crit. Rev. Ther. Drug Carrier Syst. 17:(6):2000;557-620.
29. Ehrlein H.-J. A new technique for simultaneous radiography and recording of gastrointestinal motility in unanesthetized dogs. Lab. Anim. Sci. 30:(5):1980;879-884.
30. Kelly K.A., Morley K.D., Wilbur B.G. Effect of corporal and antral gastrojejunostomy on canine gastric emptying of solid spheres and liquids. Br. J. Surg. 60:(11):1973;880-884.
31. Shalaby W.S.W., Blevins W.E., Park K. Use of ultrasound imaging and fluoroscopic imaging to study gastric retention of enzyme-digestible hydrogels. Biomaterials. 13:(5):1992;289-296.
32. Backon J., Hoffman A. The lateral decubitus position may affect gastric emptying through an autonomic mechanism: the skin pressure-vegetative reflex. Br. J. Clin. Pharmacol. 32:1991;138-139.
33. Mojaverian P., Vlasses P.H., Kellner P.E., Rocci M.L. Jr. Effects of gender, posture, and age on gastric residence time of an indigestible solid: pharmaceutical considerations. Pharm. Res. 5:(10):1988;639-644.
34. Dressman J.B., Amidon G.L., Reppas C., Shah V.P. Dissolution testing as a prognostic tool for oral drug absorption: immediate release dosage forms. Pharm. Res. 15:(1):1998;11-22.
35. Khosla R., Davis S.S. The effect of tablet size on the gastric emptying of nondisintegrating tablets. Int J. Pharm. 62:1990;R9-R11.
36. Hamilton J.K., Polter D.E. Sleisenger M.H., Fordtran J.S. Gastrointestinal Disease. V. Vol. 1:1993;286-292 W.B. Saunders, Philadelphia.
37. Coupe A.J., Davis S.S., Evans D.F., Wilding I.R. Correlation of the gastric emptying of nondisintegrating tablets with gastrointestinal motility. Pharm. Res. 8:(10):1991;1281-1285.
38. Mojaverian P., Reynolds J.C., Ouyang A., Wirth F., Kellner P.E., Vlasses P.H. Mechanism of gastric emptying of a nondisintegrating radiotelemetry capsule in man. Pharm. Res. 8:(1):1991;97-100.
39. R.H. Laby, Device for administration to ruminants, US Patent 3844285, October 29, 1974.
40. M.D. Brewer, G.J.L. Griffin, Sustained release compositions, US Patent 4228149, October 14, 1980.
41. G.J.L. Griffin, M.D. Brewer, Sustained drug release device, US Patent 4268497, May 19, 1981.
42. R.H. Johnson, E.L. Rowe, Medicinal dosage forms of unpolymerized thiolated gelatin with a crosslinking accelerating agent providing slowly released medication from a swollen matrix, US Patent 3574820, April 13, 1971.
43. A.S. Michaels, Drug delivery device with self actuated mechanism for retaining device in selected area, US Patent 3786813, January 22, 1974.
44. A.S. Michaels, J.D. Bashwa, A. Zaffaroni, Integrated device for administering beneficial drug at programmed rate, US Patent 3901232, August 26, 1975.
45. R.C. Mamajek, E.S. Moyer, Drug-dispensing device and method, US Patent 4207890, June 17, 1980.
46. J. Urquhart, F. Theeuwes, Drug delivery system comprising a reservoir containing a plurality of tiny pills, US Patent 4434153, February 28, 1984.
47. Shalaby W.S.W., Park K. Biochemical and mechanical characterization of enzyme-digestible hydrogels. Pharm. Res. 7:(8):1990;816-823.
48. Shalaby W.S.W., Blevins W.E., Park K. In vitro and in vivo studies of enzyme-digestible hydrogels for oral drug delivery. J. Control. Release. 19:1992;131-144.
49. L.J. Caldwell, C.R. Gardner, R.C. Cargill, Drug delivery device which can be retained in the stomach for a controlled period of time, US Patent 4735804, April 5, 1988.
50. L.J. Caldwell, C.R. Gardner, R.C. Cargill, T. Higuchi, Drug delivery device which can be retained in the stomach for a controlled period of time, US Patent 4758436, July 19, 1988.
51. L.J. Caldwell, C.R. Gardner, R.C. Cargill, Drug delivery device which can be retained in the stomach for a controlled period of time, US Patent 4767627, August 30, 1988.
52. Cargill R., Caldwell L.J., Engle K., Fix J.A., Porter P.A., Gardner C.R. Controlled gastric emptying. 1. Effects of physical properties on gastric residence times of nondisintegrating geometric shapes in beagle dogs. Pharm. Res. 5:(8):1988;533-536.
53. Cargill R., Engle K., Gardner C.R., Porter P., Sparer R.V., Fix J.A. Controlled gastric emptying. II. In vitro erosion and gastric residence times of an erodible device in beagle dogs. Pharm. Res. 6:(6):1989;506-509.
54. Fix J.A., Cargill R., Engle K. Controlled gastric emptying. III. Gastric residence time of a nondisintegrating geometric shape in human volunteers. Pharm. Res. 10:(7):1993;1087-1089.
55. S.A. Pogany, G.M. Zentner, Bioerodible thermoset elastomers, US Patent 5217712, June 8, 1993.
56. T. Sonobe, S. Watanabe, M. Katsuma, N. Takamatsu, Y. Konno, H. Takagi, Gastric retention device, Eur. Patent 0415671, March 6, 1991.
57. W.J. Curatolo, J. Lo, Gastric retention system for controlled drug release, US Patent 5443843, August 22, 1995.
58. Chen J., Park K. Synthesis and characterization of superporous hydrogel composites. J. Control. Release. 65:2000;73-82.
59. Chen J., Blevins W.E., Park H., Park K. Gastric retention properties of superporous hydrogel composites. J. Control. Release. 64:2000;39-51.
60. K. Park, H. Park, Super absorbent hydrogel foams, US Patent 5750585, May 12, 1998.
61. K. Park, J. Chen, H. Park, Hydrogel composites and superporous hydrogel composites having fast swelling, high mechanical strength, and superabsorbent properties, US Patent 6271278, August 7, 2001.
62. Klausner E.A., Lavy E., Stepensky D., Friedman M., Hoffman A. Novel gastroretentive dosage forms: evaluation of gastroretentivity and its effect on riboflavin absorption in dogs. Pharm. Res. 19:(10):2002;1516-1523.
63. Klausner E.A., Eyal S., Lavy E., Friedman M., Hoffman A. Novel levodopa gastroretentive dosage form: in vivo evaluation in dogs. J. Control. Release. 88:(1):2003;117-126.
64. E.A. Klausner, Design and characterization of novel gastroretentive dosage forms for widening the therapeutic potential of narrow absorption window drugs; Ph.D. Dissertation, The Hebrew University of Jerusalem, 2002.
65. Klausner E., Lavy E., Cserepes E., Barta M., Friedman M., Hoffman A. Novel gastroretentive dosage forms retain in the stomach of healthy volunteers for prolonged periods of time. Proceed. Int'l Symp. Control. Rel. Bioact. Mater., 29, Seoul: 2002.
66. M. Friedman, E. Klausner, E. Lavy, A. Hoffman, Gastroretentive controlled release pharmaceutical dosage forms, Int. Application WO0137812, 2001.
67. E.A. Klausner, E. Lavy, D. Stepensky, E. Cserepes, M. Barta, M. Friedman, A. Hoffman, Furosemide pharmacokinetics and pharmacodynamics following gastroretentive dosage form administration to healthy volunteers. J. Clin. Pharmacol. in press (2003).
68. E.A. Klausner, E. Lavy, E. Cserepes, M. Barta, M. Friedman, A. Hoffman, Novel gastroretentive dosage forms: evaluation of gastroretentivity and its effect on levodopa absorption in healthy volunteers. (2003) submitted for publication.
69. J.W. Shell, J. Louie-Helm, M. Markey, Extending the duration of drug release within the stomach during the fed mode, US Patent 6340475, January 22, 2002.
70. Gusler G., Gorsline J., Levy G., Zhang S.Z., Weston I.E., Naret D., Berner B. Pharmacokinetics of metformin gastric-retentive tablets in healthy volunteers. J. Clin. Pharmacol. 41:2001;655-661.
71. Gusler G., Berner B. Metformin (GR) gastric retentive tablets: GI transit and pharmacokinetics in healthy volunteers. Millennial World Congress of Pharmaceutical Sciences. Abstract 2-5019, San Francisco: 2000.
72. Louie-Helm J., Fell R., Shell J.N., Dye D., Levy G., Gorsline J., Mueller M., Dilger C., Berner B. Pharmacokinetics of ciprofloxacin gastric retentive (GR™) tablets in healthy volunteers. Proceed. Int'l. Symp. Control. Rel. Bioact. Mater., 28, San Diego: 2001.
73. A.M. Wilson, Z. Ramtoola, O. Conaghey, C.A. McGoldrick, S.Y. Hou, K.I. Cumming, Pharmacoscintigraphic evaluation of a novel controlled release technology (endogastric therapeutic systems) for gastric retention in healthy volunteers. AAPS PharmSci 4(4), Abstract T3274 (2002).
74. Chapron D.J., Korman L.B., Barry W.L. Gastric retention of enteric-coated magnesium chloride tablets. Ann. Pharmacother. 28:1994;874-877.
75. Wise C.M., Owen D.S. Jr., Jessee E.F. Jr. Another case of salicylate intoxication with enteric coated aspirin: association with gastric outlet obstruction. J. Rheumatol. 9:(3):1982;482-483.
76. Chiou W.L., Barve A. Linear correlation of the fraction of oral dose absorbed of 64 drugs between humans and rats. Pharm. Res. 15:(11):1998;1792-1795.
77. Hossain M., Abramowitz W., Watrous B.J., Szpunar G.J., Ayres J.W. Gastrointestinal transit of nondisintegrating, nonerodible oral dosage forms in pigs. Pharm. Res. 7:(11):1990;1163-1166.
78. Davies B., Morris T. Physiological parameters in laboratory animals and humans. Pharm. Res. 10:(7):1993;1093-1095.
79. Dressman J.B. Comparison of canine and human gastrointestinal physiology. Pharm. Res. 3:(3):1986;123-131.
80. Itoh T., Higuchi T., Gardner C.R., Caldwell L. Effect of particle size and food on gastric residence time of nondisintegrating solids in beagle dogs. J. Pharm. Pharmacol. 38:1986;801-806.
81. Kamba M., Seta Y., Kusai A., Nishimura K. Evaluation of the mechanical destructive force in the stomach of dog. Int. J. Pharm. 228:2001;209-217.
82. Kamba M., Seta Y., Kusai A., Ikeda M., Nishimura K. A unique dosage form to evaluate the mechanical destructive force in the gastrointestinal tract. Int. J. Pharm. 208:2000;61-70.
83. Dressman J.B., Yamada K. Welling P.G., Tse F.L.S., Dighe S.V. Pharmaceutical Bioequivalence. 1991;235-266 Marcel Dekker, New York.
84. Aoki S., Ando H., Ishii M., Ida K., Watanabe S., Ozawa H. Evaluation of the correlation between in vivo and in vitro release. Effect of the force of contraction and food on drug release. Biol. Pharm. Bull. 17:(2):1994;291-295.
85. Meyer J.H., Thomson J.B., Cohen M.B., Shadchehr A., Mandiola S.A. Sieving of solid food by the canine stomach and sieving after gastric surgery. Gastroenterology. 76:1979;804-813.
86. Kaniwa N., Aoyagi N., Ogata H., Ejima A. Gastric emptying rates of drug preparations. I. Effects of size of dosage forms, food and species on gastric emptying rates. J. Phamacobiodyn. 11:1988;563-570.
87. Mroz C.T., Kelly K.A. The role of the extrinsic antral nerves in the regulation of gastric emptying. Surg. Gynecol. Obstet. 145:1977;369-377.
88. Mann F.C., Bollman J.L. The reaction of the content of the gastrointestinal tract. J. Am. Med. Assoc. 95:(23):1930;1722-1724.
89. Yamada I., Haga K. Measurement of gastric pH during digestion of a solid meal in dogs. Chem. Pharm. Bull. 38:(6):1990;1755-1756.
90. Akimoto M., Nagahata N., Furuya A., Fukushima K., Higuchi S., Suwa T. Gastric pH profiles of beagle dogs and their use as an alternative to human testing. Eur. J. Pharm. Biopharm. 49:2000;99-102.
91. Bueno L., Fioramonti J., Ruckebusch Y. Gastric pH changes associated with duodenal motility in fasted dogs. J. Physiol. 316:1981;319-325.
92. Lui C.Y., Amidon G.L., Berardi R.R., Fleisher D., Youngberg C., Dressman J.B. Comparison of gastrointestinal pH in dogs and humans: implications on the use of the beagle dog as a model for oral absorption in humans. J. Pharm. Sci. 75:(3):1986;271-274.
93. Sagara K., Yamada I., Matsuura Y., Kawata M., Shibata M. Gastrointestinal physiology-regulated dogs for bioavailability evaluation of an oral controlled-release dosage form composed of pulsatile release granules. Biol. Pharm. Bull. 19:(9):1996;1184-1188.
94. Russell T.L., Berardi R.R., Barnett J.L., O'Sullivan T.L., Wagner J.G., Dressman J.B. pH-related changes in the absorption of dipyridamole in the elderly. Pharm. Res. 11:(1):1994;136-143.
95. Lake-Bakaar G., Tom W., Lake-Bakaar D., Gupta N., Beidas S., Elsakr M., Straus E. Gastropathy and ketoconazole malabsorption in the acquired immunodeficiency syndrome (AIDS). Ann. Intern. Med. 109:1988;471-473.
96. Katori N., Ma W.-S., Aoyagi N., Kojima S. Effect of destruction force on drug release from multiple unit controlled release dosage forms in humans. Pharm. Res. 13:(10):1996;1541-1546.
97. Chiou W.L., Jeong H.Y., Chung S.M., Wu T.C. Evaluation of using dog as an animal model to study the fraction of oral dose absorbed of 43 drugs in humans. Pharm. Res. 17:(2):2000;135-140.
98. Lin J.H. Species similarities and differences in pharmacokinetics. Drug Metab. Dispos. 23:(10):1995;1008-1021.
99. Staib A.H., Woodcock B.G., Loew D., Schuster O. Prescott L.F., Nimmo W.S. Novel Drug Delivery and its Therapeutic Application. 1989;79-88 Wiley, Chichester.
100. Agyilirah G.A., Green M., duCret R., Banker G.S. Evaluation of the gastric retention properties of a crosslinked polymer coated tablet versus those of a nondisintegrating tablet. Int. J. Pharm. 75:1991;241-247.
101. P.S.L. Wong, L.-C. Dong, D.E. Edgren, F. Theeuwes, P.I. Gardner, F. Jao, J.J. Wan, Prolonged release active agent dosage form adapted for gastric retention, US Patent 6120803, September 19, 2000.
102. Groning R., Berntgen M., Georgarakis M. Acyclovir serum concentrations following peroral administration of magnetic depot tablets and the influence of extracorporal magnets to control gastrointestinal transit. Eur. J. Pharm. Biopharm. 46:1998;285-291.
103. M. Flashner-Barak, V. Rosenberger, M. Dahan, Y. Lerner, Composition and dosage form for delayed gastric release of alendronate and/or other bis-phosphonates, US Patent 6476006, November 5, 2002.
104. Rouge N., Allemann E., Gex-Fabry M., Balant L., Cole E.T., Buri P., Doelker E. Comparative pharmacokinetic study of a floating multiple-unit capsule, a high-density multiple-unit capsule and an immediate-release tablet containing 25 mg atenolol. Pharm. Acta Helv. 73:1998;81-87.
105. Nur A.O., Zhang J.S. Captopril floating and/or bioadhesive tablets: design and release kinetics. Drug Dev. Ind. Pharm. 26:(9):2000;965-969.
106. Machida Y., Inouye K., Tokumura T., Iwata M., Nagai T. Preparation and evaluation of intragastric buoyant preparations. Drug Des. Deliv. 4:1989;155-161.
107. Wei Z., Yu Z., Bi D. Design and evaluation of a two-layer floating tablet for gastric retention using cisapride as a model drug. Drug Dev. Ind. Pharm. 27:(5):2001;469-474.
108. Ozdemir N., Ordu S., Ozkan Y. Studies of floating dosage forms of furosemide: in vitro and in vivo evaluations of bilayer tablet formulations. Drug Dev. Ind. Pharm. 26:(8):2000;857-866.
109. Akiyama Y., Nagahara N., Nara E., Kitano M., Iwasa S., Yamamoto I., Azuma J., Ogawa Y. Evaluation of oral mucoadhesive microspheres in man on the basis of the pharmacokinetics of furosemide and riboflavin, compounds with limited gastrointestinal absorption sites. J. Pharm. Pharmacol. 50:1998;159-166.
110. Eiamtrakarn S., Itoh Y., Kishimoto J., Yoshikawa Y., Shibata N., Murakami M., Takada K. Gastrointestinal mucoadhesive patch system (GI-MAPS) for oral administration of G-CSF, a model protein. Biomaterials. 23:2002;145-152.
111. El-Kamel A.H., Sokar M.S., Gamal S.S.A., Naggar V.F. Preparation and evaluation of ketoprofen floating oral delivery system. Int. J. Pharm. 220:2001;13-21.
112. Erni W., Held K. The hydrodynamically balanced system: a novel principle of controlled drug release. Eur. Neurol. 27:(Suppl. 1):1987;21-27.
113. V. Rosenberger, M. Dahan, Y. Imakov, E.I. Lerner, M. Fleshner-Barak, Rapidly expanding composition for gastric retention and controlled release of therapeutic agents, and dosage forms including the composition, Int. Application WO0200213, January 3, 2002.
114. El-Gibaly I. Development and in vitro evaluation of novel floating chitosan microcapsules for oral use: comparison with nonfloating chitosan microspheres. Int. J. Pharm. 249:2002;7-21.
115. Stepensky D., Friedman M., Srour W., Raz I., Hoffman A. Preclinical evaluation of pharmacokinetic-pharmacodynamic rationale for oral CR metformin formulation. J. Control. Release. 71:2001;107-115.
116. F. Jao, D.E. Edgren, P.S.-L. Wong, Gastric retention dosage form having multiple layers, Int. Application WO0038650, July 6, 2000.
117. Oth M., Franz M., Timmermans J., Moes A. The bilayer floating capsule: a stomach-directed drug delivery system for misoprostol. Pharm. Res. 9:(3):1992;298-302.
118. Chueh H.R., Zia H., Rhodes C.T. Optimization of sotalol floating and bioadhesive extended release tablet formulations. Drug Dev. Ind. Pharm. 21:(15):1995;1725-1747.
119. Hejazi R., Amiji M. Stomach-specific anti-H. pylori therapy. I: preparation and characterization of tetracycline-loaded chitosan microspheres. Int. J. Pharm. 235:2002;87-94.
120. Sawicki W. Pharmacokinetics of verapamil and norverapamil from controlled release floating pellets in humans. Eur. J. Pharm. Biopharm. 53:2002;29-35.
121. S. Nir-El, Floating tablets for controlled release of vitamin E; M.Sc. Dissertation, The Hebrew University of Jerusalem, 1996.
122. Tsuji A., Tamai I. Carrier-mediated intestinal transport of drugs. Pharm. Res. 13:(7):1996;963-977.
123. Antila S., Huuskonen H., Nevalainen T., Kanerva H., Vanninen P., Lehtonen L. Site dependent bioavailability and metabolism of levosimendan in dogs. Eur. J. Pharm. Sci. 9:1999;85-91.
124. Bialer M., Sussan S., Salach O.A., Danenberg H.D., Ben-David J., Gibor Y., Laor A. Criteria to assess in vivo performance of sustained release products: application to diltiazem formulations. J. Pharm. Sci. 84:(10):1995;1160-1163.
125. Bialer M., Arcavi L., Sussan S., Volosov A., Yacobi A., Moros D., Levitt B., Laor A. Existing and new criteria for bioequivalence evaluation of new controlled release (CR) products of carbamazepine. Epilepsy Res. 32:1998;371-378.
126. Wilson C.G., Washington N. Wise D.L. Handbook of Pharmaceutical Controlled Release Technology. 2000;551-565 Marcel Dekker, New York.
127. Wilding I.R., Coupe A.J., Davis S.S. The role of γ-scintigraphy in oral drug delivery. Adv. Drug Deliv. Rev. 46:2001;103-124.
128. Gansbeke B.V., Timmermans J., Schoutens A., Moes A.J. Intragastric positioning of two concurrently ingested pharmaceutical matrix dosage forms. Nucl. Med. Biol. 18:(7):1991;711-718.
129. Wilding I.R., Davis S.S., Melia C.D., Hardy J.G., Evans D.F., Short A.H., Sparrow R.A. Gastrointestinal transit of Sinemet CR in healthy volunteers. Neurology. 39:(Suppl. 2):1989;53-58.
130. Iannuccelli V., Coppi G., Sansone R., Ferolla G. Air compartment multiple-unit system for prolonged gastric residence. Part II. In vivo evaluation. Int. J. Pharm. 174:1998;55-62.
131. Horton R.E., Ross F.G.M., Darling G.H. Determination of the emptying-time of the stomach by use of enteric-coated barium granules. Br. Med. J. 1:1965;1537-1539.
132. Allan F.J., Guilford W.G., Robertson I.D., Jones B.R. Gastric emptying of solid radiopaque markers in healthy dogs. Vet. Radiol. Ultrasound. 37:(5):1996;336-344.
133. Guilford W.G., Lawoko C.R.O., Allan F.J. Accuracy of localizing radiopaque markers by abdominal radiography and correlation between their gastric emptying rate and that of a canned food in dogs. Am. J. Vet. Res. 58:(12):1997;1359-1363.
134. Tytgat G.N.J. Yamada T. Textbook of Gastroenterology. II. Vol. 2:1995;2544-2570 J.B. Lippincott, Philadelphia.
135. Keeffe E.B., Schrock T.R. Sleisenger M.H., Fordtran J.S. Gastrointestinal Disease. V. Vol. 1:1993;301-308 W.B. Saunders, Philadelphia.
136. Weitschies W., Wedemeyer J., Stehr R., Trahms L. Magnetic markers as noninvasive tool to monitor gastrointestinal transit. IEEE Trans. Biomed. Eng. 41:(2):1994;192-195.
137. Weitschies W., Kotitz R., Cordini D., Trahms L. High-resolution monitoring of the gastrointestinal transit of a magnetically marked capsule. J. Pharm. Sci. 86:(11):1997;1218-1222.
138. Weitschies W., Cardini D., Karaus M., Trahms L., Semmler W. Magnetic marker monitoring of esophageal, gastric and duodenal transit of nondisintegrating capsules. Pharmazie. 54:1999;426-430.
139. Hendee W.R. Putman C.E., Ravin C.E. Textbook of Diagnostic Imaging II. Vol. 1:1994;1-6 W.B. Saunders, Philadelphia.
140. Wiley J.W., Nostrant T.T., Owyang C. Yamada T. Textbook of Gastroenterology II. Vol. 2:1995;2901-2925 J.B. Lippincott, Philadelphia.
141. Prakash N.M., Brown M.C., Spelman F.A., Nelson J.A., Read P., Heitkemper M.M., Tobin R.W., Pope C.E. II. Magnetic field goniometry - a new method to measure the frequency of stomach contractions. Dig. Dis. Sci. 44:(9):1999;1735-1740.
142. Choe S.Y., Neudeck B.L., Welage L.S., Amidon G.E., Barnett J.L., Amidon G.L. Novel method to assess gastric emptying in humans: the Pellet Gastric Emptying Test. Eur. J. Pharm. Sci. 14:2001;347-353.
143. Itoh Z. Motilin and clinical application. Peptides. 18:(4):1997;593-608.