[Translation] A randomized, open-label, single-dose, two-formulation, crossover controlled bioequivalence study of diflunisal tablets in healthy subjects under fasting and fed conditions

主要目的：以浙江莎普爱思药业股份有限公司的二氟尼柳片为受试制剂；并以Teva Pharmaceuticals持证的二氟尼柳片为参比制剂，进行生物等效性正式试验。

[Translation]

Main purpose: To conduct a formal bioequivalence trial using diflunisal tablets produced by Zhejiang Shapuaisi Pharmaceutical Co., Ltd. as the test preparation and diflunisal tablets certified by Teva Pharmaceuticals as the reference preparation.

Start Date10 Jul 2024

Sponsor / Collaborator

Zhejiang Shapuaisi Pharmaceutical Co. Ltd.

EUCTR2019-002873-80-ES

/ Unknown statusPhase 2/3IIT

Unicentre, open, uncontrolled clinical trial to assess the morphological, biochemical and functional effects of Diflunisal treatment in patients with transthyretin cardiac amyloidosis

Start Date14 Jan 2020

Sponsor / Collaborator-

NCT04113668

/ CompletedPhase 1

AN OPEN-LABEL, SINGLE-SEQUENCE, CROSSOVER STUDY TO INVESTIGATE THE EFFECTS OF UGT1A9 INHIBITOR DIFLUNISAL, AT STEADY-STATE, ON PHARMACOKINETICS OF A SINGLE DOSE OF BMS-986165 IN HEALTHY MALE AND FEMALE VOLUNTEERS

BMS-986165 Is broken down by the body through multiple pathways. This study Investigates the effect of blocking one pathway in the drug levels of BMS-986165 in health subjects.

Start Date01 Oct 2019

Sponsor / Collaborator

Bristol Myers Squibb Co.

100 Clinical Results associated with Diflunisal

100 Translational Medicine associated with Diflunisal

100 Patents (Medical) associated with Diflunisal

1,713

Literatures (Medical) associated with Diflunisal

01 Mar 2025·Analytical and Bioanalytical Chemistry

New robust and efficient liquid membranes for conductive vial electromembrane extraction of acids with low to moderate hydrophilicity in human plasma

Article

Author: Song, Chenchen ; Hay, Anne Oldeide ; Gaznawi, Somayeh ; Hansen, Frederik André ; Dowlatshah, Samira ; Hasvold, Grete

AbstractThe current paper reports two new, robust, and efficient conditions for electromembrane extraction of acidic substances from human plasma. Two systems were developed based on eutectic solvents: A1 (“A” for acid) comprised dodecyl methyl sulfoxide and thymol in 1:2 ratio (w/w) as liquid membrane, while A2 used [6-methylcoumarin:thymol (1:2)]:2-nitrophenyl octyl ether in 2:1 ratio (w/w). The performance of A1 and A2 was characterized by extraction of 31 acidic model analytes (pharmaceutical drugs and nutrients) spiked into 100 µL human plasma diluted 1:1 (v/v) with phosphate buffer pH 7.4. The acceptor solution was 50 mM NH4HCO3 buffer pH 10.0, and extraction was performed at an agitation rate of 750 RPM. Voltage and extraction time were 30 V for 30 min and 10 V for 20 min for A1 and A2, respectively. Under optimal conditions, A1 extracted analytes with 1.8 ≤ log P ≤ 6.0 with an average recovery (R) of 85.1%, while A2 extracted in a range of 0.5 ≤ log P ≤ 6.0 with an average recovery of 79.9%. Meanwhile, extraction current was low at 9 and 26 µA, respectively, which is indicative of good system robustness. Using UHPLC-MS/MS analysis of the acceptor solution, repeatability of the A1 and A2 methods was determined to be 2.8–7.7% and 3.3–9.4% for R > 40%, matrix effects were 82–117% and 84–112%, respectively, and linear calibration curves were obtained. The performance and compatibility with human plasma represent a major improvement over previous state-of-the-art liquid membranes for acidic analytes, namely 1-octanol.Graphical Abstract

01 Mar 2025·Journal of Pharmaceutical and Biomedical Analysis

Implementation of a novel method for the determination of plasma protein binding of highly bound compounds using the equilibrium dialysis method coupled with extraction to the organic phase and its comparison to known methods

Article

Author: Novak Ratajczak, Sanja ; Gogola, Dawid ; Kowal-Chwast, Anna ; Gabor-Worwa, Ewelina ; Kuś, Kamil ; Latacz, Gniewomir ; Gaud, Nilesh ; Brzózka, Krzysztof

Accurate determination of plasma protein binding (PPB) is crucial in understanding the pharmacokinetics and pharmacodynamics of drugs, particularly for highly bound compounds where traditional methods may fall short. In this study, we present a pioneering approach for the precise determination of PPB that takes advantage of the lipophilicity of highly bound compounds. Twenty four highly bound compounds (with a fraction unbound (f_u) from 10^-1 to 10^-6) were tested with the most commonly used method, i.e., the rapid equilibrium dialysis (RED) method, along with its modifications adapted especially for strongly bound compounds, including dilution, presaturation, competition, and flux-dialysis methods. The results of these methods were compared to data obtained with the modification of RED coupled with extraction to organic phase, and the correlations between them were presented. Comparison studies demonstrate the accuracy of our approach across a set of highly bound compounds within a twofold range. Moreover, PPB values were determined for venetoclax, amiodarone, montelukast, and fulvestrant, for which, to the best of our knowledge and after extensive review of the literature, it has not been possible with the standard RED method until now. In conclusion, our new method can be a big step forward in finding the PPB of strongly plasma protein-bound compounds. It gives us a better understanding of how drugs and proteins interact, which helps us make safer and more effective medicines.

13 Feb 2025·Journal of Medicinal Chemistry

Development of a Novel Human Serum Albumin-Based Tool for Effective Drug Discovery: The Investigation of Protein Quality and Immobilization

Article

Author: Molnár, Zsófia ; Koplányi, Gábor ; Kenéz, Balázs ; Katona, Gábor ; Balogh, György T. ; Decsi, Balázs ; Horváth, Péter ; Balogh-Weiser, Diána

The binding ability of human serum albumin (HSA) on active pharmaceutical ingredients (APIs) is one of the most important parameters in the early stages of drug discovery. In this study, an immobilized HSA-based tool was developed for the rapid and easy in vitro screening of API binding. The work explored the serious incompleteness in the identification of HSA used for in vitro screening published in the last five years. To mitigate this problem, a comprehensive analysis and immobilization studies were performed on the most used HSA types. Serious differences in the colloidal stability of HSAs and their API binding ability on a selected set of APIs were observed. HSAs were immobilized on magnetic nanoparticles with glutardialdehyde (GDA) or cyclohexyl-diglycidyl ether (CDGE) linkers, which have never been used for HSA immobilization before. The HSA-MNP-CDGE complexes achieved a higher immobilization yield and preserved API binding ability; however, the esterase-like enzymatic activity of HSA reduced significantly.

News (Medical) associated with Diflunisal

17 Apr 2023

·www.drugs.com

Get Pain Relief With the Most Common Arthritis Medications

MONDAY, April 17, 2023 -- Arthritis is a common disease that causes pain and inflammation in different body joints, making it difficult to enjoy everyday tasks and physical activity. Fortunately, there are many different medications for arthritis. Depending on what type of arthritis you have and its severity, an arthritis medication may help you manage pain and other symptoms. Here is a breakdown of the most common arthritis medications, how they work and their potential side effects. The Arthritis Foundation lists the following as the medications used to treat arthritis: Analgesics including acetaminophen (Tylenol) and opioids Nonsteroidal anti-inflammatory drugs (NSAIDs) Corticosteroids Disease-modifying antirheumatic drugs (DMARDs) including biologics and targeted DMARDs Analgesics The Arthritis Foundation reports that analgesics may help with mild to moderate pain, but they will not help with the inflammation associated with arthritis. Analgesics work in the nervous system and alter how your brain perceives pain. They can be used to treat the pain associated with any type of arthritis, although more effective options are available. Analgesics can be opioid, non-opioid or a combination. Common analgesics are: Acetaminophen (Tylenol) Codeine Oxycodone Fentanyl Hydrocodone Potential side effects: Kidney damage Liver damage Addiction Constipation Gastrointestinal bleeding Use caution when taking these medications; take only as prescribed. NSAIDs NSAIDs work by blocking prostaglandin. According to the Cleveland Clinic , one role prostaglandins play is forming clots and causing inflammation at the site of an injury. NSAIDs are used to treat the pain and inflammation associated with rheumatoid arthritis and osteoarthritis . Common over-the-counter (OTC) NSAIDs are: Aspirin (Bayer, St. Joseph, Anacin, Excedrin and more) Ibuprofen (Motrin, Advil) Naproxen sodium (Aleve) Prescription NSAIDs are: Celecoxib (Celebrex) Diclofenac (Voltaren, available by brand name in topical form) Fenoprofen (Nalfon) Indomethacin (Indocin, available by brand name in liquid form) Ketorolac tromethamine (Toradol) Meclofenamate sodium (Meclomen) Diflunisal (Dolobid) Tolmetin (Tolectin) Ketoprofen (Orudis) Flurbiprofen (Ansaid) Potential side effects of NSAIDs are: Increased risk of stomach and bowel issues like ulcers and bleeding Increased risk of stroke Heart problems Stomach pain Nausea Diarrhea/constipation Corticosteroids According to the Arthritis Foundation , corticosteroids mimic cortisol, a hormone your body produces naturally. They are used to treat inflammatory types of arthritis, including rheumatoid arthritis and psoriatic arthritis. They are great for short-term relief of inflammation but are not recommended for long-term use because of their side effects. Your doctor may prescribe a lower dose if you require them for long-term use. Common corticosteroids: Prednisone (Deltasone, Prednicot, Cotolone) Prednisolone (Orapred, Omnipred) Cortisone (Cortone) Hydrocortisone (Cortef, Hydrocort) Triamcinolone (Aristocort) Dexamethasone (Decadron) Common side effects of corticosteroids: Blood sugar spikes Weight gain Bone loss Risk of cataracts High blood pressure Infections Mood changes DMARDs The Arthritis Foundation says that DMARDs work with the body to “stop or slow the disease process in inflammatory forms of arthritis.” They work by blocking inflammation. There are many different DMARDs on the market, and they all have different ways of working in the body. Conventional DMARDs work by broadly suppressing the immune system. Often they are used in combination with other therapies. Targeted DMARDs block specific pathways inside immune cells. Biologic DMARDs are produced by live cells and work on specific immune proteins called cytokines. Common DMARDs: Apremilast (Otezla) Baricitinib (Olumiant) Cyclophosphamide (Cytoxan) Cyclosporine (Gengraf, Neoral) Hydroxychloroquine (Plaquenil) Leflunomide (Arava) Methotrexate (Otrexup, Rasuvo, RediTrex) Mycophenolate mofetil (CellCept) Sulfasalazine (Azulfidine) Tofacitinib (Xeljanz, Xeljanz XR) According to the Cleveland Clinic , common side effects of traditional DMARDs include: Loss of appetite Nausea Diarrhea Abdominal pain Rash, allergic reaction Liver problem Increased risk of infection Low blood cell counts Common side effects of biologic DMARDs include: Increased risk of common and serious infections Reactivation of tuberculosis, herpes zoster, and hepatitis B and C Increased cholesterol levels, increased liver enzymes and low blood cell counts Increased risk of clotting When prescribed DMARDs, inform your doctor of any other medications, including over-the-counter medicines, you are taking to avoid drug interactions. Some of these medications can cause teratogenicity (defects in a developing fetus.) Writing recently in the Journal of the American Academy of Physician Assistants (JAAPA ), physician assistant Michelle DiBiase and Dr. Samantha Kohn remind people that "The mainstay of pharmacologic therapy is early intervention with use of nonbiologic and biologic DMARDs together with adjunctive medications such as NSAIDs, oral and intra-articular corticosteroids, and analgesic medications, including opioids." Your primary care provider or rheumatologist will work closely with you to determine which medications are best for your treatment. It is vital to keep them apprised of any side effects and let them know if the treatment is ineffective. They can work with you to find a treatment that helps relieve the pain and inflammation caused by arthritis. Posted April 2023

Drug Approval

100 Deals associated with Diflunisal

External Link

KEGG	Wiki	ATC	Drug Bank
D00130	Diflunisal	N02BA11	DB00861

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Osteoarthritis	China	Aikang Lide Pharmaceutical (Zhejiang) Co., Ltd.	01 Jan 1997
Osteoarthritis	China	Juhua Group Corp. Pharmaceutical Factory	01 Jan 1997
Pain	China	Aikang Lide Pharmaceutical (Zhejiang) Co., Ltd.	01 Jan 1997
Pain	China	Juhua Group Corp. Pharmaceutical Factory	01 Jan 1997
Rheumatoid Arthritis	China	Aikang Lide Pharmaceutical (Zhejiang) Co., Ltd.	01 Jan 1997
Rheumatoid Arthritis	China	Juhua Group Corp. Pharmaceutical Factory	01 Jan 1997

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00294671 (CTgov)	Phase 2/3	Amyloid Neuropathies, Familial	130	diflunisal (Diflunisal)	kbrvtegvsu(qwyomruryd) = pxklnnisig cvufstwmns (ijnukipioq, ydgorzcbck - ekuwwhtpal) View more	-	17 Mar 2017
				placebo (Placebo)	kbrvtegvsu(qwyomruryd) = ihwevhuykc cvufstwmns (ijnukipioq, mqsfpsbctl - vihzakxcfe) View more
NCT00294671 (Pubmed \| JAMA)	Phase 2/3	Amyloid Neuropathies, Familial	130	Diflunisal 250 mg	dlvhzwvhjp(eymluibkgn) = xlntsugbem zwgpbkrbmy (qatpakrovq, 3.3 - 14.1) View more	Positive	25 Dec 2013
				Placebo	dlvhzwvhjp(eymluibkgn) = qqmhakyhow zwgpbkrbmy (qatpakrovq, 18.4 - 31.6) View more
AAN2013	Not Applicable	Amyloid Neuropathies, Familial ATTR Val30Met FAP	18	Diflunisal 500 mg/day	kubymmrwsk(ycfqvjnqxn) = deterioration of renal function resulted in discontinuation of the study drug in two patients ogzirhutoh (vrnrdetcax ) View more	Positive	12 Feb 2013
				Diflunisal

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