Iloperidone orally disintegrating tablet

Abstract

The invention relates to an iloperidone orally disintegrating tablet, which is characterized in that: 1) the grain size D of the iloperidone is less than or equal to 90 and more than or equal to 30 mum; 2) the proportion of water-solubility components in the tablet is more than or equal to 50%; and 3) the orally disintegrating tablet can be disintegrated when meeting spittle in an oral cavity.

Description

Background technique [0001] Classic antipsychotics (tranquilizers), such as haloperidol, work by blocking mesolimbic dopamine D 2 receptors to exert therapeutic effect. However, these drugs have a relatively narrow therapeutic window, and excessive or long-term use can cause extrapyramidal side effects (EPS), such as dystonia (muscle spasms that distort the face), akathisia, Parkinson's disease-like symptoms (muscular rigidity, tremor), tardive dyskinesia [abnormal reflex and / or twisting movements], and potentially fatal neuroleptic malignancy (muscle rigidity, fever, and irregular pulse). [0002] Clozapine is the first antipsychotic drug that can significantly reduce the incidence of EPS, creating a new class of drugs-atypical antipsychotic drugs that simultaneously antagonize the 5-hydroxytryptamine receptor 5-HT-A 2 and D 2 The dual role of receptors. Clinically, this class of drugs can not only effectively treat the positive symptoms of schizophrenia (hallucinations, ...

AI Technical Summary

Problems solved by technology

[0003] Iloperidone (iloperidone) is a piperidinyl benzo derivative, in rodents, the 5-HT 2 The receptor has a high affinity (IC 50 =9.3nmol / L), while for D 2 The affinity of the receptor is relatively reduced by an order of magnitude (IC 50 =109nmol / L); to epinephrine α 1 The receptor also has a very high affinity (IC 50 =04nmol / L), but for α 2 , 5-HT-1A, σ and D1 receptors have much lower affinity (IC 50 60, 210, 180 and 750nmol / L respectively)