Shin-etsu Chemical Co., Ltd.

Other

Kondo, Tetsuo

Yoshiro Onda

Hiroaki Muto

Hiroshi Suzuki

Kazumasa Maruyama

Soji Tanioka

Tohru Chiba

Fujio Sekigawa

Kazuhisa Hayakawa

Hiroyasu Kokubo

Yuichi Nishiyama

Noboru Hoshi

Makoto Ooura

Atsushi Hatayama

Tetsuo Kondo

Kiyokazu Imai

Mitsuhiro Morita

Polysaccharide is wet pulverized by ejecting a liquid dispersion of polysaccharide from a pair of nozzles under a high pressure of 70 to 250 MPa to form a pair of jets so that the jets collide against each other. The nozzles are oriented to define a collision angle of 95-178&#xb0; and the number of pulverizing cycles is adjusted such that the polysaccharide is pulverized to an average particle length which is equal to or less than &#xbc; of the initial average particle length while undergoing a reduction in degree of polymerization of less than 10%.

Wet pulverizing of polysaccharides

A vinyl acetylsalicylate-vinyl alcohol based copolymer which comprises a structural unit having the following formula (1): ##STR1## and a structural unit having the following formula (2): ##STR2## optionally with at least one member selected from the group consisting of a structural unit having the following formula (3): ##STR3## and a structural unit having the following formula (4): ##STR4## In the copolymer, the amounts of vinyl acetylsalicylate units and vinyl alcohol units, degree of polymerization and the like can be controlled, whereby the efficacy of acetylsalicylic acid can be easily controlled as desired. Therefore, the copolymer is expected to be widely applicable as medicament.

Vinyl acetylsalicylate-vinyl alcohol based copolymer

A coated solid medicament form suitable for oral administration having reliable releasability of the active ingredient only in the large intestine is proposed. The medicament form is prepared by coating a core solid medicament form containing the active ingredient first with a chitosan having a specific degree of deacetylation and a specific degree of polymerization and then top-coated with a specific enteric-soluble polymer which is a hydroxypropyl methyl cellulose acetate succinate or a hydroxypropyl methyl cellulose hexahydrophthalate. The releasability of the active ingredient only in the large intestine can be more reliable when the core medicament form is, prior to coating with chitosan, provided with an enteric undercoating layer.

Coated solid medicament form having releasability in large intestine

Film coated pharmaceutical preparations, which are prepared by overlaying to the outer surface of pharmaceutical preparations, a coating layer comprising at least one member selected from the group consisting of methyl cellulose, hydroxypropylmethyl cellulose, hydroxypropyl cellulose, hydroxypropylmethyl cellulose phthalate, hydroxypropylmethyl cellulose acetate succinate, carboxymethylethyl cellulose and cellulose acetate phthalate, are irradiated with light including ultraviolet rays. Whereby film coated pharmaceutical preparations, the coating layer surface of which are excellent in whiteness, are prepared. Moreover, as a content of a white pigment in corporated into the coating layer of such preparations may be reduced, the stability of such preparations can be enhanced without impairing the strength of the coating layer.

Method for preparing film coated pharmaceutical preparations and method

The invention discloses a novel modified polyvinyl butyral polymer having photocurability and heat-curability containing an ethylenically unsaturated moiety, which is introduced by the reaction of, for example, N-methylol acrylamide with a part of the hydroxyl groups, in addition to the vinyl butyral moiety, vinyl acetate moiety and vinyl alcohol moiety constituting conventional polyvinyl butyral resins. The inventive polymer is useful for various types of adhesives, coating materials, interlayers of laminated shatter-proof glass and the like similarly to unmodified polyvinyl butyral resins but with a possibility of broadened utilizability and absence of the problems due to evaporation of organic solvents.

Novel photocurable and heat-curable polyvinyl butyral resin

In place of gelatin conventionally used as a material for shaping hard medicinal capsules, the invention proposes a hard capsule for medicinal use shaped of a polymer blend of a water-soluble cellulose ether, e.g., alkyl cellulose, hydroxyalkyl cellulose and alkyl hydroxyalkyl cellulose, and a polyvinyl alcohol in a weight ratio of 70:30 to 98:2. The inventive hard medicinal capsules have remarkably low permeability to oxygen and moisture with little influences on the medicament contained therein along with sufficiently high mechanical strengths and are much more stable than conventional gelatin-made capsules against the influences of the ambient conditions, such as, the crack formation unavoidable in a gelatin-made hard capsule when it is kept under an extremely low humidity.

Hard medicinal capsule

A novel aqueous coating composition is proposed for providing enteric coating on solid dosage forms such as tablets. The aqueous coating composition of the invention comprises a fine powder of an enterosoluble cellulose derivative such as hydroxypropylmethylcellulose phthalate and hydroxypropylmethylcellulose acetate succinate, which is insoluble in water but can be plasticized and solubilized with certain plasticizing agents, as dispersed in an aqueous dispersing medium and a plasticizing agent having compatibility with the enterosoluble cellulose derivative and dissolved in the aqueous dispersing medium. The particle size of the enterosoluble cellulose derivative and the boiling point of the plasticizing agent is the key parameters and should be finer than 100 .mu.m in an average particle diameter and not lower than 100.degree. C., respectively. Upon application of the aqueous coating composition to the solid dosage forms, water as the dispersing medium is first evaporated leaving the cellulose derivative and the plasticizing agent, which latter solubilizes the former to form a continuous coating layer on the solid dosage forms imparting good and satisfactory enterosolubility thereto.

Method for providing enteric coating on solid dosage forms and aqueous

The invention provides a novel enterosoluble capsule for containing a medicament, which is shaped with a hitherto not used novel cellulose derivative. The cellulose derivative is a mixed ester of an alkyl-, hydroxyalkyl- or hydroxyalkyl alkylcellulose esterified with succinyl anhydride and an aliphatic monocarboxylic acid anhydride. The enterosoluble capsules have excellent enterosolubility behavior as well as sufficient pliability even without the addition of a plasticizer which is almost indispensable in the prior art materials. The cellulose derivative can be shaped into capsules not only by the conventional dipping method but also by the plastic deformation at an elevated temperature under pressure such as compression molding, vacuum forming, matchedmold forming and the like.

Enterosoluble capsules

The present invention provides a novel compound cyanoethylpullulan which is a cyanoethylation product of pullulan. Pullulan is readily cyanoethylated by the reaction with acrylonitrile in the presence of an alkali catalyst such as sodium hydroxide. The cyanoethylpullulan having a degree of cyanoethylation of at least 50% has various unique properties in the heat resistance, solubility in organic solvents, film-forming property, adhesive bonding to metals and the like in comparison with related cyanoethylated products such as cyanoethylcellulose and cyanoethylated polyvinyl alcohol.

Cyanoethylpullulan

A novel cellulose derivative provided in this invention is a mixed ester of an alkoxy or hydroxyalkoxy substituted cellulose ether, prepared by the esterification reaction of the ether with succinic anhydride and an anhydride of an aliphatic monocarboxylic acid. The cellulose derivatives are advantageous because of their capability of producing enteric coatings having sufficient flexibility without the use of a plasticizer as well as by their chemical and physical stability against moisture, and also by easy purification after completion of the esterification reaction. The coatings produced from the derivatives have a similar chemical and physical stability. The cellulose derivatives are useful for the enteric coating of pharmaceutical dosage forms and also for providing halation-preventing layers on photographic films.

Ether-ester derivatives of cellulose and their applications

In the process for the preparation of low-substituted cellulose ethers comprising the successive steps of etherification of alkali cellulose, neutralization of the crude cellulose ether, washing, drying and pulverization, the neutralization step is carried out in two stages, i.e., by first employing 5 to 80% of an acid stoichiometrically required and then adding an additional amount of the acid to complete neutralization. The cellulose ethers thus prepared can readily be pulverized into fine powder having a very good flowing property and yet an excellent binding force, and work as a suitable disintegrator in tablets.

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Tokyo, Japan

Yoshiro Onda