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FACTORS INFLUENCING THE RELEASE OF A DRUG

IP.com Disclosure Number: IPCOM000011025D
Publication Date: 2003-Feb-10
Document File: 1 page(s) / 57K

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The IP.com Prior Art Database

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FACTORS INFLUENCING THE RELEASE PROFILE OF

PIPERIDINE, 3-[(1,3-BENZODIOXOL-5-YLOXY)METHYL]-4-(4-FLUOROPHENYL)-, (3S-TRANS)-, HYDROCHLORIDE, HEMIHYDRATE

An enteric-coated, sustained release composition of piperidine, 3-[(1,3-benzodioxol- 5-yloxy)methyl]-4-(4-fluorophenyl)-, (3s-trans)-, hydrochloride, hemihydrate was produced. Upon exposure to a non-acidic environment, the coated tablet releases the active ingredient by the primary mechanism of erosion. The active material is not fully released until the tablet has completely disintegrated. Other mechanisms such as swelling or diffusion play only minor function in the release behavior of the tablet.

The use of polymers to achieve a sustained-release effect in pharmaceutical products is a common practice. Indeed, the use of such common polymers such as polyethylene oxide and ethylcellulose at ranges of 20-40% and 10-20%, respectively, could readily provide the required sustained release effect as seen by in-vitro dissolution. The use of such an ordinary polymer matrix alone, however, was found to be insufficient to match the in-vivo properties of the commercial product.

Achievement of the desired in-vivo results was only enabled by the use of a water- insoluble polymer such as a methacrylic acid types RL, RS and NE3OD which have the required sustained-release properties but can be used in lower quantities (2- 15%). While this polymer acts as the main effector of the sustained release, it can be used in synergy with...