Development and Evaluation of Cocoa Butter Taste Masked Ibuprofen Using Supercritical Carbon Dioxide

Obaidat, Rana; Aleih, Haneen; Mashaqbeh, Hadeia; Al-Taani, Bashar; Alsmadi, Mo'tasem M; Alnaief, Mohammad

doi:10.1208/s12249-021-01962-7

Cited by 12 publications

(6 citation statements)

References 47 publications

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“…It is valid to assess taste early on during development. Many taste-masking strategies are available, among others emulsification/solvent evaporation, centrifugal extrusion, coacervation, spray drying or supercritical carbon dioxide (scCO2) assisted technique, which main advantage lies in the possibility of achieving a high separation of the supercritical solvent and the processed products, involved drug particle size reduction or the modification of some of the physicochemical and structural properties, especially of poorly water-soluble drugs [ 47 , 48 , 49 , 50 ]. While utilising the spray drying technique, the bitter drug is dissolved or dispersed along with the polymer in a suitable solvent and then subjected to spray drying.…”

Section: Resultsmentioning

confidence: 99%

Orodispersible Films with Rupatadine Fumarate Enclosed in Ethylcellulose Microparticles as Drug Delivery Platform with Taste-Masking Effect

et al. 2022

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Orally disintegrating (orodispersible) films provide a versatile tool for drug administration, especially in the pediatric and geriatric population, since they reduce the risk of choking and do not necessitate drinking water during application. By considering their direct contact with the taste buds, palatability is an influential aspect related to patient compliance. The microparticles based on taste-masking polymers containing drugs enclosed inside effectively mask the unpleasant taste of medicines. Ethylcellulose is a hydrophobic polymer widely used as a taste-masking material. Rupatadine fumarate, a second-generation antihistamine drug, is characterised by an intense bitter taste; therefore, it is crucial to achieve a tolerable taste whilst developing orodispersible formulations with its content. The objective of this study was to develop orally disintegrating films with rupatadine fumarate in the form of ethylcellulose-based microparticles obtained from aqueous dispersions of ethylcellulose—Surelease® or Aquacoat® ECD. It was a technological challenge to achieve homogenous drug content per dosage unit and sufficient mechanical properties for film operating due to the necessity to suspend the microparticles in the casting solution. Although the process of obtaining films consisted of several steps (mixing, pouring, drying), the particles were homogeneously dispersed, and each film of the desired size contained the proper dose of the drug. The taste-masking effect was also maintained. This parameter was confirmed by three independent methods: in vivo by healthy volunteers, an electronic tongue and a dissolution test. The applied taste-evaluation techniques showed that the films containing Aquacoat® ECD microparticles have the highest degree of bitter taste reduction, which confirms the results obtained in our previous studies.

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Section: Resultsmentioning

confidence: 99%

Orodispersible Films with Rupatadine Fumarate Enclosed in Ethylcellulose Microparticles as Drug Delivery Platform with Taste-Masking Effect

et al. 2022

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“…ScCO2-assisted processes can produce micro/nanoparticles with a narrow size distribution, high purity, controlled morphology, and crystal polymorphism control. Moreover, these techniques can be used for processing thermolabile molecules, can be performed in a single step, and can have an easy downstream operation (18,22,49). Numerous scCO2 techniques have been developed for the production of drug particles as variations of RESS, SAS, and PGSS processes.…”

Section: Methods For Micro and Nano-particles Productionmentioning

confidence: 99%

“…In the field of polymeric processing, scCO2 can act as a plasticizer of semicrystalline and amorphous polymers and induce polymer foaming (16). ScCO2 technologies on a lab-scale in the pharmaceutical field are usually used for the processing of poorly water-soluble drugs to improve their properties (14,17) or for masking the unpleasant taste of drugs (18). Several scCO2-assisted processes were developed on an industrial scale for food and cosmetic applications.…”

Section: The Versatility Of Supercritical Carbon Dioxidementioning

confidence: 99%

An overview on the application of supercritical carbon dioxide for the processing of pharmaceuticals

Milovanović¹,

Lukić²

2022

Arhiv za farmaciju

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Supercritical carbon dioxide (scCO2) application in the pharmaceutical industry is still undeveloped regardless of significant research interests in this processing medium shown in the last decades. ScCO2 technologies can improve drug solubility, bioavailability, and therapeutic effect. These technologies can lead to the development of new formulations that will contribute to a decrease in drug dose, medication frequency, and increase patients' well-being. Considering the significant decrease in the price of high-pressure equipment and society's growing need for cleaner production and safer products, it is expected that symbiosis between supercritical fluid and pharmaceutical technologies will happen soon. Therefore, this review was focused on the latest contributions of scCO2 technologies to the pharmaceutical field. The main aim was to bring these technologies closer to pharmaceutical specialists. For this purpose, the most commonly used technologies were explained and discussed: the preparation of solid dispersions, polymer impregnation with drugs, and drug micro/nanoparticle production using scCO2.

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“…There are also some cases where distilled water (sometimes with a surfactant) was used instead (68,93,95). Sometimes simulated salivary fluid (SSF) is used to closely mimic conditions in the oral cavity, but the composition is not the same in every study (55,65,73,99). Regarding the volume of the dissolution medium, it would probably be most appropriate to use the approximate volume of residual saliva in the oral cavity, which is 1-2 mL (88).…”

Section: Evaluation Of Taste Maskingmentioning

confidence: 99%

“…From the research reviewed in this section, it can be seen that the simultaneous implementation of techniques to improve the dissolution of poorly water-soluble drugs and to conceal their taste is rare. In fact, only 3 studies (55,94,99) used techniques such as preparation of solid dispersions and/or amorphization to improve dissolution and also showed that it is improved compared to pure API. There is some research (63,65,73) that compared their formulation to the marketed product and showed either equivalent or improved drug release properties, which is also a relevant comparison since it at least ensures that drug release is sufficient to achieve the therapeutic effect.…”

Section: Taste Masking Of Poorly Water-soluble Drugs In Multiparticul...mentioning

confidence: 99%

Taste-masking methods in multiparticulate dosage forms with a focus on poorly soluble drugs

Simšič,

Planinšek,

Baumgartner

2024

Acta Pharmaceutica

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In the past, the administration of medicines for children mainly involved changes to adult dosage forms, such as crushing tablets or opening capsules. However, these methods often led to inconsistent dosing, resulting in under- or overdosing. To address this problem and promote adherence, numerous initiatives, and regulatory frameworks have been developed to develop more child-friendly dosage forms. In recent years, multiparticulate dosage forms such as mini-tablets, pellets, and granules have gained popularity. However, a major challenge that persists is effectively masking the bitter taste of drugs in such formulations. This review therefore provides a brief overview of the current state of the art in taste masking techniques, with a particular focus on taste masking by film coating. Methods for evaluating the effectiveness of taste masking are also discussed and commented on. Another important issue that arises frequently in this area is achieving sufficient dissolution of poorly water-soluble drugs. Since the simultaneous combination of sufficient dissolution and taste masking is particularly challenging, the second objective of this review is to provide a critical summary of studies dealing with multiparticulate formulations that are tackling both of these issues.

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Development and Evaluation of Cocoa Butter Taste Masked Ibuprofen Using Supercritical Carbon Dioxide

Cited by 12 publications

References 47 publications

Orodispersible Films with Rupatadine Fumarate Enclosed in Ethylcellulose Microparticles as Drug Delivery Platform with Taste-Masking Effect

Orodispersible Films with Rupatadine Fumarate Enclosed in Ethylcellulose Microparticles as Drug Delivery Platform with Taste-Masking Effect

An overview on the application of supercritical carbon dioxide for the processing of pharmaceuticals

Taste-masking methods in multiparticulate dosage forms with a focus on poorly soluble drugs

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