METHOD OF PRODUCING DRUG-CONTAINING WAX MATRIX PARTICLES, EXTRUDER TO BE USED IN THE METHOD AND SUSTAINED-RELEASE PREPARATION CONTAINING CILOSTAZOL
First Claim
1. A method for producing drug-containing wax matrix granules comprising at least one drug and at least one wax, the method comprising the steps of:
- (i) supplying the at least one drug and the at least one wax to an extruder in which the temperature of a barrel and the temperature of a die are adjusted to be higher than the melting point of the at least one wax; and
(ii) while melting and kneading the at least one drug and the at least one wax in the extruder to give a molten kneaded mixture of the drug and wax, spraying the molten kneaded mixture of the drug and wax into an atmosphere having a temperature lower than the melting point of the wax from a spray nozzle directly mounted onto a die provided at a top end of the barrel of the extruder, thereby forming the mixture into granules.
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Abstract
The present invention aims to provide a method for producing, by a simple method, drug-containing wax matrix granules, particularly drug-containing wax matrix granules having an average particle diameter of 1 mm or lower, while avoiding liquid blockage due to the recrystallization of a molten drug during the period from a melting step to a spray step.
Drug-containing wax matrix granules having at least one wax and at least one drug are produced by the following steps (i) and (ii): (i) supplying the at least one drug and the at least one wax to an extruder in which the temperature of a barrel and the temperature of a die are adjusted to be higher than the melting point of the at least one wax; and (ii) while melting and kneading the at least one drug and the at least one wax in the extruder to give a molten kneaded drug and wax, spraying the molten kneaded drug and wax into an atmosphere having a temperature lower than the melting point of the wax from a spray nozzle directly mounted onto a die provided at a top end of the barrel of the extruder, thereby forming the mixture into granules.
76 Citations
29 Claims
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1. A method for producing drug-containing wax matrix granules comprising at least one drug and at least one wax, the method comprising the steps of:
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(i) supplying the at least one drug and the at least one wax to an extruder in which the temperature of a barrel and the temperature of a die are adjusted to be higher than the melting point of the at least one wax; and (ii) while melting and kneading the at least one drug and the at least one wax in the extruder to give a molten kneaded mixture of the drug and wax, spraying the molten kneaded mixture of the drug and wax into an atmosphere having a temperature lower than the melting point of the wax from a spray nozzle directly mounted onto a die provided at a top end of the barrel of the extruder, thereby forming the mixture into granules. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11)
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12. An extruder for producing drug-containing wax matrix granules, the extruder comprising:
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a barrel having a temperature controller; a supply port for supplying at least one drug and at least one wax to the barrel; an outlet die provided in the barrel; an extrusion screw for preparing a molten kneaded mixture of the at least one drug and the at least one wax and conveying the mixture to the outlet die, the extrusion screw being disposed within the barrel; and a spray nozzle capable of spraying the molten kneaded mixture of the drug and wax, the spray nozzle being directly mounted on the outlet die. - View Dependent Claims (13)
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14. A sustained-release preparation containing granules comprising:
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(A) cilostazol crystals; and (B) glycerol fatty acid ester and/or polyglycerol fatty acid ester; and an average particle diameter of the granules ranges from 40 to 200 μ
m. - View Dependent Claims (15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29)
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Specification