Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Reexamination Certificate
2001-10-25
2003-05-13
Shah, Mukund J. (Department: 1624)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
C564S443000
Reexamination Certificate
active
06562871
ABSTRACT:
BACKGROUND OF THE INVENTION
Mexiletine, 1-(2,6- dimethyl-phenoxy)-2-propanamine, is an approved and well-known pharmaceutical useful as an anti-arrhythmic. Its structure and use are described in U.S. Pat. Nos. 3,659,019 and 3,954,872. Pharmaceutical formulations comprising mexiletine are described in U.S. Pat. No. 4,031,244.
Mexiletine hydrochloride is a finely divided, crystalline substance and is used in commercial pharmaceutical formulations for mexiletine. However, the hydrochloride has a low bulk density, and so consequently also provides a large bulk volume. One commercial mexiletine product, sold under the trademark MEXITIL by Boehringer Ingelheim Pharmaceuticals, Inc., is a capsule where the hydrochloride represents approximately 62% (w/w) of the fill weight of the capsule. The inert excipients in the MEXITIL product include corn starch (bulking agent and granulation aid), colloidal silicon dioxide (drying agent and to prevent granulation caking), and magnesium stearate (lubricant). During processing to manufacture the MEXITIL product, a 1:1 solution of purified water and SD3A (specifically denatured ethanol for pharmaceutical use) alcohol is prepared. This solution is then used to increase the density of the above-mentioned MEXITIL ingredients (except magnesium stearate). The wetted combination is then dried (to evaporate or remove the water/denatured ethanol), sized by milling and then combined with the lubricant magnesium stearate. This final blend is then filled into capsules.
As indicated above, a solution of water and denatured ethanol is prepared in order to increase the density of the mexiletine hydrochloride blend. This is necessary in order to produce a powder that can be effectively handled and placed into capsules. Use of water alone does not achieve the necessary and required densification of the powder blend. However, current and future environmental regulations restrict the amount of organic solvent emissions into the atmosphere. Accordingly, the current manufacturing process for the MEXITIL product will become more costly and less efficient as such emissions become more restricted.
BRIEF SUMMARY OF THE INVENTION
A dry, granulation process involving roller compaction results in a powder blend of mexiletine hydrochloride suitable for use in capsules. Dry granulation and compaction does not result in emission of organic solvents into the atmosphere.
REFERENCES:
patent: 3659019 (1972-04-01), Koppe et al.
patent: 4031244 (1977-06-01), Koppe et al.
patent: 6056968 (2000-05-01), Gilbert et al.
Boehringer Ingelheim Pharmaceuticals Inc.
Devlin Mary-Ellen M.
McKenzie Thomas C
Raymond Robert P.
Shah Mukund J.
LandOfFree
Dry granulation of pharmaceutical formulation comprising... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Dry granulation of pharmaceutical formulation comprising..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Dry granulation of pharmaceutical formulation comprising... will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-3061116