Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Particulate form
Patent
1997-06-19
1999-01-12
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Particulate form
424470, 514951, A61K 916
Patent
active
058584110
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP95/02594 filed Dec. 18, 1995.
TECHNICAL FIELD
This invention relates to sustained-release granular preparations permitting control of the release rates of their medicinal ingredients and also to a production process thereof.
BACKGROUND ART
Sustained release preparations have a function to control the release rate of its medicinal ingredient, and they can maintain the effective blood level of the medicinal ingredient for a long time following administration to patients. In addition, it can also reduce the frequency of administration so that the compliance and QOL (quality of life) of the patient can be improved. Further, control of a blood level of the medicinal ingredient in the range of its minimum effective level to its minimum toxic level can make assure its effectiveness and safety to the human body.
Such sustained release preparations include preparations wherein a medicinal ingredient is coated with a film and preparations of matrix type wherein a medicinal ingredient is dispersed in a matrix. Illustrative preparation forms include multiple-unit preparations and single unit preparations. These multiple-unit preparations in turn include granules and fine granules, which are composed of a number of subunits, and capsules and tablets containing granules or pellets which promptly disintegrate into subunits in the digestive tract after oral administration thereof. On the other hand, such single unit preparations include non-disintegrative matrix tablets, and tablets coated with a release-controlling film.
Multiple-unit preparations are advantageous over single unit preparations in that they have high reproducibility of movement in the digestive tract, have a lower hazardous problem of local irritation owing to their movement in a wide-spread manner through the digestive tract, and permit Jissai To Kadai (Practice and Problems in the Development of Dosable Preparations)", Chapter 3, 215-228, 1986, R & D Planning!. As a production method of multiple-unit preparations, commonly employed is a method in which granules with a medicinal ingredient contained therein are coated with a release-controlling film is commonly employed. Also proposed include a method in which ion-exchange resin beads with a medicinal ingredient bound thereon are coated with a polymer, a method in which granules with a medicinal ingredient dispersed in an enteric solid are prepared by solid dispersion, a method in which matrix-type granules or fine granules with a medicinal ingredient dispersed in a polyglycerin No. 223533/1990!, and as a production method of sustained-release granular preparations of a dihydropyridine-type Ca channel blocker, a method in which the sustained-release granular preparations are produced by extrusion granulation while using an enteric polymer, especially a water-base latex dispersion of a methacrylic acid copolymer LD as a binder (European Patent Application No. 87118948.6 filed on Dec. 21, 1987).
However, the coating method causes a safety problem to the human body because a polymer is dissolved using an organic solvent. Further, there is another problem that cumbersome control is required because the dissolution rate of a medicinal ingredient varies by a change in the thickness of a coating film or in the size of pores present in the coating film. Moreover, the coating method is accompanied by a further problem that, if a crack is formed in the coating film, the medicinal ingredient is rapidly released. On the other hand, in the method in which matrix-type granules or fine granules are produced, production procedures and quality control are relatively easy. It is, however, accompanied by a problem that a special apparatus such as a spray-chilling drier has to be used to obtain granular preparations.
Incidentally, Japanese Language Laid-Open Publication (PCT) No. 503315/1990 discloses a process for producing sustained-release dosable preparations by blending a medicinal ingredient and a polymer having a glass transition temperature (Tg) of from 30.degree. to 150.degr
REFERENCES:
patent: 4329451 (1982-05-01), Zweigle
patent: 4330338 (1982-05-01), Banker
patent: 5326572 (1994-07-01), Mehra et al.
Kojima Masazumi
Nakagami Hiroaki
Sagasaki Shinji
Daiichi Pharmaceutical Co. Ltd.
Page Thurman K.
Spear James M.
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