Evaluation of dissolution consistency of Iloperidone Tablets / 药物评价研究

Objective To compare the dissolution curves of reference preparation and self-prepared Iloperidone Tablets in four different pH dissolution media (0.1 mol/L HC1 solution,pH 4.5 acetate buffer solution,pH 6.8 phosphate buffer solution,and water).Methods The solubility of Iloperidone in different pH solutions was measured,the dissolution curves of two preparations in four different pH dissolution media were determined by HPLC,and the similarity was investigated according to the f2 factor method.Results The f2 factors between reference preparation and self-prepared Iloperidone Tablets in four different media were more than 50.Conclusion The two preparations are equivalent in four different pH dissolution media in vitro.

Patent analysis of pharmaceutical cocrystals technology in China / 中国药科大学学报

@#Pharmaceutical cocrystals are formed from the active pharmaceutical ingredients and cocrystal formers through hydrogen bonding or other noncovalent bonds, which have attracted much attention in pharmaceutical field in recent years. From the analysis of patent application situation, patent applicant, legal status, and patent application techniques, guiding directions for the future research and development of the pharmaceutical cocrystals are proposed in this article.

Synthesis of iloperidone / 军事医学

Objective To optimize the synthesis process of iloperidone 1 for industrial production.Methods Piperi-dine-4-carboxylic acid, acetic acid and acetic anhydride were used as starting materials to generate 2 via amidation, Friedel-Crafts acylation, hydration, oximation, intramolecular cyclization and salification.Compound 2 was treated with 4-(3-chloropropoxy)-3-methoxyphenylethanone through condensation to afford iloperidone.The target compound 1 was prepared with an overall yield of 34.9%.Results and Conclusion Such factors as the ratio of the raw materials, the catalyst, reactive time were investigated and optimized to make the reaction conditions mild and easy to control with less side effects.The structure has been confirmed by IR, 1 H-NMR and MS.

Iloperidone – A Newer Antipsychotic.

The optimal treatment of schizophrenia poses a challenge to develop more effective treatments and safer drugs, to overcome poor compliance, discontinuation and frequent switching with available antipsychotics. Iloperidone is a new antipsychotic developed to overcome some of the limitations in the drug treatment of schizophrenia. It has been approved by regulating agencies for use in treatment of adult schizophrenia.

Newer Atypical Antipsychotic Drugs / 대한정신약물학회지

During the last decade, new era of antipychotic drugs has begun with the introduction of risperidone and olanzapine following clozapine. These atypical drugs are characterized by fewer extrapyramidal side effects and at least equal or superior clinical efficacy, although their effects on negative symptoms and refractory cases remain controversial. For these reasons, these atypical antipsychotic drugs are now recommended as a choice of first line treatments for schizophrenia and these new atypical drugs are replacing conventional antipsychotic drugs. These atypical drugs, however, are not same in terms of efficacy and side effects. Risperidone produces more frequent dose-dependent extrapyramidal symptoms and olanzapine causes significant weight gains more frequently compared to other atypical antipsychotic drugs. More recently, several newer atypical drugs are being released or will be available in the near future. Quetiapine and amisulpride are already being used in Europe and will be available soon in Korea. Quetiapine, even at high doses, has been reported to have placebo-level extrapyramidal side effects. It has been well tolerated in patients with parkinson's diseases who are particularly sensitive to extrapyramidal side effects. Amisulpride is known to have dual dopamine blockade effects. Ziprasidone, which had not been approved due to concerns about possible QTc prolongation, has been finally approved by FDA. Ziprasidone has been reported to cause little weight gain compared to other atypical drugs. Aripiprazole, data on which has been submitted to FDA for approval, has a unique mechanism of action as a dopamine partial agonist. Iloperidone is known to be under large-scale phase III clinical trial as a promising new antipsychotic drug. In this paper, these newer atypical antipsychotic drugs were reviewed with respect to efficacy and safety based on the data of clinical trials.