Design and testing in vitro of a bioadhesive and floating drug delivery system for oral application

Jiménez-Castellanos, M.R.; Zia, Hossein; Rhodes, C. T.

doi:10.1016/0378-5173(94)90236-4

Cited by 146 publications

(35 citation statements)

References 12 publications

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“…It was interesting to note that the tablets floated in less than 30 sec in the dissolution cell of the FTC apparatus during the in vitro dissolution study (dynamic test) (Figure 3), compared with the beaker method (static test) (Figure 4). This observation has been also pointed out by Jiménez-Castellanos et al (44) where sotalol HCl tablets floated after 27.7 min in the beaker method under static conditions and after 10.3 min during the dissolution test using USP basket method.…”

Section: Resultssupporting

confidence: 57%

In Vitro Release Evaluation of Gastroretentive Amoxicillin Floating Tablets Employing a Specific Design of the Flow-Through Cell

Emara¹,

Abdou²,

El-Ashmawy³

et al. 2013

Dissolution Technol.

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Floating amoxicillin trihydrate (AmoxT) tablets, used for eradication of Helicobacter pylori (H. pylori), were prepared according to a gas-generating technique to extend the drug residence time in the stomach. The drug release rate from the floating tablets in acidic dissolution medium, in which AmoxT is known to be unstable, was studied using two dissolution techniques: openloop system of the flow-through cell (FTC) and the beaker method. Analysis of AmoxT in the dissolution medium was carried out by UV spectrophotometric and HPLC methods. The comparison indicates that the open-loop system of the FTC, which is based on non-cumulative (fresh) dissolution samples, is the preferred dissolution technique, and in this case, the drug could be analyzed by UV spectrophotometric and HPLC methods. However, in the case of a large number of QC samples, UV spectrophotometry is preferred to the HPLC method, which requires relatively longer time for analysis thereby increasing drug degradation. On the other hand, in the case of the beaker method, which is based on cumulative dissolution samples, the drug must be analyzed by HPLC. Generally, the beaker method is not recommended due to the problems associated with the accumulation of AmoxT degradation product in the dissolution medium. This study describes a simple dissolution method capable of discriminating between different AmoxT gastroretentive formulations without any additional experimental or calculational steps.

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Section: Resultssupporting

confidence: 57%

In Vitro Release Evaluation of Gastroretentive Amoxicillin Floating Tablets Employing a Specific Design of the Flow-Through Cell

Emara¹,

Abdou²,

El-Ashmawy³

et al. 2013

Dissolution Technol.

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“…Tablets were crushed in a mortar and accurately average weighed amount of powdered tablets was taken for the analysis. [12] Samples were transferred to different volumetric flasks and were diluted up to the mark using 0.1 N HCl. The content was shaken well and kept for 30 minutes to dissolve the drug completely.…”

Section: Content Uniformitymentioning

confidence: 99%

Formulation Development and in-Vitro Evaluation of Oral Sustained Release Floating Tablets of Chlorogenic Acid

Mool¹

2017

WJPPS

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The purpose of the study was to develop sustained release floating tablet of chlorogenic acid (CGA) and optimize its drug release for enhanced oral bioavailability. A relatively new approach, 3 2 full factorial design, was used to formulate floating sustained release tablets of CGA and to systematically optimize its drug release using varying levels of sodium bicarbonate and hydroxypropyl methylcellulose (HPMC) K 15 M polymer. Sodium bicarbonate was used as gas generating agent. After setting the levels by preliminary trials, nine tablet formulations (F1 -F9) were prepared by wet granulation method using Design Expert Software® -suggested combinations. The concentrations of HPMC K15M (X1) and sodium bicarbonate (X2) were chosen as control variables. Conversely, the response variables selected were percentage (%) of drug released within 12 hours (Y1) and time taken by the tablet to float (Y2). Fourier transform infrared (FTIR) spectroscopy was used to assess compatibility between the drug and the excipients. The response surface and 3D plots drawn demonstrated the suitability of the hydrophilic matrix forming agents for formulating sustained release floating tablets of CGA. FTIR and DSC spectra showed no noticeable incompatibility between drug and polymers in both physical mixtures and in

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“…Those formulations, which released calcium rapidly within the first couple of minutes of the experiment, corresponded to low T 50% values (F3, F7, F9, and F12). Several formulations had their T 50% 3 MgSt 0.1042 n/a n/a 0.52 4.47 n/a n/a b 4 HPMC*MgSt n/a -0.5038 6.5 n/a n/a n/a n/a b 5 HPMC*CA n/a n/a 6.0 n/a n/a n/a n/a b 6 MgSt*CA n/a -0.4363 n/a n/a n/a n/a n/a b 7 HPMC*HPMC n/a n/a n/a n/a n/a -3.35 -0.3927 b 8 CA*CA n/a n/a n/a n/a n/a n/a -0.3079 b 9 MgSt*MgSt 0.0518 -0.2569 5.62 n/a n/a n/a n/a R The values of another response variable, the release of calcium at 6 hours (Rel), of the 20 formulations were obtained directly from the calcium release profiles (Figures 1-3). Formulations with low T 50% values generally have a high Rel value ( Table 3).…”

Section: Release Propertiesmentioning

confidence: 99%

“…A gastric floating drug delivery system (GFDDS) [1][2][3][4][5][6][7][8] can overcome at least some of these problems and is particularly useful for drugs that are primarily absorbed in the duodenum and upper jejunum segments. The GFDDS is be able to prolong the retention time of a dosage form in the GI tract, thereby improving the oral bioavailability of the drug [2].…”

Section: Introductionmentioning

confidence: 99%

Statistical optimization of gastric floating system for oral controlled delivery of calcium

Lin

Chien

et al. 2001

AAPS PharmSciTech

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The development of an optimized gastric floating drug delivery system is described. Statistical experimental design and data analysis using response surface methodology is also illustrated. A central, composite Box-Wilson design for the controlled release of calcium was used with 3 formulation variables: X 1 (hydroxypropyl methylcellulose [HPMC] loading), X 2 (citric acid loading), and X 3 (magnesium stearate loading). Twenty formulations were prepared, and dissolution studies and floating kinetics were performed on these formulations. The dissolution data obtained were then fitted to the Power Law, and floating profiles were analyzed. Diffusion exponents obtained by Power Law were used as targeted response variables, and the constraints were placed on other response variables. All 3 formulation variables were found to be significant for the release properties (P < .05), while only HPMC loading was found to be significant for floating properties. Optimization of the formulations was achieved by applying the constrained optimization. The optimized formulation delivered calcium at the release rate of 40 mg/hr, with predicted n and T 50% values at 0.93 and 3.29 hours, respectively. Experimentally, calcium was observed to release from the optimized formulation with n and T 50% values of 0.89 (± 0.10) and 3.20 (± 0.21) hours, which showed an excellent agreement. The quadratic mathematical model developed could be used to further predict formulations with desirable release and floating properties.

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Design and testing in vitro of a bioadhesive and floating drug delivery system for oral application

Cited by 146 publications

References 12 publications

In Vitro Release Evaluation of Gastroretentive Amoxicillin Floating Tablets Employing a Specific Design of the Flow-Through Cell

In Vitro Release Evaluation of Gastroretentive Amoxicillin Floating Tablets Employing a Specific Design of the Flow-Through Cell

Formulation Development and in-Vitro Evaluation of Oral Sustained Release Floating Tablets of Chlorogenic Acid

Statistical optimization of gastric floating system for oral controlled delivery of calcium

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