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. CarbopolĀ®. P NF. NoveonĀ® AA Polycarbophil. Hot Melt. Extrusion.

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It is generally used for formulations that provide a targeted drag delivery in the colon. A pelletizer equipped with a cutting wheel or rolling knife will be useful for wamr the cylindrical extradate, whereas a sieve can be used for sizing the ribbon-shaped extradate by forcing the extradate through the sieve.

Hot-melt extrusion, a widely applied processing technique used in the plastics industry, is becoming a viable technique for use in the pharmaceutical industry. Drug Development and Industrial Pharmacy: International Journal of Pharmaceutics Extrusion dies having geometrically-shaped or irregular cross-sections will generally be used.

Preservatives include compounds used to prevent the growth of microorganisms. Other useful flavors include vanilla, citrus oil, including lemon, orange, grape, lime and grapefruit, and fruit essences, including apple, pear, peach, strawberry, raspberry, cherry, plum, pineapple, apricot and so forth. Formulations prepared by other methods and film coated with acrylate- methacrylate copolymers or ethylcellulose as retardant materials, are known to demonstrate unstable release profiles when the products are stored over extended periods.

May be used alone or in combination with a colorant. Some solvents are also potentially dangerous for plant workers and for the environment. Some factors rirect may affect the temperature at which the composition being extraded is extraded: The difference in bead matrices is illustrated by scanning electron microscopy.

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The heat gun was used only as needed to soften the polymer pellets so that they would deform. Spheronization of hot-melt extruded pellets results in spheres with dimples on either side that was cut by the pelletizer.

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 dosage form of the invention can also include oils, for example, fixed oils, such as peanut oil, sesame oil, cottonseed oil, corn oil direcg olive oil; fatty acids, such as oleic acid, stearic acid and isotearic acid; and fatty acid esters, such as ethyl oleate, isopropyl myristate, fatty acid glycerides and acetylated fatty acid glycerides.


These solvents may degrade the active agent in a formulation, and in practice, it is difficult to remove all traces of solvent from a spheronized granule made according to the wet method.

The present invention concerns a combination process for spheronization of a formulation. When the wet-mass granulated spheres awrm tested in a dissolution medium of pH 7. Ref legal event code: The coating formulation described below further controls the release of drug from the bead.

More particularly, the invention concerns a process wherein a hot-melt extruded solid substrate, such as a pellet, is spheronized. A comparative study of the utility of two superdisintegrants in microcrystalline cellulose pellets prepared by extrusion-spheronization. DE Ref legal event code: Cooling can be done be employing a cooling apparatus between the extruder and sizing apparatus or by exposing the extradate to a cooler ambience. Active agents include physiological substances or pharmacological active substances that produce a systemic or localized effect or effects on animals and human beings.

This method can be used to prepare granules, sustained-release tablets, and transdermal drug delivery systems. Suitable soaps include fatty acid alkali metal, ammonium, and triethanolamine salts. Consequently, the spherical particle produced by spheronization has a more homogeneous composition, smoother surface and more controlled release of active agent.

As used herein, the term “antioxidant” is intended to mean an agent that inhibits oxidation and thus is used to prevent the deterioration of preparations waarm oxidation. The release profiles for the formulation of Example 13 are depicted in FIG. A sweetening agent may be included in the time-release coating or other exterior coating of the tablet. Such compounds include, by way of example and without limitation, titanium dioxide and other materials known to one of ordinary skill in the art.

The following parameters were used for the pelletizer: As used herein, the term “antiadherent” is intended to mean an agent that prevents the sticking of solid formulation ingredients to punches and dies in a machine, for example, during production. Thus, if a compound named herein is mentioned only once or is used to define more than one term herein, its purpose or function should not be construed as being limited solely to that named purpose s or function s. The coating formulation contained the spheronozation listed below in the amounts indicated.


The bead samples were exposed serially to the media as follows: All references made to these examples are for the purposes of illustration. Direcct apparatus 3 is useful for mimicking the conditions to which the dlrect will be exposed in the GI tract. Distinct drag and excipient particle are visible in the wet-mass granulated bead.

Dies of different shapes and sizes can be used to form the extradate; however, cylindrical dies may provide more uniform particle size distribution and smoother surface of the resulting particles.

The skilled artisan will, in light of these figures and the description herein, be able to practice the invention without undue experimentation.

PDF of Use of powdered cellulose for the production of pellets by extrusion/spheronization

The pellets were spheronized for approximately 0. European Spheronizatiion of Pharmaceutics and Biopharmaceutics 61 Depending upon the die employed for extrasion, an extradate with a predetermined shape will be formed. These materials may be further described as carriers, and may be used alone or in combination with other materials of the present disclosure. 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 waem sodium metabisulfite and others known spheroniztion those of ordinary skill in the art.

Both formulations exhibit a pH dependent release profile with the formulation of Example 2 exhibiting a slightly faster release rate in lower pH media as compared to the formulation of Example 7 in the same media.

In addition, content uniformity of the layered beads is often a problem. Control of drug release by incorporation of sorbitol or mannitol in microcrystalline-cellulose-based pellets prepared by extrusion-spheronization.

The glass transition temperature is further reduced upon the addition of a plasticizer.

Use of cellulose ether containing excipients with microcrystalline cellulose for the production of pellets containing metformin hydrochloride by the process of extrusion-spheronization. Tamper-resistant dosage form with immediate release and resistance virect solvent extraction.

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.