Ashland Inc. to present research on key challenges in pharmaceutical formulation development

WILMINGTON, Del. – Ashland Specialty Ingredients, a commercial unit of Ashland Inc. (NYSE: ASH), today announced that it will present new research on excipients and tablet coatings at the American Association of Pharmaceutical Scientists Annual Meeting and Exposition (AAPS) in Washington, DC, Oct. 23-27. The research, which includes solutions for enhancing drug solubility, formulating controlled-release systems, improving tablet properties and reducing costs, is based on recent studies conducted by Ashland researchers.

Ashland Specialty Ingredients was formed in August when Ashland completed its acquisition of International Specialty Products (ISP) Inc. and combined it with its Functional Ingredients business. Together, Ashland scientists focus on advancing active pharmaceutical ingredient (API) delivery, protection and solubility through a dynamic excipient portfolio.

As a result of high-throughput screening and rational drug design, formulators today are identifying a larger number of drug candidates with poor solubility during the discovery process. Reportedly as many as 60 percent of drugs in development have issues related to poor solubility. Ashland scientists will publish results of studies on emerging solid-dispersion technology, using spray drying and hot-melt extrusion to improve solubility, bioavailability and stability of poorly soluble drugs using Klucel™ (HPC), Plasdone™ povidone and Plasdone copovidone.

In one study, Ashland scientists were able to reduce the dosing regimen of an API from sixteen capsules to one tablet in a clinical trial using screening techniques to quickly select the optimum polymer and polymer level for stable, amorphous solid dispersions with the largest dissolution enhancement. This is one example of how Ashland’s products and knowledge help bring new products to market, and reduce development times and product costs.

As hot-melt extrusion is gaining popularity for solubilization of insoluble drugs, twin-screw extrusion is also gaining attention as a continuous alternative to traditional high-shear granulation. This continuous process enables faster throughput and easier scale-up, which translates to cost savings. Ashland will present results on how Klucel HPC, Plasdone povidone, and Benecel™ hypromellose (HPMC) perform in continuous low-temperature extrusion granulation as compared to traditional wet granulation. The results show twin-screw extrusion as a promising cost saving method for high-dose formulations and highlight how tablets made via extrusion showed improved strength and low friability compared to traditional wet granulation.

Ashland scientists will be present during the technical posters sessions as well as at Booths 519 and 1229 to answer questions pertaining to the 20 contributed papers:

Monday – Oct. 24, (1 – 5 p.m.)
Poster M1070 - An examination of the use of high-solids film-coating systems as a means of reducing the costs of aqueous coating processes
Poster M1074 - The application of an aqueous high-solids coatings system at low bed temperatures
Poster M1107 - Effect of spray-drying process parameters on solid dispersion powder properties
Poster M1108 - Effect of solution and polymer properties on solid dispersion powder properties
Poster M1109 - Effect of scale-up from laboratory to clinical-scale spray dryer on solid dispersion powder properties
Poster M1384 - Effect of super-disintegrants on compactability/ bondability of tablet fillers

Tuesday – Oct. 25, (1 – 5 p.m.)
Poster T3277 - Tablets manufactured via HME as a processing technique for solubility enhancement: stability assessment and in vitro release comparison to a marketed formulation
Poster T3285 - Use of a compaction simulator to compare the compaction behavior of dry binders in model pharmaceutical formulations
Poster T3282 - The effect of moisturebarrier film coating and packaging selection on moisture-sensitive multivitamin tablets

Wednesday – Oct. 26
Poster W4226 (8 a.m. – noon)  – Taste masking performance of two grades of Hydroxypropylcellulose melt extruded pellets
Poster W4237 (8 a.m. – noon) – Preparation and characterization of solid dispersion tablets of Efavirenz with Benecel™ E5 PH
Poster W4350 (8 a.m. – noon) - Polymer selection and optimization in development of a spray-dried dispersion with enhanced bioavailability
Poster W4238 (8 a.m. – noon) – Characterization of hot-melt extruded immediate-release solid dosage forms with cellulose either polymers for a poorly soluble drug
Poster W4248 (8 a.m. – noon) - Continuous twin-screw extrusion granulation using HPC as a binder
Poster W5172  (1 – 5 p.m.) - Erosion and dissolution performance of intermediate molecular weight HPMC controlled-release polymers
Poster W5227 (1 – 5 p.m.) - In vitro evaluation of Hydroxypropylcellulose immediate-release tablets produced by melt extrusion technology
Poster W5259 (1 – 5 p.m.) - Process development and analysis of hot-melt extrudates with enhanced solubility

Thursday – Oct. 27, (8 a.m. – noon)
Poster R6168 - Characterization of hot-melt extruded immediate-release solid dosage forms with cellulose ether polymers for a poorly soluble drug
Poster R6279 - Ethylcellulose and Hydroxypropylcellulose as rate-controlling polymers for hot-melt extrusion of highly soluble drugs

For more information about the papers Ashland has contributed to AAPS, contact Ann Druffner in Wayne, N.J. Telephone: (973) 628-4103.

Delivering pharmaceutical and nutraceutical performance since the 1950s, Ashland creates value for its customers through applications knowledge, regulatory support and a powerful product portfolio:
Aquarius™ and Advantia™ coating systems
Aqualon™ ethylcellulose
Aqualon™ and Blanose™ sodium carboxymethylcellulose
Benecel™ methylcellulose and hypromellose
Klucel™ hydroxypropylcellulose
Natrosol™ hydroxyethylcellulose
Plasdone™ povidone
Plasdone™ copovidone
Polyplasdone™ crospovidone

Ashland Specialty Ingredients offers industry-leading products, technologies and resources for solving formulation and product performance challenges in key markets including personal care, pharmaceutical, food and beverage, coatings and energy. Using natural, synthetic and semi-synthetic polymers derived from plant and seed extract, cellulose ethers and vinyl pyrrolidones, Ashland Specialty Ingredients offers comprehensive and innovative solutions for today's demanding consumer and industrial applications.

In more than 100 countries, the people of Ashland Inc. (NYSE: ASH) provide the specialty chemicals, technologies and insights to help customers create new and improved products for today and sustainable solutions for tomorrow. Our chemistry is at work every day in a wide variety of markets and applications, including architectural coatings, automotive, construction, energy, food and beverage, personal care, pharmaceutical, tissue and towel, and water treatment. Visit www.ashland.com to see the innovations we offer through our four commercial units – Ashland Specialty Ingredients, Ashland Water Technologies, Ashland Performance Materials and Ashland Consumer Markets (Valvoline).

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