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Oral pharmaceutical delivery system with improved sustained releaseRelated Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Preparations Characterized By Special Physical Form, Tablets, Lozenges, Or Pills, Sustained Or Differential Release TypeOral pharmaceutical delivery system with improved sustained release description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20070026066, Oral pharmaceutical delivery system with improved sustained release. Brief Patent Description - Full Patent Description - Patent Application Claims
CROSS REFERENCE TO RELATED PATENTS [0001] The application is a continuation-in-part of pending U.S. patent application Ser. No. 10/348,372, filed Jan. 21, 2003, which is a continuation-in-part of pending U.S. patent application Ser. No. 09/656,297, issued as U.S. Pat. No. 6,541,025, filed Sep. 6, 2000, which is a continuation-in-part of U.S. patent application Ser. No. 09/476,483 issued as U.S. Pat. No. 6,340,471B1, filed Dec. 30, 1999, all of which are hereby incorporated in their entirety by reference. FIELD OF THE INVENTION [0002] The present invention relates to a pharmaceutical delivery system that increases the sustained release properties of drugs. Said delivery system includes both human and veterinary applications. More specifically, the present invention relates to an orally ingested pharmaceutical delivery system that is a solid lipid suspension that provides improved sustained release. BACKGROUND OF THE INVENTION [0003] Drug efficacy generally depends upon the ability of the drug to reach its target in sufficient quantity to maintain therapeutic levels for the desired time period. Orally ingested drugs must overcome several obstacles to reach their desired targets. Before orally ingested drugs enter the general circulation of the human body, they are absorbed into the capillaries and veins of the upper gastrointestinal tract and are transported by the portal vein to the liver. The pH and enzymatic activities found in gastrointestinal fluids may inactivate the drug or cause the drug to dissolve poorly and not be absorbed. In addition, following their absorption in the intestine, orally ingested drugs are often subject to a "first pass" clearance by the liver and excreted into bile or converted into pharmacologically inactive metabolites. [0004] The oral ingestion of hormones, such as testosterone or estrogen, has proven challenging. Testosterone is administered for oral ingestion in a bonded form as testosterone undecanoate, methyltestosterone, or testosterone cyclodextrin, to avoid the first pass effect. When it is administered in a regiment of hormone replacement therapy, it is desired to have sustained release properties, yet these forms of testosterone must be taken multiple times daily. [0005] Of particular interest is the delivery of testosterone in the unbonded form. The unbonded form of testosterone is more stable than its bonded predecessors. More of the active ingredient is delivered in a smaller dosage. The unbonded form is a simpler and less expensive manufacturing process in that the additional step of bonding the testosterone is eliminated. Further, the unbonded testosterone is administered with or without food, unlike the bonded form which is administered with food consumption. [0006] "Sustained Release" generally refers to release of a drug whereby the drug concentration in the serum of the patient is maintained at the desired level over a period of time. The longer the drug is at the desired level, the better the sustained release properties are. It is desirable to have the desired level be maintained for 12 h or more, so that only one to two doses of a drug need to be taken daily. A second indicator of sustained release properties is the t.sub.max of the drug, which is the time after administration of the drug that the serum concentration reaches its maximum level. A larger t.sub.max may indicate a slower and more sustained release of the drug into the blood. A variety of methods and formulations are used to provide sustained release of drugs. Some of the methods are disclosed in U.S. Pat. No. 5,567,439, which is hereby incorporated by reference, which discloses controlled release systems using a shearform matrix. [0007] The use of a lipid-based solid oral delivery system with improved taste masking is disclosed in U.S. Pat. No. 6,340,471B1. U.S. Pat. No. 5,229,131 discloses a sustained release system that uses one or more individual drug-containing subunits in a unitary drug depot, such as a tablet or capsule. [0008] The use of coatings on pharmaceuticals to provide sustained release properties, taste and odor masking, and delayed release are known in the art. One line of products commercially available for the coating of pharmaceuticals is EUDRAGIT.RTM. polymers marketed by Pharma Polymers. Polymer coatings are prepared that release at the desired pH to deliver drugs to targeted portions of the gastrointestinal system. [0009] None of the above-referenced patents describe the present invention as disclosed and claimed herein. SUMMARY OF THE INVENTION [0010] The present invention comprises a solid orally ingested delivery system comprising at least one lipid, dry particles including at least one pharmaceutical, and at least one filler, wherein the dry particles are continuously coated by the lipid and form a homogeneous suspension with the lipid. At least part of the pharmaceutical is microencapsulated with a polymer that releases in the pH range of from about 5.0 to 7.0. The suspension, when melted, exhibits thixotropic and/or pseudoplastic properties. The suspension is formed into the desired dose by molding or pouring the suspension when in a liquid or semi-liquid state. The process for preparing the present delivery system comprises melting the lipid, blending the dry particles which include the pharmaceutical, at least one filler and, optionally, flavorings with the melted lipid, and pouring or molding the suspension to provide the solid dose. The suspension, when melted, exhibits thixotropic and pseudoplastic flow properties. BRIEF DESCRIPTION OF THE DRAWINGS [0011] FIG. 1 is a graph demonstrating the serum concentration of various doses of testosterone over time when administered in a lipid formulation to dogs by oral ingestion. [0012] FIG. 2 is a graph demonstrating the serum concentration of various doses of testosterone over time when administered in a micronized formulation to dogs by oral ingestion. [0013] FIG. 3 is a graph demonstrating the serum concentration of 250 mg dose of testosterone with various amounts of rupturing agent over time when administered in a lipid formulation to dogs by oral ingestion. [0014] FIG. 4 is a graph demonstrating the serum concentration of 250 mg dose of testosterone with various types of surfactant over time when administered in a lipid formulation to dogs by oral ingestion. [0015] FIG. 5 is a graph demonstrating the serum concentration of 250 mg dose of testosterone with 100 mg microencapsulated with various coatings and 250 mg micronized, over time when administered in a lipid formulation to dogs by oral ingestion. DETAILED DESCRIPTION OF THE INVENTION [0016] The lipids of the present invention may be of animal, vegetable or mineral origin, which are substantially water-insoluble, inert, non-toxic hydrocarbon fats and oils and derivatives thereof, and may comprise any of the commonly commercially available fats or oils approved by the Food & Drug Administration, having melting points in the range of about 90 to 160.degree. F. (32 to 71.degree. C.). The lipid may comprise a vegetable oil base commonly known as hard butter. Hard butters are hydrogenated, press fractionated, or other processed oils that are processed or recombined to have a solid fat index (percent solid fat vs. temperature) similar to that of cocoa butter. However, other lipids may be used that are relatively hard or solid at room temperature, but melt rapidly in the mouth at a temperature of about 92.degree. to 98.degree. F. (29 to 32.degree. C., mouth temperature). The lipid is employed in the amounts within the range of from about 20 to 50%. Above about 50%, the suspension flows too readily and does not exhibit thixotropic or pseudoplastic flow properties. When present below about 20%, the amount of lipid is not sufficient to completely coat the dry particles. [0017] It is expected that the lipid formulation would have improved sustained release properties over that of granulated pharmaceuticals alone, since the lipids may hinder the solubilizing of the pharmaceutical in the gastrointestinal tract and retard absorption. [0018] Examples of suitable lipids include tallow, hydrogenated tallow, hydrogenated vegetable oil, almond oil, coconut oil, corn oil, cottonseed oil, light liquid petrolatum, heavy liquid petrolatum, olein, olive oil, palm oil, peanut oil, persic oil, sesame oil, soybean oil or safflower oil. Additionally, stearines can be used as a lipid in the present invention. The addition of stearines to the product provides the favorable property of mold-release. Further, the addition of stearines raises the melting point of the composition as high as about 100.degree. F. (38.degree. C.), which is particularly beneficial when the product is shipped or stored in unrefrigerated compartments. Continue reading about Oral pharmaceutical delivery system with improved sustained release... 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