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ketoprofen (Menamin SR / ketoprofen, Biovail / Oruvail)

✓ Approved

Roche · PTGS1 · 小分子

什么是 ketoprofen？

ketoprofen 是一种小分子，由Roche研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

商品名Menamin SR, ketoprofen, Biovail, Oruvail
公司Roche
药物类别小分子
分子靶点PTGS1, PTGS2
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Roche

作用机制

分子靶点

ketoprofen 作用于 2 个分子靶点：

PTGS1prostaglandin-endoperoxide synthase 1 (COX3, PCOX1)
PTGS2prostaglandin-endoperoxide synthase 2 (GRIPGHS, hCox-2)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

ketoprofen 针对 2 个适应症，涉及 2 个治疗领域。

治疗领域疾病/病症分期
Gastrointestinal disordersAbdominal pain✓ Approved
Hepatobiliary disordersHepatitis✓ Approved

相关研究文献

PubMedThe Science of the total environment2026-08-02

Exposure to pharmaceutical contaminants in stranded wild dolphins of the Western Mediterranean.

Navas Isabel I, Felipo-Benavent Mar M, Crespo-Picazo Jose Luis JL, García-Párraga Daniel D et al.

Pharmaceutical contamination in aquatic ecosystems is a growing concern for marine biodiversity and human health. We have detected six different non-steroideal anti-inflamatory drugs (carprofen, ibuprofen, ketoprofen, phenylbutazone, diclofenac and flunixin), five antibiotics (florfenicol, enrofloxacin, ciprofloxacin, oxytetracycline and trimethoprim), acetaminophen and caffeine in liver samples from 13 bottlenose dolphins (Tursiops truncattus) and 14 striped dolphins (Stenella coeruleoalba) inhabiting the western Mediterranean Sea and stranded in the coast of Valencian Community (Spain) between 2010 and 2024. To our knowledge, this study is the first documentation of some of these pharmaceuticals in wild marine-mammal tissues. Our results confirm the presence of these contaminants in the Mediterranean marine ecosystem and their incorporation into the top predator level, likely mainly through the food chain. These pollutants could cause physiological alterations in exposed individuals and may represent a potential risk for population health and resilience under chronic exposure scenarios. Potential sources of such contamination include domestic wastewater and discharges from large cruise ships, as well as open aquaculture plants, highlighting the need for enhanced monitoring and awareness to mitigate the impact of pharmaceutical contamination in marine mammals and advocate for effectively protecting marine biodiversity and human health.

PMID 42541946
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PubMedCPT: pharmacometrics & systems pharmacology2026-07-30

Sex-Related Differences in Physiologically-Based Biopharmaceutics Modeling.

Chavarría-Rojas Marianela M, Murshed Mubtasim M, Lorier Marianela M, Fotaki Nikoletta N et al.

Physiologically based pharmacokinetic (PBPK) and physiologically-based biopharmaceutics (PBBM) modeling are valuable tools in drug development, allowing mechanistic predictions of drug absorption and disposition. However, sex-related differences in gastrointestinal physiology are often underrepresented in virtual populations, potentially limiting prediction accuracy. This study aimed to evaluate how sex-related physiological differences are incorporated into commonly used PBPK platforms and to illustrate their impact on pharmacokinetic predictions using ketoprofen as a case study. Three PBPK platforms were systematically reviewed to assess predefined sex-specific gastrointestinal parameters. All three platforms incorporated sex-related differences in general anatomy and physiology but overlooked sex-specific variability in gastrointestinal tract parameters. In addition, three PBBM models of ketoprofen were developed and verified in males and subsequently extrapolated to females using default and refined sex-specific parameters. Under default female settings, the models overpredicted Cmax and underestimated Tmax, resulting in concentration-time profiles that were nearly indistinguishable from those of males. Refining gastrointestinal tract parameters for females population improved prediction performance and better reflected observed sex differences. These findings indicate that current PBPK platforms may require user-defined adjustments to adequately represent sex-specific gastrointestinal physiology and that incorporating such parameters could lead to more representative PBBM applications.

PMID 42528013
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PubMedEuropean journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences2026-07-29

Integrated Formulation and Thermal Modulation Strategies for Enhancing Anti-Inflammatory Transdermal Delivery of Dracorhodin and Ketoprofen.

Wang Zhixiong Z, Fang Renhua R, He Yi Y, Liao Weiwei W et al.

Transdermal patches are widely used for local anti-inflammatory therapy, but their delivery efficiency is often limited by the barrier function of the stratum corneum. This study aimed to develop an optimized dracorhodin transdermal patch and to evaluate temperature-controlled heating as a physical enhancement strategy using ketoprofen patches as a representative anti-inflammatory model. Dracorhodin ethanol extract was prepared by ethanol extraction and rotary evaporation, and a high-performance liquid chromatography method was established for quantitative analysis. Azone, isopropyl myristate, and acrylate pressure-sensitive adhesive were screened as key excipients, and dracorhodin patches were prepared using a coating method. The optimized patches were evaluated for appearance, content uniformity, adhesion, in vitro skin permeation, and anti-inflammatory activity using an egg white-induced rat paw swelling model. Meanwhile, the effects of heating temperature and heating duration on ketoprofen patch permeation were investigated using in vitro skin permeation experiments, in vivo fluorescence imaging, and pharmacokinetic analysis. The optimized dracorhodin patch formulation contained 19.6% azone, 11.5% isopropyl myristate, and 47.1% pressure-sensitive adhesive. The three batches of patches showed uniform appearance, acceptable content uniformity, stable adhesion, and a cumulative permeation amount of 13-20 μg/cm² within 28 h. In vivo pharmacodynamic evaluation showed that the dracorhodin patch produced a swelling inhibition rate of 62.18% at 4 h, approaching that of the ketoprofen positive control. For ketoprofen patches, temperature-controlled heating significantly enhanced transdermal permeation, with the permeation rate increasing from 10.11 to 20.56 μg/cm²·h as the heating temperature increased from 33°C to 45°C. Heating for 90 min at 40°C provided an effective balance between permeation enhancement and practical application. Fluorescence imaging and pharmacokinetic results further confirmed that thermal treatment improved drug diffusion and systemic exposure. These findings suggest that formulation optimization and temperature-controlled physical enhancement are complementary strategies for improving anti-inflammatory transdermal patch delivery and may provide a basis for the development of advanced patch-based drug-device combination products.

PMID 42521102
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PubMedRSC advances2026-07-29

Tuning photoactivity and photoprotection of TiO2 via TiO2/CeO2 heterostructure composite engineering.

Gackowski Michał M, Mlynarczyk Dariusz T DT, Alem Halima H, Budna-Tukan Joanna J et al.

Titanium dioxide (TiO2) is a widely used UV-shielding excipient for topical pharmaceutical and cosmetic formulations, but its ability to generate reactive oxygen species under UV irradiation limits its safety. Here, we report a MOF-derived TiO2/CeO2 heterostructure designed to suppress TiO2 photoactivity while preserving its UV-protective properties. Under UVA irradiation, CeO2 incorporation strongly inhibits superoxide radical generation and reduces hydroxyl radical formation by ca. 58% compared with rutile TiO2. Importantly, this reduced photoactivity translates into improved pharmaceutical performance: in hydrogel formulations, 0.1 wt% TiO2/CeO2 protects ketoprofen more effectively than TiO2 (77.54% vs. 52.56% remaining after irradiation), while 0.5 wt% TiO2/CeO2 provides almost complete photoprotection. The composite also has a lower impact on hydrogel matrix stability than pristine TiO2 and shows no acute toxicity in the Microtox assay. Overall, these results demonstrate that TiO2/CeO2 heterostructuring is an effective, safe-by-design strategy for developing photoprotective excipients that stabilize photosensitive drugs in topical formulations.

PMID 42524395
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PubMedInternational journal of pharmaceutics2026-07-29

Bidirectional thermo-switch hydrogels with size-selective diffusion for programmable delivery of medicines.

Kang Ji-Hye JH, Park Misun M, Lee Yu-Jin YJ, Kim Han-Sem HS et al.

The precise manipulation of molecular transport in physiological environments remains a central challenge for stimulus-responsive drug delivery. Here, Bidirectional Thermo-Switch (BiTS) hydrogels encode temperature-dependent release behavior within a single poly(N-isopropylacrylamide) (pNIPAam) network integrating imidazolium ionic domains and imidazolium-based ionic crosslink junctions. This architecture yields a mechanically robust yet thermally reconfigurable matrix with transitions tuned to near-physiological temperatures. Cooling induces hydration-driven mesh expansion, enabling enhanced release of the macromolecular immunosuppressant cyclosporine A (CsA). In contrast, mild heating relevant to inflamed or hyperthermic tissue contracts the network, suppressing CsA permeation while accelerating squeeze-driven release of the smaller anti-inflammatory drug ketoprofen (Keto). Spectroscopic and thermal characterization confirms network integration, and swelling and release studies demonstrate reversible, repeatable two-way transport under thermal cycling, including ex vivo Franz-cell permeation of co-loaded therapeutics. BiTS hydrogels maintain high cytocompatibility and sustain immunoregulatory activity, evidenced by reduced T cell proliferation and IL-2 secretion. Collectively, the BiTS platform enables temperature-dependent inversion of molecular transport within a single hydrogel matrix, establishing a thermo-responsive dual-regime drug delivery system.

PMID 42521062
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PubMedACS omega2026-07-28

Impact of Menthol Concentration on Ketoprofen Permeation and Photostability in Compounded Topical Preparations in a Pentravan Base.

Adamiak-Giera Urszula U, Gackowski Michał M, Malinowski Damian D, Osmałek Tomasz T et al.

Topical nonsteroidal anti-inflammatory drugs provide localized pain relief while reducing the risk of systemic adverse effects. Menthol is frequently used in topical formulations both as an analgesic agent and as a penetration enhancer. This study evaluated the effect of menthol concentration on ketoprofen permeation through Strat-M membranes and photostability in compounded topical formulations based on a Pentravan vehicle. Semisolid formulations containing ketoprofen, lidocaine hydrochloride, and increasing concentrations of menthol were prepared using the Pentravan base. In vitro permeation experiments were performed using Franz diffusion cells with Strat-M membranes as a screening model. Ketoprofen concentrations were determined using UHPLC analysis. Photostability under UVA exposure (0-200 Wh/m2) was also assessed. Ketoprofen permeation increased with increasing menthol concentration. After 12 h, the cumulative amount detected in the acceptor phase ranged from 194.9 μg for the menthol-free formulation to 475.9 μg for the formulation containing 10% menthol. Photostability studies showed formulation-dependent degradation profiles. The menthol-free formulation retained the highest proportion of ketoprofen during UVA exposure, whereas the menthol-containing formulation and the commercial product showed more pronounced drug degradation. Menthol enhanced ketoprofen permeation in the applied in vitro model while also influencing the drug's photodegradation behavior under UVA exposure, highlighting the importance of formulation composition in compounded topical preparations.

PMID 42518428
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