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The present disclosure is directed to compositions and methods for making a pharmaceutical composition by thermokinetic compounding, wherein the compositions include one or more thermolabile components, for example one or more active pharmaceutical ingredients (API) with one or more pharmaceutically acceptable excipients. The methods comprise thermokinetic processing of the thermolabile components into a composite by blending certain thermolabile components in a thermokinetic mixer using multiple speeds during a single, rotationally continuous operation. The composite can be further processed into pharmaceutical compositions by conventional methods known in the art, such as hot melt extrusion, melt granulation, compression molding, tablet compression, capsule filling, film-coating, or injection molding.


Patent
Dispersol Technologies | Date: 2016-06-17

The disclosure provides for improved pharmaceutical compositions containing deferasirox (DFX) and methods of manufacturing the same. In particular, the compositions are prepared using thermokinetic compounding and provide improved properties as well as more efficient methods of manufacture.


Brough C.,University of Texas at Austin | Brough C.,Dispersol Technologies | Williams III R.O.,University of Texas at Austin
International Journal of Pharmaceutics | Year: 2013

Poor water-solubility is a common characteristic of drug candidates in pharmaceutical development pipelines today. Various processes have been developed to increase the solubility, dissolution rate and bioavailability of these active ingredients belonging to BCS II and IV classifications. Over the last decade, nano-crystal delivery forms and amorphous solid dispersions have become well established in commercially available products and industry literature. This article is a comparative analysis of these two methodologies primarily for orally delivered medicaments. The thermodynamic and kinetic theories relative to these technologies are presented along with marketed product evaluations and a survey of commercial relevant scientific literature. © 2013 Elsevier B.V. All rights reserved.


Hughey J.R.,University of Texas at Austin | Keen J.M.,University of Texas at Austin | Miller D.A.,Dispersol Technologies | Kolter K.,BASF | And 2 more authors.
European Journal of Pharmaceutical Sciences | Year: 2013

The dissolution enhancement advantages inherent to amorphous solid dispersions systems are often not fully realized once they are formulated into a solid dosage form. The objective of this study was to investigate the ability of inorganic salts to improve the dissolution rate of carbamazepine (CBZ) from tablets containing a high loading of a Soluplus®-based solid dispersion. Cloud point and viscometric studies were conducted on Soluplus® solutions to understand the effect of temperature, salt type and salt concentration on the aqueous solubility and gelling tendencies of Soluplus®, properties that can significantly impact dissolution performance. Studies indicated that Soluplus® exhibited a cloud point that was strongly dependent on the salt type and salt concentration present in the dissolving medium. The presence of kosmotropic salts dehydrated the polymer, effectively lowering the cloud point and facilitating formation of a thermoreversible hydrogel. The ability of ions to impact the cloud point and gel strength generally followed the rank order of the Hofmeister series. Solid dispersions of CBZ and Soluplus® were prepared by KinetiSol® Dispersing, characterized to confirm an amorphous composition was formed and incorporated into tablets at very high levels (70% w/w). Dissolution studies demonstrated the utility of including salts in tablets to improve dissolution properties. Tablets that did not contain a salt or those that included a chaotropic salt hydrated at the tablet surface and did not allow for sufficient moisture ingress into the tablet. Conversely, the inclusion of kosmotropic salts allowed for rapid hydration of the entire tablet and the formation of a gel structure with strength dependent on the type of salt utilized. Studies also showed that, in addition to allowing tablet hydration, potassium bicarbonate and potassium carbonate provided effervescence which effectively destroyed the gel network and allowed for rapid dissolution of CBZ. Subsequent dissolution studies in 0.1 N HCl showed that potassium bicarbonate was an effective tablet disintegrant at levels as low as 1% and provided for tablets that rapidly disintegrated over a wide range of applied compression forces, presumably due to synergy between the ability to form a weak hydrogel structure and carbon dioxide liberation. Similar dissolution performance was measured in pH 4.5 acetate buffer, despite reduced polymer solubility caused by kosmotropic salts in solution, demonstrating robustness. With the use of inorganic salts such as potassium bicarbonate, it may be possible to substantially improve disintegration and dissolution characteristics of tablets containing Soluplus®. © 2013 Elsevier B.V. All rights reserved.


Hughey J.R.,University of Texas at Austin | Keen J.M.,University of Texas at Austin | Brough C.,Dispersol Technologies | Saeger S.,Free University of Berlin | McGinity J.W.,University of Texas at Austin
International Journal of Pharmaceutics | Year: 2011

Poorly water-soluble drug substances that exhibit high melting points are often difficult to successfully process by fusion-based techniques. The purpose of this study was to identify a suitable polymer system for meloxicam (MLX), a high melting point class II BCS compound, and investigate thermal processing techniques for the preparation of chemically stable single phase solid dispersions. Thermal and solution based screening techniques were utilized to screen hydrophilic polymers suitable for immediate release formulations. Results of the screening studies demonstrated that Soluplus ®(SOL) provided the highest degree of miscibility and solubility enhancement. A hot-melt extrusion feasibility study demonstrated that high temperatures and extended residence times were required in order to render compositions amorphous, causing significant degradation of MLX. A design of experiments (DOE) was conducted on the KinetiSol ® Dispersing (KSD) process to evaluate the effect of processing conditions on the chemical stability and amorphous character of MLX. The study demonstrated that ejection temperature significantly impacted MLX stability. All samples prepared by KSD were substantially amorphous. Dissolution analysis of the KSD processed solid dispersions showed increased dissolution rates and extent of supersaturation over the marketed generic MLX tablets. © 2011 Elsevier B.V. All rights reserved.


Patent
Dispersol Technologies and The University Of Texas System | Date: 2012-02-23

The present disclosure is directed to compositions and methods for formulating a pharmaceutical dosage form by forming a composition comprising acetyl-11-keto--boswellic acid, diindolylmethane, or curcumin with one or more pharmaceutically acceptable excipients for enhanced solubility to increase bioavailability and improve therapeutic efficacy. The composition can be processed by thermo-kinetic compounding along with conventional methods known in the art, such as hot melt extrusion, melt granulation, compression molding, tablet compression, capsule filling, film-coating, or injection molding.


Patent
The University Of Texas System and Dispersol Technologies | Date: 2016-05-13

Compositions and methods for making a pharmaceutical dosage form include making a pharmaceutical composition that includes one or more active pharmaceutical ingredients (API) with one or more pharmaceutically acceptable excipients by thermokinetic compounding into a composite. Compositions and methods of preprocessing a composite comprising one or more APIs with one or more excipients include thermokinetic compounding, comprising thermokinetic processing the APIs with the excipients into a composite, wherein the composite can be further processed by conventional methods known in the art, such as hot melt extrusion, melt granulation, compression molding, tablet compression, capsule filling, film-coating, or injection molding.


DiNunzio J.C.,University of Texas at Austin | Brough C.,Dispersol Technologies | Miller D.A.,University of Texas at Austin | Williams R.O.,University of Texas at Austin | McGinity J.W.,University of Texas at Austin
European Journal of Pharmaceutical Sciences | Year: 2010

Thermal manufacturing methods for the production of solid dispersions frequently require the addition of a plasticizer in order to achieve requisite molten material flow properties when processed by unit operations such as hot melt extrusion. KinetiSol® Dispersing, a rapid high energy thermal manufacturing process, was investigated for the ability to produce amorphous solid dispersions without the aid of a plasticizer. For this study itraconazole was used as a model active ingredient, while Eudragit® L100-55 and Carbomer 974P were used as model solid dispersion carriers. Triethyl citrate (TEC) was used as necessary as a model plasticizer. Compositions prepared by KinetiSol® Dispersing and hot melt extrusion were evaluated for solid state properties, supersaturated in vitro dissolution behavior under pH change conditions and accelerated stability performance. Results showed that both manufacturing processes were capable of producing amorphous solid dispersions, however compositions produced by hot melt extrusion required the presence of TEC and yielded a glass transition temperature (Tg) of approximately 54°C. Plasticized and unplasticized compositions were successfully produced by KinetiSol® Dispersing, with plasticizer free solid dispersions exhibiting a Tg of approximately 101°C. Supersaturated in vitro dissolution testing revealed a significantly higher dissolution rate of plasticized material which was attributed to the pore forming behavior of TEC during the acidic phase of testing. A further contribution to release may also have been provided by the greater diffusivity in the plasticized polymer. X-ray diffraction testing revealed that under accelerated stability conditions, plasticized compositions exhibited partial recrystallization, while plasticizer free materials remained amorphous throughout the 6-month testing period. These results demonstrated that KinetiSol® Dispersing could be used for the production of amorphous solid dispersions without the aid of a plasticizer and illustrated the enhanced solid state stability that can be achieved by producing solid dispersions with higher glass transition temperatures. © 2010 Elsevier B.V.


DiNunzio J.C.,University of Texas at Austin | Brough C.,Dispersol Technologies | Hughey J.R.,University of Texas at Austin | Miller D.A.,University of Texas at Austin | And 2 more authors.
European Journal of Pharmaceutics and Biopharmaceutics | Year: 2010

Many techniques for the production of solid dispersions rely on elevated temperatures and prolonged material residence times, which can result in decomposition of temperature-sensitive components. In this study, hydrocortisone was used as a model temperature-sensitive active ingredient to study the effect of formulation and processing techniques as well as to characterize the benefits of KinetiSol® Dispersing for the production of solid dispersions. Preformulation studies were conducted using differential scanning calorimetry and hot stage microscopy to identify optimum carriers for the production of amorphous solid dispersions. After identification, solid dispersions were prepared by hot melt extrusion and KinetiSol® Dispersing, with material characterized by X-ray diffraction, dissolution and potency testing to evaluate physicochemical properties. Results from the preformulation studies showed that vinylacetate:vinylpyrrolidone (PVPVA) copolymer allowed for hydrocortisone dissolution within the carrier at temperatures as low as 160 °C, while hydroxypropyl methylcellulose required temperatures upward of 180 °C to facilitate solubilization. Low substituted hydroxypropyl cellulose, a high glass transition temperature control, showed that the material was unable to solubilize hydrocortisone. Manufacturing process control studies using hot melt extruded compositions of hydrocortisone and PVPVA showed that increased temperatures and residence times negatively impacted product potency due to decomposition. Using KinetiSol® Dispersing to reduce residence time and to facilitate lower temperature processing, it was possible to produce solid dispersions with improved product potency. This study clearly demonstrated the importance of carrier selection to facilitate lower temperature processing, as well as the effect of residence time on product potency. Furthermore, KinetiSol® Dispersing provided significant advantages over hot melt extrusion due to the reduced residence times and lower required processing temperatures. This allowed for the production of solid dispersions with enhanced product potency. © 2009 Elsevier B.V. All rights reserved.


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