Design and optimization of gastro-floating sustained-release tablet of pregabalin: In vitro and in vivo evaluation

Chao, Qin; Wu, Mengmeng; Xu, Siyuan; Wang, Xiaowei; Shi, Wenxing; Dong, Yangyu; Yang, Lei; He, Wei; Han, Xiaoyan; Yin, Lifang

doi:10.1016/j.ijpharm.2018.04.011

Cited by 52 publications

(27 citation statements)

References 16 publications

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“…Medium uptake and mass loss were evaluated by comparing the weights of swollen and dried tablets. In the controlled release EFT, hydration capability of the polymer may govern drug release kinetics, as well as tablet buoyancy efficiency [ 13 , 26 ]. As shown in Figure 2 a, higher medium uptake was observed in the tablets with higher amounts of PEO, irrespective of compression force in the experimental range.…”

Section: Resultsmentioning

confidence: 99%

“…Among various hydrophilic polymer types (cationic, anionic, and non-ionic polymer), the non-ionic hydrophilic polymers, such as hydroxypropyl methylcellulose (HPMC), hydroxypropyl cellulose (HPC), and polyethylene oxide (PEO), are commonly used in controlled release tablets because these polymers are not affected by pH [ 13 , 26 ]. As a result, drug release and floating behavior of tablets are also not influenced by the pH of gastric fluid [ 13 , 26 ]. In addition, non-ionic hydrophilic polymers are non-toxic, economic, and safe to use for EFT [ 27 , 28 , 29 ].…”

Section: Introductionmentioning

confidence: 99%

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Effects of Formulation and Process Variables on Gastroretentive Floating Tablets with A High-Dose Soluble Drug and Experimental Design Approach

Thapa

Jeong

2018

Pharmaceutics

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To develop sustained release gastro-retentive effervescent floating tablets (EFT), a quality-based experimental design approach was utilized during the composing of a hydrophilic matrix loaded with a high amount of a highly water-soluble model drug, metformin HCl. Effects of the amount of polyethylene oxide WSR 303 (PEO), sodium bicarbonate, and tablet compression force were used as independent variables. Various times required to release the drug, tablet tensile strength, floating lag time, tablet ejection force, and tablet porosity, were selected as the responses. Polymer screening showed that PEO had the highest gel strength among the various tested polymers. Sodium bicarbonate had the most significant effect on the release rate and floating lag time by retarding the rate from the hydrophilic matrices, whilst tablet compression force and PEO exerted the greatest influence on tablet properties (p < 0.0001). The design space was built in accordance with the drug release profiles, tensile strength, and floating lag time, following failure probability analysis using Monte Carlo simulations. The kinetic modeling revealed that the release mechanism was best described by the Korsmeyer-Peppas model. Overall, the current study provided a perspective on the systematic approach of gastro-retentive EFT, loaded with highly water-soluble drugs by applying quality by design concepts.

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Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Effects of Formulation and Process Variables on Gastroretentive Floating Tablets with A High-Dose Soluble Drug and Experimental Design Approach

Thapa

Jeong

2018

Pharmaceutics

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“…Results obtained for different evaluation parameters were subjected to software for analysis and further optimization of the formulations. [9][10][11][12] Formulation of gastro retentive in-situ gelling liquid Sodium alginate, at solution concentrations of 0.5-1.5% (w/v) were prepared in de-ionized water by heating to 60°C with continuous stirring. After cooling below 40°C, various concentrations of calcium carbonate and drug solutions were added and dispersed well with continuous stirring.…”

Section: Optimization Of Floating In-situ Gelling Formulation Using Dmentioning

confidence: 99%

Formulation, Optimization and Evaluation of in-situ Gelling Liquid Oral Formulation of a Novel Antidiabetic Drug: Canagliflozin

Bhatta¹,

Rudragangaiah²,

Kotappa³

2019

IJPER

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Aim: The present research work involves the development and optimization of an in-situ gel forming formulation by face centered central composite response surface design methodology to increase buoyancy and controlled release of a novel antidiabetic drug; Canagliflozin hemihydrate, having absorption window in upper part of gastrointestinal tract. Materials and Methods: The drug and excipient compatibility studies were performed by subjecting to Fourier Transform Infra-red spectroscopy and Differential Scanning Calorimetry analysis. Nine primary formulations suggested by Design Expert software were formulated and subjected for the evaluation by measurement of rheological properties, buoyancy studies, drug content and in-vitro drug release studies. The optimization method adopted in the present study was face centered central composite response surface design. Result: The effect of two independent factors namely concentration of sodium alginate and concentration of gas generating agent calcium carbonate on responses like floating lag time, viscosity and in-vitro drug release were considered for the optimization by plotting three dimensional surface response plots. The results of these studies were subjected to analysis by software to obtain an optimized formulation. The software suggested the optimized formulation must consists of 0.868 % of sodium alginate and 0.957 % of calcium carbonate and these compositions are much near to the composition of SF5. Conclusion: By considering the effect of calcium cations on the gelling properties of various concentration of sodium alginate, it was concluded that the effective gelling was achieved in the formulation comprised of 1 % sodium alginate with 0.5 %, 1.0 % and 1.5 % of calcium carbonate.

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“…An advantage of this technique is that the optimal parameters are found with minimum experimental conditions and therefore is time‐ and cost‐effective. This mathematical model has wide range of usage and was applied for example for optimizing the composition of gastroretentive floating tablets, for evaluating the influence of the composition on the tablets' drug delivery characteristics, for isolation of CS from sternal cartilage or for extraction of CS from bone soup obtained by boiling the chicken bones . In case of usage of the sternal cartilage the CS yields were approximately 0.24% and three independent variables were chosen (amount of papain, time of hydrolysis and temperature) .…”

Section: Discussionmentioning

confidence: 99%

Waste products from the poultry industry: a source of high‐value dietary supplements

Stiborová

Kronusová

Kaštánek

et al. 2019

J of Chemical Tech & Biotech

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BACKGROUND The production and consumption of chicken has doubled in the last 17 years. Since slaughter yields range from 70 to 80%, during production various chicken waste residues are generated. One of these residues is waste created after the mechanical separation of chicken meat (W‐MSM). The goal of the circular economy is to manage this waste and transform it into a valuable product. RESULTS W‐MSM was subjected to hydrolysis by the proteolytic enzymes pepsin and papain to obtain bioactive compounds. Papain digestion resulted in several times higher yields of chondroitin sulfate (CS), hyaluronic acid (HA), peptides and amino acids in comparison with pepsin. The hydrolysis conditions were further optimized using the software Design Expert to evaluate the impact of added enzyme, buffer and duration of the hydrolysis. In addition, the scale‐up of this process was verified with 5 kg of W‐MSM and the obtained product contained approximately 77% (w/w) of peptides, 9% (w/w) of CS, 7% (w/w) of HA and 4% (w/w) of amino acids. CONCLUSIONS We tested and optimized the method for evaluating the direct waste from poultry processing and transformed it into a product containing bioactive compounds which can be utilized as an ingredient for improving the properties of feed. © 2019 Society of Chemical Industry

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Design and optimization of gastro-floating sustained-release tablet of pregabalin: In vitro and in vivo evaluation

Cited by 52 publications

References 16 publications

Effects of Formulation and Process Variables on Gastroretentive Floating Tablets with A High-Dose Soluble Drug and Experimental Design Approach

Effects of Formulation and Process Variables on Gastroretentive Floating Tablets with A High-Dose Soluble Drug and Experimental Design Approach

Formulation, Optimization and Evaluation of in-situ Gelling Liquid Oral Formulation of a Novel Antidiabetic Drug: Canagliflozin

Waste products from the poultry industry: a source of high‐value dietary supplements

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