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  Method for producing preparation containing bioactive substanceUSPTO Application #: 20060241045Title: Method for producing preparation containing bioactive substance Abstract: A method for producing a preparation containing a bioactive substance, characterized in that it comprises forming a solid material containing the bioactive substance and a polymer, and contacting the solid material with a high pressure gas. The method allows the production of a preparation which is suppressed in excessive initial release of the bioactive substance immediately after the administration thereof, is capable of releasing a predetermined amount of the bioactive substance over a long period of time, and is extremely reduced in the deterioration of the bioactive substance and in the amount of a residual organic solvent. (end of abstract) Agent: Wenderoth, Lind & Ponack, L.L.P. - Washington, DC, US Inventors: Yoshihiro Ohmachi, Masafumi Misaki, Shigeyuki Takada USPTO Applicaton #: 20060241045 - Class: 514012000 (USPTO) Related Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), Peptide Containing (e.g., Protein, Peptones, Fibrinogen, Etc.) Doai, Cyclopeptides, 25 Or More Peptide Repeating Units In Known Peptide Chain Structure The Patent Description & Claims data below is from USPTO Patent Application 20060241045. Brief Patent Description - Full Patent Description - Patent Application Claims
TECHNICAL FIELD [0001] The present invention relates to a method for producing a preparation containing a bioactive substance. More specifically, the present invention relates to a method for producing a preparation comprising a bioactive substance, which is unstable to heat or solvents, and a polymer. BACKGROUND ART [0002] Peptidic or non-peptidic bioactive substances are known to exhibit various pharmacological activities in a living body, and the application thereof as medicaments have been attempted. However, it is required to administer these bioactive substances frequently since their half-life in a living body is generally short. Then, physical burden of patients due to administration by injection cannot be ignored. For example, growth hormone, a representative hormone which is originally produced and secreted in the anterior portion of the pituitary gland, is a bioactive peptide having widely diverse physiological activities such as, in addition to promotion of growth in the body, metabolism of saccharides and lipids, anabolism of proteins, cell proliferation and differentiation, and the like. At present, growth hormone is produced on a large scale by Escherichia coli using genetic recombination technology, and put to medicinal use clinically and worldwide. However, it is required to administer growth hormone frequently in order to maintain an effective blood level because of its short biological half-life. Especially, in the case of pituitary dwarfism, a daily subcutaneous administration to infants or young patients over a long period of time ranging from a few months to 10 years or more is actually taken place. [0003] In order to deal with problems inherent in such bioactive substances, various drug delivery systems have been studied. For example, a sustained-release agent that provides sustained-release of a bioactive peptide over a long period of time has been studied. JP 8-217691 A (WO96/07399) discloses a method for producing a sustained-release preparation comprising a water-insoluble or poorly water soluble polyvalent metal salt of a water-soluble peptidic bioactive substance, which is formed by an aqueous solution of zinc chloride, etc., and a biodegradable polymer. [0004] Further, for a sustained-release preparation using a biodegradable polymer, it is desired to maintain the activity of a bioactive substance with suppressing the initial release of a bioactive substance, in particular, release of the excess amount within one day, and to control the release of the bioactive substance arbitrarily over a long period of time. Regarding this problem, JP 11-322631 A discloses a method for producing a sustained-release preparation comprising adding a water-miscible organic solvent and/or a volatile salt to an aqueous solution of a bioactive peptide, followed by lyophilizing to obtain a bioactive peptide powder, dispersing the powder in a solution of a biodegradable polymer in an organic solvent, and removing the organic solvent. Furthermore, JP 9-132524 A discloses a method for producing sustained-release microcapsules comprising a bioactive substance and a biodegradable polymer which comprises, after forming microcapsules, heat-drying the microcapsules at a temperature of not less than the glass transition temperature of the biodegradable polymer for about 24 to 120 hours. These are methods for producing a sustained-release preparation containing very little residual organic solvent and having very superior clinical properties as medicaments. OBJECTS OF THE INVENTION [0005] However, according to the solvent-removing procedures in the above-mentioned production methods, since it takes long period of time for removing the solvent, there is still room for improvement in view of the production costs for the industrial application. [0006] On the other hand, as a procedure for removing a solvent that remains in a component (e.g., polymer) used for formulating a preparation of a medicament, heat drying method, vacuum drying method and flash drying with dried gas have been known. However, in these procedures, when a substance has strong affinity for a solvent and is unstable to heat, the removal of the solvent tends to be insufficient or, in some cases, the substance is decomposed. Furthermore, in these procedures, when the boiling point of a solvent to be removed is high, the properties of a preparation obtained may be deteriorated. SUMMARY OF THE INVENTION [0007] The present inventors have studied intensively to solve the above-mentioned problems and unexpectedly found that, in a method for producing a sustained-release preparation comprising a bioactive substance and a biodegradable polymer, a sustained-release preparation having superior clinical properties as a medicament, in which excess initial release of the bioactive substance immediately after administration is markedly suppressed, a constant amount of the bioactive substance is being released from immediately after administration over a long period of time and very little residual organic solvent is contained therein, can be obtained by, after forming a solid material, contacting the solid material with high-pressure gas for about 10 minutes to about 12 hours. The present invention has been completed based on these findings. [0008] That is, the present invention provides: [0009] (1) A method for producing a preparation containing a bioactive substance, which comprises forming a solid material containing the bioactive substance and a polymer, and contacting the solid material with high-pressure gas; [0010] (2) The method according to the above (1), wherein the bioactive substance is that being unstable to heat or solvents; [0011] (3) The method according to the above (1), wherein the bioactive substance is a bioactive peptide having a molecular weight of about 2,000 to about 500,000; [0012] (4) The method according to the above (1), wherein the bioactive substance is a bioactive peptide having a molecular weight of about 5,000 to about 500,000; [0013] (5) The method according to the above (4), wherein the bioactive substance is human growth hormone; [0014] (6) The method according to the above (1), wherein the bioactive substance is a non-peptidic compound; [0015] (7) The method according to the above (6), wherein the non-peptidic compound is a compound having an oxygen atom in the molecule; [0016] (8) The method according to the above (6), wherein the non-peptidic compound is a compound having an ether bond or a carbonyl group; [0017] (9) The method according to the above (6), wherein the non-peptide compound is a compound represented by the formula (I): wherein R.sup.1 represents a group capable of forming an anion or a group which may be converted into said group, X represents that the phenylene group and the phenyl group are linked directly or via a spacer of an atomic chain having two or less atom(s), n represents an integer of 1 or 2, ring A represents a benzene ring which may be further substituted, R.sup.2 represents a group capable of forming an anion or a group which may be converted into said group, R.sup.3 represents a hydrocarbon residue which may link via a heteroatom and may be substituted, or a salt thereof; [0018] (10) The method according to the above (6), wherein the non-peptidic compound is losartan, eprosartan, candesartan cilexetil, candesartan, valsartan, telmisartan, irbesartan, tasosartan or olmesartan; [0019] (11) The method according to the above (6), wherein the non-peptide compound is candesartan; [0020] (12) The method according to the above (1), wherein the polymer is biodegradable; Continue reading... Full patent description for Method for producing preparation containing bioactive substance Brief Patent Description - Full Patent Description - Patent Application Claims Click on the above for other options relating to this Method for producing preparation containing bioactive substance patent application. Patent Applications in related categories: 20080167221 - Heterocarpine, a plant-derived protein with anti-cancer properties - The invention relates to a plant-derived protein with anti-cancer properties which binds the human growth hormone-releasing hormone (hGHRH). Said protein, which is obtained from the Pilocarpus Heterophyllus plant, is particularly adapted for preparing a medicament that is intended for the treatment of cancers for which growth is dependant on the ... ###  How KEYWORD MONITOR works... a FREE service from FreshPatents1. Sign up (takes 30 seconds). 2. Fill in the keywords to be monitored. 3. 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