The Pharmacokinetics of Pranoprofen in Humans

Yoshio, Ikumi; Iwata, Akihiro; Isobe, Masao; Higashi, Miwako

doi:10.1248/yakushi1947.110.7_509

Cited by 8 publications

(2 citation statements)

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“…To predict if systemic levels of PF would be achieved after the topical application of PF-NLC-N6 to a specific surface area, we calculated the predicted plasma concentration at the steady state ( Css ) using the Equation (6):

where Css is the concentration in plasma at the steady-state, J ss is the flux computed in this study, A is the hypothetical application area of 1 cm 2 , and Clp is the plasma clearance obtained from the literature; we considered two populations, the young subjects ( Clp = 1146.60 cm 3 /h) and the elderly subjects ( Clp = 609.00 cm 3 /h) [ 1 , 51 ].…”

Section: Methodsmentioning

confidence: 99%

Quality by Design of Pranoprofen Loaded Nanostructured Lipid Carriers and Their Ex Vivo Evaluation in Different Mucosae and Ocular Tissues

et al. 2022

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Transmucosal delivery is commonly used to prevent or treat local diseases. Pranoprofen is an anti-inflammatory drug prescribed in postoperative cataract surgery, intraocular lens implantation, chorioretinopathy, uveitis, age-related macular degeneration or cystoid macular edema. Pranoprofen can also be used for acute and chronic management of osteoarthritis and rheumatoid arthritis. Quality by Design (QbD) provides a systematic approach to drug development and maps the influence of the formulation components. The aim of this work was to develop and optimize a nanostructured lipid carrier by means of the QbD and factorial design suitable for the topical management of inflammatory processes on mucosal tissues. To this end, the nanoparticles loading pranoprofen were prepared by a high-pressure homogenization technique with Tween 80 as stabilizer and Lanette® 18 as the solid lipid. From, the factorial design results, the PF-NLCs-N6 formulation showed the most suitable characteristics, which was selected for further studies. The permeability capacity of pranoprofen loaded in the lipid-based nanoparticles was evaluated by ex vivo transmucosal permeation tests, including buccal, sublingual, nasal, vaginal, corneal and scleral mucosae. The results revealed high permeation and retention of pranoprofen in all the tissues tested. According to the predicted plasma concentration at the steady-state, no systemic effects would be expected, any neither were any signs of ocular irritancy observed from the optimized formulation when tested by the HET-CAM technique. Hence, the optimized formulation (PF-NLCs-N6) may offer a safe and attractive nanotechnological tool in topical treatment of local inflammation on mucosal diseases.

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Section: Methodsmentioning

confidence: 99%

Quality by Design of Pranoprofen Loaded Nanostructured Lipid Carriers and Their Ex Vivo Evaluation in Different Mucosae and Ocular Tissues

et al. 2022

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“…It was reported that pranoprofen is strongly bound to plasma protein (Kato et al, 1976) and shows rapid absorption and a urinary recovery of over 90% after the oral administration of a marketed conventional tablet to humans (Yoshio et al, 1990).…”

Section: Introductionmentioning

confidence: 99%

Enhanced Bioavailability by Transdermal Administration of Pranoprofen Gels Containing Octanoic Acid to Rats

Shin¹

2008

Biomolecules and Therapeutics

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− The pharmacokinetic parameters and bioavailability of pranoprofen from the gel were measured to determine the enhancing effect of octanoic acid on the transdermal absorption of pranoprofen in rats. 8 mg/kg of pranoprofen was administered from gel with octanoic acid (the enhancer group) or that without octanoic acid (the control group) via the transdermal route, and the results were compared with those obtained from the intravenously (0.5 mg/kg, IV group) or orally administered group (4 mg/kg, oral group). The AUC of the control, the enhancer, the IV, and the oral groups were 20.2±5.1, 50.7±12.7, 19.9±2.5, and 70.5±17.6 ug/ml·h respectively. The average C max of the control and the enhancer group were 0.93±0.23 and 2.82±0.71 ug/ml, respectively, and the mean T max of the control and the enhancer group was 7.00 h. The relative bioavailability of the transdermally administered pranoprofen gel containing octanoic acid was approximately 2.50 times higher than the control group, showing a relatively constant, sustained blood concentration with minimal fluctuation. This suggests that it might be feasible to develop a pranoprofen gel preparation containing an enhancer for the transdermal administration, which is more convenient dosage form than the oral dosage forms.

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Pranoprofen

2006

Meyler's Side Effects of Drugs: The International Encyclopedia of Adverse Drug Reactions and Interactions

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The Pharmacokinetics of Pranoprofen in Humans

Cited by 8 publications

References 0 publications

Quality by Design of Pranoprofen Loaded Nanostructured Lipid Carriers and Their Ex Vivo Evaluation in Different Mucosae and Ocular Tissues

Quality by Design of Pranoprofen Loaded Nanostructured Lipid Carriers and Their Ex Vivo Evaluation in Different Mucosae and Ocular Tissues

Enhanced Bioavailability by Transdermal Administration of Pranoprofen Gels Containing Octanoic Acid to Rats

Pranoprofen

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