Blends of enteric and GIT-insoluble polymers used for film coating: physicochemical characterization and drug release patterns

Lecomte, Florence; Siepmann, Juergen; Walther, Mathias; MacRae, Ross J.; Bodmeier, Roland

doi:10.1016/s0168-3659(03)00155-x

Cited by 128 publications

(66 citation statements)

References 23 publications

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“…Therefore, it can be expected that the leaching of HPMCP out of film coatings at pH 7.2 increases the permeability of the coated film, but the underlying mass transport phenomena might be more complex. 14) In comparison with the HPMCP content (X 1 ), the HPMC content (X 2 ) showed significant synergistic effects on all responses, Y 1 , Y 2 and Y 3 . These effects may be attributed to the increased permeability of the coated film due to dissolution of HPMC, since HPMC has pH-independent solubility, in contrast to HPMCP.…”

Section: Resultsmentioning

confidence: 96%

Statistical Optimization of Tamsulosin Hydrochloride Controlled Release Pellets Coated with the Blend of HPMCP and HPMC

Kim

Park

et al. 2007

CHEMICAL & PHARMACEUTICAL BULLETIN

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Tamsulosin hydrochloride is a highly selective a 1A -adrenoreceptor antagonist that was developed for the treatment of lower urinary tract symptoms suggestive of benign prostatic hyperplasia (LUPS/BPH). Since tamsulosin hydrochloride can have dose-related adverse effects, a controlled release dosage is necessary.1) Moreover, following oral administration of 0.2-0.4 mg tamsulosin hydrochloride, the drug is absorbed from the intestine and is almost completely bioavailable. Therefore, the preferred formulation of tamsulosin hydrochloride provides controlled release that can modulate both the release rate of the drug and the absorption of drug in the intestinal tract. 2)We previously described tamsulosin hydrochloride controlled release pellets prepared using ethylcellulose aqueous dispersion (Surelease ® ) alone or with additives such as sodium alginate, HPMCP.3,4) Addition of HPMCP to Surelease ® effectively provided pH-dependent drug release. Moreover, the addition of HPMC into film coats improves various film-forming properties such as toughness, elasticity and tensile strength. 4,5) In the present study, we applied the coating system containing Surelease ® , HPMC and HPMCP to drug loaded spherical pellets prepared by conventional extrusion/spheronization techniques.Statistical optimization designs have been previously documented for the formulation of many pharmaceutical solid dosage forms. [6][7][8] Additionally, it is a powerful, efficient and systematic tool that shortens the time required for the development of pharmaceutical dosage forms. 9)The objective of the present study was to prepare tamsulosin hydrochloride controlled release pellets coated with a blend of HPMCP and HPMC in aqueous dispersions (Surelease ® ) and statistically determine the optimal levels of these factors using response surface methodology combined with Box-Behnken design. In addition, controlled release pellets coated with the optimized levels of the coating parameters were compared with commercially available controlled release pellets (Harunal ® capsule) using difference (f 1 ) and similarity (f 2 ) factors. Experimental MaterialsThe following materials were gifted: tamsulosin hydrochloride (Reyon Pharmaceutical Co., Korea), poloxamer 407 (Lutrol ® F127, BASF, Germany), microcrystalline cellulose (Avicel™ PH102, FMC, U.S.A.), carbopol 974P NF (Noveon, U.S.A.) and ethylcellulose aqueous dispersion (Surelease ® E-7-19010, Colorcon, U.S.A.). Sodium alginate (Duckalgin ® NSPH) was purchased from Kibun Food Chemica (Japan). Hydroxypropyl methylcellulose (HPMC, Pharmacoat ® 606) and hydroxypropyl methylcellulose phthalate (HPMCP, HP-55) were obtained from Shin-Etsu Chemical (Japan). All other chemicals were HPLC grade.Experimental Design Response surface methodology combined with Box-Behnken design (BBD) 10) was used to ascribe the relationship between the independent variables and the responses as well as to determine the coating parameters for tamsulosin hydrochloride controlled release pellets. A three-factor, three-level BBD with th...

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Section: Resultsmentioning

confidence: 96%

Statistical Optimization of Tamsulosin Hydrochloride Controlled Release Pellets Coated with the Blend of HPMCP and HPMC

Kim

Park

et al. 2007

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…Polymeric coating materials have been widely used for achieving modified release of various dosage forms to provide sustained or pulsed drug release (1)(2)(3)(4)(5)(6). Pharmaceutically available polymers such as polymethacrylates (Eudragit RS100, and Eudragit S100), hydroxypropylmethyl cellulose (HPMC), and ethylcellulose (EC) in either a single or mixed composition are widely applicable as matrix carriers and coating materials of pharmaceutical dosage forms to obtain modified releases.…”

Section: Introductionmentioning

confidence: 99%

“…and processing parameters (air pressure and temperature, etc.) on physicochemical properties of the coated films and drug release using a single polymer or blends of various polymers (2,(7)(8)(9). The physicochemical properties of the coated film in a single or binary blend of coating materials are related with drug release profiles from coated dosage forms.…”

Section: Introductionmentioning

confidence: 99%

Comparison of Release-Controlling Efficiency of Polymeric Coating Materials Using Matrix-type Casted Films and Diffusion-Controlled Coated Tablet

et al. 2010

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Abstract. Polymeric coating materials have been widely used to modify release rate of drug. We compared physical properties and release-controlling efficiency of polymeric coating materials using matrix-type casted film and diffusion-controlled coated tablet. Hydroxypropylmethyl cellulose (HPMC) with low or high viscosity grade, ethylcellulose (EC) and Eudragit ® RS100 as pH-independent polymers and Eudragit S100 for enteric coatings were chosen to prepare the casted film and coated tablet. Tensile strength and contact angle of matrix-type casted film were invariably in the decreasing order: EC> Eudragit S100> HPMC 100000> Eudragit RS100>HPMC 4000. There was a strong linear correlation between tensile strength and contact angle of the casted films. In contrast, weight loss (film solubility) of the matrix-type casted films in three release media (gastric, intestinal fluid and water) was invariably in the increasing order: EC< HPMC 100000HPMC 100000>Eudragit RS100>HPMC 4000>Eudragit S100. Interestingly, diffusion-controlled coated tablet also followed this rank order except Eudragit S100 although release profiles and lag time were highly dependent on the coating levels and type of polymeric coating materials. EC and Eudragit RS100 produced sustained release while HPMC and Eudragit S100 produced pulsed release. No molecular interactions occurred between drug and coating materials using 1 H-NMR analysis. The current information on release-controlling power of five different coating materials as matrix carrier or diffusion-controlled film could be applicable in designing oral sustained drug delivery.

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“…The coated pellets with a coating level of 12% and 15% showed much slower drug release than the ones with lower coating levels (5%, 6%, 8% and 10%). As the film-controlled drug release, whether or not the crack occurs in the polymeric membranes were determined by the mechanical stability of the film coatings and the hydrostatic pressure (Schultz & Kleinebudde, 1997;Lecomte et al, 2003). When the formulation contacts with the aqueous media, water diffuses into the pellets core and a monotonically increased hydrostatic pressure is induced inside the pellets.…”

Section: Effect Of Coating Thickness On Emz Releasementioning

confidence: 99%

Preparation and in vitro/in vivo evaluation of esomeprazole magnesium-modified release pellets

et al. 2014

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To reduce the drug plasma concentration fluctuation without being destroyed by gastric fluid, novel Esomeprazole magnesium modified-release pellets (EMZ-MRPs) with suitable in vitro release profiles and good in vitro and in vivo correlation (IVIVC) were developed. Fluid-bed was used to obtain EMZ-loaded pellets by spraying drug suspension onto blank sugar pellets. The drug-loaded pellets were subsequently coated with Eudragit Õ RS30D/RL30D (ERS/ERL) aqueous dispersion to achieve sustained-release (SR) characteristics. Furthermore, the SR pellets were coated with Eudragit Õ L30D-55 (EL-55) aqueous dispersion to achieve enteric properties. Besides, isolated coating film was necessary between drug layer and SR layer, as well as SR and enteric-coated layer to protect from their possible reaction. The resulting pellets were filled into the hard gelatin capsules for in vitro release processing and single-dose pharmacokinetic study in rats. The optimal formulation achieved good SR feature both in vitro and in vivo with a relative bioavailability of 103.50%. A good IVIVC was characterized by a high coefficient of determination (r ¼ 0.9945) by deconvolution method. Compared to those of EMZ entericcoated pellets (EMZ-ECPs, trade name NEXIUM), the in vivo study make known that the EMZ-MRPs with decreased maximum plasma concentration (C max ), prolonged peak concentration time (T max ) and mean residence time (MRT), and similar values both area under concentration-time curve from 0 to t (AUC 0-t ) and 0 to infinity (AUC 0-1 ). Collectively, these results manifested EMZ-MRPs had a satisfactory sustained-release behavior, a desired pharmacokinetic property, improved in vivo retention and decreased plasma drug concentration fluctuation.

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Blends of enteric and GIT-insoluble polymers used for film coating: physicochemical characterization and drug release patterns

Cited by 128 publications

References 23 publications

Statistical Optimization of Tamsulosin Hydrochloride Controlled Release Pellets Coated with the Blend of HPMCP and HPMC

Statistical Optimization of Tamsulosin Hydrochloride Controlled Release Pellets Coated with the Blend of HPMCP and HPMC

Comparison of Release-Controlling Efficiency of Polymeric Coating Materials Using Matrix-type Casted Films and Diffusion-Controlled Coated Tablet

Preparation and in vitro/in vivo evaluation of esomeprazole magnesium-modified release pellets

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