Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Particulate form
Patent
1994-12-19
1999-03-02
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Particulate form
424490, 424491, 424493, 424497, 264 41, 264 433, 264 46, 264 13, 4272133, 42721333, 42721335, 42721336, 4284022, 42840224, 5147722, 5147723, 514773, 514774, 514776, 514777, 514778, 514779, 514781, 514782, 514783, A61K 914
Patent
active
058767541
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/DE93/00038 filed Jan. 18, 1993.
The invention relates to accurately meterable powders, granules or pellets comprising hydrophilic macromolecules, active compounds and optionally other pharmaceutically acceptable structure-forming substances and auxiliaries, the active compound being dissolved, suspended or emulsified in a matrix, and a novel process for the production of these powders, granules or pellets, and furthermore their use as a medicament, cosmetic, diagnostic or dietetic foodstuff (healthcare). Active compounds employed are preferably dihydropyridine derivatives, in particular nifedipine, nitrendipine or nisoldipine.
Granules or pellets as shaped articles serve in the pharmaceutical industry mainly as intermediates for tableting. Shaping here should lead to a free-flowing, granular and dust-free product which, on account of its homogeneity, improves technological processing and dosage accuracy. Moreover, pellets, as a modern multiple-unit pharmaceutical form, for example filled into hard gelatin capsules, possess a number of advantages compared with single-unit pharmaceutical forms, such as e.g. tablets or coated tablets: contrast to monolithic pharmaceutical forms, especially with enterically coated pharmaceutical forms. tract in contrast to a compressed tablet, which must first disintegrate into its granule particles. metered in mixed form.
However, the fundamental problem of the necessary shaping of pulverulent-crystalline active compounds and auxiliaries to processable granules (pellets) as shaped articles underlies all processes of the prior art.
A distinction is made here between building up and breaking down processes. It is common to all processes that until now granules or pellets as shaped articles were only obtained via various and complicated partial steps.
In the breaking down processes--presented in simplified form--the pharmaceutical substances and auxiliaries are first comminuted, brought to a uniform grain size by sieving and then mixed. Dry or moist granulation then takes place, in which the powder mixture is aggregated and then comminuted to give grains of granular material. In the next step, if necessary, it is dried and sieved again.
In the case of the building-up granules, grains of granular material are formed from the powdered pharmaceutical substances and auxiliaries with continuous addition of granulation fluid with simultaneous drying in a controlled process (e.g. fluidized bed process).
By means of subsequent, special rounding processes (e.g. Marumerizer.RTM.), round, bead-shaped granule particles (pellets) are obtained. A disadvantage in this case is that in the rounding of already prepared, unshaped granule particles substance matter containing pharmaceutical substance is lost and cannot be directly fed to the granulation process again. This is certainly a problem in terms of cost and disposal. At the same time, the mechanical shaping leads to a non-uniform product.
Special pelleting techniques are, for example, build-up dry pelleting by compaction and fluidized bed granulation, which produce very unsatisfactory results with respect to shape and mechanical strength of the pellets.
All these preparation processes are technologically complicated multi-step processes. They are characterized by a multiplicity of process parameters of technological type, such as e.g. temperature, moisture content, homogeneity of the mixtures etc.
Furthermore, in all granulation and pelleting processes the use of a whole series of auxiliaries is necessary. Thus, for example, binders or granulation fluids must be employed to bring the powdered material into a solid, compact and processable form. The most accurate knowledge about the physicochemical behavior e.g. heat of solution, solubility or crystal formation tendency and great experience in working with these substances is necessary to be able to assess the interaction of these auxiliaries with one another and with the pharmaceutical substance in combination with all process parameters to be taken into ac
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Freidenreich Jurgen
Schick Ursula
Werry Jurgen
Wunderlich Jens-Christian
Alfatec-Pharma GmbH
Page Thurman K.
Spear James M.
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