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ISSN 2063-5346
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Self-Emulsifying Drug Delivery System (SEDDS) for Enhancement of Solubility and Photostability of Amlodipine Besilate

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Prashant H. Khade, Gururaj Shahabade, Sachin V.Kotwal, Priyanka D. Borude, Jyoti B.Darkunde, Harshal M.Shinde
» doi: 10.31838/ecb/2023.12.si4.168

Abstract

Amlodipine besilate (AMB) with IUPAC name of 3-ethyl-5- methyl-(4RS)-2-((2-aminoethoxy) methyl)-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate monobenzenesulfonate is the most widely used drug for the treatment of hypertension and ischemia by blocking dihydropyridine calcium-channel. Although AMB has excellent performance against the treatment of hypertension, but its low water solubility (2.93 g/L (0.0052 mol/L) in water at 32 °C) is one of the limitations of using AMB in pharmaceutical industry. AMB is in class IV of the biopharmaceutical classification system with slight solubility in water and sparingly soluble in ethanol. To increase the therapeutic efficacy of AMB, the solubility of AMB should be increased in aqueous systems because drugs with low aqueous solubility have poor absorption and low bioavailability. Amlodipine is also known as photosensitive since light catalyzes oxidation of amlodipine to pyridine derivatives that are therapeutically ineffective. To overcome the problem of solubility and photosensitivity, Amlodipine was formulated in the form of Self-Emulsifying Drug Delivery System (SEDDS). Liquid SEDDS was prepared by dissolving amlodipine in various Smix which were further evaluated and F1 and F2 were found to be optimized. F1 and F2 were solidified using spray drying method. After evaluation of Solid SEDDS F1 and F2 batch showed 91.041±2.96 % and 93.059±1.53% Drug release and increase in Photostability was observed.

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