Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Patent
1994-12-23
1997-03-04
Webman, Edward J.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
424488, 424499, 424490, 424495, 424497, 424498, 264 15, 428402, A61K 910, A61K 916, A61K 922, A61K 4738
Patent
active
056076959
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND
1. Field of the Invention
The present invention is related to a process for the manufacturing of new multiple unit carriers and release controlling systems for bioactive materials as well as the manufacturing of a new additive to be used in the formation of tablets and especially in direct compression and to obtain multiple unit preparations in the form of compressed and disintegrating tablets.
2. Background of the Invention
This invention relates to the administration or dispersion of bioactive materials in the form of small discrete particles, often referred to as multiple unit (MU) preparations or systems. It is well known that MU systems offer several advantages such as good dosing and handling properties as well as excellent possibilities to obtain a controlled release of the active ingredient, or ingredients.
The control of the release rate, or other release properties, can be achieved in a number of different ways such as using hydrophobic and or hydrophilic materials in which the bioactive material is embedded and released by a diffusion or erosion process as well as coating particles (crystals, beads, pellets etc.) with a release controlling barrier.
The barrier may be designed e.g. to control the release rate by diffusion- or osmotic processes or to delay the release by a controlled disintegration of the barrier, which may be designed to be affected by environmental conditions such as humidity, pH, microorganisms or enzymes.
The above mentioned release controlling systems have been of special importance within the pharmaceutical field during the last decades. Apart from the possibilities to control the delivery of drugs to humans or creatures, and thus to obtain therapeutical advantages for a large number of drugs, several advantages with MU preparations compared to single unit preparations have been described in the literature.
It is, for example, possible to obtain a more reproducible emptying of small units (e.g. less than 1-2 mm, c.f. Bogentoft C et al, Influence of food on the absorption of acetylsalicylic acid from enteric coated dosage forms, Europ. J. Clin. Pharmacol. (1978), 14, 351-355) and thus a dispersion over a large area of the gastrointestinal canal. This may promote the absorption process, causing reduced variability, as well as reduced local irritation in the oesophagus or other parts of the gastrointestinal tract.
A large number of processes have been developed to produce the MU cores. The cores may include release retarding components, be intended for further processing such as coating with suitable materials or may simply act as a carrier for the active material. The processes includes for example controlled crystallization and mechanical formation of spherical particles from mixtures of active substances and hydroplastic additives as well as spray drying and spray chilling processes. There are numerous ways to form spherical small particles by mechanical processes, e.g. by using coating drums, pans and extrusion/spheronization and fluid bed equipment (Pharmaceutical Pelletization Technology, Ed. I Ghebre Sellassie, Marcel Dekker, Inc New York 1989).
It is, in general, very critical to get particles of a well defined size, form and surface area (Ragnarsson and Johansson, ref. Drug Dev. Ind. Pharm. 14, 2285 (1988) in order to obtain good handling properties, good dose uniformity or accurate control of the release properties. To fulfill these requirements, the production processes are in general complex including several steps and often finished by e.g. a sieving process to obtain uniform particles. A manufacturing process including many steps will be time consuming and expensive but may also pose environmental hazards when handling toxic or irritating substances. Of special importance is the loss of active material in the different production steps and, especially, when sieving materials in order to obtain the required particle size fraction.
The optimal solution would be to produce spherical inert particles of the required particle size and size distribution that
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Ek Bo R.
Eriksson Kjell G.
Nyqvist Per Gustaf H.
Ragnarsson Gert A.
Pharmacia & UpJohn AB
Webman Edward J.
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