In vitro and in vivo investigation of taste-masking effectiveness of Eudragit E PO as drug particle coating agent in orally disintegrating tablets

Objective: The aim of the present research work was to prepare and evaluate taste-masked oral disintegrating tablets (ODT) of Fexofenadine hydrochloride. Methods: In the present work, Eudragit EPO, a taste masking agent and Karaya gum (GK) (natural), Sodium starch glycolate, and Croscarmellose sodium (CCS) (semi-synthetic) super disintegrants in three ratios (3, 6,9%) were used. Taste masked granules were prepared by different ratios of the drug: Eudragit EPO (1:1, 1:1.5, 1:2) by wet granulation method. The optimized taste-masked granules (1:2) were selected by sensory evaluation test to prepare 9 Fexofenadine ODT (FH1-FH9) formulations. These were evaluated for different parameters. Then desirability function (DF) was calculated for all formulations using disintegration time (DT), time taken for the tablet to release 90% of the drug (t 90%), and % drug dissolved in 10 min (Q10) as significant parameters. Results: The best formulation (FH6) showed the highest DF value due to less DT and 100% in vitro drug release within 15 min. Thus, FH6 formulation containing 9% CCS was selected as the best among the prepared formulations to which in vivo studies were performed on rabbits to find maximum plasma concentration (Cmax), time taken to reach maximum concentration (tmax), area under the curve (AUC), rate of elimination (Kel), absorption rate (Ka) and half-life(t1/2) and compared with Fexofenadine (Allegra) marketed tablets. Total bioavailability was increased for the test formulation compared to the reference formulation. Conclusion: Fexofenadine was successfully prepared as ODT with increased AUC and decreased tmax to which stability studies were conducted which were found to be stable.

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TASTE MASKING OF OXYBUTYNIN CHLORIDE USING LIPID EXCIPIENTS AND FORMULATION AS ORODISPERSIBLE TABLETS FOR GERIATRIC POPULATION

INDIAN DRUGS ◽

10.53879/id.50.10.p0039 ◽

2013 ◽

Vol 50 (10) ◽

pp. 39-46

Author(s):

V Prakash ◽

◽

L. Keshri ◽

V. Sharma ◽

K. Pathak

Keyword(s):

In Vitro Release ◽

In Vitro Dissolution ◽

Taste Masking ◽

Dissolution Time ◽

Disintegration Time ◽

Geriatric Population ◽

Orodispersible Tablets ◽

Lipid Excipients

The aim of the present study was to mask the bitter taste of oxybutynin chloride by lipid excipients and to develop its fast disintegrating tablet. For this purpose, a blend of two lipids, glyceryl behenate and glyceryl palmitostearate was utilized for taste masking by solvent evaporation method. The evaporation of solvent was accomplished by freeze drying and taste masked granules were characterized for their micromeritic and rheological properties. The state of dispersion was analyzed by SEM and DSC. Orodispersible tablets were then formulated (F1- F6) using Polyplasdone XL as extragranular superdisintegrant and evaluated for hardness, disintegration time, in vitro dissolution time and in vivo disintegration time. Results indicated that the formulation F6 exhibited minimum in vivo disintegration time of 8 sec with effective taste masking. In vitro release analysis indicated %DE10 and %DE25 of 51.48 and 76.53 respectively. Conclusively, taste masked orodispersible formulation of oxybutynin chloride was developed that could be beneficial for geriatric population.

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In vitro and in vivo particle coating for oral targeting and drug delivery

Handbook of Modern Coating Technologies ◽

10.1016/b978-0-444-63240-1.00009-7 ◽

2021 ◽

pp. 231-258

Author(s):

Camillo Benetti ◽

Paolo Colombo ◽

Tin Wui Wong

Keyword(s):

Drug Delivery ◽

Particle Coating

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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

Polymers ◽

10.3390/polym11030522 ◽

2019 ◽

Vol 11 (3) ◽

pp. 522 ◽

Cited By ~ 2

Author(s):

Katarzyna Wasilewska ◽

Marta Szekalska ◽

Patrycja Ciosek-Skibinska ◽

Joanna Lenik ◽

Anna Basa ◽

...

Keyword(s):

Spray Drying ◽

Electronic Tongue ◽

Aqueous Dispersion ◽

Taste Masking ◽

Organic Solution ◽

Aqueous Dispersions ◽

Innovative Methods ◽

Pharmaceutical Properties

The taste of drugs is an important factor affecting pharmacotherapy effectiveness, and obtaining formulations with acceptable organoleptic properties is still an ongoing issue in pharmaceutical technology. One of the innovative methods of taste masking is preparation of microparticles by the spray drying technique, utilizing polymers with different physicochemical properties. Rupatadine fumarate (RUP) is one of the newest antihistamines, with an innovative and multidirectional mechanism of action, and an extremely bitter taste. The aim of this work was to investigate the feasibility of utilizing organic or aqueous forms of ethylcellulose (EC) for the preparation of microparticles with RUP by the spray drying technique. Spray dried samples at different drug:polymer ratios were prepared using organic solution (Ethocel®) or aqueous dispersions of EC (Surelease®, Aquacoat® ECD). Evaluation of the taste masking efficacy was performed in vivo in human taste panel, in vitro based on dissolution test, and by self-constructed electronic tongue. It was shown that microparticles obtained from aqueous dispersions of EC have superior pharmaceutical properties in terms of both morphology and taste masking efficacy in comparison to those obtained from organic solution.

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Colon specific delivery of budesonide based on triple coated pellets: in vitro/in vivo evaluation

Acta Pharmaceutica ◽

10.2478/v10007-012-0025-y ◽

2012 ◽

Vol 62 (3) ◽

pp. 341-356 ◽

Cited By ~ 3

Author(s):

Jaleh Varshosaz ◽

Jaber Emami ◽

Naser Tavakoli ◽

Mohsen Minaiyan ◽

Nakisa Rahmani ◽

...

Keyword(s):

Trinitrobenzenesulfonic Acid ◽

In Vivo Evaluation ◽

Pore Former ◽

Hydroxypropylmethyl Cellulose ◽

Colon Delivery ◽

Core Composition ◽

Eudragit E ◽

Extrusion Spheronization

Three layered pellets of budesonide were prepared for colon delivery by the extrusion-spheronization method. The coatings consisted of hydroxypropylmethyl cellulose (HPMC) (as barrier layer), Eudragit E (as rate controlling layer) and hydroxypropylmethyl cellulose acetate succinate (HPMC AS) (as enteric layer). The rate controlling layer was further modified using various pore formers. Dissolution studies were carried out at pH 1.2, 7.4 and 6.8. Pellet core composition and type and level of pore former affected the drug release from pellets. Pellets containing 20 % (m/m) citric acid in the cores coated with HPMC at a coating level of 6 % (m/m), Eudragit E containing Avicel RC 581 (30 %) as pore former at a coating level of 30 % (m/m) and HPMC AS at a coating level of 15 % (m/m) had the best release profiles. These pellets showed promising results in alleviating the conditions of an experimental model of colitis induced by trinitrobenzenesulfonic acid in rats.

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Waktu Inkubasi pada Derajat Distilasi Kitosan Enzim dan Efektifitas Penghambatannya terhadap Penyakit Antraknosa

Jurnal Fitopatologi Indonesia ◽

10.14692/jfi.12.6.209 ◽

2017 ◽

Vol 12 (6) ◽

pp. 209

Author(s):

Yadi Suryadi ◽

Tri Puji Priyatno ◽

I Made Samudra ◽

Dwi Ningsih Susilowati ◽

Hermawati Nurzulaika ◽

...

Keyword(s):

Spore Germination ◽

Burkholderia Cepacia ◽

Fungal Growth ◽

The Other ◽

In Vitro Assays ◽

Incubation Condition ◽

Coating Agent ◽

Optimal Incubation

The use of chitosan as a coating agent of harvested fruits is an alternative method in controlling anthracnose disease (Colletotrichum sp.). This study aimed to obtain an optimal enzymatic chitosan (EC) that hydrolyzed using chitinase from Burkholderia cepacia isolate E76. The optimal incubation condition to produce EC was 2 h with the yield of 3.52 ± 0.38 g. The degree of deacetylation (DD) chitosan and EC was 66.91% and 80.91%, respectively. Based on in vitro assays, EC 2% was the most effective in inhibiting the growth of Colletotrichum sp. (94.22%) than chitosan, while the highest inhibition for chitosan 3% was 55.26%. Moreover, the EC 2% showed the highest inhibition of spore germination (74.12%). The in vivo assay revealed that EC 2% showed the highest inhibition on the fungal growth (88.88%), compared to the other concentrations. On the other hand, the EC 2% and 3% gave similar results on inhibition of Colletotrichum sp.of chili (55.55%).

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Double Coated Tablets of Nimesulide for Colon Targeting

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2010.3.2.14 ◽

2010 ◽

Vol 3 (2) ◽

pp. 1000-1005

Author(s):

M S Shaikh

Keyword(s):

Targeted Drug Delivery ◽

Film Coating ◽

In Vitro Dissolution ◽

In Vitro Drug Release ◽

Novel Approach ◽

Eudragit E ◽

Coating Weight ◽

Targeted Drug Delivery System

The present study was aimed at developing oral colon targeted drug delivery system for Nimesulide utilizing recently designed and patented system called CODESTM, which consisted of a lactulose containing core overcoated with both Eudragit E and Eudragit L designed to rapidly disintegrate in the colon, in order to give a new life for an existing banned drug. CODESTM tablets were prepared by tabletting Nimesulide and lactulose, followed with film coating of Eudragit. The prepared tablets were evaluated on the basis of in vitro dissolution study and in vivo disintegration study was performed by gamma scintigraphic evaluation in rats. The onset of Nimesulide release was found to dependent on the coating level of Eudragit E, and at Eudragit E coating level of 8% (coating weight gain), the onset of in vitro drug release was found to be optimum. When the same was subjected on scintigraphic evaluation for in vivo disintegration study, there was a reasonable agreement between the in vitro/in vivo data. It is concluded that Nimesulide can be targeted to hindgut by a novel approach of CODESTM.

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Preparation and Evaluation of Rapidly Disintegrating Glimepiride Tablets

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2010.3.4.7 ◽

2011 ◽

Vol 3 (4) ◽

pp. 1220-1229

Author(s):

Adel M Aly ◽

Bassam I Amro ◽

Feras D El Hajji

Keyword(s):

Fasting Blood Glucose ◽

Diabetic Patients ◽

Onset Of Action ◽

Disintegration Time ◽

Glucose Levels ◽

Orally Disintegrating Tablets ◽

Accelerated Stability ◽

The Stability

The objective of this work was to prepare Glimepiride (1 mg) rapidly disintegrating tablets (RDT) by direct compression, and also, to evaluate Pharmaburst™ as a newly introduced diluent for this type of tablets, either alone or in combination with other well known tablet excipients. Another goal was to study the stability, as well as, the in vivo effects of selected formulations. Orange flavor was the most preferred flavor for the prepared rapidly disintegrating tablets containing Pharmaburst™ as a single diluent. Pharmaburst™ alone is sufficient to produce rapidly (orally) disintegrating tablets of Glimepiride with good physical characteristics, better compactability and shorter in-vivo and in-vitro disintegration time. The prepared Glimepiride RDT were found to have faster onset of action than the conventional Glimepiride tablets. Also, they were effective in lowering fasting blood glucose levels (FBG) in rabbits. Glimepiride RDT containing Pharmaburst™ alone were found to be stable when subjected to accelerated stability conditions (40 °C / 75 % relative humidity) for at least 3 months. Packaging the prepared Glimepiride RDT in 40 CC high density polyethylene (HDPE) bottles with 2 grams silica gel desiccant canisters and rayon had provided sufficient protection for the tablets. The used packaging system is believed to be very practical and convenient for elderly diabetic patients. It is also assumed to be preferred by the manufacturers.

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