US 11,452,689 B2Granted

Taste-masked pharmaceutical compositions

AssigneeAdare Pharmaceuticals, Inc.

InventorGopi M. Venkatesh

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Abstract

There is provided a method for preparing an orally disintegrating tablet (ODT) composition comprising microparticles of one or more taste-masked active pharmaceutical ingredient(s), rapidly-dispersing microgranules, and other optional, pharmaceutically acceptable excipients wherein the ODT disintegrates on contact with saliva in the buccal cavity in about 60 seconds forming a smooth, easy-to-swallow suspension. Furthermore, the microparticles (crystals, granules, beads or pellets containing the active) applied with a taste-masking membrane comprising a combination of water-insoluble and gastrosoluble polymers release not less than about 60% of the dose is in the stomach in about 30 minutes, thus maximizing the probability of achieving bioequivalence to the reference IR product having rapid onset of action (short Tmax). A process for preparing such compositions for oral administration using conventional fluid-bed equipment and rotary tablet press is also disclosed.

Claims31

Dependent claims

An orally dispersing tablet (ODT) comprising:

(1) a plurality of taste-masked particles, wherein each taste-masked particle comprises:
(a) a drug-containing core particle;
and
(b) a taste-masking membrane disposed on said drug-containing core particle comprising a combination of a water-insoluble polymer and a gastrosoluble polymer, wherein the ratio of the water-insoluble polymer to the gastrosoluble polymer is in the range of from about 95/5 to about 50/50, wherein the weight gain from the taste-masking membrane ranges from about 5% to about 50% by total weight of the taste-masked particle;
and
(2) a plurality of rapidly-dispersing microgranules comprising (i) a disintegrant and (ii) a sugar alcohol or a saccharide or a combination thereof, wherein the ratio of said sugar alcohol, said saccharide or combination thereof to said disintegrant in the rapidly-dispersing microgranules is from about 90/10 to about 99/1, and wherein each of said disintegrant and sugar alcohol or saccharide is present in the form of particles having an average particle diameter of not more than 30 μm,
wherein the ratio of rapidly-dispersing microgranules to taste-masked particles ranges from about 6/1 to about 2/1;
and
wherein the ODT releases greater than or equal to 60% of the total amount of drug in 30 minutes when tested for dissolution using United States Pharmacopoeia Apparatus 2 using paddles at 50 rpm in 900 mL of pH 1.2 buffer.

6 more elements

A method of manufacturing an orally dispersing tablet (ODT) comprising:

(a) preparing core particles comprising a drug;
(b) coating the core particles by applying a membrane comprising a mixture of water-insoluble polymer and a gastrosoluble polymer, wherein the ratio of the water-insoluble polymer to the gastrosoluble polymer in the taste-masking membrane ranges from about 95/5 to about 50/50, wherein the membrane is present in an amount of from about 5% to about 50% based on the total weight of the coated particles;
(c) granulating particles of a sugar alcohol and/or a saccharide, each particle of sugar alcohol and/or saccharide having an average particle diameter of not more than 30 μm, with a disintegrant having an average particle diameter of not more than 30 μm to produce rapidly-dispersing microgranules, wherein the ratio of said sugar alcohol and/or saccharide to said disintegrant in the rapidly-dispersing microgranules is from about 90/10 to about 99/1;
(d) blending the membrane coated microparticles of step (b) with the rapidly dispersing microgranules of step (c) at a ratio of about 1/6 to about 1/2;
and
(e) compressing the blend of step (d) into orally disintegrating tablets,
wherein the ODT releases greater than or equal to 60% of the total amount of drug in 30 minutes when tested for dissolution using United States Pharmacopoeia Apparatus 2 using paddles at 50 rpm in 900 mL of pH 1.2 buffer.

4 more elements

Dependencies are inferred from the claim text.

Facts

Application: 16/738,436Filed 9 Jan 2020 · continuation
Priority: 12 Oct 2004
Published: US 2020/0146978 A114 May 2020
Granted: 27 Sep 2022
Term ends: Not estimatedThe source records don’t support an estimate.

Classification3 codes

A61K 9/0056
Mouth and digestive tract, i.e. intraoral and peroral administration: mouth soluble or dispersible forms; Suckable, eatable, chewable coherent…
A61K 9/2077
Characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets;…: tablets…
A61K
Medicines and medical preparations

Family

Application60/617,737Us provisional application · filed 12 Oct 2004
Application11/248,596Parent of this continuation · filed 12 Oct 2005
Application15/852,486Parent of this continuation · filed 22 Dec 2017
US 9,884,014 B2Parent of this continuation · filed 6 Feb 2018
US 2020/0146978 A1Pre-grant publication · published 14 May 2020
US 10,568,832 B2Parent of this continuation
US 2006/0078614 A1Published application
US 2018/0228727 A1Published application
US 11,452,689 B2This patent

From the US filing history. Foreign family members aren’t listed.