Super-fast-starting-sustained release tablet

• US 4,503,031 A
• Filed: 03/12/1984
• Issued: 03/05/1985
• Est. Priority Date: 12/17/1982
• Status: Expired due to Fees

• Current Assignee: Jacob A. Glassman
• Original Assignee: Jacob A. Glassman
• Inventors: Glassman, Jacob A.
• Primary Examiner(s): Rose, Shep K.
• Application Number:
  US06/588,904
• Time in Patent Office: 358 Days
• Field of Search: 424/15, 424/21, 424/44, 264/113
• US Class Current: 424/467
• CPC Class Codes: A61K 9/0007 Effervescent A61K9/0065 takes precedence
• CPC Class Codes: A61K 9/2072 characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms A61K9/0004, A61K9/0056, A61K9/0065 take precedence
• CPC Class Codes: A61K 9/209 containing drug in at least two layers or in the core and in at least one outer layer

Abstract

A super-fast-starting, slow release medicinal tablet, wherein the tablet is comprised of two layers of compressed matrix that are fused together by means of a readily dissolvable adhesive substance, and in which one of the layers is a lightly compressed top layer containing a pure unadulterated, uncoated, active drug and which has one or more radial grooves in it'"'"'s top surface to enhance rapid breakdown of the tablet; and the other layer has a strongly compressed portion comprised of a medically inert or inactive matrix having embedded throughout a multitude of pellets, each containing an active ingredient and having enteric coatings of various thicknesses so as to variably delay disintegration of the pellets.

Claims

1.

(a) A medically active tablet including top and bottom layers of compressed medically inert granular-like matrix material,

(b) a number of pure unadulterated pellets of active medicament embedded in the matrix material of the bottom layer

(c) an enteric coating on each of said pellets resistant to stomach juices,

(d) the matrix material of the said bottom layer being strongly compressed to resist rapid release of the pellets,

(e) said top layer being lightly compressed, a quantity of pure unadulterated uncoated pellets of active medicament embedded in the matrix material of the top layer,

(f) at least one groove in the said top layer dividing it into segments, and

(g) a midlayer including an effervescent mixture of a bicarbonate and an acid arranged between said two layers,

(h) said midlayer securing said two layers together and being subject to rapid dissolution by fluid and stomach juices to separate the segments from the bottom layer and obtain quick dissolution and immediate absorption of the active drug in said segments and a super-fast therapeutic start.

2. The tablet recited in claim 1, wherein release lift-off of the top layer segments enhances rapid fragmentation and dissolution of the top layer.

3. The tablet recited in claim 1, wherein there are several deep grooves in the top layer dividing it into independent segments down to the bottom layer.

4. The tablet recited in claim 1, wherein the lightly compressed top layer includes a proportioned effervescent mixture of sodium bicarbonate and an acid.

5. The tablet recited in claim 1, wherein the lightly compressed mid-layer includes a desired and proportioned mixture of sodium bicarbonate and citric acid which upon being moistened liberates carbon dioxide.

6. The tablet recited in claim 1, wherein there are a multitude of deep-cut grooves in the top layer dividing said layer into a multitude of segments to hasten their separation from the bottom layer and increase the rate of drug absorption and therapeutic action.

7. A medically active tablet consisting of an upper and a lower layer of compressed medicinally inert granular like matrix material, the lower layer having a number of enteric-coated medicinal pellets embedded therein, said lower layer being strongly compressed to resist rapid release of the medicaments therein, the upper layer including a quantity of pure unadulterated crystalline and micro-crystalline active medicaments admixed with an effervescent mixture to assist quicker dissolution of the upper layer embedded in the matrix material of said upper layer, said top layer being lightly compressed to allow for early disassociation from the bottom layer and rapid dissolution of the medicaments contained therein, a mid-layer arranged between the said two layers, said mid-layer including medicinally inert granular-like matrix material and an effervescent mixture of a bicarbonate and an acid to assist separation and disintegration of the top layer and quicker absorption of the active drug, thus resulting in a much faster therepeutic start.

8. The tablet recited in claim 7, wherein the upper surface of the top layer is grooved with at least one diametrical groove scored deep enough to penetrate the top layer to aid it'"'"'s breaking up and disassociation from the bottom layer.

9. The tablet recited in claim 7, wherein the top surface of the tablet is multiply grooved with diametrically arranged depressions scored deep enough to extend through the mid-layer and into the bottom layer.