PaliperidoneCAS# 144598-75-4 |
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Quality Control & MSDS
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Chemical structure
3D structure
Cas No. | 144598-75-4 | SDF | Download SDF |
PubChem ID | 115237 | Appearance | Powder |
Formula | C23H27FN4O3 | M.Wt | 426.48 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Solubility | DMSO : 5 mg/mL (11.72 mM; Need ultrasonic) | ||
Chemical Name | 3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one | ||
SMILES | CC1=C(C(=O)N2CCCC(C2=N1)O)CCN3CCC(CC3)C4=NOC5=C4C=CC(=C5)F | ||
Standard InChIKey | PMXMIIMHBWHSKN-UHFFFAOYSA-N | ||
Standard InChI | InChI=1S/C23H27FN4O3/c1-14-17(23(30)28-9-2-3-19(29)22(28)25-14)8-12-27-10-6-15(7-11-27)21-18-5-4-16(24)13-20(18)31-26-21/h4-5,13,15,19,29H,2-3,6-12H2,1H3 | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
Description | Atypical antipsychotic; metabolite of risperidone . Exhibits high affinity for 5-HT2A receptors (Ki = 0.4 nM for cloned human 5-HT2A receptors). Also displays nanomolar affinity for human D2 receptors. |
Paliperidone Dilution Calculator
Paliperidone Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 2.3448 mL | 11.7239 mL | 23.4478 mL | 46.8955 mL | 58.6194 mL |
5 mM | 0.469 mL | 2.3448 mL | 4.6896 mL | 9.3791 mL | 11.7239 mL |
10 mM | 0.2345 mL | 1.1724 mL | 2.3448 mL | 4.6896 mL | 5.8619 mL |
50 mM | 0.0469 mL | 0.2345 mL | 0.469 mL | 0.9379 mL | 1.1724 mL |
100 mM | 0.0234 mL | 0.1172 mL | 0.2345 mL | 0.469 mL | 0.5862 mL |
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. |
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Paliperidone is a SR (5-HT2) receptor antagonist and D2DR inhibitor.
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Risk assessment and experimental design in the development of a prolonged release drug delivery system with paliperidone.[Pubmed:28331293]
Drug Des Devel Ther. 2017 Mar 13;11:733-746.
This study focuses on the development of a drug product based on a risk assessment-based approach, within the quality by design paradigm. A prolonged release system was proposed for Paliperidone (Pal) delivery, containing Kollidon((R)) SR as an insoluble matrix agent and hydroxypropyl cellulose, hydroxypropyl methylcellulose (HPMC), or sodium carboxymethyl cellulose as a hydrophilic polymer. The experimental part was preceded by the identification of potential sources of variability through Ishikawa diagrams, and failure mode and effects analysis was used to deliver the critical process parameters that were further optimized by design of experiments. A D-optimal design was used to investigate the effects of Kollidon SR ratio (X1), the type of hydrophilic polymer (X2), and the percentage of hydrophilic polymer (X3) on the percentages of dissolved Pal over 24 h (Y1-Y9). Effects expressed as regression coefficients and response surfaces were generated, along with a design space for the preparation of a target formulation in an experimental area with low error risk. The optimal formulation contained 27.62% Kollidon SR and 8.73% HPMC and achieved the prolonged release of Pal, with low burst effect, at ratios that were very close to the ones predicted by the model. Thus, the parameters with the highest impact on the final product quality were studied, and safe ranges were established for their variations. Finally, a risk mitigation and control strategy was proposed to assure the quality of the system, by constant process monitoring.
Health care resource use analysis of paliperidone palmitate 3 month injection from two phase 3 clinical trials.[Pubmed:28277864]
Curr Med Res Opin. 2017 Jun;33(6):1083-1090.
OBJECTIVE: The objective of this study was to compare occupational status and health care resource use between treatment groups in clinical trials 3012 (PP3M versus placebo) and 3011 (PP3M versus PP1M). METHODS: Occupational status was assessed at each study visit. Logistic regressions modeled the probability of hospitalization during the double-blind phase. RESULTS: At the start of each study, a low percentage of patients were full-time employed or gainfully self-employed (approximately 10% in trial 3012 and 11%-13% in trial 3011). Improvement from baseline in occupational status was slightly higher in the PP3M group than in placebo or PP1M groups. The odds of a hospitalization for psychiatric and social reasons during 1 year was 7.74 (95% CI, 2.39-25.05; p < .001) for a patient on placebo compared with the odds of hospitalization during 1 year for a patient on PP3M. No statistically significant difference was observed between PP3M and PP1M (odds ratio, 1.16; 95% CI, 0.70-1.93). Very similar results were observed for hospitalizations due to psychiatric reasons only, within each trial. CONCLUSIONS: In both trials, most patients were unemployed and not seeking work or were retired at open-label baseline, and only a small number of patients changed their occupational status during the trials. In trial 3012, subjects who received placebo had significantly higher odds of hospitalization for either psychiatric and social reasons or for psychiatric reasons alone compared with subjects who received PP3M. In contrast, in trial 3011, the odds of hospitalizations were not significantly different between PP3M and PP1M.
[Comparative evaluation of clinical and economic efficiency of paliperidone in various dosage forms used in patients with schizophrenia].[Pubmed:28374699]
Zh Nevrol Psikhiatr Im S S Korsakova. 2017;117(2):85-92.
AIM: To evaluate clinical and economic efficacy of schizophrenia treatment with three forms of Paliperidone (peroral form, intramuscular injections once a month and once in three month). MATERIAL AND METHODS: Pharmacoeconomic analysis based on the results of earlier foreign randomized clinical studies on Paliperidone in treatment of schizophrenia was carried out. Indirect comparison of different medication forms of Paliperidone compared to placebo was performed. The analysis of costs was based on a Markov model built for the study. Two categories of costs: costs of pharmacological treatment with Paliperidone and costs of disease exacerbation due to the violation of treatment regimen were considered. To assess pharmacoeconomic efficacy of Paliperidone, a cost-benefit analysis with calculation of cost utility ratio (CUR) and incremental cost utility ratio (ICUR) was used. RESULTS AND CONCLUSION: In view of the influence on the budget, all forms of Paliperidone have similar pharmacoeconomic efficacy with the advantage of prolonged release injectable (depot) forms that increase patient's adherence to treatment. As a result, CUR of injectable forms was lower compared to that of the peroral form by 11,1 and 46,3% of month and 3-month forms, respectively. ICUR for Paliperidone used once in 3 month (trevicta) was more effective compared to Paliperidone used monthly (xeplion). It has been concluded that Paliperidone for prolonged release injections used once in 3 month is most pharmacoeconomically effective.
Paliperidone Long-Acting Plasma Level Monitoring and a New Method of Evaluation of Clinical Stability.[Pubmed:28278537]
Pharmacopsychiatry. 2017 Jul;50(4):145-151.
The second generation long-acting antipsychotics can be a pharmacologic strategy, both in the early phase of illness and in the case of low compliance. The aim of the study was to evaluate the clinical efficacy and tolerability of one monthly injection of Paliperidone palmitate (PP1M), Paliperidone plasma levels (PLs), and the clinical outcome. 21 outpatients, affected by Schizophrenia or Schizoaffective Disorder, were recruited. PP1M started with 150 mg on day 1 and 100 mg on day 8. Following patients were given a dosage ranging from 50 mg to 150 mg every 28 days. At baseline, and then monthly, patients were clinically evaluated. BPRS and PANSS total score showed a statistically significant decrease from T2 (after 2 months) to T12 (after 12 months). The PLs steady-state was approximatively reached after the fifth injection (T4). All the patients showed a clinical stabilization: BPRS and PANSS scores showed a significant improvement from T2. PLs data seems to suggest the initial possibility of an oral supplementation, although clinical evaluation demonstrated no relapse during the study.