Research ArticlesDesign, development, physicochemical, and in vitro and in vivo evaluation of transdermal patches containing diclofenac diethylammonium salt
Section snippets
INTRODUCTION
Diclofenac is a well‐established nonsteroidal anti‐inflammatory agent, widely used in musculoskeletal disorders, arthritis, toothache, dysmenorrhea, etc., for symptomatic relief of pain and inflammation.1 Diethylammonium salt of diclofenac (diclofenac diethylamine) is reportedly used for topical applications.2 The drug undergoes substantial hepatic first‐pass metabolism and thus only about 50% of the administered dose reaches systemic circulation.3,4 This originates the need of an alternative
Materials
EC (ethoxy content 47.5–49%, viscosity 14 cps in 5% w/w solution in 80:20 toluene/ethanol at 25°C) was purchased from BDH Chemicals Ltd., Poole, England. PVP (K value: 26–35) and Polyvinylalcohol (PVA) were purchased from HiMedia Laboratories Pvt. Ltd, Mumbai, India and S.D. Fine‐Chem. Ltd. Boisar, India, respectively. di‐n‐Butylphthalate was purchased from Central Drug House (P) Ltd., Mumbai, India.
A gift sample of diclofenac diethylamine was received from Kothari Laboratories, Saugor, India.
Solubility Study
An attempt was made at this point to learn whether the media phosphate buffer, pH 7.4, was able to maintain sink conditions in dissolution as well as in permeation studies. E was 317.512 [where mean absorbance was 0.0335 (n = 3), drug concentration was 2.637 mg/mL phosphate buffer pH 7.4, volume taken was 10 mL, dilution used was 1:2500] obtained from the solubility studies. Thus, phosphate buffer was chosen as the dissolution and permeation media because sufficient amount of drug
DISCUSSION
Diclofenac diethylamine is a well‐established nonsteroidal antiinflammatory drug, which undergoes substantial hepatic first‐pass metabolism, and thus only about 50% of the administered drug reaches the circulation.1,2 Therefore, there is a need to search for an alternative route of administration, which may bypass the hepatic first‐pass metabolism. The transdermal patch delivery system may be an attractive choice of an alternative route of administration of this drug because the drug also
Acknowledgements
We are indebted to UGC for financial support for conducting this work and to Kothari Laboratories, Sagour, India, for providing the drug as a free gift sample.
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