Highly effective soluble copovidone for dry binding due to a finer particle size and specifically designed for roller compaction and dry binding in Direct Compression formulations.
Kollidon® VA 64 Fine is a vinylpyrrolidone-vinyl acetate copolymers. It is used as dry binder in tablets, as granulating agents, as retarding and as a film-forming agents. Kollidon® VA 64 Fine is especially suitable for markets with high humidity exposure. Kollidon(R) VA 64 can be applied in direct compression processes such as roller compaction, hot melt extrusion processes and for controlled release preparations.
Benefits of Kollidon® VA 64 Fine
Kollidon® VA 64 Fine is an excellent binders for tablets and granules. Between 2% and 8%, as a proportion of the final weight of the preparation, is usually used. An important property of Kollidon® VA 64 Fine in this application is the plasticity, which distinguishes the products from povidone (e.g. Kollidon® 30). This property often gives granules and mixtures that are less susceptible to capping during tabletting, and tablets that are less brittle.
Kollidon® VA 64 Fine has been found to be an excellent dry binder for direct compression. It gives much better results than any of the Povidone grades or other dry-binders of the group of cellulose derivatives. The hardness, friability, porosity and disintegration time of lactose and starch placebo tablets produced with Kollidon® VA 64 Fine is directly related to the compression force Kollidon® VA 64 Fine can be added to materials such as sorbitol, mannitol, starch, or direct compression aids, e.g. micro crystalline cellulose, whose own binding strength is inadequate, to give tablets with very good properties.
Kollidon® VA 64 Fine can also be used as a binder in wet granulation for the production of tablets and granules, since it is readily soluble in all the usual solvents. It can then be added either as a solution during granulation, or dry to the other ingredients, in which case the solvent is added alone during granulation. Trials so far conducted with both methods, using equal quantities of liquid, produced tablets of much the same hardness. A combination of the two methods, i.e. mixing some of the Kollidon® VA 64 Fine with the active ingredient, and dissolving the rest in the solvent, sometimes gives the best results. This is particularly recommended if the active ingredient does not readily absorb the solvent. Since it is less hygroscopic than povidone (e.g. Kollidon® 25 or Kollidon® 30), Kollidon® VA 64 Fine gives granules that have less tendency to stick to the punches of the tableting machine, when operating under humid conditions. The binding power of Kollidon® VA 64 Fine is comparable to that of Kollidon® 25 and Kollidon® 30.
Kollidon® VA 64 Fine was specifically suitable for the application in roller-compaction and is the material of choice in terms of particle size distribution and particle shape for this application. Due to the particle size it is able to cover a bit surface area and to form numerous bridges in the tablet structure that lead to hard tablets with a reduced friability.
Kollidon® VA64 Fine forms films that are soluble at all pH values. They are less hygroscopic and more elastic than those formed by povidone (e.g. Kollidon® 30). Nevertheless, Kollidon® VA 64 Fine usually still absorbs too much water, so that it can seldom be used as the sole film-forming agent in a formulation. It is therefore recommended to combine it with less hygroscopic substances such as cellulose derivatives, shellac or polyethylene glycol. Plasticizers are normally not required. Kollidon® VA 64 Fine significantly improves their brittleness and solubility when it is combined with cellulose derivatives. When it is used in film coatings based on shellac, the properties of the film are more consistent.
If it is intended to coat tablet cores with aqueous solutions or suspensions, it is recommended to provide them with a barrier if they contain a water-sensitive active ingredient or a highly effective disintegrant (e.g. Kollidon® CL) that is activated by water. This also applies if the cores are too soft or if their adhesive properties are inadequate for aqueous coatings. The cores are warmed to about 35 °C and sprayed with a 10% solution of Kollidon® VA 64 Fine dissolved in an organic solvent, e.g. isopropanol, ethanol, ethyl acetate or acetone. As soon as a barrier film of adequate thickness has been built up, the aqueous coating can be applied.
Kollidon® VA b64 Fine is used in sugar-coating to improve the adhesion of the coating to the surface of the tablet core and to increase the capacity of the coating solution for pigments and improve their dispersibility. However, Kollidon® VA 64 Fine helps not only in the application of sugar coatings but also in the automation of the sugar-coating process.
Kollidon® VA 64 Fine is frequently cited in the literature as a matrix material for instant release and for sustained release dosage forms. Formulations with cellulose derivatives, polyacrylic acid, stearyl alcohol or polyhydroxyethyl methacrylate have been described for sustaining or controlling release. The formulations can be treated in various ways, e.g. freeze-dried or extruded, to produce a granulate, or melted and extruded, to produce pellets. Any relevant patents must be respected.
The solubility and bioavailability of poorly soluble APIs is often enhanced when they are molecularly dispersed in a polymeric carrier. This makes Hot Melt Extrustion (HME) a valuable technology for the pharmaceutical industry – and opens new doors for formulators working with promising actives that cannot otherwise be solubilized. HME also grants manufacturers a great amount of flexibility, as the viscous fluid obtained from the extrusion process can be directly shaped into any desired form. In addition, the extrudates usually have a high density, which makes them suitable for producing controlled-release dosage forms. Kollidon® VA 64 Fine is especially suitable for hot melt extrusion processes. In matrices it acts as solubilizing agent, dispersant, crystallization inhibitor as well as is suitable in immediate-release matrices.
|Chemical name:||Vinylpyrrolidone-vinyl acetate copolymer|
|Regulatory Status:||Kollidon® VA 64 Fine meets current Ph. Eur., USP monograph "Copovidone" and the JPE monograph "Copolyvidone"|
|Applications:||The main application is as soluble binder for granulation and as dry-binder in direct compression technology, as a film-forming agent in sprays and as pore-former in coating and taste-masking applications.|
|Description:||Kollidon® VA 64 Fine is a white or slightly yellowish, free-flowing powder with a faint characteristic odor and practically no taste.|
|Solubility:||Kollidon VA 64 Fine readily dissolve in all hydrophilic solvents. Solutions of more than 10% concentration can be prepared in water, ethanol, isopropanol, methylene chloride, glycerol and propylene glycol. It is less soluble in ether, cyclic, aliphatic and alicyclic hydrocarbons.|
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