Development of taste masked caffeine citrate formulations utilizing hot melt extrusion technology and in vitro–in vivo evaluations

Pimparade, Manjeet B.; Morott, Joseph T.; Park, Jun-Bom; Kulkarni, Vijay; Majumdar, Soumyajit; Murthy, S. Narasimha; Lian, Zhuoyang; Pinto, Elanor; Bi, Vivian; Dürig, Thomas; Murthy, Reena; Shivakumar, H.N.; Vanaja, K.; Kumar, Pradeep; Repka, Michael A.

doi:10.1016/j.ijpharm.2015.04.030

Cited by 53 publications

(25 citation statements)

References 31 publications

(35 reference statements)

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“…This study is also in accordance with the Code of Ethics of the World Medical Association (Declaration of Helsinki). The experimental procedure for this study was as per our previously published work [10, 32]. …”

Section: Methodsmentioning

confidence: 99%

“…Commercially available orodispersible tablets (ODT) and orally disintegrating films or orodispersible films (ODF) are the most successful platforms for pharmaceutical product development. ODTs are solid oral dosage forms that disintegrate rapidly, typically within 30 s, with or without the administration of additional water [10]. They provided great comfort to patients with swallowing difficulties [11].…”

Section: Introductionmentioning

confidence: 99%

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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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Section: Methodsmentioning

confidence: 99%

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 extruded is cut or pulverized and subsequently compressed. This technology produces tablets of high aqueous solubility and good mechanical resistance (29,30).…”

Section: Sublimationmentioning

confidence: 99%

The Popularization of Orodispersible Tablets in the Pharmaceutical Market

Pinho

Temer

Ribeiro

et al. 2018

Infarma

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Orodispersible tablets are getting popular due to its easy administration which leads to a higher therapeutic adherence. This study aimed to evaluate the state of the art of these drug products based on the scientific literature. Also, orodispersible tablets available in the US, Europe and Brazil markets based on information extracted from the health agencies were analyzed. Those tablets are designed to be placed on the tongue and instantly disintegrated by the fast capitation of the saliva without the additional intake of water. The orodispersible technology enables oral administration of tablets to patients with dysphagia, especially children, and elderlies. Moreover, orodispersible make possible rapid drug intervention and mouth absorption. The drug is partially absorbed in the oral cavity, pharynx, and esophagus without first pass effect, increasing drug bioavailability and reaching faster therapeutic effect. This is a low-cost technology that fits in a conventional solid production area and adds value to the product without requiring high investment. A market analysis showed there is a predominance of antihistamine drugs or medicines for mental disorders using orodispersible matrices. However, the orodispersible technology shows great versatility and potential application to other pharmacological groups. It is expected that in coming years a massive commercial insertion of this tablet technology occurs. In this scenery, it is indispensable that health professionals are prepared with updated technical information for the use of this therapeutic resource safely and efficiently. RESUMOOs comprimidos orodispersíveis têm ganhado popularidade por serem de fácil administração e levarem a uma maior adesão terapêutica. Esse estudo teve como objetivo avaliar o estado da arte desses medicamentos com base na literatura científica. Adicionalmente, foram levantados os comprimidos orodispersíveis disponíveis nos mercados dos EUA, Europa e Brasil com base em informações extraídas das agências sanitárias dessas regiões. Esses comprimidos são concebidos para serem colocados na boca e instantaneamente desintegrados pela captação da saliva, sem a necessidade de água. A tecnologia orodispersível viabiliza a administração oral de comprimidos em usuários com disfagia. Adicionalmente, esses medicamentos possibilitam uma rápida intervenção medicamentosa e absorção bucal, fazendo com que uma fração do fármaco seja absorvido na cavidade oral, faringe e esôfago sem sofrer efeito de primeira passagem, incrementando sua biodispobibilidade e permitindo alcançar um efeito terapêutico mais rápido. O barateamento dessa tecnologia, que se adapta a áreas de produção de sólidos convencionais, agrega valor ao medicamento sem demandar alto investimento.

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“…The drug was embedded in ethyl cellulose matrix along with different pore formers such as calcium phosphate and magnesium oxide to enhance drug release. The crystallinity of the API was preserved by modifying the screw configuration [16]. Alshehri et al (2015) and Singh et al (2013) have also used a pH-dependent polymer Eudragit ® E PO to mask the bitter taste of mefenamic acid and efavirenz, respectively [17, 18].…”

Section: Introductionmentioning

confidence: 99%

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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Development of taste masked caffeine citrate formulations utilizing hot melt extrusion technology and in vitro–in vivo evaluations

Cited by 53 publications

References 31 publications

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

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

The Popularization of Orodispersible Tablets in the Pharmaceutical Market

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

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