A Facile Synthesis of Mutual Prodrug of Diclofenac Sodium and Paracetamol and Its Preformulation Studies

Visagaperumal, D; Candasamy, Mayuren; Anbalagan, N.; Varma, Raghuveer P; Banala, Srinivas; Bontha, V. B. Shanker; Ravikumar, G.

doi:10.53879/id.49.10.p0025

Cited by 3 publications

(2 citation statements)

References 4 publications

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“…117 Other merged hybrids 48-52 containing two different APIs connected via a carboxylic ester function (Fig. 13) were designed and prepared [118][119][120][121][122] using the Steglich esterication reactions of APAP and the NSAIDs mentioned above 4-6, 8 (Fig. 4) and fulfenamic acid, another NSAID.…”

Section: Direct-and Spacer-linked Apap Codrugsmentioning

confidence: 99%

“…Another codrug, diclofenac–APAP hybrid 50 , was also studied by Visagaperumal et al 122 They showed that its anti-inflammatory activity (male Wistar rats) resulted in better activity than diclofenac (% inhibition of paw volume for 8 h, 84% and 76%, respectively) and the ulcerogenic activity produced by 50 is negligible compared to diclofenac (ulcer index, 1.4 and 6.3, respective).…”

Section: Apap-prodrugs and -Hybrid Moleculesmentioning

confidence: 99%

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Exploring acetaminophen prodrugs and hybrids: a review

Kouznetsov

2024

RSC Adv.

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Section: Direct-and Spacer-linked Apap Codrugsmentioning

confidence: 99%

Section: Apap-prodrugs and -Hybrid Moleculesmentioning

confidence: 99%

Exploring acetaminophen prodrugs and hybrids: a review

Kouznetsov

2024

RSC Adv.

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Mutual Prodrugs - Codrugs

Nudelman

2023

CMC

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This review encapsulates an extensive variety of substances identified as mutual prodrugs or codrugs, wherein two, or sometimes three, biologically active moieties are linked using an assortment of metabolically unstable bridging entities. Following the administration of the mutual prodrugs, these undergo a bridge cleavage releasing the active molecules, which then elicit their respective biological effects. In some cases, the released drugs act synergistically, other times the biological activity of only one of the drugs is elicited, and in such cases, the accompanying drug serves only as a carrier, which may have an affinity to the desired receptor. The most promising results are commonly observed when the two released drugs are efficacious at similar concentrations and particularly when the two drugs are effective against similar diseases. For instance, the best results are observed, when two analgesics, two anticancer agents, two drugs for the treatment of cardiac conditions, etc., are the substances comprising the codrug. Mutual prodrugs/codrugs described herein have been reported, primarily since the year 2000, as potential drugs for use against a plethora of diseases including pain, inflammation, cancer, bacterial infections, sickle cell anemia, Alzheimer’s disease, and others.

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A Short Review on Biological Activities of Paracetamol Derivatives

Begum¹,

G²,

S³

2023

PCI- Approved-IJPSN

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Paracetamol reduces body temperature with multiple mechanisms. Paracetamol is chemically 4-hydroxy acetanilide and has a good safety profile. Following its successful use as an over-the-counter antipyretic and analgesic medication, several attempts were made to increase the potency, mask the bitter taste, and decrease the toxicity of this drug by modifications at the phenyl ring, acetamido group, and hydroxyl group. The free hydroxyl group of paracetamols was masked to obtain prodrugs (carbonate prodrugs, ester prodrugs like alanine-prodrug, proline-prodrug, galactosylated prodrug, and mutual prodrugs with other drugs and NSAIDs). Propacetamol is a commercially available prodrug derived from paracetamol that is effective in parenteral form. Paracetamol ester prodrugs with sulfur-containing amino acids such as N-acetyl cysteine, cysteine, and methionine showed low hepatotoxicity compared to the parent drug. In addition, paracetamol derivatives including metal complexes, chalcones, Mannich bases, nucleoside analogs, hybrids with the aryl-imidazolidinyl ring, thymol, and triazole ring displayed diverse activities like antioxidant, anticancer, and antimicrobial activities.

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A Facile Synthesis of Mutual Prodrug of Diclofenac Sodium and Paracetamol and Its Preformulation Studies

Cited by 3 publications

References 4 publications

Exploring acetaminophen prodrugs and hybrids: a review

Exploring acetaminophen prodrugs and hybrids: a review

Mutual Prodrugs - Codrugs

A Short Review on Biological Activities of Paracetamol Derivatives

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