The Effects of Screw Configuration and Polymeric Carriers on Hot-Melt Extruded Taste-Masked Formulations Incorporated into Orally Disintegrating Tablets

Morott, Joseph T.; Pimparade, Manjeet B.; Park, Jun-Bom; Worley, Chelsea P.; Majumdar, Soumyajit; Lian, Zhuoyang; Pinto, Elanor; Bi, Yunxia Vivian; Dürig, Thomas; Repka, Michael A.

doi:10.1002/jps.24262

Cited by 37 publications

(25 citation statements)

References 15 publications

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“…The all conveying element screw design preserved a considerable portion of the crystalline phase of the API, but there was still a noticeable presence of the amorphous form in the carrier. The shorter screw design with one mixing zone enhanced the preservation of the API crystalline nature (83). These and other similar studies, therefore, provide convincing evidence that the HME process can be successfully used as an alternative taste-masking technique for bitter APIs.…”

Section: Taste Maskingsupporting

confidence: 50%

Hot-Melt Extrusion: from Theory to Application in Pharmaceutical Formulation

2015

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Abstract. Hot-melt extrusion (HME) is a promising technology for the production of new chemical entities in the developmental pipeline and for improving products already on the market. In drug discovery and development, industry estimates that more than 50% of active pharmaceutical ingredients currently used belong to the biopharmaceutical classification system II (BCS class II), which are characterized as poorly water-soluble compounds and result in formulations with low bioavailability. Therefore, there is a critical need for the pharmaceutical industry to develop formulations that will enhance the solubility and ultimately the bioavailability of these compounds. HME technology also offers an opportunity to earn intellectual property, which is evident from an increasing number of patents and publications that have included it as a novel pharmaceutical formulation technology over the past decades. This review had a threefold objective. First, it sought to provide an overview of HME principles and present detailed engineered extrusion equipment designs. Second, it included a number of published reports on the application of HME techniques that covered the fields of solid dispersions, microencapsulation, taste masking, targeted drug delivery systems, sustained release, films, nanotechnology, floating drug delivery systems, implants, and continuous manufacturing using the wet granulation process. Lastly, this review discussed the importance of using the quality by design approach in drug development, evaluated the process analytical technology used in pharmaceutical HME monitoring and control, discussed techniques used in HME, and emphasized the potential for monitoring and controlling hot-melt technology.

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Section: Taste Maskingsupporting

confidence: 50%

Hot-Melt Extrusion: from Theory to Application in Pharmaceutical Formulation

2015

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“…TGA is very critical before performing HME because the drug and excipients are exposed to high temperature during the extrusion process, and there are possibilities of drug degradation or thermally-induced chemical reactions or both [16]. The TGA results (Figure 2) specified that API, polymer, and excipients were chemically stable in the HME processing temperature range.…”

Section: Resultsmentioning

confidence: 99%

“…Hot melt extrusion (HME) is a one-step, solvent-free continuous manufacturing process, which established itself in the pharmaceutical arena for the development of various solid oral formulations [16–25]. This technology involves the use of temperature and shear to process polymer blends and extrude them through a die of the desired design [26].…”

Section: Introductionmentioning

confidence: 99%

Development and evaluation of an oral fast disintegrating anti-allergic film using hot-melt extrusion technology

Pimparade

Maurya

et al. 2017

European Journal of Pharmaceutics and Biopharmaceutics

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The main objective of this novel study was to develop chlorpheniramine maleate orally disintegrating films (ODF) using hot-melt extrusion technology and evaluate the characteristics of the formulation using in vitro and in vivo methods. Modified starch with glycerol was used as a polymer matrix for melt extrusion. Sweetening and saliva-simulating agents were incorporated to improve palatability and lower the disintegration time of film formulations. A standard screw configuration was applied, and the last zone of the barrel was opened to discharge water vapors, which helped to manufacture non-sticky, clear, and uniform films. The film formulations demonstrated rapid disintegration times (6–11 s) and more than 95% dissolution in 5 min. In addition, the films had characteristic mechanical properties that were helpful in handling and storage. An animal model was employed to determine the taste masking of melt-extruded films. The lead film formulation was subjected to a human panel for evaluation of extent of taste masking and disintegration.

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“…Morott et al (2015) used HME to embed a bitter taste drug sildenafil citrate in ethyl cellulose along with calcium carbonate as a pH-dependent pore former. This study also found that taste-masking efficiency is affected by using different screw configurations which change the physical state of the API [15]. Pimparade et al (2015) have also demonstrated HME as an effective tool to mask the bitter taste of caffeine citrate.…”

Section: Introductionmentioning

confidence: 86%

Preparation and Evaluation of Hot-Melt Extruded Patient-Centric Ketoprofen Mini-Tablets

Alshetaili¹,

Almutairy²,

Tiwari³

et al. 2016

CDD

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Background Bitter tasting drugs represent a large portion of active pharmaceutical ingredients. Mini-tablets are specifically designed for patients with difficulty in swallowing particular in young children up to 10 years of age, geriatric patients and patients with esophagitis. Objective The present study was aimed to prepare, taste-masked mini-tablets, which are easily swallowed dosage forms, primarily to be used by pediatric and geriatric patients. Methods Ketoprofen (10%–50% w/w) and Eudragit® EPO were blended and extruded with a 5-mm strand die and cut into consistent mini-tablets by using an adapted downstream pelletizer. Results Differential scanning calorimetry and polarized light microscopy-hot stage microscopy studies confirmed that the binary mixtures were miscible under the employed extrusion temperatures. In-vitro release studies showed that drug release was less than 0.5% within the first 2 min in simulated salivary fluid (pH 6.8) and more than 90% in the first 20 min in gastric media (pH 1.0). The results of the electronic tongue analysis were well correlated with the drug release profile of the mini-tablets in the artificial saliva. Scanning electron microscopy revealed no cracks on the surface of the mini-tablets, confirming that the mini-tablets were compact solids. Chemical imaging confirmed the uniform distribution of ketoprofen inside the polymer matrices. Conclusion Eudragit® EPO containing ketoprofen at various drug loads were successfully melt extruded into tasted-masked mini-tablets. The reduced drug release at salivary pH correlated well with Astree e-Tongue studies for taste masking efficiency.

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The Effects of Screw Configuration and Polymeric Carriers on Hot-Melt Extruded Taste-Masked Formulations Incorporated into Orally Disintegrating Tablets

Cited by 37 publications

References 15 publications

Hot-Melt Extrusion: from Theory to Application in Pharmaceutical Formulation

Hot-Melt Extrusion: from Theory to Application in Pharmaceutical Formulation

Development and evaluation of an oral fast disintegrating anti-allergic film using hot-melt extrusion technology

Preparation and Evaluation of Hot-Melt Extruded Patient-Centric Ketoprofen Mini-Tablets

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