Synthesis, In Vitro and In Vivo Evaluation of the  N-ethoxycarbonylmorpholine Ester of Diclofenac as a Prodrug

Jilani, Jamal; Idkaidek, Nasir; Alzoubi, Karem H.

doi:10.3390/ph7040453

Cited by 11 publications

(5 citation statements)

References 21 publications

(27 reference statements)

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“…The prodrug synthesized N-ethoxycarbonylmorpholine ester of diclofenac (Fig. 107 ) [ 93 ]. The stability of the prodrug was evaluated in buffer solution and in plasma.…”

Section: Resultsmentioning

confidence: 99%

Prodrugs of NSAIDs: A Review

Shah¹,

Gupta²,

Chauhan³

et al. 2017

TOMCJ

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Intoroduction:Prodrug approach deals with chemical biotransformation or enzymatic conversion or involves inactive or less active bio-reversible derivatives of active drug molecules. They have to pass through enzymatic or chemical biotransformation before eliciting their pharmacological action.Methods & Materials:The two different pharmacophores combine to give synergistic activity or may help in targeting the active drug to its target. Prodrug super seeds the problems of prodrug designing, for example solubility enhancement, bioavailability enhancement, chemical stability improvement, presystemic metabolism, site specific delivery, toxicity masking, improving patient acceptance, or eradicating undesirable adverse effects.Results:As an outcome the search for a prodrug or mutual prodrug with reduced toxicity has continued during recent years. This present review emphasizes the common help to revamp physiochemical, pharmaceutical and therapeutic effectiveness of drugs.Conclusion:This gives the researcher a common platform where they can find prodrugs of commonly used NSAIDs to overcome the gastrointestinal toxicity (irritation, ulcergenocity and bleeding).

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“…The prodrug synthesized N-ethoxycarbonylmorpholine ester of diclofenac (Fig. 107 ) [ 93 ]. The stability of the prodrug was evaluated in buffer solution and in plasma.…”

Section: Resultsmentioning

confidence: 99%

Prodrugs of NSAIDs: A Review

Shah¹,

Gupta²,

Chauhan³

et al. 2017

TOMCJ

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“…We believe that this is the first attempt that compares the antipyretic effectiveness of the rectal forms of Paracetamol and Diclofenac. Diclofenac is rapidly absorbed in those parts of the gastrointestinal tract that have pH values higher than five ( 23 ). Paracetamol is also highly absorbed under alkaline conditions; however, its absorption is less dependent on the environmental pH ( 24 , 25 ).…”

Section: Discussionmentioning

confidence: 99%

Rectal Diclofenac Versus Rectal Paracetamol: Comparison of Antipyretic Effectiveness in Children

Sharif

Rezaei

Aalinezhad

et al. 2016

Iran Red Crescent Med J

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BackgroundFever is the most common complaint in pediatric medicine and its treatment is recommended in some situations. Paracetamol is the most common antipyretic drug, which has serious side effects such as toxicity along with its positive effects. Diclofenac is one of the strongest non-steroidal anti-inflammatory (NSAID) drugs, which has received little attention as an antipyretic drug.ObjectivesThis study was designed to compare the antipyretic effectiveness of the rectal form of Paracetamol and Diclofenac.Patients and MethodsThis double-blind controlled clinical trial was conducted on 80 children aged six months to six years old. One group was treated with rectal Paracetamol suppositories at 15 mg/kg dose and the other group received Diclofenac at 1 mg/kg by rectal administration (n = 40). Rectal temperature was measured before and one hour after the intervention. Temperature changes in the two groups were compared.ResultsThe average rectal temperature in the Paracetamol group was 39.6 ± 1.13°C, and 39.82 ± 1.07°C in the Diclofenac group (P = 0.37). The average rectal temperature, one hour after the intervention, in the Paracetamol and the Diclofenac group was 38.39 ± 0.89°C and 38.95 ± 1.09°C, respectively (P = 0.02). Average temperature changes were 0.65 ± 0.17°C in the Paracetamol group and 1.73 ± 0.69°C in the Diclofenac group (P < 0.001).ConclusionsIn the first one hour, Diclofenac suppository is able to control the fever more efficient than Paracetamol suppositories.

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“…90). 304 The prodrug exhibited good intrinsic chemical stability, with t 1/2 values of 8 h and 47 h at pH 1.0 and 7.4, respectively, but degraded more readily in human plasma, with a t 1/2 of 21 min. This indicated that the prodrug would have sufficient stability in the GI tract to ensure intact absorption, while undergoing rapid activation in the plasma by esterases to release the parent.…”

Section: Design Of Prodrugs That Mitigate Toxicity For Non-oncology I...mentioning

confidence: 95%

Prodrugs as empowering tools in drug discovery and development: recent strategic applications of drug delivery solutions to mitigate challenges associated with lead compounds and drug candidates

Subbaiah,

Rautio,

Meanwell

2024

Chem. Soc. Rev.

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Synthesis, In Vitro and In Vivo Evaluation of the N-ethoxycarbonylmorpholine Ester of Diclofenac as a Prodrug

Cited by 11 publications

References 21 publications

Prodrugs of NSAIDs: A Review

Prodrugs of NSAIDs: A Review

Rectal Diclofenac Versus Rectal Paracetamol: Comparison of Antipyretic Effectiveness in Children

Prodrugs as empowering tools in drug discovery and development: recent strategic applications of drug delivery solutions to mitigate challenges associated with lead compounds and drug candidates

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