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CAS NUMBER: 25086-89-9
DEFINITION:
Kollidon VA 64 is a white or slightly yellowish, free-flowing powder with a faint characteristic odor and practically no taste.
Kollidon VA 64 readily dissolves in all hydrophilic solvents.
Solutions of more than 10 % concentration can be prepared in water, ethanol, isopropanol, methylene chloride, glycerol and propylene glycol.
Kollidon VA 64 is less soluble in ether, cyclic, aliphatic and alicyclic hydrocarbons.
Kollidon VA 64 is vinylpyrrolidone-vinyl acetate copolymers.
Kollidons VA 64 are used in the pharmaceutical industry as dry binder in tablets, as matrix formers for amorphous solid dispersions, as retarding and as film-forming agents.
BENEFITS:
-Kollidon VA 64 provides erodible instant release matrix
-Kollidon VA 64 is a solubilizer, dispersant, crystallization inhibitor and matrix former
-For direct compression, roller compaction and wet granulation, suitable for markets with higher humidity exposure
-Kollidon VA 64 has excellent stability throughout the extrusion process
-A coarse powder provides a dust free handling, good flowability and faster extruder feeding
PROPERTIES:
-Quality Level: 100
-composition: polyvinylacetate, 75.0-85.0% (saponification value * 0.1534), povidone, 18.0-21.0 (N content/0.126)
-impurities: ≤100 ppm vinyl acetate, ≤20 ppm heavy metals (verified on random samples only), ≤5000 ppm residual solvents (acetic acid, acetate, formic acid (GLC)
-ign. residue: ≤2.00% (verified on random samples only)
-loss: ≤5.0% loss on drying
-pH: 3.5-5.5 (10% in H2O)
GENERAL DESCRIPTION:
Kollidons VA 64 consist of soluble and insoluble grades of polyvinylpyrrolidone (PVP) of various molecular weights and particle sizes.
The polymers are used as dry binders, film-formers, stabilizers in suspensions, dispersants for pigments, enzyme stabilizers, and for improvement of bioavailability.
APPLICATION:
Kollidon VA 64 is a blend of polyvinyl acetate and povidone (K 30) in the ratio 8:2 used in the pharmaceutical industry as a matrix-forming agent.
This research grade product is intended for use in R&D and development only.
DEFINITION:
Kollidons VA 64 are spray dried polymer powders of a copolymer derived from the monomers N-vinylpyrrolidone (NVP) and vinyl acetate (VAc).
The molar ratio of the monomers NVP and VAc in the copolymer is approx. 6 : 4.
The powders are white or slightly yellowish, have a faint characteristic odor and practically no taste.
MOLECULAR WEIGHT:
The average molecular weight is usually expressed as a K value.
The exact weightaverage molecular weight, Mw of the product is best determined by measuring the light scatter of a solution.
Values in the range of 45,000 – 70,000 have been determined for Kollidon® VA 64 and Kollidon® VA 64 Fine.
SOLUBILITY:
Kollidon VA 64 readily dissolves in all hydrophilic solvents.
Solutions of more than 10% concentration can be prepared in: water, ethanol, isopropanol, methylene chloride, glycerol and propylene glycol.
VISCOSITY:
The values shown in Fig. 2 were determined at 25 °C in a capillary viscometer.
They represent typical values.
BULK DENSITY:
The bulk density of Kollidon VA 64 usually lies in the range of 0.08 – 0.15 g/ml.
The bulk density of Kollidon VA 64 is above that one of Kollidon® VA 64 Fine and is in the range of about 0.2 – 0.3 g/ml.
APPLICATION:
Kollidons VA 64 are 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 has been found to be excellent dry binders for direct compression.
Especially the Kollidon VA 64 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 are directly related to the compression force used.
Kollidon VA 64 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 can also be used as a binder in wet granulation for the production of tablets and granules, since Kollidon VA 64 is readily soluble in all the usual solvents.
Kollidon VA 64 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 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 Kollidon VA 64 is less hygroscopic than povidone, Kollidon® VA 64 gives granules that have less tendency to stick to the punches of the tabletting machine, when operating under humid conditions.
The binding power of Kollidon® VA 64 is comparable to that of Kollidon® 25 and Kollidon® 30.
Kollidon VA 64 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 usually still absorbs too much water, so that it can seldom be used as the sole film-forming agent in a formulation.
Kollidon VA 64 is therefore recommended to combine it with less hygroscopic substances such as cellulose derivatives, shellac or polyethylene glycol.
Plasticizers are normally not required.
The formulations in Tables 4 and 5 are typical formulations for tablet coatings.
They were tested on 9 mm diameter, 3.4 mm thick, 200 mg placebo tablet cores in the laboratory.
Kollidon VA 64 significantly improves their brittleness and solubility when Kollidon VA 64 is combined with cellulose derivatives.
When Kollidon VA 64 is used in film coatings based on shellac, the properties of the film are more consistent.
If Kollidon VA 64 is intended to coat tablet cores with aqueous solutions or suspensions, Kollidon VA 64 is recommended to provide them with a barrier if they contain a watersensitive 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 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 64 has been found that 0.4 mg Kollidon® VA 64/cm2 is adequate.
Kollidon VA 64 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 helps not only in the application of sugar coatings but also in the automation of the sugar-coating process.
Because of Kollidon VA 64 good film-forming properties, Kollidon® VA 64 can also be used in topical sprays.
The formulation in Table 6 provides a typical example of a spray bandage.
For the manufacturing of solid dispersions using spray drying, it is essential that both API and matrix polymer are soluble in a suitable volatile organic solvent.
Kollidon VA 64 is soluble in a number of organic solvents (see section 2.5) at levels greatly exceeding 10 % [w/w] while simultaneously retaining a low viscosity, which is crucial for successful spray drying.
Kollidon VA 64 exhibits these effects when utilized with poorly water-soluble compounds.
In this case, the oral dose primarily includes a hard or softgel capsule where Kollidon® VA 64 is dissolved in hydrophilic fill formulations such as low molecular weight polyethylene glycols.
With Kollidon VA 64, Kollidon VA 64 is possible to prevent recrystallisation and to achieve a “Parachute Effect” in both low pH stomach conditions and high pH intestinal conditions.
Under stomach conditions, this is shown in Figure 5 for the model poorly soluble drug Danazol with Kollidon® VA 64 used at 5% w/w in a PEG 400 liquid fill.
The effect is compared with known crystallization inhibitor Kollidon VA 64 and solubilizer Kolliphor RH 40, which exhibits a spring effect.
Kollidon VA 64 is a white or slightly yellowish, free-flowing powder with a faint characteristic odour and practically no taste.
Kollidon VA 64 readily dissolves in all hydrophilic solvents.
Solutions of more than 10 % concentration can be prepared in water, ethanol, isopropanol, methylene chloride, glycerol and propylene glycol.
Kollidon VA 64 is less soluble in ether, cyclic, aliphatic and alicyclic hydrocarbons.
FUNCTION:
-Binder
-coating
-Crystallisation inhibitor
-Direct compression
-film former
-Moisture protection
-Solubility enhancement
-Wetting-dissolution enhancement
TECHNICAL INFORMATION:
Kollidon VA 64 is a vinylpyrrolidone-vinyl acetate copolymer that is soluble both in water and in alcohol.
Kollidon VA 64 is used as a dry binder in tabletting, as a granulating auxiliary and as a film-forming agent in the pharmaceutical industry.
STORAGE:
Kollidon VA 64 can be stored at room temperature (max. 25 °C) in the unopened original containers for at least 3 years.
APPLICATION:
Kollidon VA 64 is an excellent binder for tablets and granules.
Between granules 2% and 5%, as a proportion of the final weight of the preparation, is usually used.
Kollidon VA 64 can be added to materials such as sorbitol, mannitol, starch, or direct compression aids, e.g. microcrystalline cellulose, whose own binding strength is inadequate, to give tablets with very good properties.
Kollidon VA 64 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.
Kollidon VA 64 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 with the active ingredient, and dissolving the rest in the solvent, sometimes gives the best results.
Kollidon VA 64 is particularly recommended if the active ingredient does not readily absorb the solvent.
Since Kollidon VA 64 is less hygroscopic than povidone, Kollidon VA 64 gives granules that have less tendency to stick to the punches of the tabletting machine, when operating under humid conditions.
Kollidon VA 64 and Kollidon® VA 64 Fine are vinylpyrrolidone-vinyl acetate copolymers which are soluble both in water and in alcohols.
Kollidons VA 64 are used in the pharmaceutical industry as binders in tablets and as granulating, retarding and fi lm-forming agents.
Kollidon VA 64 and Kollidon® VA 64 Fine are white or slightly yellowish, free-fl owing powders with a faint characteristic odor and practically no taste.
Kollidon VA 64 is a free-flowing powder with a faint characteristic odour and practically no taste.
Kollidon VA 64 readily dissolves in all hydrophilic solvents.
DESCRIPTION:
Kollidon VA 64 is vinylpyrrolidone-vinyl acetate copolymers or copovidone.
Due to Kollidon VA 64s exceptionally high binding capacity, Kollidon VA 64 can be used as a dry binder for direct compression tableting and as a soluble binder for granulation; these properties make it an attractive and cost-effective alternative to natural binders.
In addition, Kollidon VA 64 is ideal as a solubilizer in hot-melt extrusion processes.
Kollidon VA 64 is specifically designed for roller compaction and binding in DC formulations.
Kollidon VA 64 is a 6:4 linear random copolymer of N-vinylpyrrolidone and vinyl acetate.
The vinyl acetate component of Kollidon VA 64 reduces the hydrophilicity and glass transition temperature (Tg) compared to povidone homopolymers of similar molecular weight.
As a result, Kollidon VA 64 is the ultimate tablet binder that extends its excellent adhesive property in wet granulation, as well as in dry granulation and direct compression.
Due to Kollidon VA 64's spherical, hollow particle morphology and high plasticity, Kollidon VA 64 performs exceptionally well as a binder for direct compression.
In addition, a lower Tg makes Kollidon VA 64 an ideal polymer matrix for solid dispersions/solutions via hot melt extrusion, which enhances the dissolution of poorly soluble drug actives.
BENEFITS:
-Suitability for use in direct compression, dry granulation, wet granulation, hot melt extrusion, and film coating.
-Good flowability
-Large surface area due to hollow particle morphology – enhances particle bonding and good compressibility
-Ideal glass transition temperature (Tg) for hot melt extrusion
SYNONYM:
Soothe
Crospovidone
Polyplasdone
Polyvidonum
Agrimer
Disadine
Refresh
Toxobin
Povidone
Tears Plus
Aldacol Q
Kollidon CL
Kollidin CLM
Plasdone 4
Luviskol K30
Luviskol K90
Polyclar A. T
Polyvinyl pyrrolidone
Polividone [DCIT]
K25 (polymer)
K30 (polymer)
K60 (polymer)
K115 (polyamide)
Polyvinylpolypyrrolidone
Agent AT 717
Plasdone K-26/28
Povidone
PVP10_SIAL
PVP40_SIAL
Povidone
PVP-K 15
Poly(1-ethenyl-2-pyrrolidinone)
CHEBI:185135
Polyvinylpyrrolidone, cross-linked
K 25
K 30
K 60
1-Ethenyl-2-pyrrolidinone (9CI)
Tolpovidone I 131 [USAN:INN]
1-Vinyl-2-pyrrolidinone homopolymer
1-Ethenyl-2-pyrrolidinone homopolymer
2-Pyrrolidinone, 1-vinyl-, polymers
1-Ethenyl-2-pyrrolidinone, homopolymer
2-Pyrrolidinone, 1-ethenyl, homopolymer
1-(1,2-Diphosphanylethyl)pyrrolidin-2-one
1-Ethenyl-2-pyrrolidinone homopolymer, 9CI
1-[1,2-bis(phosphanyl)ethyl]pyrrolidin-2-one
1-Vinyl-2-pyrrolidinone cross-linked insoluble polymer
