Title:
【発明の名称】ビスホスホン酸のドライミックス製剤
Document Type and Number:
Japanese Patent JP3365634
Kind Code:
B2
Abstract:
Prepn. of a tablet contg. a bisphosphonic acid deriv. (BP), comprises (a) forming a mixt. contg. the BP, anhydrous or fast flow lactose, dry binder and disintegrant; (b) opt. adding compression aids, flavours, flavour enhancers, sweeteners, and preservatives; (c) lubricating with a lubricant; and (d) compressing to the desired tablet form. The (BP) are chosen from 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid; and its N-methyl and N,N-dimethyl analogues, 3-amino-1-hydroxypropylidene-1,1-bisphosphonic acid and its N,N-dimethyl and N-methyl-N-pentyl analogues; 1-hydroxy-2-(3-pyridyl)ethylidene-1,1-bisphosphonic acid and 4-hydroxymethylene-1,1-bisphosphonic acid piperidine; or their salts. More pref. is 4-amino-1-hydroxybutylidene -1,1-bisphosphonic acid (BP-1) partic. as monosodium salt trihydrate (BP-2). The dry binder is microcrystalline cellulose (MC). The disintegrant is modified starch or cellulose polymer, croscarmellose sodium (CC-Na) or a mixt. esp. CC. The lubricant is Mg stearate. Compsn. range is basic BP 0.5-25, lactose 30-70, MC 30-50, CC-Na 0.5-5 and mg stearate 0.1-2, all %. Closer limits, for BP-2 are BP-2 1-25, lactose 40-60, MC 35-45, CC-Na 0.5-2, and Mg stearate 0.1-1 all %.
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Inventors:
Vitiyard, Simon Earl
Klammer, Kenneth A
Kazdare, Ashiyok buoy
Klammer, Kenneth A
Kazdare, Ashiyok buoy
Application Number:
JP51323894A
Publication Date:
January 14, 2003
Filing Date:
November 17, 1993
Export Citation:
Assignee:
Merck End-Campany Inc.
International Classes:
A61K9/20; A61K9/26; A61K31/4425; A61K31/452; A61K31/66; A61K31/662; A61K31/663; A61K31/675; A61K47/00; A61K47/08; A61K47/12; A61K47/26; A61K47/36; A61K47/38; A61P1/02; A61P1/16; A61P3/14; A61P9/00; A61P13/04; A61P19/02; A61P19/08; A61P19/10; A61P25/00; (IPC1-7): A61K31/66; A61K9/20; A61K47/00
Domestic Patent References:
| JP58189193A | ||||
| JP26409A | ||||
| JP6323889A | ||||
| JP6143196A | ||||
| JP6193190A | ||||
| JP63239291A | ||||
| JP63154692A | ||||
| JP1500754A |
Other References:
【文献】米国特許5047246(US,A)
【文献】米国特許4822609(US,A)
【文献】欧州特許出願公開511767(EP,A1)
【文献】米国特許4822609(US,A)
【文献】欧州特許出願公開511767(EP,A1)
Attorney, Agent or Firm:
Yusuke Hiraki (2 outside)