Azithromycin dosage forms with reduced side effects
Patent 6984403 Issued on January 10, 2006. Estimated Expiration Date: January 23, 2024. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.
424/489, Particulate form (e.g., powders, granules, beads, microcapsules, and pellets)424/400, PREPARATIONS CHARACTERIZED BY SPECIAL PHYSICAL FORM424/464, Tablets, lozenges, or pills424/451Capsules (e.g., of gelatin, of chocolate, etc.)
The present invention is related to an oral dosage form comprising an effective amount of an alkalizing agent and an azithromycin multiparticulate wherein said multiparticulate comprises azithromycin, a glyceride which comprises glyceryl monobehenate, glyceryl dibehenate, glyceryl tribehenate, or a mixture thereof and a poloxamer. Typically, the oral dosage form includes any suitable oral dosing means such as a powder for oral suspension, a unit dose packet or sachet, a tablet or a capsule.
Other References
Foulds, G., et al., “The effects of an antacid or cimetidine on the serum concentrations of azithromycin”, J. Clin. Pharmacol. 1991 Feb.; 31(2): 164-7 (Abstract).
Amsden, G.W., et al., “Serum and WBC pharmacokinetics of 1500 mg of azithromycin when given either as a single dose or over a 3 day period in healthy volunteers”, J. Antimicrobial Chemotherapy (2001), 47(1), 61-66 (Abstract).
Barber, J., “Assignments of the 13C and 1H NMR Spectra of Azithromycin in CDCI3,” Magnetic Resonance in Chemistry 29:7(1991)740-743.
Barthelemy, P., et al., “Compritol® 888 ATO: An Innovative Hot-Melt Coating Agent for Prolonged-Release Drug Formulations,” Europ. J. Pharmaceut. and Biopharmaceutics, 47(1999)87-90.
Bhagwatwar, H., et al., “Preparation of Drug-Containing Wax Microspheres Using a Melt Dispersion Technique,” Pharmaceutical Research, 6:7(1989)S-177, Abstract No. PD 1201.
Breitenbach, J., et al., “Solid Dispersions by an Integrated Melt Extrusion System,” Proceed. Int'l Symp. Control Re. Bioact. Materials, 25(1998)804-805.
Craig, D.Q.M., “The Physical Characterisation of Gelucire 50/13,” Bulletin Technique Gattefosse, 89(1996)39-51.
DeMan, J.M., et al., “Thermal Analysis Microscopy for the Study of Phase Changes in Fats,” Food Microstructure, 4(1985)233-239.
Eldem T., et al., “Polymorphic Behavior of Sprayed Lipid Micropellets and its Evaluation by Differential Scanning Calorimetry and Scanning Electron Microscopy,” Pharmaceutical Research, 8:2(1991)178-184.
Eldern, T., et al., “Optimization of Spray-Dried and -Congealed Lipid Micropellets and Characterization of Their Surface Morphology by Scanning Electron Microscopy,” Pharmaceutical Research, 8:1(1991)47-54.
Emas, M., and H. Nyqvist, “Methods of Studying Aging and Stabilization of Spray-Congealed Solid Dispersions with Carnauba Wax. 1. Microcalorimetric Investigation,” Int'l J. Pharmaceutics, 197(2000)117-127.
Faham, A., et al., “Hot-Melt Coating Technology. I. Influence of Compritol 888 Ato and Granule Size on Theophyline Release,” Drug Dev. Industrial Pharm., 26:2(2000)167-176.
Follonier, N., et al, “Hot-Melt Extruded Pellets for the Sustained Release of Highly Dosed Freely Soluble Drugs,” Proceed. Intern. Symp. Control. Release Bioactive Materials, 18(1991)578-579.
Forster, A., et al., “Characterization of Glass Solutions of Poorly Water-Soluble Drugs Produced by Melt Extrusion with Hydrophific Amorphous Polymers, ” J. Pharmacy Pharmacology, 53(2001)303-315.
Foulds, G., et al., “The Absence of an Effect of Food on the Bioavailability of Azithromycin Administered as Tablets, Sachet or Suspension,” J. Antimicrobial Chemotherapy, 37:Suppl. C(1996)37-44.
Gattefosse, “Gelucire®—Pharmaceutical Excipients for Oral Semi-Solid Formulations,” Technical Dossler, 2nd edition, Gattefosse s.a., Cedex, France (1996).
Ghali, E.S., et al., “Thermal Treatment of Beads with Wax for Controlled Release,” Drug Development and Industrial Pharmacy, 15:9(1989)1311-1328.
Hancock, B.C., and G. Zografi, “The Relationship Between the Glass Transition Temperature and the Water Content of Amorphous Pharmaceutical Solids,” Pharmaceutical Research, 11:4(1994)471-477.
Joachim, J., et al., “Le Compritol”, Etudes Galenique, Physique et Statstique, APGI, IV(1989)291-296.
Johnson, D.E., et al., “A New Method for Coating Glass Beads for Use in Gas Chromatography of Chloropromazine and its Metabolites,” Source unknown, and date unknown. (may be 1964-1965).
Jorgensen, K., et al., “Dissolution Stability of Multiparticulate Controlled Release Tablets,” Int'l J. Pharmaceutics, 153(1997)1-11.
Meshall, M.M., et al., “Optimization of Theophylline Release from Tablets Containing Compritol,” S.T.P. Pharma Sciences, 5:6(1995)429-434.
Perez, M. deLos A, et al., “Sustained Release Phenylpropanolamine Hydrochloride from Compritol ATO-888 Matrix,” Pharmaceutical Research, 9:10(1992)S-162, Abstract No. PT6191.
Perez, M.A., et al., “Sustained Release Phenylpropanolamine Hydrochloride from ATO 888 Matrix,” PRHSJ, 12:4(1993)263-267.
Perissutti, B., et al., “Solid Dispersions of Carbamazepine with Gelucire 44/14 and 50/13,” S.T.P. Pharma Sciences, 10:6(2000)479-484.
Physician's Desk Reference, Information cited on ZITHROMAX® capsules (equivalent to 250 mg azithromycin), tablets (equivalent to 600 mg azithromycin), and oral suspension (equivalent to 1g azithromycin).
Reis, R. and F. Moll, “Matrix Formation of Polyglycolic Acid Tablets by Annealing,” European J. Pharm. and Biopharm., 40:1(1994)14-18.
Rxlist.com, “Azithromycin,” description of drug, categories, brand names, from internet website, Mar. 14, 2001.
San Vincente, A., et al., “Effect of Aging on the Release of Salbutamol Sulfate from Lipid Matrices,” Int'l J. Pharmaceutics, 208(2000)13-21).
Schwartz, J.B., et al., “A Potential Controlled Release Wax Matrix Excipient for Tablets,” Pharmaceutical Research, 9:10(1992)S-162, Abstract No. PT6189.
Schwartz, J.B., et al., Preliminary Evaluation of Controlled Release Agents for Tablets, Pharmaceutical Research, 9:10(1992)S-162, Abstract No. PT6190.
Sugao, H., et al, “Taste Masking of Bitter Drug Powder without Loss of Bioavailability by Heat Treatment of Wax-Coated Microparticles,” J. Pharmaceutical Sci., 87:1(1998)96-100.
Thomasen, L.J., et al., “Prolonged Release Matrix Pellets Prepared by Melt Pelletization. I. Process Variables,” Drug Development and Industrial Pharmacy, 19:15(1993)187-1887.
Wang, A.E. and J.B. Schwartz, “Effect of Temperature on Drug Release from Wax Matrix Tablets After Thermal Treatment,” Pharmaceutical Research, 11:10(1994)S-155. Abstract No. 6099.
Zhang, Y.-E., et al., Effect of Processing Methods and Heat Treatment on the Formation of Wax Matrix Tablets for Sustained Drug Release, Pharm. Dev. Technol., 6:2(2001)131-144.
Arguendas, A., “Single Dose Therapy in Otitis Media, Clinical Microbiology and Infection,” Abstract, S130, vol. 5, Supplemental 3, (1999).
Block, S., et al., “Single-Dose Azithromycin (30 mg/kg) in Acute Otitis Media,” ICAAC, New Orleans, La, Sep. 7-10, 2003, Abstract 174.
Curatolo, W., et al., “Site-Specific Absorption and Toleration of Azithromycin,” Proceedings Intern. Symposium Rel. Bioact. Mater., 23, 1996.
Luke, D.R., et al, “Clinical Pharmacology of Azithromycin Given at Various Sites Along the Gastrointestinal Tract in Healthy Subjects,” pp. 464-468.
Physicians Desk Reference, “Appendix A Summary of Pediatric Suspension Commercial Products,” 55th edition, Phase III Clinical Dosage Form Nomination, pp 19 and 28 (2001).
Pfizer, Inc., Zithromax [package insert], “Zithromax (azithromycin tablets) and (azithromycin for oral suspension),” www.pfizer.com/download/uspi —zithromax.pdf (2004).
January 23, 2024. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.
