Polymer film formulations for the preparation of enteric pharmaceutical capsules

Smith, Alan M.; Ingham, Andrew; Grover, Liam M.; Perrie, Yvonne

doi:10.1211/jpp.62.02.0003

Cited by 28 publications

(13 citation statements)

References 11 publications

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“…Previous attempts to produce enteric hard capsules have been reported in literature, however these rely on an additional coating step (AstraZeneca, 2017;Huyghebaert et al, 2004;Miller et al, 2015;Sharma and Sinha, 2018) or the incorporation of a gum which would provide protection to acid-sensitive ingredients by a delayed-release mechanism, such as DRCaps™ (Smith et al, 2010;Marzorati et al, 2015). These formulations do not exhibit a pH triggered release and instead rely on a time-delay in anticipation of timely emptying from stomach.…”

Section: Introductionmentioning

confidence: 99%

Achieving gastroresistance without coating: Formulation of capsule shells from enteric polymers

Barbosa

Al-Kauraishi

Smith

et al. 2019

European Journal of Pharmaceutics and Biopharmaceutics

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Capsules are a widely used oral dosage form due to their simplicity and ease of manufacture. They are equally popular for both pharmaceutical and nutraceutical products and since they do not need extensive formulation development; it is a dosage form of choice for new drugs undergoing animal or clinical trials. In addition to the standard hard-gelatin or cellulose-based vegetarian capsules, functional capsules such as those with built-in gastroresistance would be of great value. In this work, commonly used enteric polymers were investigated for the production of hard-capsules. The polymers used in this study included cellulose derivatives (HPMC AS-LF and HP-55) and acrylic/methacrylic acid derivatives (EUDRAGIT L100 and S100). A range of concentrations of polymers and plasticisers were tested to optimise the formulation for the production of capsule shells with desirable physicochemical and gastroresistance characteristics. Drug release from optimised capsules produced from HPMC AS-LF, HP-55, EUDRAGIT L100 and S100 was shown to be comparable to drug release from corresponding polymer-coated tablets in both compendial and physiological bicarbonate buffer. In summary, herein we report a simple method for producing enteric capsule shells which do not need an additional coating step which, if validated at large scale, can significantly reduce the cost of manufacturing of conventional enteric coated dosage forms and are also likely to improve the inter-tablet variability in post-gastric drug release inherent in coating variability in conventional coated dosage forms.

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Section: Introductionmentioning

confidence: 99%

Achieving gastroresistance without coating: Formulation of capsule shells from enteric polymers

Barbosa

Al-Kauraishi

Smith

et al. 2019

European Journal of Pharmaceutics and Biopharmaceutics

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“…More recently capsule films prepared from tertiary mixtures of HPMC/gellan/alginate have shown good film-forming properties and acid-delayed rupture at gastric pH due to the presence of alginate and gellan (Smith and Perrie, 2007).…”

Section: Pharmaceutical Capsulesmentioning

confidence: 99%

Hydrocolloids and Medicinal Chemistry Applications

Grover

Smith

2009

Modern Biopolymer Science

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“…Another technique to achieve gastric resistance was described by Smith et al who prepared capsules with bulk enteric properties, thus omitting the need of applying an enteric coating [11]. However, in a recent study by our group DRcaps ® , a commercially available example of capsules with bulk enteric properties [12], was inferior to coated capsules regarding the acid-resistance and showed considerable deformation after 1 h in acidic media [13].…”

Section: Introductionmentioning

confidence: 99%

In Vitro Evaluation of Enteric-Coated HPMC Capsules—Effect of Formulation Factors on Product Performance

Blechar

Sauer³

et al. 2020

Pharmaceutics

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A comparative study on different enteric-coated hard capsules was performed. The influence of different formulation factors like choice of enteric polymer, triethyl citrate (TEC) concentration (plasticizer), talc concentrations (anti-tacking agent), and different coating process parameters on the sealing performance of the capsule and the disintegration time were investigated. Furthermore, the influence of different disintegration test methods (with disc vs. without disc and 50 mM U.S. Pharmacopoeia (USP) buffer pH 6.8 vs. biopredictive 15 mM phosphate buffer pH 6.5) was evaluated. All formulations showed sufficient but not equivalent acid resistance when tested. Polymer type was the main factor influencing the capsule sealing and disintegration time. In addition, TEC and talc could affect the performance of the formulation. Regarding the choice of the disintegration test method, the presence of a disc had for the most part only limited influence on the results. The choice of disintegration buffer was found to be important in identifying differences between the formulations.

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Polymer film formulations for the preparation of enteric pharmaceutical capsules

Abstract: Selected formulations from this study have potential for use as delayed release capsules.

Cited by 28 publications

References 11 publications

Achieving gastroresistance without coating: Formulation of capsule shells from enteric polymers

Achieving gastroresistance without coating: Formulation of capsule shells from enteric polymers

Hydrocolloids and Medicinal Chemistry Applications

In Vitro Evaluation of Enteric-Coated HPMC Capsules—Effect of Formulation Factors on Product Performance

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