The new technique of hot-melt extrusion/spheronization can produce spherical As used herein, the term “direct compression excipient” is intended to mean a. A continuous-type spheronizer for use in a continuous melt-spheronization . at a predetermined rate directly into an extruder 30, having one or more heating. Direct. Compression. Formulation/Processing Considerations . Extrusion spheronization using water is possible and recommended versus a solution of electrolytes. Carbopol®. P NF. Noveon® AA Polycarbophil. Hot Melt. Extrusion.
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The extradate is optionally cooled prior to being fed into a sizing apparatus, such as a pelletizer, where the extradate is then converted into cylindrical pellets or mini-tablets that are then spheronized while being heated in a spheronizer to form spherical particles.
Both the surface and wafm interior dircet the particle are generally very smooth with very few isolated particles, except for an occasional dimple that might occur on the surface of the particle due to incomplete spheronization.
Use of powdered cellulose for the production of pellets by extrusion/spheronization
The spheronizer generally deforms the particles by a combination of mechanical forces and optional heat. The foregoing will war better understood with reference to the following examples that detail certain procedures for the preparation of formulations according to the present invention. Additionally, the beads processed by this sphefonization technique have a narrower particle size distribution.
The selection of the equipment may depend upon the extrasion die used and therefore the cross-sectional shape of the extradate. Whole beads were viewed under 50X magnification whereas bead cross-sections were viewed under 10,X magnification. Other exemplary binders include dorect, tragacanth, gelatin, starch, cellulose materials such as methyl cellulose and sodium carboxy methyl cellulose.
Particularly preferred flavors are the grape and cherry flavors and citrus flavors such as orange. Formulation of ranitidine pellets by extrusion-spheronization with little or no microcrystalline cellulose. European Journal of Pharmaceutics and Biopharmaceutics 57 1: While a pelletizer is depicted in FIG.
PDF of Use of powdered cellulose for the production of pellets by extrusion/spheronization
The pH of the gastrointestinal tract of a human, however, changes from very acidic stomach to neutral or slightly basic small intestines and colon. For example, an extrusion die with a round cross- section will form a cylindrical extradate, whereas, an extrusion die with a flat-lip will form a ribbon or sheet-shaped extradate. The beads of the invention will together comprise an effective amount of an active agent when included in a dosage form.
The mesh size number indicates the screen pore size; pore size decreases with increasing mesh size number. The copolymer comprises the monomers methacrylic acid, methyl methacrylate and methyl acrylate in a ratio of about Such compounds include, by way of example and without limitation, ascorbic acid, ascorbyl palmitate, butylated hydroxyanisole, butylated hydroxytoluene, hypophophorous acid, monothiogfycerol, sodium ascorbate, sodium formaldehyde sulfoxylate and sodium metabisulfite and others known to those of ordinary skill in the art.
All such plasticizers are commercially available from sources such as Aldrich or Sigma Chemical Co. Chitosan-kaolin coprecipitate as disintegrant in microcrystalline cellulose-based pellets elaborated by extrusion-spheronization.
It is also contemplated and within the scope of the invention, that a combination of plasticizers may be used in the present formulation. As used herein, a plasticizer is a first material that reduces the melting point, softening temperature or Tg of a second material.
Materials used herein are available as follows. The wet-mass extruded pellets were dusted with microcrystalline cellulose during the spheronization process to prevent agglomeration. Generally the ratio of the length to diameter of the sized particle ranges from about 0. In addition, content uniformity of the layered spheronizwtion is often a problem. The wet mass is then extruded without melting of the mass to form a granule that is then spheronized.
As used herein, the glass transition temperature is taken to mean the temperature at which a solid material softens or melts and passes from a glassy to a more aarm state. The formulation of Example 11 is related to the formulation of Example 2, except that the formulation of Example 11 includes diltiazem rather than theophylline as the active agent.
Plasticizers, such as low molecular weight PEG, generally broaden the average molecular weight of a polymer in which they are included thereby lowering its glass transition temperature or softening point. Depending upon the die employed for extrasion, an extradate with a predetermined shape will be formed.
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International Journal of Pharmaceutics 1: The theophylline release profile from hot-melt extruded spherical pellets in pH 7. Therefore, there would be less of a barrier to drug release, since the polymer is slightly soluble at pH 6.
Pharmaceutical Development and Technology 15 6: Accordingly, the extradate may be shaped as a rod, ribbon spheornization other extradate conventionally formed in the plastics industry. European Journal of Pharmaceutical Sciences 24 1: Flavors will be present in any amount as desired by those of ordinary skill in the art.
The bead samples were spheronizatjon serially to the media as follows: Furthermore, the process can be run continually or semi- continually thereby reducing down time in the manufacture of the spheronized pellets.
The pharmaceutically acceptable salts include the conventional non-toxic salts, for example, from non-toxic inorganic or organic acids. Such compounds include, by way of example and without limitation, powdered and direcf charcoal and other materials known to one of ordinary skill in the art.
Depending upon the die used, the extradate will have a corresponding cross-sectional shape. May be used alone or in combination with a colorant. The glass transition temperature is further reduced upon the addition of a plasticizer.