Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Implant or insert
Patent
1994-09-30
1996-07-30
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Implant or insert
424426, 424425, 424484, 424486, 514818, A61K 970
Patent
active
055409121
DESCRIPTION:
BRIEF SUMMARY
This invention lies in the field of controlled- or sustained-release drug delivery systems. More particularly, this invention relates to particulate suspensions designed for local administration of drugs.
BACKGROUND OF THE INVENTION
Therapeutic drugs, local anesthetics and other agents, which are collectively referred to in this specification as "biologically effective agents" or "drugs", are often topically applied when concentrated, localized action is desired at specifically delineated regions of a patient's anatomy. These regions may be open wounds or any otherwise afflicted areas, such as cavities. The need for this type of administration may for example arise in the treatment of incisional wounds following surgery, or of accidental incisions, punctures, scrapes or bruises, or in the treatment of localized infections such as insect stings or bites, poison ivy, poison oak, or other allergic skin reactions, burns and sunburn, skin rashes and roughness such as dermatitis, psoriasis, and broken or cracked skin in general, as well as more serious traumas such as wounds caused by accidents or recesses or cavities caused by the removal of tumors from bones. The substance to be administered may be a therapeutic agent or a preventive agent, such as, for example, an antibiotic, antibacterial, antifungal, or anti-infective, applied either prior to or subsequent to the onset of the condition, or an analgesic or anesthetic applied either as the sole treatment or in conjunction with additional treatment such as surgery or first aid.
Localized administration has certain advantages over systemic administration. One is the avoidance of adverse side effects, such as those which accompany the use of narcotics and other systemic pain-killers. Another is the faster action and the concentration of the agent's activity at the area where it is needed, i.e., the more economical and efficient use of the agent.
Topical or other localized administrations which are the most effective, however, are those in which the effect of the agent once administered is prolonged over a period of time. In post-surgical applications and accidental wounds, for example, the anesthetic or antibiotic effect supplied by the agent is often needed for a longer period than can be achieved by simple bolus administration of a drug. Many localized skin infections and rashes also require prolonged treatment. One manner in which this has been achieved is by the combination of the biologically effective agent with a polymeric binder to form solid particles of microscopic size. Release of the agent to the environment, i.e., the surface of the wound or afflicted area to which the formulation has been applied, varies with the concentration of the agent in the particle, the size and shape of the particle, and the lattice or pore structure of the polymer binder matrix.
The use of bioerodible polymers adds a further variable affecting the rate of release. Bioerodible polymers are polymers which, upon exposure to bodily fluids or membranes with which they come into contact upon administration, degrade into low molecular weight species which are innocuously absorbed into or excreted by the patient's body. When bioerodible polymers are used, release occurs by any combination of one, two, three or more mechanisms, examples of which mechanisms are the diffusion of the agent through the polymer itself, the diffusion of the agent through the pores in the polymer matrix, and the erosion of the polymer.
The particles are generally of a very small size which permits them to be applied by spraying or injection. For these types of application, the particles are dispersed in a suitable carrier or vehicle such as a low viscosity or volatile liquid. The small particle size has its limitations, however, particularly in the degree to which the particle can prolong the release rate. Due to the high surface area of the particles and the short diffusion path of the agent through each particle, the release of agent from particles small enough to be applied by spraying or injection
REFERENCES:
patent: 4070347 (1978-01-01), Schmitt
patent: 4093709 (1978-06-01), Choi et al.
patent: 4122158 (1978-10-01), Schmitt
patent: 4131648 (1978-12-01), Choi et al.
patent: 4138344 (1979-02-01), Choi et al.
patent: 4155992 (1979-05-01), Schmitt
patent: 4180646 (1979-12-01), Choi et al.
patent: 4249531 (1981-02-01), Heller et al.
patent: 4351337 (1982-09-01), Sidman
patent: 4780320 (1988-10-01), Baker
patent: 4917892 (1990-04-01), Speaker et al.
patent: 4919939 (1990-04-01), Baker
patent: 4940588 (1990-07-01), Sparks et al.
patent: 4962091 (1990-10-01), Eppstein et al.
patent: 4994281 (1991-02-01), Muranishi et al.
patent: 5008117 (1991-04-01), Calanchi et al.
patent: 5183662 (1993-02-01), Morita et al.
patent: 5332576 (1994-07-01), Mantelle
Maninder Singh Hora, Rajsharan K. Rana, Jack H. Nunberg, Thomas R. Tice, Richard M. Gilley and Michael E. Hudson, "Controlled Release of Interleukin-2 from Biodegradable Microspheres", Bio/Technology, vol. 8, pp. 755-758, Aug., 1990.
Toshiro Heya, Hiroaki Okada, Yusuke Tanigawara, Yasuaki Ogawa and Hajime Toguchi, "Effects of Counte-anion of TRH and Loading Amount on Control of TRH Release from Copoly(dl-lactic acid) Microspheres Prepared by an In-Water Drying Method", International Journal of Pharmaceutics, vol. 69 (1991) pp. 69-75.
Wakiyama, Naoki; Juni, Kazuhiko and Nakano, Masahiro, "Preparation and Evaluation in Vitro of Polylactic Acid Microspheres Containing Local Anesthetics", Chem. Pharm. Bull., vol. 29, No. 11, pp. 3363-3368, (1981).
Juni, K., "Poly(Hydroxy Acids) in Drug Delivery", CRC Critical Reviews in Therapeutic Drug Carrier Systems, vol. 3, Issue 3, pp. 209-232.
Sinclair, R., Cassuto, J., Hogstrom, S., Linden, I., Faxen, A., Hedner, T. and Ekman, R., "Topical Anesthesia with Lidocaine Aerosol in the Control of Postoperative Pain", Anesthesiology, vol. 68, No. 6, Jun., 1988.
William D., et al. "Wound Dressing in Maxilli-facial Trauma"Abcor Report No. 2679-F (1979) Skin & Allergy News, vol. 21, No. 10, Says Antibiotic Microspheres Might Allow Better Wound Care.
Nakano, M. et al. "Biodegradable Microspheres for Prolonged Local Anesthesia", Ninth Cascade, p. 51.
Tice, T. R. and Cowsar, D. R., "Biodegradable Controlled-Release Parenteral Systems", Pharmaceutical Technology, Nov., 1984, pp. 26-34.
Ehnow Fred
Roorda Wouter E.
ALZA Corporation
Dillahunty Mary Ann
Howard Sharon
Ito Richard T.
Page Thurman K.
LandOfFree
Viscous suspensions of controlled-release drug particles does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Viscous suspensions of controlled-release drug particles, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Viscous suspensions of controlled-release drug particles will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1656417