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IP.com Disclosure Number: IPCOM000009158D
Publication Date: 2002-Aug-12
Document File: 1 page(s) / 9K

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The IP.com Prior Art Database

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A coated tablet with a sustained release composition suitable for once daily administration of 6-O-methylerythromycin was produced. The coated tablet releases the active ingredient by the primary mechanism of erosion such that the active material is not fully released until the tablet has completely disintegrated. Other mechanisms such as swelling or diffusion play only minor functions in the release behavior of the tablet.

The use of poly mers to achieve a sustained-release effect in pharmaceutical products is a common practice. The sustained release characteristics of the above mentioned coated tablets were achieved using polymers of ethylene oxide, ethylcellulose and hydroxypropyl cellulo se representing about 10-35%, about 0.1-5% and about 1-5% (w/w), respectively, of the uncoated tablet core. The use of polymers alone, however, was found to be insufficient to fully regulate the in-vivo/in-vitro properties of a poorly-soluble drug.

The use of disintegrants is essential for the full release of 6-O-methylerythromycin . Commonly used tablet disintegrants are exemplified by s odium starch glycolate and pregelatinized starch. Pregelatinized starch is used at a concentration of about 1 to about 15% and sodium starch glycolate is used at a concentration of about 1 to about 8%. The sustained- release effect can best be achieved in-vivo/in-vitro with a about 0.5 to about 5.0:1 proportion of polymer : disintegrant. This use of disintegrant in proportion to the polymer is not obvious but is extremely important for control of the drug release.

Increasing the solubility of the Active Pharmaceutical Ingred...