The pharmacokinetics of pranoprofen in the elderly.

Kajiyama, Hiroyuki; Fujimura, Akio; Ebihara, Akio; Y, Hino

doi:10.3999/jscpt.17.657

Cited by 4 publications

(5 citation statements)

References 3 publications

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“…In view of the pharmacokinetic parameters of the PRA for young and old-age humans, the estimated steady-state plasma theoretical concentration C ss of the drug that would penetrate the skin post topical administration was estimated with the following equation:

where J ss is the flux, A is the hypothetical area of application (considering in this case 100 cm 2 ), and CL p is the human plasma clearance of PRA (reported values of 609.00 cm 3 /h and 1146.60 cm 3 /h, for old-age and young humans, respectively) [ 31 , 42 ].…”

Section: Methodsmentioning

confidence: 99%

“…where J ss is the flux, A is the hypothetical area of application (considering in this case 100 cm 2 ), and CL p is the human plasma clearance of PRA (reported values of 609.00 cm 3 /h and 1146.60 cm 3 /h, for old-age and young humans, respectively) [31,42]. Male Mus musculus mice (10-12 weeks; 12-30 g) (n = 9) were used for the mouse ear inflammation model.…”

Section: Ex Vivo Permeation Studymentioning

confidence: 99%

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Semi-Solid Dosage Forms Containing Pranoprofen-Loaded NLC as Topical Therapy for Local Inflammation: In Vitro, Ex Vivo and In Vivo Evaluation

Ahmadi

Rincón

Silva-Abreu

et al. 2023

Gels

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Pranoprofen (PRA)-loaded nanostructured lipid carriers (NLC) have been dispersed into blank gels composed of 1% of Carbomer 940 (PRA-NLC-Car) and 3% of Sepigel® 305 (PRA-NLC-Sep) as a novel strategy to refine the biopharmaceutical profile of PRA, for dermal administration in the treatment of skin inflammation that may be caused by possible skin abrasion. This stratagem intends to improve the joining of PRA with the skin, improving its retention and anti-inflammatory effect. Gels were evaluated for various parameters such as pH, morphology, rheology, and swelling. In vitro drug release research and ex vivo permeation through the skin were carried out on Franz diffusion cells. Additionally, in vivo assays were carried out to evaluate the anti-inflammatory effect, and tolerance studies were performed in humans by evaluating the biomechanical properties. Results showed a rheological profile common of semi-solid pharmaceutical forms for dermal application, with sustained release up to 24 h. In vivo studies using PRA-NLC-Car and PRA-NLC-Sep in Mus musculus mice and hairless rats histologically demonstrated their efficacy in an inflammatory animal model study. No signs of skin irritation or modifications of the skin’s biophysical properties were identified and the gels were well tolerated. The results obtained from this investigation concluded that the developed semi-solid formulations represent a fitting drug delivery carrier for PRA’s transdermal delivery, enhancing its dermal retention and suggesting that they can be utilized as an interesting and effective topical treatment for local skin inflammation caused by a possible abrasion.

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Section: Methodsmentioning

confidence: 99%

Section: Ex Vivo Permeation Studymentioning

confidence: 99%

Semi-Solid Dosage Forms Containing Pranoprofen-Loaded NLC as Topical Therapy for Local Inflammation: In Vitro, Ex Vivo and In Vivo Evaluation

Ahmadi

Rincón

Silva-Abreu

et al. 2023

Gels

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“…This investigation discloses sufficient evidence that targeting and a prolonged effect can be accomplished with immense perspective in dermal delivery. Regarding the results obtained from the predicted steady-state plasma concentrations of PRA (Css) for both PRA-NLC and the PRA solution, assuming an area of application of 100 cm 2 of skin, they were far below the reported therapeutic plasma concentration achieved through oral administration (4.89 ± 1.29 µg/mL and 10.19 ± 2.43 µg/mL for older and younger humans, respectively) [39][40][41]. These values guarantee that the dermal application of the nanosuspension would not have any systemic effect; thus, they guarantee a safe local anti-inflammatory and analgesic effect.…”

Section: Discussionmentioning

confidence: 84%

“…The results of the permeation parameters-flux (J ss , µg/h/cm 2 ), permeability coefficient (Kp, cm/h), lag time (TL, h), the cumulative amount of PRA permeated after 24 h of experiment (Q 24h µg), and the amount retained in the skin (Q ret µg/g/cm 2 )-are described in Table 6. Table 7 shows the predicted steady-state plasma concentrations (C ss , µg/mL), the values of which were below the reported therapeutic plasma concentration (4.89 ± 1.29 µg/mL for older humans and 10.19 ± 2.43 µg/mL for younger humans) [39][40][41]. These results suggest that the dermal application of PRA-NLC may not have systemic effects, which guarantees a safe local anti-inflammatory and analgesic effect of the PRA.…”

Section: Ex Vivo Skin Permeation Studiesmentioning

confidence: 85%

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A Novel Approach for Dermal Application of Pranoprofen-Loaded Lipid Nanoparticles for the Treatment of Post-Tattoo Inflammatory Reactions

De Grau-Bassal,

Mallandrich,

Sosa

et al. 2024

Pharmaceutics

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Recently, the number of people acquiring tattoos has increased, with tattoos gaining significant popularity in people between 20 and 40 years old. Inflammation is a common reaction associated with tattooing. The purpose of this study was to evaluate a nanostructured lipid carrier loading pranoprofen (PRA-NLC) as a tattoo aftercare formulation to reduce the inflammation associated with tattooing. In this context, the in vitro drug release and the ex vivo permeation-through-human-skin tests using Franz cells were appraised. The tolerance of our formulation on the skin was evaluated by studying the skin’s biomechanical properties. In addition, an in vivo anti-inflammatory study was conducted on mice skin to evaluate the efficacy of the formulation applied topically after tattooing the animals. PRA-NLC showed a sustained release up to 72 h, and the amount of pranoprofen retained in the skin was found to be 33.48 µg/g/cm2. The formulation proved to be well tolerated; it increased stratum corneum hydration, and no signs of skin irritation were observed. Furthermore, it was demonstrated to be non-cytotoxic since the cell viability was greater than 80%. Based on these results, we concluded that PRA-NLC represents a suitable drug delivery carrier for the transdermal delivery of pranoprofen to alleviate the local skin inflammation associated with tattooing.

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The Influence of Fever on the Pharmacokinetics of Pranoprofen in Elderly Subjects

Fujimura

Kajiyama

Ebihara

1989

The Journal of Clinical Pharma

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Pranoprofen (75 mg) was given orally during febrile (mean body temperature 38.3 degrees C) and afebrile (mean body temperature 36.3 degrees C) periods in nine elderly subjects. Blood samples for plasma drug concentrations were taken for a 10 hour post-drug period. The mean elimination half-life (t1/2 beta) was significantly prolonged and the mean area under the time-concentration curve from 0 to 10 hrs (AUC0-10) was greater, although not significantly, during fever. No significant difference was observed in the time to maximum concentration (tmax), maximum plasma concentration (Cmax) or apparent volume of distribution (Vd/F) between the both dosages. There was a positive correlation (r = 0.448, 0.05 less than P less than 0.10) between the body temperature and t1/2 beta of pranoprofen. These data indicate that the clearance of pranoprofen is reduced during fever in elderly subjects.

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The pharmacokinetics of pranoprofen in the elderly.

Cited by 4 publications

References 3 publications

Semi-Solid Dosage Forms Containing Pranoprofen-Loaded NLC as Topical Therapy for Local Inflammation: In Vitro, Ex Vivo and In Vivo Evaluation

Semi-Solid Dosage Forms Containing Pranoprofen-Loaded NLC as Topical Therapy for Local Inflammation: In Vitro, Ex Vivo and In Vivo Evaluation

A Novel Approach for Dermal Application of Pranoprofen-Loaded Lipid Nanoparticles for the Treatment of Post-Tattoo Inflammatory Reactions

The Influence of Fever on the Pharmacokinetics of Pranoprofen in Elderly Subjects

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