Process for polishing granulates of active principles

Details Process for polishing granulates of active principles Process for polishing granulates of active principles

1992-04-17

1994-04-05

Beck, Shrive

Coating processes

Particles, flakes, or granules coated or encapsulated

4274071, 426 96, 426303, 426656, 426807, B05D 700, A23L 1216, A23B 500

Patent

active

053003187

DESCRIPTION:

BRIEF SUMMARY
The present invention relates to the treatment of granulates of active principles, and provides, more particularly, a process for polishing granulates of active principles intended for feeding and/or treating ruminants.
It is known, for example according to U.S. Pat. Nos. 4,181,708, 4,181,709 and 4,181,710, to prepare granulates which are suitable for administration to ruminants, consisting of a core of active substance and of a coating based on a hydrophobic substance and on a polymer which withstands the neutral PH of the rumen but is degradable at the more acidic pH of the abomasum.
In these granulates, the core, consisting of active principle, is granular in form. It is obtained by dry blending the active substances, binders and, optionally, neutralising agents and densifying agents. The blend is then wetted and converted into a pasty mass which is granulated by extrusion at room temperature and prilling. The moist granulate is dried in an oven or fluidised bed, and may then be employed directly for the coating operation. The polymer, hydrophobic substance and fillers are mixed, and the mixture is dispersed in an organic solvent and then sprayed onto the granulate.
To obtain proper protection of the active principle at least 20 g of the mixture of polymer and hydrophobic substance must be sprayed per 100 g of granulated active substance and the coating layer is approximately 150 .mu.m in thickness (see Example 1 of U.S. Pat. No. 4,181,710).
Since the polymer is expensive, industry has for a long time been searching for a means of reducing its weight percentage in the final granulate, while retaining good protection of the active substance as it passes through the rumen.
This objective has been attained in accordance with the present invention by employing, as the core of active principle subjected to coating, a granulate which has been subjected to an additional polishing operation. A "polishing" operation means an operation which reduces the specific surface area of the granulate by reducing surface nonuniformities. The polished granulate then requires a smaller quantity of coating material for the same quantity of active substance, since the quantity of coating material needed for good protection is related to the specific surface area of the starting granulate.
According to the present invention a granulate of an alimentary and/or medicinal active principle for feeding to or treating ruminants is polished by depositing, more especially by spraying, onto the granulate of active principle a solution of active principles and/or sugars and/or resins. It is preferred to employ an aqueous solution of active principle and especially a solution of sprayed onto a lysine and/or methionine granulate.
The base granulate which is subjected to the polishing operation may be made from lysine hydrochloride crystals or may be prepared according to the operating method of patents U.S. Pat. No. 4,181,708 or U.S. Pat. No. 4,181,710 by mixing one or more active principles in powder form, a binding agent and, optionally, a diluent and/or a filler.
The active principle is generally an amino acid such as methionine, lysine or one of its salts, phenylalanine, histidine, arginine, or tyrosine, a medicament such as a vitamin, antibiotic, or antiparasitic agent, or a protein. The preferred active principle is lysine, in which case a homogeneous granulate is obtained, consisting of a lysine core polished with a lysine film. The diluents and fillers may be sugars, cellulose and/or silica. The binding agent may be a cellulose derivative such as hydroxypropyl methyl cellulose, a resin, or any derivative known in the feedstuff industry for thickening or promoting the preparation of tablets.
The various constituents are granulated by any technique known to a person skilled in the art, for example by extrusion, after wetting, through a die, followed by drying; they may also be subjected to compacting followed by milling.
The granulate obtained is screened so as to retain a granulate distribution between 200 and 4,000 .mu.m and prefer

REFERENCES:
"CRC Handbook of Chemistry and Physics", 60th edition 1979-1980.

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