Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Patent
1988-05-27
1989-11-07
Davis, Curtis R.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
514 29, 514 50, 514179, 514183, 514212, 514269, 514273, 514315, 514316, 514327, 514328, 514330, 514514, 514946, 514947, A01N 3119, A01N 3140, A01N 4336
Patent
active
048792756
ABSTRACT:
This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals in a transdermal device or formulation comnprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer having the structural formula ##STR1## wherein X represents sulfur, oxygen or 2 hydrogen radicals; Y represents --CH.sub.2 --, --NH-- or oxygen; n and m are integers of from 1 to 3; p is an integer of from 3 to 17; wherein p.gtoreq.9; q is 2, 4, 6 or 8; and R' is selected from the group consisting of H, a lower alkyl group having from 1 to 4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carbalkoxy, carboxamide, and alkanoyl.
REFERENCES:
patent: 3051616 (1962-08-01), Drapal
patent: 3085931 (1963-04-01), Darlington
patent: 3157641 (1964-02-01), Walles et al.
patent: 3306910 (1967-02-01), Louthan
patent: 3306911 (1967-02-01), Doss
patent: 3332938 (1967-07-01), Mayhew et al.
patent: 3341517 (1967-09-01), Buechel et al.
patent: 3342673 (1967-09-01), Kaufman et al.
patent: 3391757 (1975-06-01), Higuchi
patent: 3551544 (1970-12-01), Herschler
patent: 3598122 (1971-08-01), Zaffaroni
patent: 3598123 (1971-08-01), Zaffaroni
patent: 3678156 (1972-07-01), Mac Millan et al.
patent: 3731683 (1973-05-01), Zaffaroni
patent: 3742951 (1973-05-01), Zaffaroni
patent: 3814097 (1974-06-01), Ganderton et al.
patent: 3823152 (1974-07-01), Morimoto et al.
patent: 3865814 (1975-02-01), Lussi et al.
patent: 3921636 (1975-11-01), Zaffaroni
patent: 3954966 (1976-05-01), Lim et al.
patent: 3960922 (1976-06-01), Baker et al.
patent: 3966806 (1976-06-01), Baker et al.
patent: 3972995 (1976-08-01), Tsuk et al.
patent: 3989815 (1976-11-01), Rajadkyaksha
patent: 3989816 (1976-11-01), Rajadhyaksha
patent: 3991203 (1976-11-01), Rajadkyaksha
patent: 3993072 (1976-11-01), Zaffaroni
patent: 3993073 (1976-11-01), Zaffaroni
patent: 3996934 (1976-12-01), Zaffaroni
patent: 4021224 (1977-05-01), Pallos et al.
patent: 4031894 (1977-06-01), Urfahart
patent: 4060084 (1977-11-01), Chandrasek et al.
patent: 4069307 (1978-01-01), Higuchi et al.
patent: 4077407 (1978-03-01), Theemes
patent: 4118500 (1978-10-01), Pritzlaff et al.
patent: 4122170 (1978-10-01), Rajadkyaksha
patent: 4201211 (1980-05-01), Chandrasek et al.
patent: 4230105 (1981-08-01), Hussain et al.
patent: 4264594 (1981-04-01), McGovern et al.
patent: 4284648 (1981-08-01), Hussain et al.
patent: 4292299 (1981-09-01), Suziki
patent: 4292303 (1981-09-01), Keith et al.
patent: 4310525 (1982-01-01), Nelson
patent: 4311481 (1982-01-01), Nelson
patent: 4316893 (1982-02-01), Rajadhyaksha
patent: 4364952 (1982-12-01), Materne
patent: 4405616 (1983-09-01), Rajadhyaksha
patent: 4415563 (1983-11-01), Rajadhyaksha
patent: 4423040 (1983-12-01), Rajadkyaksha
patent: 4424210 (1984-01-01), Rajadhyaksha
patent: 4440777 (1984-04-01), Zupan
patent: 4444762 (1984-04-01), Rajadhyaksha
patent: 4525199 (1985-06-01), Rajadkyaksha
patent: 4537776 (1985-08-01), Cooper
patent: 4552872 (1985-11-01), Cooper
patent: 4557934 (1985-12-01), Cooper
patent: 4562075 (1985-12-01), Rajadhyaksha
patent: 4565823 (1986-01-01), Ohata et al.
patent: 4605670 (1986-08-01), Saito
patent: 4620949 (1986-11-01), Lin
patent: 4621143 (1986-11-01), McGovern et al.
patent: 4626539 (1986-12-01), Aungst et al.
Bennett, S. L. et al., "Optimization of Bioavailability of Topical Steroids: Non-Occluded Penetration Enhancers Under Thermodynamic Control", J. Pharm. Pharmacol., 37(5): 298-304, 1985.
Goldman, L. et al., "Preliminary Investigative Studies with DDT in Dermatologic and Plastic Surgery", Lasers Surg Med, 5(5): 453-456, 1985.
Chow, DS-L et al., "Concentration-Dependent Enchancement of 1-Dodecylazacyloheptan-2-one on the Percutaneous Penetration Kinetics of Triamcinolone Acetonide", J. Pharm Sci, 73(12):1794-1799, 1984.
DeClercg, E., "Topical Treatment of Cutaneous Herpes Simplex Virus Infection in Hairless Mice with (E)-5-(2-Bromovinyl)-2'-Dioxyurdine and Related Compounds", Antimicrob Agents Chemother, 26(2): 155-159, 1984.
Goodman, M. et al., Differential Scanning Colorimetry (DSC) of Human Stratum Corneum: Effect of Azone, Presentation at the British Pharmaceutical Conference Leeds, 1985.
Hadgraft, J. et al., "Facilitated Transport of Sodium Salicylate Across an Artificial Lipid Membrane by Azone", I. Pharm Pharmacol, 37(10): 725-727, 1985.
Higuchi, W. I., "Macro- and Micro-Physical Chemical Considerations in Understanding Drug Transport in the Stratum Corneum", Second Int'l Symp. Recent Advances in Drug Delivery Systems, Salt Lake City, Utah, 1985.
Higuchi, W. I. et al., "Tropical Delivery of Antiviral Agents: In Vivo/In Vitro Correlations", Proc. Int. Symp., pp. 1-7, 1984.
Hoelgaard, A., "Dermal Drug Delivery-Improvement by Choice of Vehicle or Drug Derivative", 2nd Int'l Symp Recent Adv Drug Delivery Systems, 1985.
Chemical Abstracts: 69:86313p, 82:39533u, 83:93905e, 83:1758d, 83:91780g, 102:183860x, 104:174644u.
Liang, W. Q. et al., "Affect of Axone of Local Pharmacokinetics of Para-Aminobenzoic Acid in Skin", 11th Int'l Symp., Controlled Release Bioactive Mat., 1984.
Maibach, H. I. et al., "Phototoxicity (Photoirritatiion) of Topical and Systemic Agents", Advances in Modern Toxicology, 4:211-223.
Marzulli F. N. et al., "Contact Allergy: Predictive Testing in Humans, Advances", in Modern Toxicology, 4:253-372, 1977.
McCullogh, J. L. et al., "Regulation of Epidermal Prolifieration in Mouse Epidermis by Combination of Difluoromethyl Ornithine (DFMO) and Methylglyoxal Bis (guancylhydrazone) (MGBG)", J. Invest. Dermatol, 85(6): 518-521, 1985.
McCullogh, J. L. et al., "Development of a Topical Hematoporphysin Derivative Formulation: Characterization of Photosensitizing Effects. In Vivo", J. Invest Dermatol, 81(6): 528-532, 1983.
Ohshima, T. et al., "Enhancing Effect of Absorption Promoters on Percutaneous Absorption of a Model Dye (6-Carboxyfluorescein) as Poorly Absorbable Drugs. II, Study on the Absorption Promoting Effect of Azone", J. Pharm Dyn 8:900-905, 1985.
Ryatt, J. K., "Pharmacodynamic Measurement of Percutaneous Penetration Enhancement in Vivo", J. Pharm Sci 75:(4) 374-377, 1986.
Stoughton, R. B., "Azone as a Promoter of Percutaneous Absorption", (1983), Acta Pharm 20(1):62.
Shannon, W. M. et al., "Influence of 1-Dodecylazacydoheptan-2-one (Azone) on the Topical Therapy of Cutaneous Herpes Simples Virus Type 1 Infection in Hairless Mice with 2', 3'-D-arabinofuranosyladenine", J Pharm Sci 74(11):1157-1161, 1985.
Spruance, S. I. et al., "Effect of Azone and Propylene Glycol on Penetration of Trifluorothymidine Through Skin and Efficacy of Different Topical Formulations Against Cutaneous Herpes Simplex Virus Infections in Guinea Pigs", Antimicrob Agent Chemother 25(5):819-823, 1984.
Stoughton, R. B. et al., "Azone.RTM.: A New Non-Toxic Enhancer of Cutaneous Penetration", Drug Dev. Iind. Pharm 9(4):725-744, 1983.
Stoughton, R. B., "Azone Enhances Percutaneous Penetration", IN: Psoriasi Proceedings of the Third Int'l Sump., 397-398, 1982.
Stoughton, R. B., "Enhanced Percutaneous Penetration with 1-Dodecylazacycloheptan-2-one", Archives of Derm 118:474-477, 1982.
Sugibayashi, K. et al., "Effect of the Absorption Enhancer, Azone, on the Transport of 4-Fluorouracil Across Hairless Rat Skin", J. Pharm Pharm 37(8):578-580, 1985.
Toutitou, E. et al., "Effect of Propylene Glycol, Azone and N-Decylmethyl Suphoxide on Skin Permeation Kinetics of 5-Fluorouracil", Int J. Pharm 1(27): 89-98, 1985.
Wooton, P. K. et al., "Vehicle Effect on Topical Drug Delivery, III, Effect of Azone on the Cutaneous Permeation of Metronidazole and Propylene Glycol", Int J Pharm 1(24):19-26, 1985.
Rajadkyaksha, V. et al., "Transdermal Delivery of ISDN from Hercon Patches Containing Azone", Proceed Itern Symp Control Rel Biact Mater, 12, (222-323), 1985.
Zoler, M. L., "Skin Penetration of Antiherpes Drugs Can Be Enchanced by Azone", Dermatology Times, 5(2), 1984.
Hadgraft, J., "Percutaneous Absorption", Cos & Toiletries 1
Minaskanian Gevork
Peck James V.
Baran Robert J.
Bostich June M.
Davis Curtis R.
Nelson Research & Development Co.
LandOfFree
Penetration enhancers for transdermal delivery of systemic agent does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Penetration enhancers for transdermal delivery of systemic agent, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Penetration enhancers for transdermal delivery of systemic agent will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-83869