Process for the preparation of drug pellets

Details Process for the preparation of drug pellets Process for the preparation of drug pellets

1995-07-31

1998-01-20

Page, Thurman K.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Particulate form

424470, A61K 914

Patent

active

057098859

DESCRIPTION:

BRIEF SUMMARY
This application is a 371 of PCT/FI93/00409, filed Oct. 8, 1993.
The object of this invention is a process for the preparation of drug pellets, which method comprises the stages wherein a drug containing powder is granulated in a granulator which operates by the rotor principle, i.e. in a rotor type granulator, by exerting a centrifugal force on the powder and, at the periphery of the rotor or in its vicinity, bringing the powder in contact with a separately fed granulating liquid converted to a mist to make a granulate, extruding the granulate and spheronizing the extrudate obtained into pellets, which are dried and optionally coated.
Drug containing powders to be formulated into drug forms, such as pellets or tablets, seldom exhibit optimal formulation characteristics, such as flow, binding and solubility characteristics. Thus in order to provide optimal dosage forms the drug thus usually has to be combined with various adjuvants and additives which, on the one hand, impart to the dosage form suitable and desired characteristics and, on the other hand, facilitate the preparation of the dosage form.
In order to obtain a product of even quality, a granulate is first formed from the powder mixture containing adjuvants and additives, either by wet or by dry granulation, wherefrom subsequently pellets are formed and/or tablets are compressed.
Adjuvants generally in use in drug forms, such as pellets and tablets, are i.a. lactose, mannitol, microcrystalline cellulose, starch, sucrose, etc., the main purpose of which is to function as a filler or a diluent for the drug. Their amount as calculated from the final drug form can vary within wide limits, and can constitute even 99% or more of the weight of the whole formulation.
Binders are added to bind the powders and to prepare coherent drug formulations. Generally used binders are, for example, gelatin, various cellulose derivatives, polyvinyl-pyrrolidone, but also sucrose and starch may function as a binder. The binder is added either in dry form to the powder, or as a liquid. Binders are generally used in an amount of appr. 2-10% (w/w).
Glidants are added to the dry powders primarily in order to improve the pour and flow characteristics of the powders so that they may be fed at an even rate to the apparatus, thus allowing for the preparation of a product which is as homogenous as possible. The glidants are solid; typical glidants are colloidal silicon dioxide, magnesium stearate, starch and talcum. The amount to be added is naturally dependant on the powder used and also on the glidant, for example magnesium stearate is added to the powder in an amount of appr. 0.3-1%, whereas the amount of talcum to be added can be as high as 5%.
In the formulation, besides the above mentioned substances, also other adjuvants may be used, such as disintegrating agents and pH regulating agents. Surface active agents, such as polysorbates and sodium laurylsulfate have been proposed to be used for improving the wettability of the powder and the solubility of poorly soluble and hydrophobic drugs. It has been stated, however, that the addition of surface active agents to the treatment liquid should be avoided as such an addition makes the pellets so prepared brittle (Pharmaceutical Pelletization Technology, Drugs and the Pharmaceutical Sciences, vol. 37, Ed. I. Ghebre-Sellassie (Marcel Decker, 1989).
In the granulation, different kinds of mixing apparatuses have traditionally been used, e.g. high-shear or planetary mixers, which all operate on the batch principle, that is, they can be used for the manufacture of only one batch at a time. In order to obtain a good granulation result with these apparatuses, usually various adjuvants have to be added, for example binders or even organic solvents. Irrespective of carefully chosen substances and amounts it is not always possible to make, for example, a product which remains even as to its moisture content with a mixer of this type. This is naturally a big disadvantage especially in the preparation of drug forms. In addition, with regar

REFERENCES:
patent: 4728513 (1988-03-01), Ventouras
patent: 4882169 (1989-11-01), Ventouras
patent: 5051262 (1991-09-01), Panoz et al.

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