Design and statistical optimization of an effervescent floating drug delivery system of theophylline using response surface methodology

Meka, Venkata Srikanth; Li, Chew Ee; Sheshala, Ravi

doi:10.1515/acph-2016-0002

Cited by 4 publications

(4 citation statements)

References 21 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The dissolution data were fitted into the different drug release kinetic models (zero order, first order, Higuchi, Hixson-Crowell, and Korsmeyer–Peppas model) to evaluate the rate and mechanism of drug release from the matrix tablets [ 20 ]. The order and mechanism of drug release from the matrix system were determined based on regression (R 2 ) values [ 21 ].…”

Section: Methodsmentioning

confidence: 99%

“…The GRDDS has many advantages such as reduced fluctuations in plasma drug levels, increased gastric retention times, enhanced drug absorption within the stomach, higher bioavailability, an improvement in therapeutic effectiveness, controlled release of active substances in the upper part of gastrointestinal (GI) tract and improvement of reduction in drug administration frequency [ 3 – 5 ]. Drug candidates that can benefit from such approach include (a) drugs with narrow absorption window in the upper part of the GIT, (b) acidic drugs, (c) drugs for local action in the stomach, (d) drugs that degrade at higher pH, (e) drugs with poor solubility at higher pH, (f) drugs which degrade in the intestine and colon, and (g) drugs with low biological half-life [ 6 ].…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Design, development and optimization of sustained release floating, bioadhesive and swellable matrix tablet of ranitidine hydrochloride

2021

View full text Add to dashboard Cite

Ranitidine HCl, a selective, competitive histamine H2-receptor antagonist with a short biological half-life, low bioavailability and narrow absorption window, is an ideal candidate for gastro-retentive drug delivery system (GRDDS). Controlled release with an optimum retentive formulation in the upper stomach would be an ideal formulation for this drug. The aim of the present study was therefore to develop, formulate and optimize floating, bioadhesive, and swellable matrix tablets of ranitidine HCl. The matrix tablets were prepared using a combination of hydroxypropyl methylcellulose (HPMC) and sodium carboxymethyl cellulose (NaCMC) as release retarding polymers, sodium bicarbonate (NaHCO3) as gas generating agent and microcrystalline cellulose (MCC) as direct compression diluent. Central composite design (CCD) was used to optimize the formulation and a total of thirteen formulations were prepared. Concentration of HPMC/NaCMC (3:1) (X1) and NaHCO3 (X2) were selected as independent variables; and floating lag time (Y1), bioadhesive strength (Y2), swelling index at 12 h (Y3), cumulative drug release at 1 h (Y4), time to 50% drug release (t50%) (Y5) and cumulative drug release at 12 h (Y6) were taken as the response variables. The optimized batch showed floating lag time of 5.09 sec, bioadhesive strength of 29.69 g, swelling index of 315.04% at 12 h, t50% of 3.86 h and drug release of 24.21% and 93.65% at 1h and 12 h, respectively, with anomalous release mechanism. The results indicate that sustained release matrix tablet of ranitidine HCl with combined floating, bioadhesive and swelling gastro-retentive properties can be considered as a strategy to overcome the low bioavailability and in vivo variation associated with the conventional ranitidine HCl tablet.

show abstract

Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Design, development and optimization of sustained release floating, bioadhesive and swellable matrix tablet of ranitidine hydrochloride

2021

View full text Add to dashboard Cite

show abstract

“…Amongst these are the gastroretentive tablet matrices based on novel floating, high density, bioadhesive or swellable delivery technologies for improving the absorption and pharmacotherapeutic benefits of bioactive molecules (Bera et al, 2019). They have been utilized as release retardants (Meka et al, 2016), combination coats (Czarnocka and Alhnan, 2015) and matrix forming agents (Singh and Saini, 2016) in gastroretentive tablet formulations (Fig. 3(c)).…”

Section: Macro-structured Delivery Systems Fabricated From Ethylcellumentioning

confidence: 99%

Premium ethylcellulose polymer based architectures at work in drug delivery

Adeleke

2019

International Journal of Pharmaceutics: X

View full text Add to dashboard Cite

show abstract

“…Although several works have formulated theophylline floating delivery, many as directly compressible tablets, capsules, microbeads and as suspension, this original work was aimed at preparing sustained release effervescent floating tablet matrix of theophylline after wet granulation method and then determine the effect of HPMC concentration on ideal buoyancy and drug release [6,8,9].…”

Section: Fig 1: Chemical Structure Of Theophyllinementioning

confidence: 99%

Formulation and in-Vitro Evaluation of Theophylline Hydrochloride Effervescent Floating Tablets: Effect of Polymer Concentration on Tablet Buoyancy

Akpabio

Effiong

Uwah

et al. 2019

Int J Pharm Pharm Sci

View full text Add to dashboard Cite

Objective: This study was undertaken to formulate a floating drug delivery system of theophylline hydrochloride using different concentrations of a chosen polymer and then investigate how polymer concentration affects buoyancy and drug release properties of the tablets. Methods: Hydroxypropyl methylcellulose (HPMC) at different concentration levels of 15% (F1), 20% (F2) and 30% (F3) was used to form the three formulation batches of floating tablets. Wet granulation method was used for the granule preparation while Sodium bicarbonate and citric acid were used as the gas generating agent. The physical properties of the granules and the floating tablets were evaluated. Also determined were the physicomechanical properties, buoyancy and swelling characteristics of the tablets. The in vitro drug release study was carried out according to the USP I (basket method) for 8h in 900 ml 0.1N HCl at 50 rpm. Samples withdrawn at the regular predetermined time were analyzed spectrophotometrically at a wavelength of 271 nm and data obtained statistically analyzed by one-way analysis of variance (ANOVA). The differences between means were considered significant at P<0.05. Results: The result showed that polymer (HPMC) concentration significantly (p>0.05) increased swelling index and improved floating lag time, it had no significant effect on the total floating time. Percentage drug release at the end of 8 h was 100%, 98.2% and 96.13% for formulation F1, F2 and F3, respectively. All three formulations followed the Higuchi drug release kinetics model and the mechanism of drug release was the non Fickian diffusion with exponents of 0.46, 0.51 and 0.56 for the respective batch. Conclusion: Batch F3 gave a better-controlled drug release and floating properties in comparison to batch F1 and F2 thus Polymer concentration influenced the onset of floating and controlled the release of Theophylline.

show abstract

Design and statistical optimization of an effervescent floating drug delivery system of theophylline using response surface methodology

Abstract: V. Srikanth Meka et al.: Design and statistical optimization of an eff ervescent fl oating drug delivery system of theophylline using response surface methodology, Acta Pharm. 66 (2016) 35-51.

Cited by 4 publications

References 21 publications

Design, development and optimization of sustained release floating, bioadhesive and swellable matrix tablet of ranitidine hydrochloride

Design, development and optimization of sustained release floating, bioadhesive and swellable matrix tablet of ranitidine hydrochloride

Premium ethylcellulose polymer based architectures at work in drug delivery

Formulation and in-Vitro Evaluation of Theophylline Hydrochloride Effervescent Floating Tablets: Effect of Polymer Concentration on Tablet Buoyancy

Contact Info

Product

Resources

About