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.
The elevated temperatures and high pressures utilized in hot-melt extrusion reduced the free volume of the resulting exudates.
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One aspect of the invention provides a spheronized particle made according to a process comprising the steps of: Powdered cellulose as excipient for extrusion-spheronization pellets of a cohesive hydrophobic drug.
The disadvantage of this method is the difficulty of calculating the amount of drug spheronizatikn since coating solution is lost onto the coating apparatus.
As used herein, the term “sweetening agent” is intended to mean a compound used to impart sweetness to a preparation. As used herein, the term “lubricant” is intended to mean substances generally used in tablet formulations to reduce friction during tablet compression.
Essentially any known extrasion die can be used. All references made to these examples are for the purposes of illustration.
For example, an extrusion die with a round cross- section will form a cylindrical extradate, whereas, warn extrusion die with a flat-lip will form a ribbon or sheet-shaped extradate. The hot-melt extruded spheres displayed an initial burst in drag release, due to theophylline on or near to the bead surface, but drug release was zero-order after the initial burst. Water was removed from powders and pellets by lyophilization for 72 hours prior to density determinations Freeze Dryer 5; Kansas City, MO.
Other methods such as varying composition of the material to be hot-melt extruded may be used to minimize the dimple size or remove the dimple during spheronization. Dissolution media was sample periodically and the samples were diluted with additional dissolution media as needed and then assayed by spectrophotometry at a wavelength of nm.
Drag layering uses driect fluid-bed coater to apply a drug containing film onto non-pareil beads. The amount of flavoring may diredt on a number of factors, including the organoleptic effect desired. As used herein, the term “binder” is intended to mean substances generally used to cause adhesion of powder particles in solid granulations.
In each case, the active agent theophylline was completely released from the wet-mass granulated sphere after approximately 4 hours. The dissolution tests conducted for FIGS.
Use of powdered cellulose for the production of pellets by extrusion/spheronization
The particle size distribution of beads made according to Direcg 1 and 2 was determined by sieving the beads through a series of U. These materials may include the above-listed thermoformable materials. Such compounds include, by way of example and without limitation, carnauba wax, white wax and other materials known to one of ordinary skill in the art.
The PEG based plasticizers are available commercially or can be made by a variety of methods, such as disclosed in Poly ethylene glycol Chemistry: When an identical dry powder formulation was employed, the hot-melt extruded beads exhibited greater control over drug release than the wet-mass granulated beads.
International Journal of Pharmaceutics Kidlington 1: Such compounds include, by way of example and without limitation, powdered and activated charcoal and other materials known to one of ordinary skill in the art. To date, however, no process combining the steps of hot-melt extrusion and spheronization has been developed. Such compounds include, by way of example and without limitation, aspartame, dextrose, glycerin, mannitol, saccharin sodium, sorbitol and sucrose and other materials known to one of ordinary skill in the art.
Hot-melt extrusion is rapidly gaining popularity in the pharmaceutical industry because it provides several advantages over traditional production techniques.
PDF of Use of powdered cellulose for the production of pellets by extrusion/spheronization
However, unlike the wet-granulated beads that rapidly disintegrated at pH 7. As used herein, a “thermoformable” material or composition refers to one that will soften or melt during the hot-melt extrusion step.
All such plasticizers are commercially available from sources such as Aldrich or Sigma Chemical Co. A cylindrical die 1. European Journal of Pharmaceutical Sciences 24 1: The following examples should not be considered exhaustive, but merely illustrative of only a few of the many embodiments contemplated by the present invention.
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 by oxidation. Whole beads were viewed under 50X magnification whereas bead cross-sections were viewed under 10,X magnification.