Delayed release film coating applications on oral solid dosage forms of proton pump inhibitors: case studies

Missaghi, Shahrzad; Young, Cara J.; Fegely, Kurt A.; Rajabi‐Siahboomi, Ali R.

doi:10.3109/03639040903468811

Cited by 35 publications

(22 citation statements)

References 15 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…To protect these acid-labile prodrugs from rapid destruction within the gastric lumen, PPIs are formulated for delayed release as acid-resistant, enteric-coated tablets. After passing through the stomach into the alkaline intestinal lumen, the enteric 760 coatings dissolve, and the prodrug is absorbed (Missaghi et al, 2010). Because omeprazole is a basic molecule (pK a of 3.97), it accumulates in the acidic secretory parietal cells after protonation of its pyridyl group (Sachs et al, 1995).…”

Section: E Overcoming Toxicity Problemsmentioning

confidence: 99%

Prodrugs—from Serendipity to Rational Design

2011

View full text Add to dashboard Cite

Section: E Overcoming Toxicity Problemsmentioning

confidence: 99%

Prodrugs—from Serendipity to Rational Design

2011

View full text Add to dashboard Cite

“…According to the International Conference on Harmonisation guidelines, the microspheres from selected formulation were exposed to 6 months stability study at 40°C/75% RH (19)(20)(21). At the end of 3 and 6 months, the formulations were evaluated by visual observation of any physical changes that occurred, determination of drug content, and carrying out in vitro release studies for 16 h.…”

Section: Physical Characterization Of the Microspheresmentioning

confidence: 99%

Influence of Some Formulation Variables on the Optimization of pH-dependent, Colon-targeted, Sustained-release Mesalamine Microspheres

El-Bary¹,

Aboelwafa²,

Sharabi³

2011

AAPS PharmSciTech

View full text Add to dashboard Cite

Abstract. The aim of this work was to understand the influence of different formulation variables on the optimization of pH-dependent, colon-targeted, sustained-release mesalamine microspheres prepared by O/O emulsion solvent evaporation method, employing pH-dependent Eudragit S and hydrophobic pHindependent ethylcellulose polymers. Formulation variables studied included concentration of Eudragit S in the internal phase and the ratios between; internal to external phase, drug to Eudragit S and Eudragit S to ethylcellulose to mesalamine. Prepared microspheres were evaluated by carrying out in vitro release studies and determination of particle size, production yield, and encapsulation efficiency. In addition, morphology of microspheres was examined using optical and scanning electron microscopy. Emulsion solvent evaporation method was found to be sensitive to the studied formulation variables. Particle size and encapsulation efficiency increased by increasing Eudragit S concentration in the internal phase, ratio of internal to external phase, and ratio of Eudragit S to the drug. Employing Eudragit S alone in preparation of the microspheres is only successful in forming acid-resistant microspheres with pulsatile release pattern at high pH. Eudragit S and ethylcellulose blend microspheres were able to control release under acidic condition and to extend drug release at high pH. The stability studies carried out at 40°C/75% RH for 6 months proved the stability of the optimized formulation. From the results of this investigation, microencapsulation of mesalamine in microspheres using blend of Eudragit S and ethylcellulose could constitute a promising approach for site-specific and controlled delivery of drug in colon.

show abstract

“…The polymers contain carboxylic groups and thus reveal pH-dependent solubility; at higher pH, the carboxylic groups became ionized and make the polymers dissolve; at lower pH, the carboxylic groups are not ionized and render them insoluble (9,10). Among the polymers, Eudragit L, containing an anionic copolymer based on methacrylic acid/ethyl acrylate (1:1), is the most widely used in the pharmaceutical industry.…”

Section: Introductionmentioning

confidence: 99%

“…However, enteric polymers influence the drug stability and bioavailability greatly, since an interaction between the free carboxyl groups contained in enteric polymer and the drug would occur (10,12,13). A conventional enteric coating applied to LSP formulations contains one enteric polymer.…”

Section: Introductionmentioning

confidence: 99%

Eudragit L/HPMCAS Blend Enteric-Coated Lansoprazole Pellets: Enhanced Drug Stability and Oral Bioavailability

Wang²,

Zhang³

et al. 2014

AAPS PharmSciTech

View full text Add to dashboard Cite

Abstract. The objectives of the present work were to use blends of Eudragit L and hydroxypropyl methylcellulose acetate succinate (HPMCAS) as enteric film coatings for lansoprazole (LSP) pellets. The entericcoated pellets were prepared with a fluid-bed coater. The influence of the blend ratio, type of plasticizer, plasticizer level, coating level, and curing conditions on gastric stability in vitro drug release and drug stability was evaluated. Furthermore, the bioavailability of the blend-coated pellets in beagle dogs was also performed. The blend-coated pellets exhibited significant improvement of gastric stability and drug stability compared to the pure polymer-coated pellets. Moreover, the AUC values of blend-coated pellets were greater than that of the pure polymer-coated pellets. It was concluded that the using blends of Eudragit L and HPMCAS as enteric film coatings for LSP pellets improved the drug stability and oral bioavailability.

show abstract

Delayed release film coating applications on oral solid dosage forms of proton pump inhibitors: case studies

Abstract: Results showed that Acryl-EZE enteric coating systems provide excellent performance in both media (0.1N HCl and acetate buffer pH 4.5) for monolithic and multiparticulate dosage forms.

Cited by 35 publications

References 15 publications

Prodrugs—from Serendipity to Rational Design

Prodrugs—from Serendipity to Rational Design

Influence of Some Formulation Variables on the Optimization of pH-dependent, Colon-targeted, Sustained-release Mesalamine Microspheres

Eudragit L/HPMCAS Blend Enteric-Coated Lansoprazole Pellets: Enhanced Drug Stability and Oral Bioavailability

Contact Info

Product

Resources

About