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Sustained release oral preparationsRelated Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Preparations Characterized By Special Physical Form, Tablets, Lozenges, Or Pills, Sustained Or Differential Release TypeSustained release oral preparations description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20070116763, Sustained release oral preparations. Brief Patent Description - Full Patent Description - Patent Application Claims
TECHNICAL FIELD [0001] The present invention relates to 2-amino-3-cyano-5-(2-fluorophenyl)-4-methylpyrrole having the following structure (I): BACKGROUND ART [0002] 2-Amino-3-cyano-5-(2-fluorophenyl)-4-methylpyrrole is known to be an excellent therapeutic drug for treating pollakiuria and urinary incontinence having a bladder-selective calcium-sensitive potassium channel activating effect (see PCT WO99/36068). [0003] On the other hand, the above described drug was found to have a short plasma half life, which may cause nocturnal pollakiuria or urinary incontinence, due to which a patient is forced to dose the drug at night, resulting in a problematic reduction in the QOL (quality of life) or the compliance of the patient. DISCLOSURE OF THE INVENTION [0004] An object of the present invention is to provide a pharmaceutical preparation containing the drug as an active ingredient, which is capable of improving the QOL and the compliance of the patient who doses the drug while avoiding any excessive increase in the plasma level of the drug by means of controlling the in vivo release rate of the drug and also by means of reducing the frequency of taking the drug. [0005] In order to solve the above described problem, the present invention provides a controlled release oral preparation (hereinafter, referred to as "the preparation of the present invention") containing 2-amino-3-cyano-5-(2-fluorophenyl)-4-methylpyrrole (hereinafter, referred to as "the present compound") as an active ingredient. [0006] The term "controlled release oral preparation" employed herein means an oral preparation with the release or dissolution (hereinafter, simply referred to as "release") of an active ingredient controlled. In the present invention, the dosage form or composition of the preparation is not limited particularly, as long as the preparation is a controlled release oral preparation having the above described functions. [0007] A preparation which does not have the release controlling ability according to the present invention usually exhibits a release ratio of the drug 90% by weight or more within one hour, for example, when it is subjected to the dissolution test as directed in Method 2 under the 13th Japanese Pharmacopoeia which will be described later. The preparation of the present invention, when it is subjected to a similar test, exhibits a release ratio of the present compound, for example, of 0 to 70% by weight after 1 hour, 0 to 80% by weight after 2 hours, 5 to 95% by weight after 4 hours, 10 to 100% by weight after 8 hours, 20 to 100% by weight after 12 hours and 50 to 100% byweight after 24 hours, preferably, of 5 to 60% by weight after 1 hour, 10 to 70% by weight after 2 hours, 20 to 90% by weight after 4 hours, 30 to 100% by weight after 8 hours, 40 to 100% by weight after 12 hours and 50 to 100% by weight after 24 hours. [0008] However, a preparation which releases the present compound in an intestinal tract due to its nature, such as an enteric-coated preparation, can be included in the preparations according to the present invention since it is controlled so that the present compound is released in the intestinal tract, although it does not exhibit the release ratio in the above described test. [0009] Generally, a controlled release oral preparation can be classified into a delayed release oral preparation and a sustained release oral preparation, both of which are included in the present invention. [0010] The "delayed release oral preparation" can be regarded as a controlled release oral preparation which is designed so that the migration of the preparation from stomach to small intestine is retarded or so that the release of the drug from the preparation is effective in a site in intestine rather than in stomach. A concrete example thereof may include an enteric-coated preparation. [0011] The "sustained release oral preparation" can be generally regarded as a controlled release oral preparation which is designed so that the release of the drug from a preparation is effected gradually in a digestive tract regardless of whether it occurs in stomach or intestine. This sustained release type can be classified into a controlled release type intended to prolong the effect by maintaining a certain plasma level of the drug and a prolonged release type intended to prolong the effect without any ability of maintaining a certain plasma level of the drug, both of which are included in the present invention. Concrete examples of the sustained release oral preparation may include a sustained release film-coated preparation, SPAN-THRU preparation and wax matrix preparation. [0012] The preparation of the present invention may employ only one of various controlled release means described above, or may be a combined oral preparation employing both of a delayed release oral preparation and a sustained release oral preparation. An instantaneous release property may also be combined partially. [0013] A concrete preparation capable of exerting the above described release controlling ability, i.e., a concrete example of the preparation of the present invention may include any of those shown below which are known to those skilled in the art. [0014] (1) Controlled Diffusion Oral Preparation [0015] A controlled diffusion oral preparation is a preparation capable of controlling the release of a drug using a material which undergoes almost no dissolution in a fluid in a digestive tract, and examples thereof may be as follows, for example. <1> Insoluble Film-Coated Preparation [0016] An insoluble film-coated preparation basically has a core containing a drug (the present compound) coated with a pharmaceutically acceptable material which undergoes almost no dissolution in a fluid in a digestive tract (insoluble material). Such an insoluble film-coated preparation can control the release of the drug (the present compound) from a preparation due to the barrier of the insoluble material present as a coating film thereon. [0017] An example of the insoluble film-coated preparation according to the present invention may include a sustained release granule preparation or a sustained release film-coated preparation containing the present compound as an active ingredient. The present compound which exists in the core of the preparation of the present invention is released gradually through this coating film into the outside of the preparation. [0018] A core containing a drug, i.e., the present compound may be the present compound itself or a mixture, for example, of one or more of the following pharmaceutically acceptable additives (hereinafter, simply referred to as "additives") and the present compound in an amount of 1 to 99% by weight in the core. 1. Cellulose Derivatives [0019] Crystalline cellulose, sodium carboxymethyl cellulose,alkyl celluloses such as methyl cellulose and ethyl cellulose, hydroxyalkyl celluloses such as hydroxypropyl cellulose or low substituted hydroxypropyl cellulose and hydroxypropylmethyl cellulose (2208, 2906, 2910), carboxymethyl cellulose, calcium carboxymethyl cellulose and sodium crosscarmellose. Continue reading about Sustained release oral preparations... Full patent description for Sustained release oral preparations Brief Patent Description - Full Patent Description - Patent Application Claims Click on the above for other options relating to this Sustained release oral preparations 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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