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Spacer/Linker based synthesis and biological evaluation of mutual prodrugs as antiinflammatory agents.

Velingkar VS, Jain DR, Ahire DC - Indian J Pharm Sci (2010)

Bottom Line: All mutual prodrugs exhibited encouraging hydrolysis profile in 80% human plasma.Biological activity of title compounds was studied by carrageenan-induced paw edema method.From the results obtained, it was concluded that these compounds retain the antiinflammatory action.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutical Chemistry, Prin. K. M. Kundnani College of Pharmacy, Jote Joy Building, Rambhau Salgaonkar Marg, Cuffe parade, Mumbai-400 005, India.

ABSTRACT
Mutual prodrugs of some antiinflammatory agents were synthesized with the aim of improving the therapeutic index through prevention of gastrointestinal complications and to check the efficiency of release of the parent drug in presence of spacer. These mutual prodrugs were synthesized by direct condensation method using dicyclohexyl carbodiimide as a coupling agent and glycine as a spacer. The title compounds were characterized by spectral techniques and the release of the parent drug from mutual prodrug was studied in two different non-enzymatic buffer solutions at pH 1.2, pH 7.4 and in 80% human plasma. All mutual prodrugs exhibited encouraging hydrolysis profile in 80% human plasma. Biological activity of title compounds was studied by carrageenan-induced paw edema method. From the results obtained, it was concluded that these compounds retain the antiinflammatory action.

No MeSH data available.


Related in: MedlinePlus

Paw volume vs time interval plots for test and standard drugs (a) Control  Test 1, NapGlyPara  standard 1 is naproxen  and (b) Control  Test 2: IbuGlyPara  standard 2: ibuprofen
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Figure 1: Paw volume vs time interval plots for test and standard drugs (a) Control Test 1, NapGlyPara standard 1 is naproxen and (b) Control Test 2: IbuGlyPara standard 2: ibuprofen

Mentions: Wistar rats weighing between 100-150 g were divided into 5 groups of 6 rats each. The rats were injected subcutaneously 0.1 ml of 1% (w/v) of carrageenin into the planter region of each hind-paw. NapGlyPara and IbuGlyPara were evaluated at single dose level; naproxen and ibuprofen were used as standard antiinflammatory drugs for comparison. The paw edema volumes were measured using plethysmometer at various time intervals like 0, 1, 2, 3, 4, 6 h after carrageenin injection. The hind paw edema inhibition at doses of test drug and standard was calculated by comparing with vehicle treated control rats shown in fig. 1


Spacer/Linker based synthesis and biological evaluation of mutual prodrugs as antiinflammatory agents.

Velingkar VS, Jain DR, Ahire DC - Indian J Pharm Sci (2010)

Paw volume vs time interval plots for test and standard drugs (a) Control  Test 1, NapGlyPara  standard 1 is naproxen  and (b) Control  Test 2: IbuGlyPara  standard 2: ibuprofen
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC3116311&req=5

Figure 1: Paw volume vs time interval plots for test and standard drugs (a) Control Test 1, NapGlyPara standard 1 is naproxen and (b) Control Test 2: IbuGlyPara standard 2: ibuprofen
Mentions: Wistar rats weighing between 100-150 g were divided into 5 groups of 6 rats each. The rats were injected subcutaneously 0.1 ml of 1% (w/v) of carrageenin into the planter region of each hind-paw. NapGlyPara and IbuGlyPara were evaluated at single dose level; naproxen and ibuprofen were used as standard antiinflammatory drugs for comparison. The paw edema volumes were measured using plethysmometer at various time intervals like 0, 1, 2, 3, 4, 6 h after carrageenin injection. The hind paw edema inhibition at doses of test drug and standard was calculated by comparing with vehicle treated control rats shown in fig. 1

Bottom Line: All mutual prodrugs exhibited encouraging hydrolysis profile in 80% human plasma.Biological activity of title compounds was studied by carrageenan-induced paw edema method.From the results obtained, it was concluded that these compounds retain the antiinflammatory action.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutical Chemistry, Prin. K. M. Kundnani College of Pharmacy, Jote Joy Building, Rambhau Salgaonkar Marg, Cuffe parade, Mumbai-400 005, India.

ABSTRACT
Mutual prodrugs of some antiinflammatory agents were synthesized with the aim of improving the therapeutic index through prevention of gastrointestinal complications and to check the efficiency of release of the parent drug in presence of spacer. These mutual prodrugs were synthesized by direct condensation method using dicyclohexyl carbodiimide as a coupling agent and glycine as a spacer. The title compounds were characterized by spectral techniques and the release of the parent drug from mutual prodrug was studied in two different non-enzymatic buffer solutions at pH 1.2, pH 7.4 and in 80% human plasma. All mutual prodrugs exhibited encouraging hydrolysis profile in 80% human plasma. Biological activity of title compounds was studied by carrageenan-induced paw edema method. From the results obtained, it was concluded that these compounds retain the antiinflammatory action.

No MeSH data available.


Related in: MedlinePlus