Paliperidone - CAS 144598-75-4
Catalog number: 144598-75-4
Category: APIs
Molecular Formula:
Molecular Weight:
Yellow crystalline powder
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1. Solid lipid nanoparticles of stearic acid for the drug delivery of paliperidone
Sacheen Kumar and Jaspreet Kaur Randhawa*. RSC Adv.,2015, 5,68743–68750
Paliperidone is an antipsychotic drug having many advantages over other drugs that are currently in use. It has a faster onset of action and offers a lot of flexibility of administration. Moreover, it does not require refrigeration for safe storage. Unfortunately, its poor bioavailability overshadows its advantages. Formulating paliperidone to enhance its bioavailability is actively pursued in pharmaceutical research. Among the various formulation strategies, solid lipid nanoparticles (SLN) could be promising vehicles for the delivery of paliperidone. In an earlier study, we have explored the drug entrapment and encapsulation efficiency of in a lipid Capmul® GMS 50K which is the trade name of glycerol monostearate and is a mono-triglyceride of hydrogenated vegetable oil. It was found that the particle size of the SLNs can be controlled by the use of a suitable surfactant as emulsifier. We have explored the use of two surfactants: sodium deoxycholate and Gelucire® 50/13. Doughnut shaped particles of size 180 to 250 nm were formed with sodium deoxycholate as the surfactant. The entrapment efficiency was 55% with this surfactant.
2. HPTLC method development and validation: Quantification of paliperidone in formulations and in vitro release study
Rashmin B. Patel,* Mrunali R. Patel, Kashyap K. Bhatt and Bharat G. Patel. Anal. Methods, 2010, 2, 525–531
Paliperidone (PPD), (±)-3-{2-[4-(6-Fluoro-1,2-benzisoxazol-3-yl)piperidino]ethyl}-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one is a primary active metabolite of older antipsychotic drug resperidone. PPD is indicated for acute and maintenance treatment of schizophrenia. PPD is marketed by Janssen under the brand name of InvengaTM in 3 mg, 6 mg and 9 mg doses. These dosage forms exhibit low bioavailability due to extensive first-pass metabolism, and the nontargeted delivery results in numerous side effects. As the target site of the PPD is brain, thereby a strategy is desirable that not only improves the bioavailability by preventing first pass metabolism but also provides targeting to the receptor site and bypasses the blood–brain barrier so as to achieve desired drug concentration at the site of action, hence preventing the availability of drug at nontargeting sites and reducing the side effects. Earlier studies have demonstrated direct transport of drugs to brain, circumventing the brain barriers following intranasal (i.n.) administration that provides a unique feature and better option for targeting drugs to brain.
3. Paliperidone-loaded spherical solid lipid nanoparticles
Sacheen Kumar and Jaspreet K. Randhawa*. RSC Adv.,2014, 4,30186–30192
Among the CNS disorders, schizophrenia is a brain disorder that is usually treated with antipsychotic drugs, which include “typical” or “first generation” and “atypical” or “second generation” drugs. Paliperidone or 9-hydroxyrisperidone is the most recently available atypical antipsychotic drug. It is the primary active metabolite of risperidone, which is a well-established second-generation antipsychotic drug. Paliperidone has been developed as an extended-release (ER) tablet formulation and is approved in the US and EU for the treatment of schizophrenia in adults.
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CAS 144598-75-4 Paliperidone

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