Fabrication and Analysis of Hydroxypropylmethyl Cellulose and Pectin‐Based Controlled Release Matrix Tablets Loaded with Loxoprofen Sodium

Zaman, Muhammad; Rasool, Shahid; Ali, Muhammad Yasir; Qureshi, Junaid; Adnan, Sherjeel; Hanif, Muhammad; Sarfraz, Rai Muhammad; Ijaz, Hira; Mahmood, Asif

doi:10.1002/adv.21493

Cited by 14 publications

(5 citation statements)

References 25 publications

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“…Therefore, by controlling the concentration of the polymer, thickness can be controlled, and hence the release of the drug. Findings of the current studies were in agreement with the stated claim, as the formulations with lower amounts of TAX released greater amounts of TZN HCl, and vice versa (figure 11) [24,43].…”

Section: In Vitro Drug Release Studiessupporting

confidence: 87%

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Synthesis of thiolated arabinoxylan and its application as sustained release mucoadhesive film former

et al. 2018

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The present work aimed to synthesize thiolated arabinoxylan (TAX), and to evaluate its mucoadhesive potential. Synthesis of TAX was accomplished by esterification of arabinoxylan (AX) with thioglycolic acid (TGA). The appearance of a characteristic peak at 2516 cm in the FTIR spectrum of TAX, and presence of 6.01 ± 1.03 m moles of thiol per gram of the polymer confirmed successful thiolation of AX. The incorporation of the thiol group considerably promoted mucoadhesive strength of the polymer-viz. 3.99-fold. Moreover, in vivo safety analysis in albino rats revealed TAX to be safe in the concentration range of 750-1000 mg kg body weight. Synthesized TAX was utilized to prepare Tizanidine HCl (TZN HCl) loaded sustained release (SR) mucoadhesive buccal films using a solvent casting technique. Results proved that the prepared films were of uniform thickness, good mechanical strength (with folding endurance >300), acceptable moisture contents (5%-7%) and surface pH (6.23 ± 0.81 to 6.43 ± 0.49) compatible to that of the buccal cavity. Presence of greater that 90% of drug contents indicated the excellent drug loading ability of the prepared films. Results of in vitro dissolution studies and ex vivo permeation studies conducted respectively by USP dissolution apparatus II and Franz diffusion cell indicated that sustained effect of TAX was achieved for 8 h. These results have conclusively proven that TAX has the potential to improve the bioavailability of TZN HCl due to enhanced mucoadhesion in buccal cavity, hence signifying its suitability as a mucoadhesive buccal film former.

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Section: In Vitro Drug Release Studiessupporting

confidence: 87%

“…A fixed funnel and cone method was used to measure the angle of repose [24]. A glass petri dish was placed on a flat surface, and a glass funnel fixed over it with the help of a tripod stand, in such a way that the distance between its tip and a paper surface was 20 mm.…”

Section: Angle Of Reposementioning

confidence: 99%

Synthesis of thiolated arabinoxylan and its application as sustained release mucoadhesive film former

et al. 2018

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“…Positive values of constant, which was the mean of the variable in the polynomial Equation , described that response was optimistic and results were signifying the impact of both independent variables, on the drug release (Figures e and ). HPMC E5 showed negative impact, which means that increase in the concentration of polymer would lower down the release of the drug . PEG 400 had shown positive effect and positive values predicted that increase in PEG 400 concentration would enhance the dissolution of MLX and hence the amount of the drug release.…”

Section: Resultsmentioning

confidence: 99%

“…However, cumulative percentage drug of initial 5 min was taken for analysis. [58] PEG 400 had shown positive effect and positive values predicted that increase in PEG 400 concentration would enhance the dissolution of MLX and hence the amount of the drug release. (a) Showing amount of drug released from F1 to F3, (b and c) showing amount of the drug released from F4 to F6 and from F7 to F9, respectively, while (d) describing permeated amount of drug through goat buccal mucosa from F2, F4, and F7 | 1831 ZAZAN ZANnd ZANNIF as the p value was less than .05 (.0460).…”

Section: Percent Drug Releasementioning

confidence: 99%

In vitro and ex vivo assessment of hydrophilic polymer‐ and plasticizer‐based thin buccal films designed by using central composite rotatable design for the delivery of meloxicam

Zaman

Hanif

2017

Adv Polym Technol

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The purpose of the study was to design a dosage form with ability to deliver drug immediately, hence providing rapid relief in certain pain ailments. Meloxicam (MLX) was selected as a model drug and buccal films were designed by using the solvent casting technique. A central composite rotatable design (CCRD) was used as a statistical tool to design and optimize the film formulations. No noticeable interaction was found between the drug and polymer when they were subjected to Fourier transform infrared spectroscopy (FTIR). Scanning electron microscopy (SEM) revealed the smooth surface of the film and uniform mixing of drug and polymer.X-ray diffractometry (XRD) was carried out to observe crystalline and amorphous nature of meloxicam. Differential scanning calorimetric (DSC) analysis was used to investigate the thermal behavior of free drug and drug-loaded formulation. The prepared film showed good mechanical property as folding endurance was found to be greater than 100 in all formulations. The cumulative drug release was found to be more than 80% in initial at dissolution time of 5 min, when the prepared films were subjected to dissolution studies in phosphate buffer at pH 6.8. Thus, it can be concluded that the hydrophilic polymer and plasticizer have definite impact on formulation and characteristics of rapidly dissolving buccal films and have the ability to prepare a suitable immediate release buccal film of meloxicam. K E Y W O R D Sbuccal films, drug delivery system, ex-vivo permeation, hydrophilic polymer, meloxicam, plasticizer, solvent casting method

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“…Due to the short elimination half-life of approximately 65 min [12], the commercial tablet of LXP has to be administrated three times a day to maintain the therapeutic concentration in plasma, which might cause high risks of gastrointestinal (GI) lesions and systemic side effects [13,14]. Several studies have been reported on the preparation of LXP sustained release dosage forms [15,16,17]. However, due to its high solubility, most of the preparations, especially for the matrix-based formulations, showed a burst release (drug release >30%) during the first 2 h [18], which could cause unexpected GI mucosal injury for patients.…”

Section: Introductionmentioning

confidence: 99%

Development and In Vitro-In Vivo Evaluation of a Novel Sustained-Release Loxoprofen Pellet with Double Coating Layer

et al. 2019

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This study aimed to develop a novel sustained release pellet of loxoprofen sodium (LXP) by coating a dissolution-rate controlling sub-layer containing hydroxypropyl methyl cellulose (HPMC) and citric acid, and a second diffusion-rate controlling layer containing aqueous dispersion of ethyl cellulose (ADEC) on the surface of a LXP conventional pellet, and to compare its performance in vivo with an immediate release tablet (Loxinon®). A three-level, three-factor Box-Behnken design and the response surface model (RSM) were used to investigate and optimize the effects of the citric acid content in the sub-layer, the sub-layer coating level, and the outer ADEC coating level on the in vitro release profiles of LXP sustained release pellets. The pharmacokinetic studies of the optimal sustained release pellets were performed in fasted beagle dogs using an immediate release tablet as a reference. The results illustrated that both the citric acid (CA) and ADEC as the dissolution- and diffusion-rate controlling materials significantly decreased the drug release rate. The optimal formulation showed a pH-independent drug release in media at pH above 4.5 and a slightly slow release in acid medium. The pharmacokinetic studies revealed that a more stable and prolonged plasma drug concentration profile of the optimal pellets was achieved, with a relative bioavaibility of 87.16% compared with the conventional tablets. This article provided a novel concept of two-step control of the release rate of LXP, which showed a sustained release both in vitro and in vivo.

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Fabrication and Analysis of Hydroxypropylmethyl Cellulose and Pectin‐Based Controlled Release Matrix Tablets Loaded with Loxoprofen Sodium

Cited by 14 publications

References 25 publications

Synthesis of thiolated arabinoxylan and its application as sustained release mucoadhesive film former

Synthesis of thiolated arabinoxylan and its application as sustained release mucoadhesive film former

In vitro and ex vivo assessment of hydrophilic polymer‐ and plasticizer‐based thin buccal films designed by using central composite rotatable design for the delivery of meloxicam

Development and In Vitro-In Vivo Evaluation of a Novel Sustained-Release Loxoprofen Pellet with Double Coating Layer

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