Microenvironmental pH-modified Amisulpride-Labrasol matrix tablets: development, optimization and in vivo pharmacokinetic study

Younes, Nihal Farid; Assasy, Abd El-Halim I. El; Makhlouf, Amal

doi:10.1007/s13346-019-00706-2

Cited by 13 publications

(8 citation statements)

References 39 publications

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“…In addition, the incorporation of boric acid in the formula decreased the pH in the microenvironment surrounding the tablet which provided favorable conditions for drug dissolution and increased the dissolution rate. These results coincided with those reported by Younes et al who found that the incorporation of organic acid as a pH modifier imparted pH-independent release of the weakly basic amisulpride (Younes et al, 2021 ). Furthermore, the decrease in drug crystallinity, which was proven by X-ray diffractometry, fastened the dissolution rate.…”

Section: Resultssupporting

confidence: 91%

“…Since FLB is a weakly basic drug, the incorporation of acidic excipient might provide an acidic microenvironment surrounding the tablet which increases drug solubility (Younes et al, 2021 ). Therefore, boric acid was chosen as a lubricant in the prepared FLB sublingual tablets.…”

Section: Resultsmentioning

confidence: 99%

“…The saturation solubility of pure FLB and the lyophilized FLB-NC formulae was determined in distilled water (Younes et al, 2021 ). Excess amounts of the tested samples were added to 5 mL distilled water in screw-capped glass vials.…”

Section: Methodsmentioning

confidence: 99%

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Scalable flibanserin nanocrystal-based novel sublingual platform for female hypoactive sexual desire disorder: engineering, optimization adopting the desirability function approach and in vivo pharmacokinetic study

Naguib

Makhlouf

2021

Drug Delivery

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Flibanserin (FLB) was approved by FDA for the treatment of pre-menopausal female hypoactive sexual desire disorder (HSDD). FLB suffers from low oral bioavailability (33%) which might be due to hepatic first-pass metabolism in addition to its poor aqueous solubility. The sublingual route could be a promising alternative for FLB due to the avoidance of enterohepatic circulation. However, the drug needs to dissolve in the small volume of saliva in order to be absorbed through the sublingual mucosa. Therefore, FLB nanocrystals were prepared by sono-precipitation technique according to 2 3 full factorial design. FLB-nanocrystals were formulated using two surfactants (PVP K30 and PL F127) in two different amounts (200 and 400 mg) and the volume of ethanol was either 3 or 5 mL. Nanocrystal formulation was optimized according to the desirability function to have a minimum particle size, zeta potential, polydispersity index, and maximum saturated solubility. The optimized formula had a particle size of 443.12 ± 14.91 nm and a saturated solubility of 23.27 ± 4.62 mg/L which is five times the saturated solubility of FLB. Nanocrystal dispersion of the optimized formula was solidified by freeze-drying and used to prepare rapidly disintegrating sublingual tablets containing Pharmaburst ® as superdisintegrant. Sublingual tablet formulation with the shortest disintegration time (36 s) was selected for the in vivo study. FLB nanocrystal-based sublingual tablets exhibited a two-fold increase in bioavailability with a faster onset of action compared to the commercially available oral formulation. These findings prove the potential application of FLB nanocrystal-based sublingual tablets in the treatment of HSDD.

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Section: Resultssupporting

confidence: 91%

Section: Resultsmentioning

confidence: 99%

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Scalable flibanserin nanocrystal-based novel sublingual platform for female hypoactive sexual desire disorder: engineering, optimization adopting the desirability function approach and in vivo pharmacokinetic study

Naguib

Makhlouf

2021

Drug Delivery

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“…The differential scanning calorimeter (DSC-50, Shimadzu, Japan) calibrated with purified indium was used to generate the thermograms of pure ATV, GMO, Kolliphor ® P 407, eugenol, Gelucire ® 44/14, physical mixture of the OEEPC, and the lyophilized OEEPC. Approximately 5 mg of each sample was sealed in an aluminum pan and heated at a temperature range of 25 °C to 300 °C at a scanning rate of 10 °C/min under a nitrogen purge of 50 ml/min (Younes et al., 2021 ).…”

Section: Methodsmentioning

confidence: 99%

“…FTIR-8400 (Shimadzu, Kyoto, Japan) was used to analyze the IR spectra of ATV, GMO, Kolliphor ® P 407, eugenol, Gelucire ® 44/14, physical mixture of the OEEPC, and the lyophilized OEEPC at ambient temperature. Approximately 2 – 3 mg of each sample was compressed into a disk using dry KBr and then scanned at the scanning range of 400–4000 cm −1 (Younes et al., 2021 ).…”

Section: Methodsmentioning

confidence: 99%

Syringeable atorvastatin loaded eugenol enriched PEGylated cubosomes in-situ gel for the intra-pocket treatment of periodontitis: statistical optimization and clinical assessment

et al. 2023

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Atorvastatin calcium (ATV) is a well-known anti-hyperlipidemic drug currently being recognized for possessing an anti-inflammatory effect. Introducing it as a novel remedy for periodontitis treatment necessitates developing a syringeable modified delivery system capable of targeting inflammation within the periodontal pockets. Thus, a 3 3 Box-Behnken design was used to generate eugenol enriched PEGylated cubosomes. Based on the desirability function, the optimized formulation (OEEPC) was selected exhibiting a solubilization efficiency (SE%) of 97.71 ± 0.49%, particle size (PS) of 135.20 ± 1.11 nm, polydispersity index (PDI) of 0.09 ± 0.006, zeta potential (ZP) of −28.30 ± 1.84 mV and showing a sustained drug release over 12 h. It displayed a cubic structure under the transmission electron microscope, furthermore, it was stable upon storage for up to 30 days. Hence, it was loaded into an optimum syringeable in-situ gel (ISG) which displayed the desired periodontal gelation temperature (34 ± 0.70 °C) and an adequate gelation time (46 ± 2.82 sec), it also released approximately 75% of the drug within 72 h. Clinical evaluation of the ISG showed a promising percentage reduction of about 58.33% in probing depth, 90% in the bleeding index, 81.81% in the plaque index, and 70.21% in gingival levels of transforming growth factor–β1. This proved that the formulated syringeable intra-pocket delivery system of ATV is an efficient candidate for diminishing inflammation in periodontitis.

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Bioequivalence of 200 mg Amisulpride Tablets in Healthy Chinese Volunteers under Fasting and Fed Conditions

Cao,

2023

Clinical Pharm in Drug Dev

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In this study, we compared the pharmacokinetics and safety of a new generic product and a branded reference product of amisulpride tablets. Additionally, we assessed the bioequivalence of the 2 products in healthy Chinese volunteers to acquire sufficient evidence for the marketing approval of the generic drug. Thirty volunteers under fasting and fed conditions were randomly administered a single dose of the test or reference drug orally, followed by a 7‐day washout period. The pharmacokinetic parameters were obtained by the concentration‐time profiles, including the area under the plasma concentration‐time curve (AUC) over the dosing interval, AUC from time zero to infinity, maximum plasma concentration, time to achieve maximum plasma concentration, and elimination half‐life. AUC from time zero to infinity of amisulpride in the postprandial group was reduced by approximately 25%, suggesting that a high‐fat diet can affect this parameter. In the aspect of safety, no serious adverse events occurred. This study demonstrated that generic and reference products of amisulpride tablets were bioequivalent in healthy Chinese volunteers under fasting and fed conditions.

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Microenvironmental pH-modified Amisulpride-Labrasol matrix tablets: development, optimization and in vivo pharmacokinetic study

Cited by 13 publications

References 39 publications

Scalable flibanserin nanocrystal-based novel sublingual platform for female hypoactive sexual desire disorder: engineering, optimization adopting the desirability function approach and in vivo pharmacokinetic study

Scalable flibanserin nanocrystal-based novel sublingual platform for female hypoactive sexual desire disorder: engineering, optimization adopting the desirability function approach and in vivo pharmacokinetic study

Syringeable atorvastatin loaded eugenol enriched PEGylated cubosomes in-situ gel for the intra-pocket treatment of periodontitis: statistical optimization and clinical assessment

Bioequivalence of 200 mg Amisulpride Tablets in Healthy Chinese Volunteers under Fasting and Fed Conditions

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