公开(公告)号：JPS6348228A

公开(公告)日：1988-02-29

申请号：JP18957186

申请日：1986-08-14

Applicant: TOA EIYO LTD

Inventor： NISHINOMIYA YOZO ,  HATORI TOKUO ,  NARA TAKESHI

IPC: A61K47/32 ,  A61K47/00 ,  A61K47/24 ,  A61K47/36 ,  A61K47/38

Abstract: PURPOSE:To obtain an easily absorbable solid preparation of a hardly soluble drug having remarkably improved dispersibility, by mixing a hardly soluble drug with a phospholipid and a disintegrant. CONSTITUTION:A hardly soluble drug is dissolved or dispersed together with a phospholipid in an organic solvent (e.g. methanol), a disintegrant is added to the solution or dispersion and the organic solvent is removed from the mixture to obtain the objective preparation. As an alternative method, the objective preparation is produced by mixing and crushing a hardly soluble drug together with a phospholipid and a disintegrant in the absence of solvent. The hardly soluble drug is those having a water-solubility of

公开(公告)号：JPS6314724A

公开(公告)日：1988-01-21

申请号：JP15872586

申请日：1986-07-08

Applicant: TOA EIYO LTD

Inventor： NARA TAKESHI ,  HATORI TOKUO ,  NISHINOMIYA YOZO ,  SENDA SATOSHI

IPC: A61K47/42 ,  A61K31/505 ,  A61K47/00 ,  A61K47/38

Abstract: PURPOSE:To provide the titled preparation containing crystalline prazosin and an enteric base (excluding acrylic resin). CONSTITUTION:The objective prazosin preparation can be produced by mixing crystalline prazosin (e.g. hydrochloride: the crystal form of the compound may be alpha-, beta- or gamma-form, etc., or their mixture; preferably fine powder with an average particle diameter of =4.5 pH: e.g. cellulose acetate phthalate, shellac, etc.) at a weight ratio of 1:(0.05-50) and, if necessary, further mixing with a nonionic surfactant, excipient, disintegrant, colorant, etc. The dissolution rate of prazosin from the preparation is high and the released prazosin can be easily absorbed through digestive tracts. Prazosin is active to circulatory system (dilates peripheral vessel, decreases peripheral flow resistance and lowers pressure level) and is useful as a remedy for hypertension.

公开(公告)号：JPS61148115A

公开(公告)日：1986-07-05

申请号：JP26859284

申请日：1984-12-21

Applicant: TOA EIYO LTD

Inventor： NARA TAKESHI ,  HATORI TOKUO ,  NISHINOMIYA YOZO ,  HAYASHI HISASHI

IPC: A61K9/16 ,  A61K9/20 ,  A61K9/22 ,  A61K31/34 ,  A61K31/505 ,  A61P9/12

Abstract: PURPOSE:The titled pharmaceutical of a slightly soluble drug consisting of the slightly soluble drug, a release inhibitor and high swelling polymer. CONSTITUTION:A sustained release pharmaceutical containing a slightly soluble drug, e.g. isosorbid nitrate, prazosin hydrochloride or furosemide, 5-80wt% release inhibitor, e.g. ethyl cellulose, acrylic acid-methacrylic ester copolymer, hardened oil or wax and 0.5-20wt% swelling high polymer, e.g. carboxyvinyl polymer, hydroxypropyl cellulose with a low substitution degree or microcrystalline cellulose. The resultant pharmaceutical has a little change in release rate due to variation in size of granular material, method of preparation, hardness of compression molded material, etc., and therefore excellent reproducibility of release rate renders the pharmaceutical suitable for mass production. The slightly soluble drug is released for a long time by given combination of the above-mentioned respective materials, and the dissolution rate of the slightly soluble drug shows a safe dissolution of about 100%.

公开(公告)号：JPH0587488B2

公开(公告)日：1993-12-16

申请号：JP26859284

申请日：1984-12-21

Applicant: TOA EIYO LTD

Inventor： NARA TAKESHI ,  HATORI TOKUO ,  NISHINOMYA YOZO ,  HAYASHI HISASHI

IPC: A61K9/16 ,  A61K9/20 ,  A61K9/22 ,  A61K31/34 ,  A61K31/505 ,  A61P9/12

公开(公告)号：JPS62158217A

公开(公告)日：1987-07-14

申请号：JP23886

申请日：1986-01-07

Applicant: TOA EIYO LTD

Inventor： NARA TAKESHI ,  NISHINOMIYA YOZO ,  HATORI TOKUO ,  SENDA SATOSHI

IPC: A61K31/505 ,  A61K9/16 ,  A61P9/12 ,  C07D239/00 ,  C07D307/00 ,  C07D405/12

Abstract: PURPOSE:To obtain the titled granule, capable of sustaining the blood level without deteriorating the absorbability and useful as an antihypertensive agent sufficiently effective by one administration a day, by adding a solution of a water-insoluble substance in an organic solvent to a mixture of prazosin with a dissolution accelerating substance and excipient and granulating the resultant blend. CONSTITUTION:A sustained release granule of prazosin, obtained by adding a solution of a water-insoluble substance dissolved in an organic solvent to a mixture of prazosin with a dissolution accelerating substance, e.g. enteric base, cyclodextrin, nonionic surfactant, etc.) and excipient and granulating the resultant blend and having nondisintegrating property. Ethyl cellulose having 5-100cP viscosity at 20 deg.C and 44-51wt% ethoxy group content, hardened oil, etc., may be preferred for the water-insoluble substance, which forms a drug holding structure and prevents the disintegration of the granule in digestive juice. The dissolved prazosin is sustainedly released since it diffuses interstices between the water-insoluble substance in a weaving way.

公开(公告)号：JPS61227524A

公开(公告)日：1986-10-09

申请号：JP6506085

申请日：1985-03-30

Applicant: TOA EIYO LTD

Inventor： NARA TAKESHI ,  HATORI TOKUO ,  SENDA SATOSHI

IPC: C07D405/12 ,  A61K31/505 ,  A61K47/00 ,  A61K47/10 ,  A61K47/30 ,  C07D405/14

Abstract: PURPOSE:To obtain a prazosin preparation useful as an antihypertensive, having prazosin dispersed in an amorphous state in a compounding base, by dissolving prazosin and a specific compounding base in an organic solvent and removing the solvent. CONSTITUTION:Prazosin and one or more compounding bases selected from PVP, PEG, propylene glycol, water-soluble gel high polymer (e.g., hydroxypropyl cellulose, MC, etc.), base soluble in the stomach (e.g., polyvinylacetal diethylaminoacetate, etc.), enteric base (e.g., hydroxypropylmethyl cellulose phthalate, etc.) is dissolved in an organic solvent and the solvent is removed, to give the titled preparation. A blending ratio of prazosin to the compounding base is preferably 1:10 (weight ratio). Prazosin is dispersed and dissolved in an amorphous state in the base and the preparation has more improved solubility and absorption properties than alpha form of prazosin hydrochloride.

公开(公告)号：JPS61221122A

公开(公告)日：1986-10-01

申请号：JP6193585

申请日：1985-03-28

Applicant: TOA EIYO LTD

Inventor： NARA TAKESHI ,  HATORI TOKUO ,  NISHINOMIYA YOZO ,  SENDA SATOSHI

IPC: C07D405/12 ,  A61K9/14 ,  A61K9/16 ,  A61K31/505 ,  A61K47/00 ,  A61K47/30 ,  C07D239/00 ,  C07D307/00

Abstract: PURPOSE:To provide a prazosin preparation having increased solubility of prazosin and remarkably improved bioavailability of prazosin and useful as a hypotensor, by compounding prazosin with a specific substrate such as cyclodextrin, carboxyvinyl polymer, etc. CONSTITUTION:The objective prazosin preparation is produced by compounding prazosin with a substrate selected from the group of cyclodextrin, carboxyvinyl polymer, polyvinyl acetal diethylaminoacetate, acrylic resin and nonionic surfactant. The weight ratio of prazosin to the substrate is preferably 1 to 0.1-20. The prazosin is preferably prazosin hydrochloride fine powder having a particle diameter of