Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Particulate form
Patent
1995-05-18
1997-02-11
Azpuru, Carlos
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Particulate form
424 45, 424423, 424426, 424427, 424436, 424442, 424451, 424464, 514291, 514294, A61K 916, A61K 950, A61K 948, A61K 3144
Patent
active
056018444
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
This invention relates to a sustained release medicinal preparation containing a macrocyclic compound or a pharmaceutically acceptable salt thereof shown by the general formula (I) presented hereinafter, which is attracting attention as a substance having a potent immunosuppressive activity, and more particularly, it relates to a sustained release medicinal preparation having said compound (I) or a salt thereof contained in a preparation in the form of so-called microspheres, and as a consequence applicable to various methods of administration including intramuscular injection and other injections, topical administration such as instillation into the eye, inhalation, intraarticular injection and the like, and further, oral administration and rectal administration.
PRIOR ART
A compound represented by the following general formula (I) and a pharmaceutically acceptable salt thereof has been known as a substance showing immunosuppressive activity (refer to Japanese Patent Laid-Open Sho 61(1986)-148181 and European Patent Laid-Open No. 0323042), for which application uses in various medical fields have been expected, including transplantation of organs such as heart, liver, kidney, bone marrow, skin, cornea, lung, pancreas, small intestine, muscle, nerve, limbs: ##STR1## wherein each vicinal pair of R.sup.1 and R.sup.2, R.sup.3 and R.sup.4, R.sup.5 and R.sup.6 independently may
a) represent two vicinal hydrogen atoms, or
b) form a second bond between the vicinal carbon atoms to which they are attached; group or, in conjunction with R.sup.1 it may represent oxo group; or more hydroxy groups, alkenyl group, alkenyl group substituted by one or more hydroxy groups, or alkyl group substituted by oxo group; hydrogen atom) or --CH.sub.2 O--; hydrogen atom) or N--NR.sup.11 R.sup.12 or N--OR.sup.13 ; or tosyl group; R.sup.22 and R.sup.23 independently represent hydrogen atom or alkyl group; independently represent (R.sup.20 a, hydrogen atom) and (R.sup.21 a, hydrogen atom) respectively; R.sup.20 a and R.sup.21 a independently represent hydroxy group, alkyloxy group, or OCH.sub.2 OCH.sub.2 CH.sub.2 OCH.sub.3 or R.sup.21 a is protected hydroxy group; atom in an epoxide ring; the carbon atoms to which they are attached, may represent a 5- or 6-membered N-, S- and/or O-containing heterocyclic ring, which may be saturated or unsaturated, and which may be substituted by one or more groups selected from alkyl group, hydroxy group, alkyl group substituted by one or more hydroxy groups, alkyloxy group, benzyl and --CH.sub.2 Se(C.sub.6 H.sub.5).
Such compound (I) and its pharmaceutically acceptable salt are prepared in the same manner as the one described in the above-mentioned two patent applications. Particularly, the macrolides, which are produced by fermentation of Streptomyces tsukubaensis No.9993 (FERM BP-927) or Streptomyces hygroscopicus subsp. yakushimaensis No.7238 (FERM BP-928), are numbered FR-900506, FR-900520, FR-900523 and FR-900525.
The compound (I) and a pharmaceutically acceptable salt thereof (hereinafter the term "compound (I)" is representatively used to show them) are expected, as described earlier, as a substance having immunosuppressive activity, and has been currently confirmed in various countries in the world of its effectiveness as an immunosuppressant for the rejection by organ transplantation. However, for inhibiting the rejection reaction after the operations it is necessary to administer the drug cautiously over a long period, and it has been desired to develop a dosage form excellent in a sustained release activity.
This invention has been started with an attention paid to the above-mentioned circumstances, and pursued with a view to provide a sustained release medicinal preparation which shows a long activity over a long period by achieving sustained release after being administered to a living body.
DISCLOSURE OF INVENTION
The sustained release medicinal preparation of this invention is produced by enclosing the active ingredient comprising the compound (I) into fin
REFERENCES:
patent: 4916138 (1990-04-01), Ueda et al.
patent: 5196437 (1993-03-01), Starzl et al.
patent: 5260301 (1993-11-01), Nakanishi et al.
patent: 5368865 (1994-11-01), Asakura et al.
patent: 5385907 (1995-01-01), Asakura et al.
Database WPI, Derwent Publications, AN 92-102775, and JP 4 49232, Feb. 18, 1992.
Hata Takehisa
Kagayama Akira
Kimura Sumihisa
Murata Saburo
Tanimoto Sachiyo
Azpuru Carlos
Fujisawa Pharmaceutical Co. Ltd.
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