AI Article Synopsis
- The study investigates the pharmacokinetics and tissue distribution of asenapine maleate (ASPM), a new antipsychotic, after oral administration in rats.
- A validated reversed-phase HPLC method was developed for analyzing ASPM, showing a good recovery rate and linearity in plasma and tissue samples.
- The results revealed a long half-life of 32.74 hours and a tendency for ASPM to accumulate in highly perfused organs, indicating effective drug distribution.
Article Abstract
Aim: Asenapine maleate (ASPM) is a newer antipsychotic drug available as a sublingual tablet in the market.
Experimental: To investigate the pharmacokinetic and tissue distribution study of ASPM following oral administration in rats, reversed-phase HPLC method was developed and validated.
Results: ASPM was extracted from plasma and tissue matrix by liquid-liquid extraction technique and analyzed using mobile phase consisted of phosphate buffer pH 3.0 and acetonitrile (65:35% v/v). The method showed good linearity (10-500 ng/ml) with recovery 83-102%. In pharmacokinetics study, half-life was 32.74 ± 7.51 h due to slow elimination of drug. The biodistribution study indicated preferential distribution of ASPM to highly perfused organs.
Conclusion: The current method can be successfully applied for estimating the drug in various biological matrices.
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| http://dx.doi.org/10.4155/bio-2017-0069 | DOI Listing |
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Article Synopsis
- Asenapine maleate (ASPM) is a second-generation antipsychotic approved for adult schizophrenia and bipolar disorder but suffers from low oral bioavailability (<2%) due to extensive first-pass metabolism in the liver.
- To improve ASPM's absorption, researchers developed nanoformulations using ligands like RGD and peptide dendrimers to target the intestinal lymphatic system.
- Various techniques, including solid phase peptide synthesis and high-performance chromatography, were used to create and characterize liposomal formulations, and in vitro and in vivo studies were conducted to assess their effectiveness and pharmacokinetics in rats.
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