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    The solid solution

    Soluplus® – The Solid Solution

    With its excellent capability to form solid solutions, Soluplus® is suitable for innovative processing technologies, such as hot melt extrusion. Soluplus® was awarded with the CPhI Silver Innovation Award in 2010.

    Soluplus® is an innovative excipient that enables new levels of solubility, and bioavailability for poorly soluble active ingredients. Developed specifically for solid solutions, Soluplus® is unique in many ways. Thanks to its high flowability and excellent extrudability, Soluplus® shows superior performance in forming solid solutions, especially in hot melt extrusion processes. This solid solution makes the active pharmaceutical ingredient (API) available in a dissolved state, resulting in improved bioavailability, once in the body. The safety of Soluplus® is documented by a comprehensive range of toxicological data.

    Benefit from the advantages of Soluplus®
    Soluplus® is designed to solubilize poorly soluble APIs
    Excellent capability to form solid solutions
    Ideal for hot melt extrusion
    High extrudability and easy processing

    Hot melt extrusion

    Hot melt extrusion technology has become increasingly popular in recent years. Although this technique has been used in the plastics and food industries for decades, it is relatively new in the pharmaceutical industry and only a few drug products manufactured this way are currently available on the market. Hot melt extrusion technology shows numerous benefits over traditional methods, including shorter processing times, environmental advantages due to the elimination of solvents and the more efficient delivery of drugs to patients.

    Great results in hot melt extrusion.

    The high flowability and excellent extrudability of Soluplus® make for first-class results in hot melt extrusion. Soluplus® was specifically designed to solubilize poorly soluble APIs in this innovative production process. Its outstanding ability to form solid solutions and excellent solubilization capabilities, combined in one molecule, distinguish Soluplus® from other molecules that are used to form solid solutions or deployed in hot melt extrusion. However, Soluplus® is not limited to solid solutions formed via hot melt-extrusion, but can also be used as a matrix former in spray drying processes. Furthermore, it can be deployed as a binder in wet or dry granulation and in drug layering. These possibilities, and many others, extend the potential scope of Soluplus®. Formulators can use the new polymer in many different ways to significantly improve solubility and bioavailability.

    Significant improvement in API release.

    Designed specifically for poorly soluble APIs.

     

    Significant improvement in bioavailability.

     

    Results from dissolution tests showed a faster release of the poorly soluble API itraconazole in solid solutions prepared with Soluplus®. Compared to other polymeric matrices, the fastest release was achieved with Soluplus®.

    For example, its solubilization capacity for the poorly soluble carbamazepine, ketoconazole and danazol is much higher compared to well-known surfactants such as Solutol® HS 15 (Kolliphor® HS 15) and Cremophor® RH 40 (Kolliphor® RH 40) in a saturated solution in phosphate buffer (pH 7.0).

    Results showed a considerable improvement in the bioavailability of the poorly soluble API Itraconazole in solid solutions prepared with Soluplus®. The bioavailability study was conducted in beagle dogs.

    Product safety demonstrated by comprehensive toxicological data.

    A wide range of toxicological studies have been performed on Soluplus®, and the safety of the product has been documented in comprehensive studies. Toxicological data can be provided upon request.

    Soluplus in standard processes. 


    Even though Soluplus® was developed for solid solutions, it can be used for other applications too. Besides hot melt extrusion, drug layering and spray drying, it can be also applied as a binder in wet granulation or dry binder in direct compression. With multiple applications like these, you stand to benefit from the solubilization capabilities of Soluplus® while using it in standard processes.

    Application Guide

    Hot Melt Extrusion with BASF Pharma Polymers - Compendium, 2nd and Enlarged Edition

    The compendium now provides readers with an even better understanding of solid dispersions and the hot-melt extrusion process, and offers even more real-world application data.

    Technical information

    Soluplus® - Technical Information

    Soluplus is a novel polymer specially designed for solid solutions.

    Brochure

    Soluplus® – The Solid Solution: Opening New Doors in Solubilization

    Soluplus® is an innovative excipient that enables new levels of solubility and bioavailability for poorly soluble active ingredients. Developed specifically for solid solutions

    Webinars

    Choosing the Proper Dissolution Method When Testing Solubilization Performance

    With the increase in use of advanced formulation methods to improve solubility of drugs, standard dissolution methods are not always capable to reflect the full in-vivo potential. This webinar will take a close look at dissolution testing of solid dispersions made with polyvinyl caprolactam–polyvinyl acetate–polyethylene glycol graft copolymer (Soluplus®) and how to design an appropriate dissolution test that is discriminatory for APIs with different prerequisites. Standard compendial dissolution tests do not necessarily reflect the actual performance potential of solid dispersions in terms of later bioavailability due to their simplistic setup. This webinar will focus on a workflow to find the proper dissolution test for solid dispersions, using a Soluplus-based formulation as an example. The target is to show a methodology to have discriminating dissolution methods, which represent the expected performance ranking in-vivo among different formulations.

    How glass-forming polymers improve bioavailability / Enhanced oral bioavailability with Soluplus® – case study

    How glass-forming polymers improve bioavailability Polymers are essential components of oral solid dosage forms and used as binders, disintegrants or coatings. Given the increase in poorly water-soluble drugs, not only well-known but also specifically designed polymers (e.g. Soluplus®) can be used to improve both drug dissolution and bioavailability. Solid dispersions – embedded drug molecules at a molecularly dispersed state into an amorphous polymer – have shown superior bioavailability in comparison to other drug delivery systems. This webinar introduces the specific process technologies, namely hot melt extrusion or spray-drying, and the polymeric excipients available in the BASF portfolio to develop stable solid solutions. Enhanced oral bioavailability with Soluplus® – case study Soluplus® based solid solutions increase the solubility and oral bioavailability of poorly soluble active ingredients. Results from an in-vivo study in dogs with itraconazole showed a more than two-fold increase in oral bioavailability of a Soluplus® based formulation compared to the commercially available drug product. The Presentation explains what is special about Soluplus® and gives recommendations for in-vitro dissolution testing and the formulation of a quickly disintegrating tablet.

    Articles

    European Journal of Pharmaceutics and Biopharmaceutics

    Micro-scale prediction method for API-solubility in polymeric matrices

    A new predictive micro-scale solubility and process model for amorphous solid dispersions (ASDs) by hot-melt extrusion (HME) is presented.

    EXCIPIENT UPDATE - Soluplus®: An Understanding of Supersaturation From Amorphous Solid Dispersions

    Amorphous Solid Dispersions (ASDs) have been widely accepted as a desired solution for enhancing solubility and bioavailability of poorly soluble drugs. 1 With a trend in increased number of poorly soluble new chemical entities (NCEs), the industry is adapting non-conventional formulation technologies, exploiting the existing polymers, and exploring innovative ones to expedite drug development. 2 However, the applicability of those polymers in such technologies has also created new challenges associated with processing and manufacturing or thermal instability, such as hot melt extrusion and Kinetisol®, or residual solvents, such as spray drying and co-precipitation.

    Bioavailability Enhancement: A Soluplus® case study of itraconazole

    Soluplus®, a graft copolymer of PEG comprising polyvinyl acetate and polyvinyl caprolactam (see Figure 1A), was specially designed to solubilize poorly water-soluble drugs. To guarantee appropriate processability (e.g., in melt-extrusion applications), the composition of the polymer was adjusted to optimize its physical properties. With a low glass-transition temperature of around 70 °C, Soluplus® can be processed at low temperatures. Soluplus® shows good stability. Its formulations remain stable so that drugs, especially those that are formulated in an amorphous state, do not show recrystallization. In addition to these composition-related properties, the physical appearance of Soluplus® has  been optimized.

    The advantages and disadvantages of hot-melt extrusion in solid dispersion formulations

    Solid dispersions represent a promising formulation approach for overcoming today's major challenge in pharmaceutical formulation development: poorly soluble and poorly permeable active pharmaceutical ingredients (APIs). Solid dispersions can be obtained using different processes; however, hot-melt extrusion (HME) is extremely suitable for this purpose.

    Webinars & Podcasts

    Webinar

    Twin Screw Wet Granulation for Solubility Enhancement of Poorly Water-Soluble Drugs

    Poorly-soluble APIs present formulation and development challenges. Excipient selection and manufacturing process development are crucial.Continuous twin-screw granulation is gaining acceptance as a manufacturing technology to address issues presented by these APIs and offers high production capacity in a small footprint. This reviews a study of the use of Soluplus as binder and matrix to generate granules. Poorly soluble drugs were investigated for solubility enhancement and good performance was found; the produced granules show approximately 80% of the dissolution performance under non-sink conditions versus amorphous solid dispersions of same drug-polymer ratio. The produced granules show a better benefit-risk ratio than amorphous solid dispersions and can to be a very attractive alternative to melt-extruded solid dispersions.

    Podcast

    Twin Screw Wet Granulation for Solubility Enhancement of Poorly Water-Soluble Drugs

    Poorly-soluble APIs present formulation and development challenges. Excipient selection and manufacturing process development are crucial. Continuous twin-screw granulation is gaining acceptance as a manufacturing technology to address issues presented by these APIs and is offering high production capacity in a small footprint. In this dedicated dialogue, solubility enhancement expert Andreas Gryczke from BASF will answer additional questions that have been posed in our recent webinar on Twin Screw Wet Granulation for Solubility Enhancement of Poorly Water-Soluble Drugs.

    Whitepapers

    Choosing the Proper Dissolution Method when Testing Solubilization Performance of Poorly Soluble Drug Molecules

    With the increase in use of advanced formulation methods to improve solubility of drugs, standard dissolution methods are not always capable to reflect the full in-vivo potential. This whitepaper will take a close look at dissolution testing of solid dispersions made with polyvinyl caprolactam–polyvinyl acetate–polyethylene glycol graft copolymer (Soluplus®) and how to design an appropriate dissolution test that is discriminatory for APIs with different prerequisites.