Continuous melt granulation to develop high drug loaded sustained release tablet of Metformin HCl

Vaingankar, Pradnya N.; Amin, Purnima D.

doi:10.1016/j.ajps.2016.08.005

Cited by 37 publications

(17 citation statements)

References 22 publications

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“…The infrared spectra of floating matrixes have clearly shown the characteristic absorption peaks of MTH; N-H in the region 3400 et 3100 cm -1 ; 3 High intensity absorption peaks around of, 3375, 3302 and 3173 cm -1 , C=N; two intense absorption bands at 1632 cm -1 and 1576 cm -1 , Aliphatic CH 3 ; three absorption peaks around of, 1477, 1450 and 1410 cm -1 , C-N of aliphatic diamines; low intensity bands in the region 1250-1050 cm -1 (Figure 3). These results are in accordance with the conclusions of the work carried out by Vaingankar and Amin 26 where FTIR spectroscopic analysis of MTH extended release tablets prepared by melt granulation with stearic acid has suggested non-existence of chemical interaction between the drug and the other excipients despite the high temperature during the melt granulation process.…”

Section: Ftir Spectroscopysupporting

confidence: 92%

Development of Floating Tablets of Metformin HCl by Thermoplastic Granulation. Part II:In VitroEvaluation of the Combined Effect of Acacia Gum/HPMC on Biopharmaceutical Performances

2020

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Purpose: The aim of this study was to evaluate the combined effect, acacia gum(AG)/ hydroxypropylmethylcellulose (HPMC), on biopharmaceutical performances of floating tablets of metformin hydrochloride (MTH) prepared by thermoplastic granulation using stearic acid. Methods: We have prepared the matrixes using AG/HPMC as a polymer combination. This combination of polymers which represents 15% of the total mass of tablet was used at various ratios 3:1, 1:1, 1:3, with two viscosity grade of HPMC (k15M and k100M). The developed matrixes have been evaluated for their pharmacotechnical and biopharmaceutical properties. Results: In addition to the satisfactory physical characteristics of matrixes, it was revealed that the Fc3 and Fc6 formulations with AG/HPMC k15M and AG/HPMC k100M respectively, at ratio, 1:3 were considered the most performance. These formulations have shown swelling, fast flotation, 360 and 480 seconds respectively, and remained floating on the surface of the medium for more than 24 hours, with the matrix integrity, while F1, containing only AG, did not show swelling and did not float. In addition, extended in vitro release (>8 hours) with decreased dissolved MTH rates was demonstrated for Fc3 and Fc6 matrixes, 95% and 91% respectively, compared to F1 where MTH dissolution was complete after 2 hours. The drug release from the highest-performance matrixes (Fc3 and Fc6) was found to follow Korsmeyer-Peppas’s model. The mechanism drug release was controlled by diffusion and erosion. Conclusion: The AG/HPMC combination was suitable as a polymer matrix to improve the in vitro biopharmaceutical properties of MTH compared to AG.

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Section: Ftir Spectroscopysupporting

confidence: 92%

Development of Floating Tablets of Metformin HCl by Thermoplastic Granulation. Part II:In VitroEvaluation of the Combined Effect of Acacia Gum/HPMC on Biopharmaceutical Performances

2020

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“…The selection of a suitable polymer, a gas generating agent, and process variables might be necessary for high-quality EFT development. A large amount of polymer is required to achieve sustained release profiles in highly water-soluble high-dose tablets, which in turn increases the weight of tablets [ 21 , 23 , 24 , 25 ]. Hydrophilic polymers have long been used in floating systems to create sustained release profiles.…”

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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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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“…3, metformin hydrochloride was loaded optimally in clinoptilolite modified by 1 % benzalkonium chloride. Metformin hydrochloride is hydrophilic and highly soluble in water [30]. This drug readily forms hydrogen bonds with molecules such as acids and phenol [31].…”

Section: Resultsmentioning

confidence: 99%

Modification of Clinoptilolite with Benzalkonium Chloride as a Carrier of Metformin Hydrochloride

Putra

Kusumawati

Permadi³

2019

Asian J. Chem.

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Clinoptilolites have a limitation in the adsorption of drug molecules due to their fixed pore structure. In this study, we modified the clinoptilolite with benzalkonium chloride. The modification was carried out by stirring 1 g of NaCl activated clinoptilolite with 100 mL of benzalkonium chloride solution with a concentration of 0.5, 1, 5, 10 and 15 % at room temperature for 24 h. After filtration and drying process, benzalkonium chloride modified clinoptilolite was stirred with 100 mL of 300 mg/L metformin hydrochloride solution at room temperature for 24 h. The result of sample characterization using FTIR spectrometer, X-ray diffractometer and N2 Sorption analyzer showed that clinoptilolite modification with benzalkonium chloride and the impregnation of metformin hydrochloride proceeded well. The optimal amount of metformin hydrochloride occurred in benzalkonium chloride 1 % modified clinoptilolite.

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Continuous melt granulation to develop high drug loaded sustained release tablet of Metformin HCl

Cited by 37 publications

References 22 publications

Development of Floating Tablets of Metformin HCl by Thermoplastic Granulation. Part II:In VitroEvaluation of the Combined Effect of Acacia Gum/HPMC on Biopharmaceutical Performances

Development of Floating Tablets of Metformin HCl by Thermoplastic Granulation. Part II:In VitroEvaluation of the Combined Effect of Acacia Gum/HPMC on Biopharmaceutical Performances

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

Modification of Clinoptilolite with Benzalkonium Chloride as a Carrier of Metformin Hydrochloride

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