Formulation of a modified release metformin. HCl matrix tablet: influence of some hydrophilic polymers on release rate and in-vitro evaluation

Rojas, John; González, César Antonio Otero; Rico, Carolina; Saez, Oswaldo

doi:10.1590/s1984-82502011000300006

Cited by 4 publications

(4 citation statements)

References 29 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Addition of PVP at 5 times, the concentration of Eudragit L100-55 (5:1) led to greater release of the drug in acid medium over 2 h. These observations can be explained by the predominance of PVP over Eudragit L100-55 as the matrix constituent polymer. Under these conditions, the matrix was eroded in acidic medium because PVP polymers are pH-sensitive, although PVP can act as a binder [9]. In F2 preparations, the percentage of drug release in acid media was smaller than from F1 preparations.…”

Section: Dissolution Testmentioning

confidence: 99%

“…Eudragit L100-55 polymer releases its contents at the small intestinal pH of >5.5, where α-glucosidase enzyme is located. PVP is a hydrophilic polymer that can be used to control and increase drug release, and also acts as a binder [9]. Thus, in this study, PVP-Eudragit L100-55 combinations were expected to increase drug release in the small intestine.…”

Section: Introductionmentioning

confidence: 97%

See 1 more Smart Citation

Formulation of Enteric Granules Containing Green Tea (Camellia Sinensis) Extract Using Eudragit L100-55 as a Delayed Release Matrix

Anwar

Sherman

2020

Int J App Pharm

View full text Add to dashboard Cite

Objective: Epigallocatechin gallate (EGCG) inhibits glucose absorption into the blood by inhibiting small intestinal α-glucosidase but is unstable ingastric fluid. Hence, we formulated EGCG into enteric preparations that prevent release in gastric fluid.Methods: Granules were prepared using a wet granulation method and were formulated into polyvinylpyrrolidone (PVP)-Eudragit L100-55 (5:1; F1),PVP-Eudragit L100-55 (1:1; F2), and Eudragit L100-55 (F3) preparations using 30% w/w Eudragit L100-55 as a matrix. EGCG contents of granuleswere evaluated and dissolution tests were performed at pH 1.2 and 6.8.Results: F1–3 formulas had good flow properties and contained EGCG at 24.05%±0.15%–24.96%±0.28%. Dissolution tests showed that F1 and F2formulas released EGCG at 50.53%±0.04% and 17.80%±0.55%, respectively, after 2 h in HCl medium at pH 1.2. Cumulative drug release from F1 andF2 formulations after 2 h under these conditions (pH 1.2) and 1 h in phosphate buffer (pH 6.8) was 94.40%±1.58% and 93.70%±1.08%, respectively.Conclusion: As the optimal formula, F3 granules limited drug release to 7.03%±0.22% in HCl at pH 1.2 over 2 h and cumulative drug release in HClmedium (pH 1.2) followed by phosphate buffer (pH 6.8) of 86.13%±0.20%.

show abstract

Section: Dissolution Testmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 97%

Formulation of Enteric Granules Containing Green Tea (Camellia Sinensis) Extract Using Eudragit L100-55 as a Delayed Release Matrix

Anwar

Sherman

2020

Int J App Pharm

View full text Add to dashboard Cite

show abstract

“…Uncoated sustainedrelease tablets are prepared by embedding the drug in the tablet matrix [10]. The hydrophilic matrix system, when exposed to an aqueous medium does not disintegrate but immediately after hydration develops a highly viscous gelatinous surface barrier, which controls the drug release from, and liquid penetration into the centre of the matrix system [11][12][13]. The primary rate limiting ingredients of hydrophilic matrix are polymers that would swell when in contact with aqueous solution and form a gel layer on the surface of the system.…”

Section: Introductionmentioning

confidence: 99%

Formulation and evaluation of sustained release diclofenac sodium matrix tablets produced using <i>Brachystegia eurycoma </i>gum

Okafo¹,

Avbunudiogba²,

Ejomafuvwe³

2020

J. Pharm Bio.

View full text Add to dashboard Cite

This study was carried out to evaluate sustained release diclofenac sodium matrix tablets formulated using Brachystegia eurycoma gum (BEG) as matrix polymer. BEG was isolated by acetone -precipitation of the filtrate obtained from the maceration of powdered dried seeds of Brachystegia eurycoma in distilled water. Diclofenac sodium matrix tablets were produced by non-aqueous wet granulation method using BEG as the hydrophilic matrix former. The tablets were evaluated using official and unofficial tests such as; uniformity of weight, content uniformity, dissolution test, tablets diameter, thickness, hardness and friability tests. The drug release profile of the matrix tablets were compared to that formulated using a standard matrix former, hydroxypropylmethylcellulose (HPMC). Hardness values ranged from 6.12 ± 1.80 to 9.73 ± 1.39 kgf, friability from 0.31 ± 0.00 to 1.00 ± 0.00%. The drug content ranged from 98 to 101 %. The percentage drug released from the matrix tablets after 10 h was between 71.27 and 98.73 % except for formulation BF3 that released 32.56 %. This study showed that sustained release diclofenac sodium matrix tablets were successfully formulated using Brachystegia eurycoma gum as the matrix former and the tablets were comparable to that formulated with HPMC. Keywords: Brachystegia eurycoma gum; Diclofenac sodium; Matrix tablets; Sustained release

show abstract

“…Plasma half-life of the drug is relatively short, i.e., 1.5-4.9 h 21 and it has proven incidence of severe gastrointestinal side effects like metabolic acidosis 22,23 . Also, the drug is usually administered in larger doses of approximately 1.5-2.5g/day, the initial dose being 500 mg 24,25 . Hence, despite being the primary option and a less complicated oral hypoglycemic agent, Metformin Hydrochloride necessarily requires an effective delivery system that facilitates controlled release of the drug, thereby enhancing bioavailability.…”

mentioning

confidence: 99%

Untitled

2022

IJPSR

View full text Add to dashboard Cite

Diabetes Mellitus is a chronic metabolic disorder that has become increasingly evident, necessitating more stable and continuous therapeutic monitoring. Metformin Hydrochloride, being the primary treatment choice in type II Diabetes, presents certain limitations like improper GI absorption and the need for multiple dosing. Controlled drug delivery proves to be a better option in such conditions to provide an uninterrupted treatment. The present study is based on the development of oral controlled matrix tablets of Metformin. Plant-derived gums like Gum Okra, Gum Moringa, Gum Xanthan were extracted suitably and used as release controlling agents individually and in combination with Eudragit RL 100 in varying proportions. EC was employed to form a secondary backing layer. Thirteen formulations with polymers in different ratios were developed using the Wet granulation technique. The physicochemical properties of the prepared matrix tablets were found to be satisfactory. In-vitro release studies were performed in simulated media, 0.1 N HCl and Phosphate buffer, pH 6.8 and results have shown that formulation F11 containing Gum Moringa and Eudragit RL-100 (2:1 ratio) and EC layer exhibited the desired release of 99.46% ±0.75 throughout 24 h. Kinetic modelling of the dissolution data has shown that the drug release from the formulations followed Zero-order kinetics and shows the best fit to the Korsmeyer/Peppas model, representing the diffusion mechanism of drug release. The formulations were also found to be stable over the accelerated study period. INTRODUCTION:Drug delivery can be hypothesized as the technology utilized to present the drug/ pharmaceutical agent to the desired body site for release and absorption or the subsequent transport of the active ingredients across the biological membranes in a safe, efficient, accurate, reproducible and convenient manner 1, 2 .

show abstract

Formulation of a modified release metformin. HCl matrix tablet: influence of some hydrophilic polymers on release rate and in-vitro evaluation

Cited by 4 publications

References 29 publications

Formulation of Enteric Granules Containing Green Tea (Camellia Sinensis) Extract Using Eudragit L100-55 as a Delayed Release Matrix

Formulation of Enteric Granules Containing Green Tea (Camellia Sinensis) Extract Using Eudragit L100-55 as a Delayed Release Matrix

Formulation and evaluation of sustained release diclofenac sodium matrix tablets produced using <i>Brachystegia eurycoma </i>gum

Untitled

Contact Info

Product

Resources

About