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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Control of drug release by incorporation of sorbitol or mannitol in microcrystalline-cellulose-based pellets prepared by extrusion-spheronization.
Use of powdered cellulose for the production of pellets by extrusion/spheronization
Such plasticizers can also include ethylene glycol, 1,2-butylene glycol, 2,3-butylene glycol, styrene glycol, diethylene glycol, triethylene glycol, tetraethylene glycol and other poly ethylene glycol compounds, monopropylene glycol monoisopropyl ether, propylene glycol monoethyl ether, ethylene glycol monoethyl ether, diethylene glycol monoethyl ether, sorbitol lactate, ethyl lactate, butyl lactate, ethyl glycolate, dibutylsebacate, acetyltributylcitrate, triethyl citrate, acetyl triethyl citrate, tributyl citrate and allyl glycolate.
This wide distribution is generally a problem for formulations wherein additional coatings will be applied to the bead. In contrast, the present inventors have discovered that the hot-melt extraded beads exhibit greater control over the release of drug. Pharmaceutical Development and Technology 15 6: The theophylline release profile from hot-melt spheronizaton spherical pellets in pH 7.
PDF of Use of powdered cellulose for the production of pellets by extrusion/spheronization
Ref legal wamr code: As used herein, a polyvinyl or polyethylene polymer is a polymer or copolymer based upon ethylene or a derivative of ethylene. The theophylline release rate increased because the wet-mass granulated spheres disintegrated quickly, presenting no barrier to drag release.
Drug Development and Industrial Pharmacy: The spherical pellets were dried for 12 hours at room temperature. Further therapeutic compounds which can be formulated into the present osmotic devices also include antibacterial substances, antiMstamines and decongestants, anti- inflammatories, antiparasitics, antivirals, local anesthetics, antifungal, amoebicidal, or trichomonocidal agents, analgesics, antiarthritics, antiasthmatics, anticoagulants, anticonvulsants, antidepressants, antidiabetics, antineoplastics, antipsychotics, neuroleptics, antihypertensives, muscle relaxants, depressants, hypnotics, sedatives, psychic energizers, tranquilizers, anti-convulsants, antiparkinson agents, muscle contractants, anti-microbials, antimalarials, hormonal agents, contraceptives, sympathomimetics, diuretics, hypoglycemics, ophthalmics, electrolytes, diagnostics agents, cardiovascular drags, other types of therapeutic compounds sphsronization to those of ordinary skill in the pharmaceutical sciences, and combinations thereof.
The size 1. Moreover, such compounds may include, by way of example and without spheronizaiton, acacia, alginic acid, carboxymethylcellulose sodium, poly vinylpyrrolidonecompressible sugar e. Specific embodiments of the invention include those wherein: Water was removed from powders and pellets by lyophilization for 72 hours prior to density determinations Freeze Dryer 5; Kansas City, MO.
Examples of pharmaceutically acceptable salts include, but are not limited to, mineral or organic acid salts of the drug. Sphernization also generally reduce the viscosity of a polymer. Therefore, these conventional beads provided very little controlled release of theophylline. Distinct drag and excipient particle are visible in the wet-mass granulated bead. A multi- zone extruder was used and the temperature of the respective zones were set as indicated below. The release profiles are virtually identical meaning that the process of the invention, and the beads prepared thereby, can provide a stable release profile that does not change substantially over an extended period of storage.
The dissolution tests conducted for FIGS. 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. Soaps and synthetic detergents may be employed as surfactants and spheronizatioon vehicles for detergent compositions.
After exiting the die, the warm polymer strand with a diameter of 1. As used herein, the term “direct compression excipient” is intended to mean a compound used in direct compression formulations.
One aspect of the invention provides a spheronized particle made according to a process comprising the steps of: After exiting the die, the polymer strand, having a diameter of 1. All dissolution tests, USP apparatus 2 and 3, were performed in triplicate.
Although the composition and average particle dkrect of the beads of FIGS. In each spheronuzation, the active agent theophylline was completely released from the wet-mass granulated sphere after approximately 4 hours. When the wet-mass granulated spheres were tested in a dissolution medium of pH 7.
European Journal of Pharmaceutical Sciences 24 1: As used herein, the term “colorant” is intended to mean a compound used to impart color to solid e. The following figures form part of the present description and describe exemplary embodiments of the claimed invention. All of the above suitable materials can be used alone or in various independent combinations. Although the drug was released quickly from these beads, the beads remained intact even after completion of the hour dissolution test because the polymer is not significantly soluble in aqueous media having a pH less than 7.
Increasing spheronization time, and optionally temperature, minimizes or eliminates the dimple. The following ingredients in the amounts indicated were used.