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    Effective solubilization in solid & liquid dosage forms.

    Excipients for Drug Formulation Solubilization Platform


    Solubilization of poorly soluble active ingredients

    Effective solubilization in solid & liquid dosage forms. The right path for greater solubility and bioavailability.

    Poorly soluble drugs are one of the major challenges pharmaceutical manufacturers are facing. More and more drugs in development exhibit low solubility. At BASF, we offer a comprehensive range of cutting-edge solubilization polymers, and have an unparalleled understanding of the corresponding process technologies. This unique combination means that we can make sure you achieve effective solubilization across a range of dosage forms – particularly in solid dispersions. Furthermore, BASF is a highly successful pioneer in the application of hot-melt extrusion technology in pharmaceutical production, which helps you combine effectiveness with cost efficiency.

    Selecting the right solubilization product and technology for a poorly soluble API often involves a lot of trial and error. But partnering with our experts, you can tap into their extensive solubilization expertise and experience with all key technologies, such as hot-melt extrusion, spray drying, and drug layering. Our experts have access to industry-leading tools such as our high-throughput screening (HTS) robot. This puts them in an excellent position to help customers tackle their solubilization and bioavailability challenges rapidly and efficiently.

    BASF delivers answers to even the toughest solubilization challenges
    Comprehensive functional portfolio for solubiliation in solid & liquid dosage forms
    Innovative excipients for poorly soluble APIs
    Proven performance and safety
    Technology leader for key technologies such as hot-melt extrusion
    High throughput screening service Solu-HTS

    Choose Your Drug Delivery System

    Solid dispersions – a great way to increase the solubility and bioavailability of your drug

    Liquid dispersions, solutions, emulsions & micro emulsions

    Application Guides

    Application Guide

    Solubility Enhancement with BASF Pharma Polymers - Solubilizer Compendium

    This book is intended for pharmaceutical technologists in industry and at universities who wish to formulate poorly water-soluble drugs or generally interested in solubility enhancement.

    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.

    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.

    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.

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    Challenges and Opportunities in Oral Formulation Development

    Over 60% of new chemical entities that are poorly soluble qualify either as BCS Class II or Class IV and they provide challenges as well as opportunities to scientists working in formulation development [1]. The conventional solubilization approaches such as physical modifications of drug crystals (surface alteration of API, micronization or micro-milling) usually lead to a limited dissolution and solubility enhancement, but when developing a medium or high dosed formulation, the non-conventional formulation approaches are often required particularly when dealing with almost water-insoluble compounds usually characterized by a high melting point and/or very high lipophilicity.

    Podcasts

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

    Date: Sep 09, 2015 - 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.

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

    Date: Oct 26, 2015 - 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.

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    Webinars / Whitepaper

    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.

    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.

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    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.

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    Product Overview

    Focusing on your needs with platform solutions

    This brochure presents an overview of our leading-edge products, grouped in the following platforms: Solubilization, Instant and Modified Release, Skin Delivery, Softgels.

    Solu-HTS – High throughput screening for rapid solubilizer identification

    Identifying the right solubilization method for a poorly soluble API can be a time-consuming and expensive process. This is where Solu-HTS, our industry-leading high-throughput screening robot, comes in. Based on the principles of automation, miniaturization and parallelization, the HTS robot can efficiently screen a variety of parameters, accelerating research processes. It helps customers rapidly and reliably identify the most suitable solubilizer or combination of solubilizers for their needs – making costly “trial and error” approaches a thing of the past. What’s more, it can be used to examine structure-property relationships.

    Solu-HTS robot scheme

    Solu-HTS can help you:

    • Screen a greater number of solubilizers
    • Achieve a higher level of automation
    • Reduce screening time
    • Improve reproducibility
    • Cut costs
    • Produce accurate documentation
    • Reduce development time, supporting your success

    Comparison of test methods: Manual vs. Solu-HTS