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Orally dosed pharmaceutical compositions comprising a delivery agent in micronized formRelated Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Preparations Characterized By Special Physical Form, Tablets, Lozenges, Or PillsOrally dosed pharmaceutical compositions comprising a delivery agent in micronized form description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20070065505, Orally dosed pharmaceutical compositions comprising a delivery agent in micronized form. Brief Patent Description - Full Patent Description - Patent Application Claims
BACKGROUND OF THE INVENTION [0001] 1. Field of the Invention [0002] The present invention relates to oral compositions for the delivery of pharmacologically active agents, to methods of enhancing the bioavailability of orally administered pharmacologically active agents, and to methods of treating and/or preventing disease in mammals, particularly humans, by orally administering a pharmacologically active agent in accordance with the invention. [0003] 2. Description of the Related Art [0004] Oral delivery of pharmacologically active agents is generally the delivery route of choice since it is convenient, relatively easy and generally painless, resulting in greater patient compliance relative to other modes of delivery. However, biological, chemical and physical barriers such as varying pH in the gastrointestinal tract, powerful digestive enzymes, and active agent impermeable gastrointestinal membranes, makes oral delivery of some pharmacologically active agents to mammals problematic, e.g. the oral delivery of calcitonins, which are long-chain polypeptide hormones secreted by the parafollicular cells of the thyroid gland in mammals and by the ultimobranchial gland of birds and fish, has proven difficult due, at least in part, to the insufficient stability of calcitonin in the gastrointestinal tract as well as the inability of calcitonin to be readily transported through the intestinal walls into the blood stream. [0005] U.S. Pat. Nos. 5,773,647 and 5,866,536 describe compositions for the oral delivery of active agents, such as heparin and calcitonin, with modified amino acids, such as, N-(5-chlorosalicyloyl)-8-aminocaprylic acid (5-CNAC), N-(10-[2-hydroxybenzoyl]aminodecanoic acid (SNAD), and N-(8-[2-hydroxybenzoyl]amino)caprylic acid (SNAC) In addition, WO 00/059863 discloses the disodium salts of formula I [0006] wherein [0007] R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently hydrogen, --OH, --NR.sup.6R.sup.7, halogen, C.sub.1-C.sub.4alkyl, or C.sub.1-C.sub.4alkoxy; [0008] R.sup.5 is a substituted or unsubstituted C.sub.2-C.sub.16alkylene, substituted or unsubstituted C.sub.2-C.sub.16alkenylene, substituted or unsubstituted C.sub.1-C.sub.12alkyl(arylene), or substituted or unsubstituted aryl(C.sub.1-C.sub.12alkylene); and [0009] R.sup.6 and R.sup.7 are independently hydrogen, oxygen, or C.sub.1-C.sub.4 alkyl; and hydrates and solvates thereof as particularly efficacious for the oral delivery of active agents, such as calcitonin, cyclosporin and heparin. [0010] The present invention describes pharmaceutical compositions which provide still greater oral bioavailability of pharmacologically active agents, e.g. peptides such as calcitonin. SUMMARY OF THE INVENTION [0011] Accordingly, the present invention is directed to pharmaceutical compositions which, quite surprisingly, greatly enhance the oral bioavailability of active agents, particularly peptides. Specifically, the invention provides solid pharmaceutical compositions suitable for the oral delivery of pharmacologically active agents, comprising [0012] 1. a therapeutically-effective amount of a pharmacologically active agent; [0013] 2. pharmaceutically acceptable inactive excipients; and [0014] 3. a delivery agent for said pharmacologically active agent, wherein said delivery agent is in micronized form. [0015] In another embodiment the present invention provides solid pharmaceutical compositions suitable for the oral delivery of calcitonin, comprising [0016] 1. a therapeutically-effective amount of a calcitonin; and [0017] 2. pharmaceutically acceptable inactive excipients, and [0018] 3. a delivery agent for said calcitonin, wherein said delivery agent is in micronized form. [0019] In an additional embodiment of the present invention the pharmaceutically acceptable inactive excipient may be either or both of the polymers crospovidone or povidone. [0020] In a still further embodiment of the present invention the solid pharmaceutical composition suitable for oral delivery may also comprise a diluent. [0021] In addition in another embodiment of the present invention the solid pharmaceutical composition suitable for oral delivery may also comprise a lubricant. [0022] In a further embodiment, the invention is directed to a method for enhancing the oral bioavailability of a pharmacologically active agent, said method comprising administering to a subject in need of said pharmacologically active agent an effective amount of a pharmaceutical composition according to the instant invention. [0023] In a still further embodiment, the invention is directed to a method of treatment of bone related diseases and calcium disorders comprising administering to a patient in need of such treatment a therapeutically effective amount of a composition according to the instant invention, wherein said pharmacologically active agent is calcitonin. [0024] Further features and advantages of the invention will become apparent from the following detailed description of the invention. DETAILED DESCRIPTION OF THE INVENTION [0025] The pharmacologically active agents suitable for use in the instant invention include both therapeutic as well as preventative agents and is directed particularly to agents which by themselves do not pass or which pass only a small amount of the administered dose through the gastrointestinal mucosa and/or are susceptible to cleavage by acids and enzymes in the gastro-intestinal tract. The pharmacologically active agents include, but are not limited to proteins; polypeptides; hormones; polysaccharides including mixtures of muco-polysaccharides; carbohydrates; lipids; and combinations thereof. [0026] Specific examples of pharmacologically active agents include, but are not limited to, the following, including synthetic, natural or recombinant sources thereof: growth hormone, including human growth hormones (hGH), recombinant human growth hormones (rhGH), bovine growth hormones, and porcine growth hormones; growth hormone-releasing hormones; interferons, including .alpha., .beta., and .gamma.-interferon; interleukin-1; interleukin-2; insulin, including porcine, bovine, human, and human recombinant, optionally having counter ions including sodium, zinc, calcium and ammonium; insulin-like growth factor, including IGF-1; heparin, including unfractionated heparin, heparinoids, dermatans, chondroitins, low, very low and ultra low molecular weight heparins; calcitonin, including salmon, porcine, eel, chicken and human; erythopoietein; atrial naturetic factor; antigens; monoclonal antibodies; somatostatin; protease inhibitors; adrenocorticotropin, gonadotropin releasing hormone; oxytocin; leutinizing-hormone-releasing hormone; follicle stimulating hormone; glucocerebrosidase; thrombopoietin; filgrastim; prostaglandins; cyclosporin; vasopressin; cromolyn sodium (sodium or disodium chromoglycate); vancomycin; desferrioxamine (DFO); parathyroid hormone (PTH), including its fragments; antimicrobials, including anti-fungal agents; vitamins; analogs, fragments, mimetics or polyethylene glycol (PEG)-modified derivatives of these compounds; or any combination thereof. [0027] An interesting pharmacologically active agent is a pharmacologically active peptide, particularly bone active agents, and even more particularly calcitonin. [0028] Bone active agents include classes of agents which display in vivo pharmacological activity in animals such as stabilization, healing, or growth of bone, deceleration or inhibition of bone turnover, deceleration or inhibition of bone resorption, inhibition of osteoclast activity, and stimulation of osteoblast activity. Some of these agents may be peptidic, for example calcitonins, parathyroid hormone (PTH), PTH fragments, analogs and releasers, and Transforming Growth Factors (TGFs) fragments, analogs and releasers. The bone active agents may also be small molecule non-peptidic structures which show in vivo pharmacological bone activities as described above in this paragraph. [0029] A known class of such pharmacologically active agents, calcitonins, have varying pharmaceutical utility and are commonly employed in the treatment of e.g. Paget's disease, hypercalcemia and postmenopausal osteoporosis. Various calcitonins, including salmon, pig and eel calcitonin are commercially available and commonly employed for the treatment of e.g. Paget's disease, hypercalcemia of malignancy and osteoporosis. The calcitonin can be any calcitonin, including natural, synthetic or recombinant sources thereof, as well as calcitonin derivatives such as 1,7-Asu-eel calcitonin. The compositions can comprise a single calcitonin or any combination of two or more calcitonins. The preferred calcitonin is synthetic salmon calcitonin. [0030] The calcitonins are commercially available or may be synthesized by known methods. Continue reading about Orally dosed pharmaceutical compositions comprising a delivery agent in micronized form... 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