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Oral glp-1 formulationsRelated Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Preparations Characterized By Special Physical FormOral glp-1 formulations description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20060286129, Oral glp-1 formulations. Brief Patent Description - Full Patent Description - Patent Application Claims
[0001] This application claims the benefit of U.S. Provisional Application No. 60/552,116, filed Mar. 10, 2004, and U.S. Provisional Application No. 60/530,931, filed Dec. 19, 2003. Both of these applications are hereby incorporated by reference in their entirety. FIELD OF THE INVENTION [0002] The present invention relates to a formulation comprising a delivery agent and a glucagon-like peptide 1 or a glucagon-like peptide 1 analog compound (collectively "GLP-1"). These formulations are useful as oral medicaments for the treatment of type 2 diabetes and obesity as well as other conditions known to be treated with GLP-1. BACKGROUND OF THE INVENTION [0003] Type 2 diabetes, also known as non-insulin dependent diabetes mellitus (NIDDM), is a condition in which patients generate insulin, but the insulin cannot be used effectively by the body's cells. This is primarily because the amount of insulin produced in response to rising blood sugar levels is not sufficient to allow cells to efficiently take up glucose and thus, reduce blood sugar levels. [0004] Glucagon-like 1 peptides and glucagon-like 1 peptide analogs (collectively GLP-1) are a potential treatment for type 2 diabetes and obesity. GLP-1 induces the secretion and production of insulin, effectively reducing blood glucose levels in diabetic patients. GLP-1 also inhibits glucagon secretion, inhibits gastric emptying, enhances glucose utilization, and induces weight loss. GLP-1 may also act to prevent the B cell deterioration that occurs as diabetes progresses. [0005] Development of an oral GLP-1 therapeutic has been extremely difficult. This is primarily due to the in vivo instability of the peptide. The high acid content and ubiquitous digestive enzymes of the digestive tract will often degrade GLP-1 before reaching the desired site of absorption. Further, GLP-1 may encounter difficulty in traversing the cells of the epithelial membrane in the small intestine to reach the bloodstream. Also, GLP-1 only remains in solution under a narrow set of conditions. [0006] In light of the above difficulties, oral administration of GLP-1 compounds has not been feasible. GLP-1 compounds are customarily delivered by subcutaneous injection or through continuous subcutaneous infusion or continuous intravenous administration. Because patients are generally adverse to injections and time consuming infusions, patient compliance with GLP-1 administration regimens will be low. [0007] Delivery agent molecules that interact with various active agents compounds in a non-covalent fashion to allow the compounds to cross gut membranes and yet remain therapeutically active have been disclosed in U.S. Pat. Nos. 6,663,898, 6,663,887, 6,646,162, 6,642,411, 6,627,228, 6,623,731, 6,610,329, 6,558,706, 6,525,020, 6,461,643, 6,461,545, 6,440,929, 6,428,780, 6,413,550, 6,399,798, 6,395,774, 6,391,303, 6,384,278, 6,375,983, 6,358,504, 6,346,242, 6,344,213, 6,331,318, 6,313,088, 6,245,359, 6,242,495, 6,221,367, 6,180,140, 5,541,155, 5,693,338, 5,976,569, 5,643,957, 5,955,503, 6,100,298, 5,650,386, 5,866,536, 5,965,121, 5,989,539, 6,001,347, 6,071,510, and 5,820,881; U.S. Published Application Nos. 20030232085, 20030225300, 20030198658, 20030133953, 20030078302, 20030072740, 20030045579, 20030012817, 20030008900, 20020155993, 20020127202, 20020120009, 20020119910, 20020102286, 20020065255, 20020052422, 20020040061, 20020028250, 20020013497, 20020001591, 20010039258, 20010003001; and International Published Application Nos. 2003/057650, 2003/057170, 2003/045331, 2003/045306, 2003/026582, 2002/100338, 2002/070438, 2002/069937, 02/20466, 02/19969, 02/16309, 02/15959, 02/02509, 01/92206, 01/70219, 01/51454, 01/44199, 01/34114, 01/32596, 01/32130, 00/07979, 00/59863, 00/50386, 00/47188, 00/40203, 96/30036. SUMMARY OF THE INVENTION [0008] The present invention provides pharmaceutical compositions comprising at least one delivery agent and GLP-1. These pharmaceutical compositions facilitate the oral delivery of GLP-1, providing an improved (e.g. increased) bioavailability of GLP-1 compared to administration of GLP-1 without a delivery agent. The delivery agent may be selected from the following, including salts thereof: TABLE-US-00001 TABLE 1 Deliv- ery Agent No. Compound 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 According to one embodiment, the pharmaceutical composition includes an effective amount of a GLP-1 compound, for example, to treat NIDDM or obesity. [0009] The delivery agents enable the oral delivery of macromolecules, providing an increased or improved bioavailability of GLP-1 compared to administration of GLP-1 without a delivery agent. [0010] Another embodiment is an administration composition that includes at least one delivery agent, GLP-1, and, optionally, a dosing vehicle, an adjuvant, an excipient, or a mixture thereof. The dosage unit form may be a liquid or a solid, such as a tablet, capsule or particles, including a powder or sachet. [0011] Another embodiment is a method for administering GLP-1 to a subject in need thereof by orally administering the pharmaceutical composition of the present invention to the subject. [0012] Yet another embodiment is a method of treating type 2 diabetes or obesity in an animal in need thereof by administering an effective amount of the pharmaceutical composition or dosage unit form of the present invention. [0013] The present invention encompasses the development of novel formulations comprising GLP-1 compounds and delivery agents that can be administered orally. The present invention provides a formulation which can be administered orally comprising a GLP-1 compound and a specified delivery agent. The GLP-1 compound can be native GLP-1; GLP-1 fragments; GLP-1 analogs; GLP-1 derivatives of native, fragments, or analogs of GLP-1; and Exendin-3 and Exendin-4. The delivery agent is selected from delivery agents described in U.S. Pat. Nos. 5,541,155; 5,693,338; 5,976,569; 5,643,957; 5,955,503; 6,100,298; 5,650,386; 5,866,536; 5,965,121; 5,989,539, 6,001,347; 6,071,510; 5,820,881; and 6,242,495; and WO 02/02509; WO 01/51454; WO 01/44199; WO 01/32130; WO 00/59863; WO 00/50386; WO 00/47188; and WO 00/40203. [0014] Preferred GLP-1 compounds are analogs or derivatives of analogs having modifications at one or more of the following positions: 8, 12, 16, 18, 19, 20, 22, 25, 27, 30, 33, and 37 and show increased potency compared with Val.sup.8-GLP-1 (7-37)OH. [0015] Preferred GLP-1 compounds are also described in SEQ ID NO.: 1, SEQ ID NO.: 2, SEQ ID NO.: 3, SEQ ID NO.: 4, SEQ ID NO.: 5, SEQ ID NO.: 6, SEQ ID NO.: 7, SEQ ID NO.: 8, SEQ ID NO.: 9, SEQ ID NO.: 10, SEQ ID NO.: 11, SEQ ID NO.: 12, SEQ ID NO.: 13, or SEQ ID NO.: 14. More preferred GLP-1 compounds are described in compounds of SEQ ID NO.: 2, SEQ ID NO.: 12, SEQ ID NO.: 13, and SEQ ID NO.: 14. [0016] Delivery agents are described in Table 1. [0017] The present invention also encompasses a method of stimulating the GLP-1 receptor in a subject in need of such stimulation, said method comprising the step of administering to the subject an effective amount of the oral formulation described herein. Subjects in need of GLP-1 receptor stimulation include those with type 2 diabetes and obesity. DETAILED DESCRIPTION OF THE INVENTION [0018] The three-letter abbreviation code for amino acids used in this specification conforms with the list contained in Table 3 of Annex C, Appendix 2 of the PCT Administrative Instructions and with 37 C. F. R. 1.822(d)(1) (2000). DEFINITIONS Continue reading about Oral glp-1 formulations... Full patent description for Oral glp-1 formulations Brief Patent Description - Full Patent Description - Patent Application Claims Click on the above for other options relating to this Oral glp-1 formulations patent application. ###  How KEYWORD MONITOR works... a FREE service from FreshPatents1. Sign up (takes 30 seconds). 2. Fill in the keywords to be monitored. 3. Each week you receive an email with patent applications related to your keywords. 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