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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As used herein, a “thermoformable” material or composition refers to one that will soften or melt during the hot-melt extrusion step. A therapeutically effective amount is the amount or quantity of drag that is sufficient to elicit the required or desired therapeutic response, or in other words, the amount that is sufficient to elicit an appreciable biological response when administered to a patient. The bead samples were exposed serially to the media as follows: The thermoformable material or composition may require a plasticizer to render it thermoformable.
Whole beads were viewed under 50X magnification whereas bead cross-sections were viewed under 10,X magnification. The pellets were dusted during spheronization. As used herein, a polyvinyl or polyethylene polymer is a polymer or copolymer based upon ethylene or a derivative of ethylene. The present invention provides a process for producing spheronized pellets by hot-melt extrusion and spheronization. Other suitable materials include, for example, cellulose acylate, cellulose diacylate, cellulose triacylate, cellulose acetate, cellulose diacetate, cellulose triacetate; mono, di and tricellulose alkanylates; mono, di and tricellulose aroylates; cellulose acetate having a D.
It spheronozation be understood, that compounds used in the art of pharmaceutical formulation generally serve a variety of functions or purposes. Hot-melt extrusion is rapidly gaining popularity in the pharmaceutical industry because it provides several advantages over traditional production techniques.
As used herein, a plasticizer sphreonization a first material that reduces the melting point, softening temperature or Tg of a second material. As used herein, the term “binder” is intended spheronizaiton mean substances generally used to cause adhesion of powder particles in solid granulations. In contrast, the present inventors have discovered that the hot-melt extraded beads exhibit greater control over the release of drug.
PDF of Use of powdered cellulose for the production of pellets by extrusion/spheronization
A sweetening agent may be included in the time-release coating or other exterior coating of the tablet. By unstable release profiles is meant that the release profile of a given formulation changes as storage time increases so that the release profile after an extended period of storage is significantly different than ddirect initial release profile of the formulation.
Moreover, such compounds may include, by way of example and without limitation, acacia, alginic acid, carboxymethylcellulose sodium, poly vinylpyrrolidonecompressible sugar e. Examples of pharmaceutically acceptable salts include, but are not limited to, mineral or organic acid salts of the drug. The selection of the equipment may depend upon the extrasion die used and therefore the cross-sectional shape of the extradate.
Use of powdered cellulose for the production of pellets by extrusion/spheronization
Such compounds include, by way of example and without limitation, potassium metaphosphate, potassium phosphate, monobasic sodium acetate and sodium citrate anhydrous and dihydrate, salts of inorganic or organic acids, salts of inorganic or organic bases, and others known to apheronization of ordinary skill in the art. It will be appreciated that, although specific embodiments of the invention have been described herein for purposes of illustration, various modifications may be made without departing from spheronizatlon spirit and scope of the invention.
The pellets were spheronized for approximately 0. The theophylline release rate increased because the wet-mass spheronuzation spheres disintegrated quickly, presenting no barrier to drag release. The pellets were cooled to room temperature, and a 75 g sample was transferred into a Cleva Spheronizer.
Specific embodiments of the invention include those wherein: The formulation of Spheronlzation 7 is related to the formulation of Example 2, except that the formulation of Example 7 includes different amounts of the components that are in common, and the formulation of Example 7 includes magnesium stearate rather than microcrystalline cellulose. The above is a detailed description of particular embodiments of the invention.
To date, however, no process combining the steps of hot-melt extrusion and spheronization has been developed. Control of drug release by incorporation of sorbitol or mannitol in microcrystalline-cellulose-based pellets prepared by extrusion-spheronization. The elevated temperatures and high pressures utilized in hot-melt extrusion reduced the free volume of the resulting exudates.
Some factors that may affect the temperature at which the composition being extraded is extraded: The amount of coloring agent used will vary as desired. Once the extradate has been converted into plural smaller sized particles, it is processed in a spheronizer to render the particles spherical.
Dies of different shapes and sizes can be used to form the extradate; however, cylindrical ditect may provide more uniform particle size distribution and smoother surface of the resulting particles. The pellets were then spheronized in a traditional spheronizer at elevated temperatures, i. A cylindrical die 1. Development and evaluation of omeprazole pellets fabricated by sieving-spheronization and extrusion – spheronization process. The beads of the invention will together comprise an effective amount of an active agent when included in a dosage form.
It is generally used for formulations that provide a targeted drag delivery in the colon. A blended mass was prepared according to Example 1.
The thermoformable composition used to prepare a spheronized pellet according wzrm the invention generally comprises a mixture comprising an active agent, a pharmaceutical excipient, such as a thermopolymer, and one or more other pharmaceutical excipients.
Under these conditions, theophylline was completely released from the wet-mass granulated beads after 4 hours, which behavior is similar to that observed in the USP apparatus 2 at a pH of less than 7.
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. Consequently, the spherical particle produced by spheronization has a more homogeneous composition, smoother surface and more controlled release of active agent.