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indometacin (IndaFlex)

✓ Approved

AlphaRx · PTGS1 · 小分子

什么是 indometacin？

indometacin 是一种小分子，由AlphaRx研发。该药已获批，用于治疗相关适应症，给药途径：Topical、Transdermal。

药物档案

商品名IndaFlex
公司AlphaRx
药物类别小分子
分子靶点PTGS1, PTGS2
给药途径Topical, Transdermal
状态Approved
来源： ClinicalTrials.gov, AlphaRx

作用机制

分子靶点

indometacin 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

indometacin 针对 5 个适应症，涉及 2 个治疗领域。

治疗领域疾病/病症分期
Musculoskeletal and connective tissue disordersRheumatoid arthritis✓ Approved
Musculoskeletal and connective tissue disordersOsteoarthritis✓ Approved
Gastrointestinal disordersAbdominal pain✓ Approved
Musculoskeletal and connective tissue disordersGouty arthritis✓ Approved
Musculoskeletal and connective tissue disordersMusculoskeletal pain✓ Approved

相关研究文献

PubMedEuropean journal of hospital pharmacy : science and practice2026-06-26

Chemical and visual compatibility of dexmedetomidine injection with parenteral medications used in neonatal intensive care settings.

De Silva D Thisuri N DTN, Hamilton Alexander J AJ, Strunk Tobias T, Mukadam Nabeelah N et al.

To investigate the chemical and visual compatibility of dexmedetomidine injection with 44 secondary intravenous (IV) drugs and six 2-in-1 parenteral nutrition (PN) solutions used in neonatal intensive care unit settings. Dexmedetomidine (1 or 4 µg/mL) was mixed 1:1 with each secondary IV drug or PN solution to simulate Y-site co-administration. Visual compatibility was evaluated for 4 hours and chemical compatibility was determined from dexmedetomidine concentrations using a validated high performance liquid chromatography (HPLC) assay. Absorption/adsorption loss of dexmedetomidine was evaluated in three syringe filters and one in-line filter. Dexmedetomidine injection was visually compatible with all 44 secondary IV drugs and six PN solutions tested, and chemically compatible with 42 drugs. Due to interference by nine secondary drugs in the HPLC analyses of dexmedetomidine at 1 µg/mL, compatibility tests were conducted at a higher concentration of 4 µg/mL against ampicillin, benzylpenicillin, flucloxacillin, hydrocortisone, ibuprofen, indometacin and rifampicin, and the combinations were found to be chemically compatible. However, dexmedetomidine 4 µg/mL was chemically incompatible with ibuprofen lysine injection. Results for cloxacillin were inconclusive due to unresolved interference in the HPLC assay. Modest absorption/adsorption loss of dexmedetomidine (<20%) occurred in the first millilitre of filtrate with clinically relevant filters. Dexmedetomidine injection was chemically and visually compatible with 42 secondary IV drugs and six PN solutions for up to 4 hours. Dexmedetomidine injection should not be combined via Y-site administration with ibuprofen lysine injection. Due to inconclusive results, combining dexmedetomidine and cloxacillin injections via Y-site administration is not recommended.

PMID 42350148
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PubMedInternational journal of pharmaceutical compounding2025-10-20

SyrSpend® SF PH 4 as a Safe Vehicle for Extemporaneous Oral Suspensions: Microbiological Stability of Seven APIs.

Kegele Carolina Schettino CS, Dijkers Eli E, Polonini Hudson H

SyrSpend® SF PH4 is a preservative-free oral suspending vehicle widely used in extemporaneous compounding. While its chemical stability has been previously demonstrated for various active pharmaceutical ingredients (APIs), microbiological stability data remain limited. This study aimed to evaluate the microbiological stability of oral suspensions containing dapsone, griseofulvin, levofloxacin, terbinafine, indometacin, naproxen, and paracetamol in SyrSpend® SF PH4, under both room temperature and refrigerated conditions. Formulations were assessed over 90 days for physical appearance and pH. Antimicrobial effectiveness testing (AET) was conducted according to USP <51> against Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Candida albicans, and Aspergillus brasiliensis. All formulations maintained stable pH and appearance throughout the study. AET results showed a reduction of microbial counts to below detectable levels (log 1.0) by day 14, sustained through day 28, meeting USP <51> acceptance criteria. SyrSpend® SF PH4 effectively preserved the microbiological integrity of all tested formulations without added preservatives. These findings complement existing chemical stability data and support the use of SyrSpend® SF PH4 as a safe and effective vehicle for extemporaneous oral suspensions, particularly in populations requiring preservative-free formulations.

PMID 41115036
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PubMedChemistry & biodiversity2025-05-30

Three Novel Flavonoid Derivatives From the Roots of Dalbergia odorifera.

Wu Wen-Yi WY, Chen Hong-Jie HJ, Cheng Hong-Ling HL, Zhu Zheng-Tian ZT et al.

Three novel flavonoid derivatives, named dalberavonoids A-C (1-3), were isolated from the roots of Dalbergia odorifera T. C. Chen. The structures of these flavonoid derivatives were determined by comprehensive spectroscopic analyses. Compounds 1 and 2 represent rare examples of isopentenyl-substituted flavanes from the genus Dalbergia. Compound 3 is a rare flavonoid containing 16 carbon atoms on the carbon skeleton. The inhibitory activities of dalberavonoids A-C against the nitric oxide (NO) production induced by lipopolysaccharide in mouse macrophage RAW 264.7 cells in vitro were evaluated. Compounds 1 and 2 exhibited significant inhibitory activities, possessing the minimum inhibitory concentration (IC50) values of 9.13 ± 0.11 and 12.58 ± 0.14 µM. The positive control, indometacin, displayed an inhibitory activity against NO production with an IC50 value of 23.86 ± 0.08 µM.

PMID 40446119
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PubMedBioorganic chemistry2025-05-24

Asymmetric total synthesis of amovillosumins A and B and their hypoglycemic and anti-inflammatory activities.

Liao Xiang-Ming XM, Gongpan Pianchou P, Wu Sheng-Li SL, Li Tian-Ze TZ et al.

Motivated by the significant bioactivities and therapeutic potential of 1,4-benzodioxan derivatives, we reported the asymmetric total synthesis of amovillosumins A (1) and B (2), two architecturally unique norlignans isolated from Amomum villosum. The target compounds were achieved in nine and seven steps, respectively, from commercially available materials, delivering exceptional overall yields (45-47 %) with excellent enantiopurity (91-95 % ee). The key synthesis strategies encompassed Williamson ether formation, stereocontrolled ketone reduction, and Ullmann coupling to establish the pivotal 1,4-dioxan scaffold. This synthetic approach unambiguously confirmed the absolute configurations of amovillosumins A and B while providing sufficient quantities for comprehensive biological evaluation. Biological studies demonstrated that (+)-7S,8S-1 significantly stimulated GLP-1 secretion by 344.4 % at 25 μM, obviously stronger than its enantiomer (-)-7R,8R-1 (149.5 %). All isomers displayed significant anti-inflammatory activity in LPS-stimulated Raw264.7 cells, and especially, (+)-R-2 and (-)-S-2 (IC50 = 20.2 and 17.8 μΜ) showed six-fold greater NO inhibition than indometacin (IC50 = 113.2 μM). Mechanistic study demonstrated that (-)-S-2 significantly suppressed the mRNA expression of both Inos and Ptgs2. Network pharmacological analysis further confirmed PTGS2 as the primary target mediating the anti-inflammatory effects of (-)-S-2. This study integrates synthetic chemistry with pharmacological evaluation, offering structural confirmation and therapeutic insights into amovillosumins A and B.

PMID 40408981
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PubMedPharmaceutics2025-01-08

Exploring 3D Printing in Drug Development: Assessing the Potential of Advanced Melt Drop Deposition Technology for Solubility Enhancement by Creation of Amorphous Solid Dispersions.

Lamrabet Nabil N, Hess Florian F, Leidig Philip P, Marx Andreas A et al.

Background: Melt-based 3D printing technologies are currently extensively evaluated for research purposes as well as for industrial applications. Classical approaches often require intermediates, which can pose a risk to stability and add additional complexity to the process. The Advanced Melt Drop Deposition (AMDD) technology, is a 3D printing process that combines the principles of melt extrusion with pressure-driven ejection, similar to injection molding. This method offers several advantages over traditional melt-based 3D printing techniques, making it particularly suitable for pharmaceutical applications. Objectives: This study evaluates the AMDD printing system for producing solid oral dosage forms, with a primary focus on the thermo-stable polymer polyvinyl alcohol (PVA). The suitability of AMDD technology for creating amorphous solid dispersions (ASDs) is also examined. Finally, the study aims to define the material requirements and limitations of the raw materials used in the process. Methods: The active pharmaceutical ingredients (APIs) indometacin and ketoconazole were used, with PVA 4-88 serving as the carrier polymer. Powders, wet granulates, and pellets were investigated as raw materials and characterized. Dissolution testing and content analyses were performed on the printed dosage forms. Solid-state characterization was conducted using differential scanning calorimetry (DSC) and X-ray diffraction (XRD). Degradation due to thermal and mechanical stress was analyzed using nuclear magnetic resonance spectroscopy (NMR). Results/Conclusions: The results demonstrate that the AMDD 3D printing process is well-suited for producing solid dosage forms. Tablets were successfully printed, meeting mass uniformity standards. Adjusting the infill volume from 30% to 100% effectively controlled the drug release rate of the tablets. Solid-state analysis revealed that the AMDD process can produce amorphous solid dispersions with enhanced solubility compared to their crystalline form. The experiments also demonstrated that powders with a particle size of approximately 200 µm can be directly processed using AMDD technology.

PMID 39771481
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PubMedDrug and chemical toxicology2024-10-16

In vivo and in silico anti-inflammatory activity of Artemisia vulgaris and β-caryophyllene oxide in carrageenan-induced paw edema in Wistar rats.

Kumar Gandham Sandeep GS, Sholapuri Payani P, K Divyateja D, Shaily Enugonda Monika M et al.

This study is aimed to evaluate the impact of methanolic extract of Artemisia vulgaris and isolated plant compound, β-Caryophyllene oxide against carrageenan-induced paw edema in rat model and its therapeutic potential compared with reference drug, Indometacin. Methanolic extract of A. vulgaris was characterized using FTIR, LC-MS, NMR spectral studies. Paw edema was induced by sub-plantar injection of 100 µl of 1% carrageenan. Oxidative enzymes, such as super oxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPx), and glutathione reductase (GR), lipid peroxidation and C-reactive protein levels were measured in paw tissue. In silico evaluation of anti-inflammatory activity of plant compounds was evaluated against the molecular targets of inflammation. C-reactive protein and lipid-peroxidation levels were significantly increased whereas the activity levels of oxidative enzymes were significantly decreased in inflammation-induced rats. The recovery of oxidative enzyme levels was seen in treated groups in a dose dependent manner. C-reactive protein and lipid-peroxidation levels were significantly decreased in treated groups, indicating the anti-inflammatory activity of the plant extract and the plant compound. Computational analysis rationalizes the inhibitory ability of plant derived compound possibly by altering the inflammatory signaling pathway.

PMID 39411871
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