Relative bioavailability and pharmacokinetic comparison of two 2-mg risperidone tablet formulations: A single dose, randomized-sequence, double-blind, 2-way crossover study in healthy male volunteers in thailand

Boonleang, Jutima; Pipatrattanaseree, Weerachai; Tanthana, Chanpa; Mahatthanatrakul, Werawath

doi:10.1016/j.clinthera.2010.09.013

Cited by 10 publications

(4 citation statements)

References 20 publications

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“…Plasma samples were analyzed using a validated, sensitive, reproducible and accurate liquid chromatography/tandem mass spectrometry (LC-MS/MS) (Boonleang et al, 2010) briefly described as follow:…”

Section: Determination Of Risperidone In Plasmamentioning

confidence: 99%

Investigation of the effect of solubility increase at the main absorption site on bioavailability of BCS class II drug (risperidone) using liquisolid technique

Khames

2017

Drug Delivery

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To cite this article: Ahmed Khames (2017) Investigation of the effect of solubility increase at the main absorption site on bioavailability of BCS class II drug (risperidone) using liquisolid technique, Drug Delivery, 24:1, 328-338, DOI: 10.1080/10717544.2016 Department of Pharmaceutics and Pharmacy Technology, Taif University, Taif, Saudi Arabia Abstract BCS class II drugs usually suffer inadequate bioavailability as dissolution step is the absorption rate limiting step. In this work, the effect of solubility increase at the main absorption site for these drugs was investigated using risperidone as a drug model. Liquisolid technique was applied to prepare risperidone per-oral tablets of high dissolution rate at intestinal pH (6.8) using versatile nonionic surfactants of high solubilizing ability [Transcutol HP, Labrasol and Labrasol/Labrafil (1:1) mixture] as liquid vehicles at different drug concentrations (10-30%) and fixed (R). The prepared liquisolid tablets were fully evaluated and the dissolution rate at pH 6.8 was investigated. The formulae that showed significantly different release rate were selected and subjected to mathematical modeling using DE 25 , MDT and similarity factor (f2). Depending on mathematical modeling results, formula of higher dissolution rate was subjected to solid state characterization using differential scanning calorimetric (DSC), infrared spectroscopy (IR) and X-ray diffraction (XRD). Finally, the drug bioavailability was studied in comparison to conventional tablets in rabbits. Results showed that liquisolid tablet prepared using Labrasol/ Labrafil (1:1) mixture as liquid vehicle containing 10% risperidone is a compatible formula with law drug crystallinity and higher dissolution rate (100% in 25 min). The drug bioavailability was significantly increased in comparison to the conventional tablets (1441.711 mg h/mL and 137.518 mg/mL in comparison to 321.011 mg h/mL and 38.673 mg/mL for AUC and Cp max , respectively). This led to the conclusion that liquisolid technique was efficiently improved drug solubility and solubility increase of BCS class II drugs at their main absorption site significantly increases their bioavailability.

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Section: Determination Of Risperidone In Plasmamentioning

confidence: 99%

Investigation of the effect of solubility increase at the main absorption site on bioavailability of BCS class II drug (risperidone) using liquisolid technique

Khames

2017

Drug Delivery

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“…For related structures, see : Johnston & Taylor (2011);Li & Cui (2011);Saeed et al (2008); Sripet et al (2012). For background to and applications of benzamide derivatives, see : Boonleang & Tanthana (2010); Brown et al (1991); Hu et al (2008) …”

Section: Related Literaturementioning

confidence: 99%

4-Bromo-N-phenylbenzamide

et al. 2012

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Key indicators: single-crystal X-ray study; T = 100 K; mean (C-C) = 0.003 Å; R factor = 0.032; wR factor = 0.076; data-to-parameter ratio = 25.8.The molecule of the title benzamide derivative, C 13 H 10 BrNO, is twisted with the dihedral angle between the phenyl and 4-bromophenyl rings being 58.63 (9) . The central N-C O plane makes dihedral angles of 30.2 (2) and 29.2 (2) with the phenyl and 4-bromophenyl rings, respectively. In the crystal, molecules are linked by N-HÁ Á ÁO hydrogen bonds into chains along [100]. C-HÁ Á Á contacts combine with the N-HÁ Á ÁO hydrogen bonds, to form a three-dimensional network. Related literature

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“…A detailed literature survey for methylparaben, mometasone furoate and eberconazole nitrate revealed that determination of individual compound or combination with other drugs have been reported by HPLC [2][3][4][5][6][7][8][9][10][11][12][13][14][15][16] , LCMS [17][18] , electrophoresis 19 and spectrophotometric method 20 .…”

mentioning

confidence: 99%

Development and Validation of a Novel Stability Indicating RP-UPLC Method for Simultaneous Estimation of Methylparaben, Mometasone Furoate and Eberconazole Nitrate in Combined Topical Pharmaceutical Dosage Form

2013

Chem Sci Trans

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A novel, rapid, simple, stability indicating RP-UPLC method development and validation for simultaneous estimation of methylparaben (MP), mometasone furoate (MF) and eberconazole nitrate (EN) in topical pharmaceutical dosage form. Isocratic chromatographic separation was achieved on Acquity BEH C18, column using mobile phase consist of buffer (0.1%v/v triethylamine in water pH 6.0 by Glacial acetic acid), acetonitrile in the ratio (40:60, v/v) at flow rate 0.4 mL/min and detection was monitored at 235 nm by using photo-diode array detector. The method shows excellent linearity over the range of 2.75-152.7 µg/mL, 4.45-60.7 µg/mL and 9.10-606.6 µg/mL for methylparaben, mometasone furoate and eberconazole nitrate respectively. Recovery was found for all the components to be in the range of 98.4-101.7%. Stability indicating capability of developed method was established by analysing forced degradation samples in which spectral purity of methylparaben, mometasone furoate and eberconazole nitrate along with separation of degradation products from analytes peak. The proposed method was successfully applied for the quantitative estimation of MP, MF and EN in cream sample.

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Relative bioavailability and pharmacokinetic comparison of two 2-mg risperidone tablet formulations: A single dose, randomized-sequence, double-blind, 2-way crossover study in healthy male volunteers in thailand

Cited by 10 publications

References 20 publications

Investigation of the effect of solubility increase at the main absorption site on bioavailability of BCS class II drug (risperidone) using liquisolid technique

Investigation of the effect of solubility increase at the main absorption site on bioavailability of BCS class II drug (risperidone) using liquisolid technique

4-Bromo-N-phenylbenzamide

Development and Validation of a Novel Stability Indicating RP-UPLC Method for Simultaneous Estimation of Methylparaben, Mometasone Furoate and Eberconazole Nitrate in Combined Topical Pharmaceutical Dosage Form

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