To this product range different types of N-vinylpyrrolidone (NVP) homopolymers such as the soluble povidones and the insoluble crospovidone belong to. Copovidone, a copolymer consisting of vinylacetate and NVP, as well as the insoluble Kollidon® SR pertain to this group of branded products, too.

Soluble Kollidon® Grades

Kollidon® 12 PF and Kollidon® 17 PF
As an increasing number of active substances are inadequately soluble in water solubilizers are needed to cope with this issue. The low molecular weight povidone grades, Kollidon® 12 PF and Kollidon® 17 PF, form a soluble complex between the active ingre-dient and povidone. Both products are available as pyrogen-free powders, suitable for use in injectables.

Kollidon® 25, Kollidon® 30 and Kollidon® 90F
These products are particularly suitable for wet granulation in concentrations between
1 and 5 %, either with a binder solution or with a solvent such as water. Kollidon® 25 and Kollidon® 30 and can also be used in compaction processes. Concentrations are comparable to those applied in wet granulation. All the soluble Kollidon® grades have applications in ophthalmic preparations as well. While Kollidon® 17 PF, Kollidon® 25 and Kollidon® 30 are usually used in eye drops Kollidon® 90 F is preferred for contact lens solutions. A very unique characteristic of the povidones is their capability to form complexes with actives, which makes them interesting tools to improve the dissolution of many drugs.

Kollidon® VA 64
The most prominent property of Kollidon® VA 64 is its very high plasticity, which makes the product extremely suitable as a dry binder for direct compression or for dry granulation technology. Due to the hydrophobic vinyl acetate moiety the polymer is less hygroscopic in comparison to the povidones. For this reason Kollidon® VA 64 can also be used for sub-coatings. Kollidon® VA 64 Fine is a further improvement of Kollidon® VA 64 and shows an advanced performance as dry binder for direct compression and roller compaction. Due to the reduced particle size compared to the standard material Kollidon® VA 64 Fine is able to show a significant binding effect even at very low concentrations in the tablet.

Insolube Kollidon® Grades

Kollidon® CL grades
One of the main properties of the Kollidon® CL range is its complete insolubility in all commonly used solvents. As it swells in contact with water in a very predictable manner it is mainly applied as disintegrant. In contrast to other compounds the capability of swelling is reversible. This means, once wetted and dried the capability to swell still exists. Kollidon® CL-F is specially designed for use in small tablets and for wet granulation purposes because of it's ability to absorbe large amounts of liquids. Kollidon® CL-SF can be used for fast dispersible tablets, where it shows an outstanding mouthfeel beside a fast disintegration. Kollidon® CL-M is a micronised product with low bulk-density and 90% of the particles smaller than 15µm. The product acts as suspension stabilizer in liquid oral dosage forms.

Kollidon® SR
Due to the polyvinyl acetate moiety of Kollidon® SR is insoluble in water. This makes the product suitable for the manufacturing of sustained release matrix products by direct compression, roller compaction, wet granulation or extrusion.

Kollicoat® - Film-coating technology by BASF
BASF offers a full range of excipients in the fields of instant release, sustained release and enteric coating under the umbrella brand Kollicoat®. The Kollicoat® grades are state of the art aqueous coating agents characterized by excellent film forming properties, a reliable adjustment of release rates, easy and cost saving coating processes.

Kollicoat® IR for instant release coating is an innovative polyvinylalcohol-polyethylene
glycol graft-copolymer with excellent film forming properties and major advantages compared to hypromellose and other instant release film-coatings (see picture). Spray solutions have a low viscosity even at polymer concentrations of up to 25 %, which reduces the spray time significantly. This increases your coating capacity without investment into new coating equipment. The resulting films have a very high flexibility, no tackiness and a smooth surface even without additional plasticizer.

Kollicoat® IR White is a coating system based on Kollicoat® IR, which already contains white pigments and a surfactant. Due to a special way of production, the product is very quickly dispersible in water (see pictures). As the pigments are embedded in the polymer, no segregation can occur as with simple mixtures. The system is miscible with colorants such as iron oxides or lakes to give coloured systems. All the benefits of Kollicoat® IR in comparison to hypromellose also apply to Kollicoat® IR White.

Kollicoat® SR 30 D and EMM 30 D are 30% aqueous dispersions of polymers intended for sustained release coating, taste masking and protective coatings. Kollicoat® SR 30 D is a polyvinylacetate dispersion stabilized with povidone and sodium laurylsulfate, which represents a breakthrough in sustained release coating. It is characterized by a strong release-retarding activity, a reliable, pH-independent adjustment of release rate, easy handling and excellent film-forming properties and used as binder for granulation processes in the production of sustained-release matrix tablets. Kollicoat® EMM 30 D is marketed as a dispersion of poly (ethylacrylate, methyl methacrylate) 2:1. It is used as film former for pH-independent, controlled release coatings, for taste masking and protective coatings. It complies with the respective monographs in the European and the Japanese Pharmacopoeia.

Kollicoat® MAE 30 DP and MAE 100 P are two different grades of a methacrylic acid/ethyl acrylate copolymer (1:1). While the Kollicoat® MAE 30 DP is an aqueous dispersion, Kollicoat® MAE 100 P is offered as a powder. Both products are used for enteric coatings, which are more cost effective and reliably generate higher resistance to gastric fluid than cellulose derivatives.

Kollicoat® Protect is a solid solution of Kollicoat® IR and polyvinyl alcohol. It combines the advantages of Kollicoat® IR with the moisture protective properties of polyvinyl alcohol (PVA) avoiding drawbacks of PVA. One major drawback of PVA is, that solutions can only be prepared at temperatures of about 80°C/176°F, whereasKollicoat® Protect coatings can be prepared at room temperature. Together with pigments Kollicoat® Protect gives an excellent moisture protection and tastemasking effect. The pigments have to be added in order to extend the diffusion way through the film and to improve the protective properties of the film

Solutol® HS 15, a solubilizer developed by BASF, meets the requirements of an effective modern solubilizer and is approved for parenteral applications. It has just been monographed in the European Pharmacopoeia under the monograph name "Macrogol 15 Hydroxystearate".

Solutol® HS 15 - The solution for your dissolution problems

Beside the outstanding toxicological characteristics like a low histamine release compared to other solubilizers also the good solubilizing capacity and the possibility to sterilize solutions with Solutol® HS 15 make it an excipient of choice for your formulation develop-ment. An article in issue 11 of our customer magazine ExAct is addressing some practical aspects for the production of solubilizates with Solutol® HS 15.

Ludipress® consists of white, free-flowing granules that are odourless and tasteless ,which contain Lactose, Kollidon® 30 and Kollidon® CL, Ludipress® has been especially developed for direct compression, but is also suitable as a filler for hard gelatin capsules.

Ludipress® LCE was developed as an extension of the BASF range of direct compression excipients for use in chewable tablets and lozenges, for effervescent tablets and as filling agent for modified release formulations. However, in combination with Kollidon® CL as tablet disintegrant, all other types of formulation are possible. Moreover high-dose forms can be produced using Kollidon® VA64.

One physical measure to enhance the solubility of an active ingredient is to increase its surface area by micronization. Others include the usage of solubilizers such as poloxamers. The currently available Lutrol® F 68 and F 127 are prilled, which results in a mean particle size of about 1000 µm, while non-crystalline active ingredients have a particle size of 20 to 200 µm. This large difference in particle sizes of the active ingredient and excipient causes a segregation of powder blends. It is almost impossible to get a homogenous mixture of actives and excipients, which can result in content uniformity concerns with tablets. As a formulator's solution, BASF can provide Lutrol® micro 68 and 127 with a mean particle size of 50 µm, which is much closer to that of active ingredients.

Soluphor® P is mainly used in veterinary injection preparations as a solvent together with water and/or in combination with low-molecular polyvinylpyrrolidone (Kollidon® 12 PF or Kollidon® 17 PF). Likewise it suggests itself for use in solutions for oral application. The solubilities of some active ingredients in Soluphor®P mixtures are listed in the technical information.

A further application of Soluphor® P could be in topical preparations for absorption acceleration of active ingredients. The penetration of active ingredients through the human skin is markedly increased by Soluphor® P and/or accelerated to the same extent as by dimethyl sulphoxide or dimethyl acetamide and even more markedly than by means of dimethyl formamide. This effect is also described for transdermal systems and for the transmucosal application.

Cremophor® EL is a nonionic solubilizer and emulsifier manufactured by reacting castor oil with ethylene oxide in a molar ratio of 1 to 35. It emulsifies or solubilizes the fat-soluble vitamins A, D, E and K in aqueous solutions for oral and topical administration. In aqueousalcoholic solutions, it very readily solubilizes essential oils. Aqueous solutions of hydrophobic drugs (e.g. Miconazole, Hexetidine, Clotrimazole, Benzocaine) can also be prepared with Cremophor® EL.. Cremophor®ELP is manufactured by purifying Cremophor® EL and is therefore suitable for parenteral applications, e.g. Taxol preparations.

The low molecular weight liquid polyethylene glycols Lutrol® E 300, Lutrol® E 400 and Lutrol® E 600 are excellent solvents for a large number of substances that do not readily dissolve in water. They are therefore widely used as solvents and solubilizing agents for active substances and excipients in liquid and semi-solid preparations.

It is the ability of PEGs to form complexes with active substances that is responsible for their excellent solvent power. However, equilibrium constants for complex formation vary considerably from one substance to another, and certain drugs such as Penicillin G and Bacitracin can even be inactivated.

The effect of the polyethylene glycol on the efficacy and absorption of a drug must therefore always be determined in tests. With regard to incompatible substances, please see the remarks in the European Pharmacopoeia. Lutrol® E grades can also be used to adjust the viscosity of liquid pharmaceutical preparations and ointments, to modify their absorption properties and to stabilize the preparation. In the manufacture of soft gelatin capsules, liquid macrogols can be used as carriers for dissolved or suspended drugs.

Mixtures of solid and liquid polyethylene glycols can be used as water-soluble bases for ointments, suppositories and ovula. Because of its good solvent power, Lutrol® E 400 is used to remove phenol, cresol, aniline and similar compounds from the surface of skin burnt by any of these toxic substances. For burns from chlorophenols or chlorocresols, a mixture of 2 parts Lutrol® E 300 and 1 part ethanol is recommended.

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