Abstract: An object of the present invention is to provide an anti-constipation composition containing a halogenated-bi-cyclic compound as an active ingredient in ratio of bi-cyclic/mono-cyclic structure of at least 1:1. The halogenated-bi-cyclic compound is represented by Formula (I): where X1 and X2 are preferably both fluorine atoms. The composition can be used to treat constipation with out substantive side-effects, such as stomachache.
Abstract: An object of the present invention is to provide an anti-constipation composition containing a halogenated-bi-cyclic compound as an active ingredient in ratio of bi-cyclic/mono-cyclic structure of at least 1:1. The halogenated-bi-cyclic compound is represented by Formula (I): where X1 and X2 are preferably both fluorine atoms. The composition can be used to treat constipation with out substantive side-effects, such as stomachache.
Abstract: A dosage unit for treating constipation in a human patient is described. The dosage unit of the invention comprises a halogenated prostaglandin analog and a pharmaceutically suitable excipient. The dosage unit relieves constipation without substantial side effects.
Abstract: Disclosed is a novel composition comprising a novel bi-cyclic compound, which is expected to be pharmaceutically active, and a glyceride. The stability of the bi-cyclic compound can be improved significantly by dissolving the same in a glyceride.
Abstract: Disclosed is a novel composition comprising a novel bi-cyclic compound, which is expected to be pharmaceutically active, and a glyceride. The stability of the bi-cyclic compound can be improved significantly by dissolving the same in a glyceride.
Abstract: The present invention provides a soft gelatin capsule formulation of a 15-keto-prostaglandin compound, which includes: a soft gelatin capsule shell including gelatin and sugar alcohol as a plasticizer, and a mixture including a 15-keto-prostaglandin compound and a pharmaceutically acceptable vehicle which is filled in the shell. By encapsulating the 15-keto-prostaglandin compound in the specified soft gelatin capsule shell, stability of the compound is significantly improved.
Abstract: An object of the present invention is to provide an anti-constipation composition containing a halogenated-bi-cyclic compound as an active ingredient in a ratio of bi-cyclic/mono-cyclic structure of at least 1:1. The halogenated-bi-cyclic compound is represented by Formula (I): where X1 and X2 are preferably both fluorine atoms. The composition can be used to treat constipation without substantive side-effects, such as stomachache.
Abstract: Disclosed is a method for stabilizing a pharmaceutically active bi-cyclic compound of formula (I): comprising the step of: admixing the same with a polyol and/or a fatty acid ester other than glyceride and a composition obtained by the method. In addition a soft gelatin capsule formulation of the compound of formula (I) obtained by incorporating the compound in a soft gelatin capsule shell comprising gelatin and a polyol plasticizer.
Abstract: Disclosed is a method for stabilizing a pharmaceutically active bi-cyclic compound of formula (I): comprising the step of: admixing the same with a polyol and/or a fatty acid ester other than glyceride and a composition obtained by the method. In addition a soft gelatin capsule formulation of the compound of formula (I) obtained by incorporating the compound in a soft gelatin capsule shell comprising gelatin and a polyol plasticizer.
Abstract: The present invention discloses a soft gelatin capsule formulation of a 15-keto-prostaglandin compound, which comprises: a soft gelatin capsule shell comprising gelatin and sugar alcohol as a plasticizer, and a mixture comprising a 15-keto-prostaglandin compound and a pharmaceutically acceptable vehicle which is filled in the shell. By encapsulating the 15-keto-prostaglandin compound in the specified soft gelatin capsule shell, stability of the compound is significantly improved.
Abstract: Disclosed is a method for stabilizing a pharmaceutically active bi-cyclic compound of formula (i): comprising the step of: admixing the same with a polyol and/or a fatty acid ester other than glyceride and a composition obtained by the method. In addition a soft gelatin capsule formulation of the compound of formula (I) obtained by incorporating the compound in a soft gelatin capsule shell comprising gelatin and a polyol plasticizer.
Abstract: Disclosed is a method for treating tumor in a mammalian subject, which comprises administering a combination of (a) an anti-tumor agent and (b) a fatty acid derivative represented by the formula (I): to the subject in need thereof. The application also discloses a method for treating damages, especially gastrointestinal damages including mucositis such as stomatitis induced by an anti-tumor agent, wherein the method comprises administering a fatty acid derivative of formula (I) to the subject who is receiving the anti-tumor agent.
Abstract: Provided is a method for promoting gastrointestinal bicarbonate secretion in a mammalian subject, which comprises administering an effective amount of a compound of Formula (I): to a subject in need thereof. The compound is also useful for protecting the gastrointestinal tract of a mammal from mucosal damage.
Abstract: Provided is a method for the long term treatment of a condition or disease which is one of the indications for NSAID use in a human patient, which comprises administering to the patient a pharmaceutically effective amount of a NSAID and at least 36 mcg per day of cobiprostone or its pharmaceutically acceptable salt, ester, ether or amide. By administering cobiprostone or its pharmaceutically acceptable salt, ester, ether or amide in combination with a NSAID, the patient can receive the NSAID for longer time period.
Abstract: Provided is a method for promoting bicarbonate secretion in the stomach or duodenum in a mammalian subject, which comprises administering an effective amount of a compound of Formula (I): to a subject in need thereof, wherein A, Y, W1, W2, X1, X2 R1 and R2 are herein defined. The compound are also useful for protecting the gastrointestinal tract of a mammal from mucosal damage.
Abstract: Disclosed is a method for modulating a claudin-mediated function in a mammalian subject which comprises administering to a subject in need thereof an effective amount of a specific fatty acid derivative. The application also discloses a method for treating a dermatological disease and a method for modulating an expression of a claudin in a mammalian subject using the same fatty acid derivative as above.
Abstract: Disclosed is a novel use of a chloride channel opener, especially a prostaglandin compound for the treatment of abdominal discomfort. Further disclosed is a novel use of a chloride channel opener, especially a prostaglandin compound for the treatment of functional gastrointestinal disorders.
Abstract: Disclosed is a method for preparing a prostaglandin derivative of formula (A): which comprises reacting an aldehyde represented by formula (1): with a 2-oxoalkyl phosphonate in a reaction solvent under the presence of alkali hydroxide as sole base. By carrying out the reaction using an alkali hydroxide as sole base in the reaction system, the desired prostaglandin derivative can be obtained by simple procedures and with high yield.
Abstract: Disclosed is a method for treating macular degeneration in a mammalian subject, which comprises administering to the subject in need thereof an effective amount of a 15-keto-prostaglandin compound such as 13,14-dihydro-15-keto-20-ethyl-prostaglandin F2? isopropyl ester.
Abstract: Disclosed is a method for preparing a prostaglandin derivative of formula (A): which comprises reacting an aldehyde represented by formula (1): with a 2-oxoalkyl phosphonate in a reaction solvent under the presence of alkali hydroxide as sole base. By carrying out the reaction using an alkali hydroxide as sole base in the reaction system, the desired prostaglandin derivative can be obtained by simple procedures and with high yield.