A novel concept in enteric coating: A double-coating system providing rapid drug release in the proximal small intestine

Liu, Feng; Lizio, Rosario; Meier, Christian; Petereit, Hans-Ulrich; Blakey, Peter; Basit, Abdul W.

doi:10.1016/j.jconrel.2008.09.083

Cited by 67 publications

(33 citation statements)

References 21 publications

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“…Thus, the swelling of the coated pellets was suppressed and then affected the rupture of coated pellets, retarding the drug release. Moreover, less water uptake was not beneficial to the production of microenvironments inside the pellets, delaying the dissolution of the enteric polymer coatings (28,29).…”

Section: Effect Of Blend Ratio On Drug Releasementioning

confidence: 99%

“…If the enteric-coated pellets were administered to the fasted dogs, the enteric films might be damaged and led to premature drug release, drug instability, and decreasing bioavailability. The drug release of conventional enteric-coated dosage forms always occurred in the distal small intestine, resulting in a delayed response to medication and decreased the drug bioavailability (28). The blend-coated pellets might get over the physiological variations and improved the conformity of disintegration in gastrointestinal tract.…”

Section: Pharmacokinetics In Dogsmentioning

confidence: 99%

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

Wang²,

Zhang³

et al. 2014

AAPS PharmSciTech

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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.

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Section: Effect Of Blend Ratio On Drug Releasementioning

confidence: 99%

Section: Pharmacokinetics In Dogsmentioning

confidence: 99%

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

Wang²,

Zhang³

et al. 2014

AAPS PharmSciTech

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“…Typically, coatings (e.g., enteric coatings) are intended to delay the release of medication until the dosage form has passed through the acidic medium of the stomach (United States Pharmacopeia & National Formulary, 2004). A major aim of enteric coating is the protection of drugs that are sensitive or unstable at acidic pH (Liu et al, 2009;Brogmann and Beckert, 2001). This is particularly important for drugs such as enzymes (Keller et al, 2009) and proteins (Brogmann and Beckert, 2001), because these macromolecules are rapidly hydrolyzed and inactivated in acidic medium.…”

Section: Introductionmentioning

confidence: 99%

Assessment of the pharmaceutical quality of marketed enteric coated pantoprazole sodium sesquihydrate products

Mostafa

Ibrahim

Mahrous

et al. 2011

Saudi Pharmaceutical Journal

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Pantoprazole sodium sesquihydrate (PSS) is a proton pump inhibitor, used in acid-related disorders, like peptic ulcer and gastroesophageal reflux. Increasing the number of pantoprazole containing products in the market, raises questions of its efficacy and generic substitution. The pharmaceutical quality of 6 generic PSS enteric coated tablets in 2 local markets was assessed relative to the innovator product (pantozol®). Uniformity of dosage unit, disintegration and in vitro drug release were determined using United States pharmacopeia for delayed release tablets. The similarity factor (f2) was assessed using the FDA recommended approach (f2 similarity factor). The content uniformity of the innovator product was 98.39% of the labeled claim with RSD value of 1.08%, while the content of generic products ranged from 96.98% to 98.80% with RSD values of 1.24-2.19%. All the products showed no disintegration, cracks or swelling in 0.1 N HCl, except product 1, which showed complete disintegration after 20 min. However, the disintegration of all the products in phosphate buffer met USP requirements. Dissolution of tablets in 0.1 N HCl showed no drug release after 2 h except product 1 in which one tablet showed a drug release more than 10% at acid stage level A1. In addition, three tablets of this product showed dissolution of 45%, 48% and 69% at acid stage level A2. The similarity factor f2 of the products was between 71 and 74 indicating the similarity in dissolution profiles of all the products in accordance to FDA requirements, except product 1 in which f2 value was 18.67.

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“…It may be attributed to the high swellability of HPMC which affects the release kinetics of the incorporated drug, and the water diffusion coefficient also has a significant dependence on the matrix swelling ratio (38,42). On the other hand, polymer coatings have been found to profoundly affect the dissolution behaviors of some drugs (43,44). Likewise, pellets are typically coated for the purpose of producing controlled-or sustainedrelease dosage forms in the pharmaceutical industry (45).…”

Section: Discussionmentioning

confidence: 99%

Preparation and In Vitro–In Vivo Evaluation of Sustained-Release Matrix Pellets of Capsaicin to Enhance the Oral Bioavailability

Huang

Omari‐Siaw

et al. 2015

AAPS PharmSciTech

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Abstract. Capsaicin has multiple pharmacological activities including antioxidant, anticancer, and antiinflammatory activities. However, its clinical application is limited due to its poor aqueous solubility, gastric irritation, and low oral bioavailability. This research was aimed at preparing sustained-release matrix pellets of capsaicin to enhance its oral bioavailability. The pellets comprised of a core of soliddispersed capsaicin mixed with microcrystalline cellulose (MCC) and hydroxypropyl cellulose (HPMC) and subsequently coating with ethyl cellulose (EC) were obtained by using the technology of extrusion/ spheronization. The physicochemical properties of the pellets were evaluated through scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray diffractometry (XRD). Besides, the in vitro release, in vivo absorption, and in vitro-in vivo correlation were also assessed. More importantly, the relative bioavailability of the sustained-release matrix pellets was studied in fasted rabbits after oral administration using free capsaicin and solid dispersion as references. The oral bioavailability of the matrix pellets and sustained-release matrix pellets of capsaicin was improved approximately 1.98-fold and 5.34-fold, respectively, compared with the free capsaicin. A good level A IVIVC (in vitro-in vivo correlation) was established between the in vitro dissolution and the in vivo absorption of sustainedrelease matrix pellets. All the results affirmed the remarkable improvement in the oral bioavailability of capsaicin owing to the successful preparation of its sustained-release matrix pellets.

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A novel concept in enteric coating: A double-coating system providing rapid drug release in the proximal small intestine

Cited by 67 publications

References 21 publications

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

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

Assessment of the pharmaceutical quality of marketed enteric coated pantoprazole sodium sesquihydrate products

Preparation and In Vitro–In Vivo Evaluation of Sustained-Release Matrix Pellets of Capsaicin to Enhance the Oral Bioavailability

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