Ethylcellulose in Organic Solution or Aqueous Dispersion Form in Designing Taste-Masked Microparticles by the Spray Drying Technique with a Model Bitter Drug: Rupatadine Fumarate

Wasilewska, Katarzyna; Szekalska, Marta; Ciosek-Skibińska, Patrycja; Lenik, Joanna; Basa, Anna; Jacyna, Julia; Markuszewski, Michał J.; Winnicka, Katarzyna

doi:10.3390/polym11030522

Cited by 18 publications

(25 citation statements)

References 18 publications

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“…To determine whether the designed particles effectively masked the bitter taste of rupatadine fumarate, three independent methods were used: a human taste panel, an in vitro release test conducted in conditions mimicking the oral cavity environment, and an electronic taste sensing system (electronic tongue). It was clearly confirmed that particles formulated from aqueous dispersions of EC provided a very effective taste-masking barrier [49]. Evaluation of the use of Surelease ® as a barrier membrane coating with pediatric precedence of use on the taste-masking of immediate-release acetaminophen granules was also conducted.…”

Section: Applicability Of Ec In Pharmaceutical Formulationsmentioning

confidence: 92%

Ethylcellulose–A Pharmaceutical Excipient with Multidirectional Application in Drug Dosage Forms Development

2019

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Polymers constitute the most important group of excipients utilized in modern pharmaceutical technology, playing an essential role in the development of drug dosage forms. Synthetic, semisynthetic, and natural polymeric materials offer opportunities to overcome different formulative challenges and to design novel dosage forms for controlled release or for site-specific drug delivery. They are extensively used to design therapeutic systems, modify drug release, or mask unpleasant drug taste. Cellulose derivatives are characterized by different physicochemical properties, such as swellability, viscosity, biodegradability, pH dependency, or mucoadhesion, which determine their use in industry. One cellulose derivative with widespread application is ethylcellulose. Ethylcellulose is used in pharmaceutical technology as a coating agent, flavoring fixative, binder, filler, film-former, drug carrier, or stabilizer. The aim of this article is to provide a broad overview of ethylcellulose utilization for pharmaceutical purposes, with particular emphasis on its multidirectional role in the development of oral and topical drug dosage forms.

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Section: Applicability Of Ec In Pharmaceutical Formulationsmentioning

confidence: 92%

Ethylcellulose–A Pharmaceutical Excipient with Multidirectional Application in Drug Dosage Forms Development

2019

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“…Much of the research work on RF is related to the analytical method development. Formulation research includes preparation of its immediate release tablets by QbD approach [12] and as a model drug for taste masking by employing ethyl cellulose [13]. Patents on liquid oral formulations of the drug have been published [14].…”

Section: Introductionmentioning

confidence: 99%

Formulation Development of Oral Fast-Dissolving Films of Rupatadine Fumarate

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2020

Asian J Pharm Clin Res

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Objective: Rupatadine fumarate (RF) is an anti-allergic drug indicated for the treatment of allergic rhinitis. It has low oral bioavailability due to its poor aqueous solubility and extensive hepatic first pass metabolism. In the present work, oral fast-dissolving films (OFDF) have been formulated and evaluated to facilitate dissolution in the oral cavity itself. Methods: Pullulan and HPMC (5, 15 cps) were employed as film formers and six formulations were tried. The physicochemical compatibility between drug and the polymers was studied by FTIR spectroscopy. RF-beta-cyclodextrin (BCD) inclusion complex was initially prepared and evaluated. The inclusion complex was incorporated into the film. OFDF were formulated and prepared by solvent casting method. The film size for one dose was 2 × 2 cm. The films were evaluated for various film parameters including disintegration time and drug release. Results: Preliminary film studies indicated % of film former solution to be between 3 and 5% for good appearance, mechanical strength, and quick disintegration. Solubility enhancement of RF is almost 40-fold from its BCD inclusion complex. Drug content in the films ranged between 83 and 90%. The pH ranged between 6 and 7 for all the formulations. All OFDF of RF disintegrated within one minute. With higher viscosity grade of HPMC, disintegration was comparatively slower and so was the drug release. Pullulan based films also showed desirable properties. F3 had disintegration time was 28 s and % drug release was 92% in 180 s. Conclusion: OFDF of RF could be formulated employing pullulan and HPMC low viscosity grades by solvent casting method. F3 containing HPMC E5 at 37% by weight of dry film showed desirable film properties. Stability studies indicated that there was no significant change in the films with respect to physicochemical properties and in vitro release.

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“…The surface morphology of the CPT microparticles was influenced by the amount of EC used, a hydrophobic polymer that is used for film coating or in polymeric matrices, in formulation. Batches manufactured with high EC content produced microparticles with smooth surfaces [55,56]. Conversely, batches produced with low EC content produced microparticles with rough, corrugated surfaces.…”

Section: Scanning Electron Microscopy (Sem)mentioning

confidence: 98%

Formulation and Characterisation of a Combination Captopril and Hydrochlorothiazide Microparticulate Dosage Form

2020

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Cardiovascular diseases such as hypertension and cardiac failure in South African children and adolescents are effectively managed long term, using a combination treatment of captopril and hydrochlorothiazide. The majority of commercially available pharmaceutical products are designed for adult patients and require extemporaneous manipulation, prior to administration to paediatric patients. There is a need to develop an age appropriate microparticulate dosing technology that is easy to swallow, dose and alter doses whilst overcoming the pharmacokinetic challenges of short half-life and biphasic pharmacokinetic disposition exhibited by hydrochlorothiazide and captopril. An emulsion solvent evaporation approach using different combinations of polymers was used to manufacture captopril and hydrochlorothiazide microparticles. Design of experiments was used to develop and analyse experimental data, and identifyoptimum formulation and process conditions for the preparation of the microparticles. Characterisation studies to establish encapsulation efficiency, in vitro release, shape, size and morphology of the microparticles were undertaken. The microparticles produced were in the micrometre size range, with an encapsulation efficiency >75% for both hydrochlorothiazide and captopril. The microparticulate technology is able to offer potential resolution to the half-life mediated dosing frequency of captopril as sustained release of the molecule was observed over a 12-h period. The release of hydrochlorothiazide of >80% suggests an improvement in solubility limited dissolution.

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Ethylcellulose in Organic Solution or Aqueous Dispersion Form in Designing Taste-Masked Microparticles by the Spray Drying Technique with a Model Bitter Drug: Rupatadine Fumarate

Cited by 18 publications

References 18 publications

Ethylcellulose–A Pharmaceutical Excipient with Multidirectional Application in Drug Dosage Forms Development

Ethylcellulose–A Pharmaceutical Excipient with Multidirectional Application in Drug Dosage Forms Development

Formulation Development of Oral Fast-Dissolving Films of Rupatadine Fumarate

Formulation and Characterisation of a Combination Captopril and Hydrochlorothiazide Microparticulate Dosage Form

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