Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Particulate form
Reexamination Certificate
1998-10-30
2001-08-07
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Particulate form
C424S493000, C424S464000, C424S465000, C424S498000, C424S501000, C424S494000, C424S495000, C424S461000, C424S462000, C424S400000
Reexamination Certificate
active
06270804
ABSTRACT:
FIELD OF THE INVENTION
The compositions of the invention are sachets, that is free flowing powders, containing combinations of coated bioaffecting microspheres and shearform floss particles. When ingested, the combinations become somewhat syrupy in the mouth, giving a pleasing mouthfeel and enhanced organoleptic acceptability.
RELATED APPLICATIONS
U.S. Ser. No. 08/642,027, filed Apr. 29, 1996, discloses the use of drug-containing microspheres in orally ingestible powder delivery systems. These systems do not contain the floss component described herein.
U.S. Ser. No. 08/642,026, also filed Apr. 29, 1996, discloses the preparation of compressed tablets from compositions containing the drug-containing microspheres of the above-referenced application.
In U.S. Ser. No. 08/915,068, filed Aug. 20, 1997, tablets from compositions containing liquiflash microspheres and shearform floss particles are discussed. Xylitol is a preferred floss constituent. The compressed tablets in this application do not have the organoleptic properties of the sachets described herein.
U.S. Ser. No. 08/874,215, filed Jun. 13, 1997, describes the preparation of microspheres which may contain bio-affecting agents using customized spinning devices.
U.S. Ser. No. 08/854,344, filed May 12, 1997, covers the use of certain thermoforming techniques to produce shearform flosses, also called shearform matrices.
The above applications, all of which are assigned to Applicants' assignee, Fuisz Technologies Ltd, are incorporated herein by reference.
BACKGROUND OF THE INVENTION
Microspheres and flosses have been used individually in a variety of products. They have also been used together to make compressed dosage forms, such as tablets.
Liquiflash microspheres are the subject of U.S. Pat. No. 5,683,720, incorporated herein by reference. The microspheres have enhanced flowability, making them easy to coat, process, and store.
PCT Publication WO 88/06558, published Sep. 7, 1998, deals with powder dosage forms containing coated pellets of bio-affecting agents. These powders do not contain a floss component.
Shearform flosses have been used in a variety of food and pharmaceutical applications, such as the following:
U.S. Pat. No. 5,429,836, incorporated herein by reference, describes the flash flow process and its use to make amorphous solid shearform matrices having flake-like form.
U.S. Pat. No. 5,587,172, also incorporated herein by reference, discusses the use of flash heat techniques to make sucrose-containing flosses, which are used to make tablets.
The use of shearform matrices to make compacted comestible units is described in co-assigned PCT application No. PCT/US95/07144, filed Jun. 6, 1995. The PCT case discloses: (1) providing a partially recrystallized shearform matrix; (2) combining the matrix with additives to form flowable, compactable blends; and (3) compacting the blends to form comestible units, such as tablets.
Additionally, PCT publication WO 95/34293 (published Dec. 21, 1995) from co-assigned PCT Application No. PCT/US95/07194, filed Jun. 6, 1995, discloses a process for making rapidly dissolving dosage units. In this PCT application, a shearform matrix is combined with an additive, and the combination is molded to make a unit dosage form. Tamping may be used to compact the dosage form and increase its integrity.
SUMMARY OF THE INVENTION
The invention provides bio-affecting sachet formulations containing organoleptically acceptable combinations of bio-affecting spherical microparticles and shearform flosses, as well as methods of making the formulations.
Applicants have discovered that the combinations described herein yield pleasant-tasting, organoleptically acceptable sachet, or powder, formulations suitable for use as dosage forms for delivering bio-affecting agents.
The sachets combine the desirable disintegration properties of partially crystalline flosses with the enhanced processability of microspheres. When mixed with excipients, the microsphere/floss combinations are solid, free-flowing consumer-ready products that can be packaged as is. When ingested, they become syrupy in the mouth and give a pleasant mouthfeel.
The sachets require no special shaping or molding operations. Thus, the compaction, compression or tamping steps used with other dosage forms are not needed.
DETAILED DESCRIPTION OF THE INVENTION
Unless otherwise stated, the parts and percentages used in the specification are weight percentages, based upon total composition weight. The terms “matrix” and “floss” are used interchangeably.
The sachet formulations of the invention are solid powders containing three essential components:
(A) coated spherical microparticles containing one or more bioaffecting agents;
(B) partially recrystallized shearform floss particles produced from compositions containing at least one saccharide-based carrier and one sugar alcohol; and
(C) one or more additives selected from the group consisting of: lubricants, flavors, flavor enhancers, glidants, fillers, colorants and perfumes.
Coated Microspheres
The bio-affecting agents are used in the form of coated microparticles of generally spherical shape. While they are preferably coated liquiflash microspheres, they can be spherical particles of bio-affecting agents coated or encapsulated with taste-masking or other coatings (e.g., DESCOTE particles).
Suitable liquiflash microspheres and other spheroidal particles have mean diameters of 0.1 to 600 microns, preferably 200 microns or less. The liquiflash particles can be made by “liquiflash” processes, such as those disclosed in U.S. Pat. No. 5,683,720, incorporated herein by reference.
“Liquiflash” processing involves the use of heat and pressure to reduce the feedstock to a condition in which resistance to flow, e.g., viscosity, which impedes the propensity to form liquid droplets, is eliminated. In this condition, the mass has become liquid or “liquiform”. Once all resistance to flow is gone, shear force is applied to the feedstock until discrete particles separate from the mass. The particles, called “liquiflash” particles, have a size and shape influenced only by natural mass separation of the flowing feedstock. U.S. Pat. Nos. 5,458,823 and 5,683,720, both incorporated herein by reference, show processes and devices used for such processing.
One useful process for making microspheres is exemplified by the production of ibuprofen spheres set out below. However, any other method of producing suitable spherical particles containing bio-affecting agents can be employed.
The microspheres of the invention include one or more bio-affecting agents, also called active ingredients. These are typically prescription or over the counter medications.
The bio-affecting agents used may be selected from a broad range of drug, therapeutic or prophylactic materials. Respective classes include those in the following therapeutic categories: ace-inhibitors; alkaloids; antacids; analgesics; anabolic agents; anti-anginal drugs; anti-allergy agents; anti-arrhythmia agents; antiasthmatics; antibiotics; anticholesterolemics; anticonvulsants; anticoagulants; antidepressants; antidiarrheal preparations; antiemetics; antihistamines; antihypertensives; anti-infectives; anti-inflammatories; antilipid agents; antimanics; anti-migraine agents; antinauseants; antipsychotics; antistroke agents; antithyroid preparations; anabolic drugs; antiobesity agents; antiparasitics; antipsychotics; antipyretics; antispasmodics; antithrombotics; antitumor agents; antitussives; antiulcer agents; anti-uricemic agents; anxiolytic agents; appetite stimulants; appetite suppressants; beta-blocking agents; bronchodilators; cardiovascular agents; cerebral dilators; chelating agents; cholecystekinin antagonists; chemotherapeutic agents; cognition activators; contraceptives; coronary dilators; cough suppressants; decongestants; deodorants; dermatological agents; diabetes agents; diuretics; emollients; enzymes; erythropoietic drugs; expectorants; fertility agents; fungicides; gastrointestinal agents; growth regulators; hormone replacement agents; hyperglycem
Frisbee Steven E.
Getz John J.
Misra Tushar K.
Sanghvi Pradeepkumar P.
Sisak John R.
Biovail Technologies Ltd.
Ghali Isis
Page Thurman K.
Pillsbury & Winthrop LLP
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