Atenolol gastrointestinal therapeutic system: optimization of formulation variables using response surface methodology

Sastry, Srikonda; Reddy, Indra K.; Khan, Mansoor A.

doi:10.1016/s0168-3659(96)01553-2

Cited by 45 publications

(23 citation statements)

References 9 publications

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“…[6][7][8] Additionally, it is a powerful, efficient and systematic tool that shortens the time required for the development of pharmaceutical dosage forms.…”

Section: )mentioning

confidence: 99%

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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“…[6][7][8] Additionally, it is a powerful, efficient and systematic tool that shortens the time required for the development of pharmaceutical dosage forms.…”

Section: )mentioning

confidence: 99%

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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“…Administration of conventional tablets of atenolol has been reported to exhibit fluctuations in the plasma drug levels, resulting either in manifestation of side effects or reduction in drug concentration at the receptor site. 7,8 Accordingly, studies have been reported on regulation of drug release by formulating its diverse CR systems such as hydrophilic matrices, 9-11 osmotic pumps, 7,8,12,13 and transdermal drug delivery systems. 14 Response surface methodology (RSM) is a widely practiced approach in the development and optimization of drug delivery devices.…”

Section: Introductionmentioning

confidence: 99%

Formulation and optimization of controlled release mucoadhesive tablets of atenolol using response surface methodology

Chakkal²,

2006

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The aim of the current study was to design oral controlled release mucoadhesive compressed hydrophilic matrices of atenolol and to optimize the drug release profile and bioadhesion using response surface methodology. Tablets were prepared by direct compression and evaluated for bioadhesive strength and in vitro dissolution parameters. A central composite design for 2 factors at 3 levels each was employed to systematically optimize drug release profile and bioadhesive strength. Carbopol 934P and sodium carboxymethylcellulose were taken as the independent variables. Response surface plots and contour plots were drawn, and optimum formulations were selected by feasibility and grid searches. Compressed matrices exhibited non-Fickian drug release kinetics approaching zero-order, as the value of release rate exponent (n) varied between 0.6672 and 0.8646, resulting in regulated and complete release until 24 hours. Both the polymers had significant effect on the bioadhesive strength of the tablets, measured as force of detachment against porcine gastric mucosa (P < .001). Polynomial mathematical models, generated for various response variables using multiple linear regression analysis, were found to be statistically significant (P < .01). Validation of optimization study, performed using 8 confirmatory runs, indicated very high degree of prognostic ability of response surface methodology, with mean percentage error (± SD) as −0.0072 ± 1.087. Besides unraveling the effect of the 2 factors on the various response variables, the study helped in finding the optimum formulation with excellent bioadhesive strength and controlled release.

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“…This may be due to gas generated in the 0.1 N HCL is trapped and protected within polymeric gel, formed by hydration of polymer, thus decreasing the density of tablet below 1 g/cm 3 and tablet becomes buoyant.…”

Section: Density Measurementmentioning

confidence: 99%

“…Administration of atenolol conventional tablets in 100 mg/day doses may cause fluctuations in the plasma concentration resulting in side effects or reduction in the drug concentration at receptor site. 3 It is reported that in case of oral administration of atenolol, it can induce side effects such as diarrhea, nausea, mesenteric arterial thrombosis, ischemic colitis and dry mouth. 4 The short half-life of Atenolol i.e.…”

Section: Introductionmentioning

confidence: 99%

Gamascintigraphic in Vivo-in Vitro Evaluation of Floating Matrix Tablet

Shinde¹,

Joshi²,

Dhas³

2014

IJPER

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Background of the work: Gastroretentive drug delivery system can retain the dosage form in the gastric region for several hours. Prolong gastric retention helps in improving bioavailability and improves solubility of drugs that are less soluble in a high pH environment. For designing of GRDDS Atenolol was selected as a model drug. It has been used for the treatment of hypertension. Atenolol has short elimination half-life, stable at pH 1.2 and as the pH increase, the drugs becomes unstable and thus low oral bioavailability.In order to improve its therapeutic effectiveness Atenolol is designed in the form of floating tablet formulation. Purpose: The aim of the present

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Atenolol gastrointestinal therapeutic system: optimization of formulation variables using response surface methodology

Cited by 45 publications

References 9 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

Formulation and optimization of controlled release mucoadhesive tablets of atenolol using response surface methodology

Gamascintigraphic in Vivo-in Vitro Evaluation of Floating Matrix Tablet

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