| 摘要 |
A pharmaceutical composition comprises (%) an idazoxan salt or idazoxan hydrate (5-20), microcrystalline cellulose (10-40), lubricant (1-5), colloidal silica (0.1-0.5) and lactose (29.5-84.8). - Independent claims are included for the following: - (a) tablets comprising the pharmaceutical composition (50 - 1000, preferably 100 - 600) mg; - (b) manufacture of the tablet involving direct tabletting of a powder mixture; - (c) use of the composition and tablet optionally in combination with an atypical antipsychotic neuroleptic exhibiting a greater antagonist affinity for the dopamine D2 receptor than is its antagonist affinity for the alpha -adrenoreceptor, a medicament for the preventive and/or curative treatment of severe psychotic disorders (preferably schizophrenia and schizoaffective disorders); - (d) polymorphic forms I, II, III, IV or V of idazoxan having X-ray diffraction pattern as given in the specification and having a differential thermal analysis thermogram exhibiting a single maximum value at 207.5 plus or minus 0.2, approx. 203 plus or minus 0.4, approx. 203.8 plus or minus 0.5, approx. 205.3 plus or minus 0.5, 205.6 plus or minus 0.4 respectively. - ACTIVITY - Antidepressant; Antiparkinsonian; Neuroleptic; CNS-Gen.. - MECHANISM OF ACTION - None given. |
