Composition for pulsatile delivery of diltiazem and process of manufacture
US6635277B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Apr 12, 2001 |
| Grant date | Oct 21, 2003 |
| Priority date | — |
| Expiry date | Jun 22, 2021 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61K9/5084
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
A once-a-day controlled release drug delivery system of diltiazem hydrochloride is provided, which is bioequivalent in plasma profile of Cardizem CD. The fast, medium, and slow release fractions are prepared using various compositions and weight gains. The individual fill weights are computed and then are filled into the same capsule using specialized encapsulation equipment using a triple-filling process. A preferred membrane dispersion that is used for preparing the fast release fraction contains 0.2% of sodium lauryl sulfate along with 20% of water soluble plasticizer (triethyl citrate), and 2% silicone dioxide, based on quaternary polymethacrylate on the weight basis. This combination provides an initial pulsatile burst after a lag time of 2 hours, leading to in-vivo bioequivalence. The preferred membrane dispersion that is used for preparing the medium release and the slow release fractions contain 16% of water soluble plasticizer along with 5% silicone dioxide, based on quaternary polymethacrylate. This combination provides an optimal glass transition temperature that allows for the preparation of exceptionally increased weight gains. Additionally, it provides targeted input …
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.