Release kinetics of highly porous floating tablets containing cilostazol

Hwang, Kyu-Mok; Cho, Cheol-Hee; Tung, Nguyen-Thach; Kim, Ju‐Young; Rhee, Yun-Seok; Park, Eun-Seok

doi:10.1016/j.ejpb.2017.01.027

Cited by 34 publications

(14 citation statements)

References 42 publications

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“…Similarly, the Carr's index, which is an indicator of compressibility of powders, showed good flow properties of all four formulations. It should be noted that the standard deviations for repose angles, Hausner's ratio and Carr's index were very small, suggesting a homogenous powder mixing with uniform particle size of components [23]. Overall, HPMC K4M based powder blend (F1) showed excellent flow properties as compared with other three viscosity grades of HPMC.…”

Section: Micromeritic Studiesmentioning

confidence: 92%

Relevancy of Nizatidine Release from Floating Tablets with Viscosity of Various Cellulose Ethers

Shahzad¹,

Ibrar²,

Hussain³

et al. 2019

Sci

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Nizatidine is a gastroprotective drug with a short biological half-life and narrow absorption window. This study aimed at developing floating tablets of nizatidine using various HPMC viscosity grades, namely K4M, E4M, K15 and K200M. Directly compressed tablets revealed an excellent uniformity in hardness, thickness and weight and nizatidine was evenly distributed within the matrix floating tablets. Buoyancy study revealed floating lag time as low as 18–38 s, and tablets remain buoyant for upto 24 h. However, the later depended upon viscosity grade of HPMC and that the higher the viscosity, the less was the total floating time. In vitro dissolution indicated viscosity dependent nizatidine release from the floating tablets. HPMC K4M and E4M based floating tablets released almost 100% drug in 12 h, whilst higher viscosity polymers such as K15 and K200M only released 81.88% and 75.81% drug, respectively. The drug release followed non-Fickian diffusion from tablets formulated with K4M, K15 and K200M, whilst super case II transport was observed with E4M based tablets. More interestingly, K4M and E4M polymers have similar viscosity yet exhibited different drug release mechanism. This was attributed to the difference in degree of substitution of methoxyl- and hydroxypropoxyl- groups on polymer backbone.

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Section: Micromeritic Studiesmentioning

confidence: 92%

Relevancy of Nizatidine Release from Floating Tablets with Viscosity of Various Cellulose Ethers

Shahzad¹,

Ibrar²,

Hussain³

et al. 2019

Sci

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“…Pharmaceutics 2021, 13, x FOR PEER REVIEW 2 of 37 window in the proximal small intestine, stability and/or solubility issues at alkaline intestinal pH, a short half-life and/or a local activity at the upper part of the intestine for the eradication of Helicobacter pylori [9,[13][14][15][16][17][18][19][20][21]. GRDDS can either be controlled-release systems intrinsically or coupled with such technologies to ensure a controlled release of drugs.…”

Section: The Stomachmentioning

confidence: 99%

Gastroretentive Technologies in Tandem with Controlled-Release Strategies: A Potent Answer to Oral Drug Bioavailability and Patient Compliance Implications

2021

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There have been many efforts to improve oral drug bioavailability and therapeutic efficacy and patient compliance. A variety of controlled-release oral delivery systems have been developed to meet these needs. Gastroretentive drug delivery technologies have the potential to achieve retention of the dosage form in the upper gastrointestinal tract (GIT) that can be sufficient to ensure complete solubilisation of the drugs in the stomach fluids, followed by subsequent absorption in the stomach or proximal small intestine. This can be beneficial for drugs that have an “absorption window” or are absorbed to a different extent in various segments of the GIT. Therefore, gastroretentive technologies in tandem with controlled-release strategies could enhance both the therapeutic efficacy of many drugs and improve patient compliance through a reduction in dosing frequency. The paper reviews different gastroretentive drug delivery technologies and controlled-release strategies that can be combined and summarises examples of formulations currently in clinical development and commercially available gastroretentive controlled-release products. The different parameters that need to be considered and monitored during formulation development for these pharmaceutical applications are highlighted.

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“…The tablets which were prepared with l-menthol exhibited significant lower bulk density values than those prepared using camphor. It could be deduced that larger pores could be created after menthol sublimation, compared to those created after camphor sublimation resulting in a lower bulk density 33 . On the other hand, increasing the sublimable agent concentration was accompanied with a decrease in tablet density.…”

Section: Densitymentioning

confidence: 99%

Low density alfuzosin hydrochloride floating tablets: in vitro characterization and in vivo gastroretentive MRI tracking in healthy volunteers

El-Aziz¹,

Ismail²,

Tadros³

et al. 2021

Pharm Sci Asia

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The current work aimed to develop promising floating sustained release systems for alfuzosin hydrochloride (ALF) utilizing sublimation technique. Gastroretentive tablets were prepared by direct compression and subsequent sublimation of the loaded sublimable agents. Polyethylene oxide WSR N-60K (PEO) or Carbopol 934 (CP) were used as release retarding polymers. Camphor or menthol were used as sublimable agents at concentrations of 3%, 6%, 9% or 12% w/w. FTIR and DSC were performed to check possible drug-excipients incompatibility. The tablets were evaluated for appearance, hardness, friability, density, floating characters, and in-vitro drug release. The drug release percentages after 0.5h (Q0.5h) and 8h (Q8h) were estimated. Based on estimation of the desirability values, the best-achieved formula (F1) was morphologically evaluated via SEM. The gastroretentive tracking of the magnetite-loaded F1 tablets was performed via MRI in healthy human volunteers. FT-IR spectra and DSC thermograms confirmed drug-excipients compatibility. PEO-and CP-based systems exhibited acceptable physicochemical characteristics regarding their appearance, hardness and friability. They exhibited low bulk density values (< 1 g/cm 3 ) allowing them to float spontaneously (zero lag times), for at least 8h. Significantly higher (p<0.0001) Q0.5h were revealed with CP-based tablets. No significant difference (p=0.3529) was elucidated between Q8h values of the corresponding CP-based and PEO-based tablets. Following sublimation, SEM micrographs of F1 confirmed the presence of a low bulk density porous matrix. The gastroretentive potential of F1 was suggested for at least 5 h in healthy human volunteers. F1 is a promising gastroretentive system for ALF.

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Release kinetics of highly porous floating tablets containing cilostazol

Cited by 34 publications

References 42 publications

Relevancy of Nizatidine Release from Floating Tablets with Viscosity of Various Cellulose Ethers

Relevancy of Nizatidine Release from Floating Tablets with Viscosity of Various Cellulose Ethers

Gastroretentive Technologies in Tandem with Controlled-Release Strategies: A Potent Answer to Oral Drug Bioavailability and Patient Compliance Implications

Low density alfuzosin hydrochloride floating tablets: in vitro characterization and in vivo gastroretentive MRI tracking in healthy volunteers

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