Process for the preparation of a granulate suitable to the preparation of rapidly disintegrable mouth-soluble tablets and compositions obtained thereby

• US 6,149,938 A
• Filed: 07/23/1998
• Issued: 11/21/2000
• Est. Priority Date: 07/25/1997
• Status: Expired due to Term

• Current Assignee: Alpex Pharma SA
• Original Assignee: Elan Pharma International Limited (Perrigo Company PLC)
• Inventors: Ciccarello, Franco, Pagano, Aberto, Bonadeo, Daniele
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): Berman, Alysia
• Application Number:
  US09/122,037
• Time in Patent Office: 852 Days
• Field of Search: 514/951, 424/464, 424/466, 424/497, 424/499, 427/213
• US Class Current: 424/464
• CPC Class Codes: A61K 9/0056 Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals

Abstract

A process for making a granulate composition suitable to the preparation of an oral solid form that can disintegrate rapidly inside the buccal cavity is provided as well as the granulate compositions and obtained.

Claims

1. A process for making a granulate for use in the preparation of mouth-soluble, rapidly disintegrating tablets, which process comprises:

(i) granulating in a fluidized bed

(a) a polyalcohol;

(b) an active ingredient;

(c) from 1 to 30% of an edible acid wherein the edible acid is not part of an effervescent mixture consisting of an acid and a base;

(d) optionally, other solid components selected from the group consisting of lubricants, sweetening agents, and flavors; and

(e) an aqueous solution or aqueous dispersion of a water-soluble or water-dispersible polymer that provides 1-10% of the final weight of the granulate; and

(ii) drying the granulate in the fluidized bed.

2. A process according to claim 1 in which the water-soluble or water-dispersible polymers are selected from the group consisting of polyethylene glycols, sodium carboxymethyl cellulose, hydroxypropylmethyl cellulose, xanthan gum, polyethylene oxide, polyoxyethylene, polyoxypropylene Pluronic®

, acrylic and methacrylic acid polymers Eudragit®

, carrageenin, polyvinyl alcohol.

3. A process according to claim 1 in which the polyalcohols are selected from the group consisting of mannitol, xylitol, sorbitol, erythritol, maltitol, lactitol.

4. A process according to claim 3, in which the polyalcohols are selected from the group consisting of xylitol and sorbitol.

5. A process according to claim 4 in which the active ingredients have been coated before the granulation.

6. Mouth-soluble, rapidly disintegrating tablets comprising the granulate of claim 1.

7. Tablets according to claim 6 having a disintegration time ranging from 30 seconds to 3 minutes.

8. A process of making a mouth-soluble, rapidly disintegrating tablet comprising comprising the granulate of claim 1 and optionally, other components to form a tablet.