Design, Fabrication and Evaluation of Drug Release Kinetics from Aceclofenac Matrix Tablets using Hydroxypropyl Methyl Cellulose

Kabir, Alamgir; Biswas, Bishyajit Kumar; Rouf, Abu Shara Shasur

doi:10.3329/dujps.v8i1.5332

Cited by 8 publications

(5 citation statements)

References 8 publications

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“…[30] In contrast, formulations containing CA F4 to F6 showed release exponent ranging from 0.6534 to 0.824 indicating anomalous transport (nonFickian) as that of F2 and F3. were within the limit at long-term condition and as well as at accelerated condition.…”

Section: Resultsmentioning

confidence: 94%

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The effect of hydrophilic and hydrophobic polymers on release profiles of diclofenac sodium from matrix tablets

Islam¹,

Hossain²,

Ahmed³

et al. 2013

Arch Pharma Pract

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Objective:The current study aimed to develop a matrix type sustained release Diclofenac tablet, using hydrophilic hydroxypropyl methylcellulose (HPMC) and hydrophobic polymer cetyl alcohol (CA). Materials and Methods: Two different polymers, that is, Methocel K15MCR ® and CA were used in various proportions as release controlling factor. Matrix tablets were prepared by wet granulation technique. The physicochemical properties of the granules and tablets were evaluated. In vitro dissolution studies of prepared matrix tablet and patent product Voltaren SR ® tablet (VSR) were performed at pH 7.4 phosphate buffer at 100 rpm, and at 37 ± 0.5°C, and subjected to in vitro bioequivalence study in terms of similarity and difference factors. Stability studies were conducted for 6 months using optimized formulation for extended period of time, both at room temperature and accelerated conditions. The dissolution data were fit to Zero-order, First-order, Higuchi, and Korsmeyer-Peppas' equations. Results: The formulated tablets showed acceptable weight variation, hardness, drug content uniformity with sustained release matrix characteristics. Hydrophilic Methocel K15 MCR ® matrices-based tablets showed zero-order and hydrophobic CA matrices-based tablets followed first-order kinetics except for formulation six (F6 showed zero-order profile). It was found that formulations containing CA showed better dissolution properties with respect to formulations containing Methocel K15 MCR ® in terms of similarity and difference factor. Furthermore, the formulations F4, F5, and F6 exhibited similar drug release profile as compared with VSR tablet, which indicated that these formulations could be bioequivalent with VSR tablet in vitro. Tablets were stable both at room temperature and as well as at accelerated conditions. Conclusion: The present study demonstrated that Diclofenac could be successfully prepared using an appropriate amount of Methocel K15 MCR ® and CA in the form of matrix tablets with similar dissolution profile of patent product Voltaren SR ® . The type of polymers used was found to induce a profound effect on release rate and mechanism.

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Section: Resultsmentioning

confidence: 94%

“…Analogous result was also demonstrated by earlier investigators. [30] To evaluate the release kinetics of DS from different formulations, obtained drug release data were extrapolated by zero-order, first-order, and the Higuchi equation. [20,21] The results are summarized in Table 4 and Figures 1-3.…”

Section: Resultsmentioning

confidence: 99%

The effect of hydrophilic and hydrophobic polymers on release profiles of diclofenac sodium from matrix tablets

Islam¹,

Hossain²,

Ahmed³

et al. 2013

Arch Pharma Pract

View full text Add to dashboard Cite

show abstract

“…Sodium CMC microspheres gave a relatively fast release as compared to Methocel microspheres, due to rapid swelling and rapid dissolution of Sodium CMC in the dissolution medium [28]. Also, the hydration rate of Methocel is higher and it forms a strong viscous gel when in contact with aqueous media which may retard the drug release [29]. …”

Section: Resultsmentioning

confidence: 99%

An Improvement of Efficacy of Moxifloxacin HCl for the Treatment of Bacterial Keratitis by Formulation of Ocular Mucoadhesive Microspheres

Dandagi

Belekar²,

Mastiholimath³

et al. 2013

Sci. Pharm.

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The aim of this study was to prepare novel ocular mucoadhesive microspheres of Moxifloxacin HCl to increase its residence time on the ocular surface and to enhance its therapeutic efficacy in ocular bacterial keratitis. Microspheres were fabricated with different grades of Methocel and Sodium CMC as polymers. Microspheres were evaluated for their particle size, morphology, encapsulation efficiency, mucoadhesion, antimicrobial efficacy, and in vitro drug release studies. In vivo studies were carried out for the promising formulation on eyes of albino rabbits by inducing bacterial keratitis. A sterile microspheres suspension in light mineral oil was applied to infected eyes twice a day. A marketed conventional eye drop was used as a positive control. Eyes were examined daily for improvement of clinical signs of bacterial keratitis by an ophthalmologist. The average particle size of microspheres was found to be less than 80 μm. Methocel microspheres were found to have a smoother surface than Sodium CMC. Entrapment efficiency was enhanced with an increased polymer concentration and viscosity. The formulation containing Methocel K100M with a drug: polymer ratio of 1:2 exerted longer corneal and conjunctival mucoadhesion time of 8.45±0.15 h and 9.40±0.53 h respectively. In vitro release of Moxifloxacin HCl from microspheres was retarded with increased viscosity and concentration of polymers, and was controlled by diffusion as well as polymer relaxation. All formulations showed comparable antimicrobial activity in comparison with conventional marketed eye drops. The formulation containing Methocel K100M with a drug: polymer ratio of 1:2 was found to be a promising formulation and was used for the in vivo studies. The in vivo studies revealed that microspheres demonstrated significantly lower clinical scores and reduced the total duration of therapy than the marketed Moxifloxacin HCl eye drops. In vitro and in vivo studies showed that ocular mucoadhesive microspheres of Moxifloxacin HCl were found to have an improved efficacy in the treatment of ocular bacterial keratitis in comparison with the marketed formulation.

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“…A micrometer was used to measure the thickness of ten different tablets. The mean ± SD values were calculated [25]. In packing operations and in counting tablets, filling equipment was utilized that employs the uniform thickness of the tablets as a counting mechanism.…”

Section: Thicknessmentioning

confidence: 99%

Tolmetin Sodium Fast Dissolving Tablets for Rheumatoid Arthritis Treatment: Preparation and Optimization Using Box-Behnken Design and Response Surface Methodology

et al. 2022

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Tolmetin sodium (TLM) is a non-steroidal anti-inflammatory drug (NSAIDs). TLM is used to treat inflammation, skeletal muscle injuries, and discomfort associated with bone disorders. Because of the delayed absorption from the gastro intestinal tract (GIT), the currently available TLM dosage forms have a rather protracted start to the effect, according to pharmacokinetic studies. The aim of this study was to create a combination for TLM fast dissolving tablets (TLM-FDT) that would boost the drug’s bioavailability by increasing pre-gastric absorption. The TLM-FDTs were developed using a Box-Behnken experimental design with varied doses of crospovidone (CP), croscarmellose sodium (CCS) as super-disintegrants, and camphor as a sublimating agent. In addition, the current study used response surface approach to explore the influence of various formulation and process factors on tablet qualities in order to verify an optimized TLM-FDTs formulation. The optimized TLM-FDTs formula was subsequently evaluated for its in vivo anti-inflammatory activity. TLM-FDTs have good friability, disintegration time, drug release, and wetting time, as well as fast disintegration and dissolution behavior. Significant increase in drug bioavailability and reliable anti-inflammatory efficacy were also observed, as evidenced by considerable reductions in paw thickness in rats following carrageenan-induced rat paw edema. For optimizing and analyzing the effect of super-disintegrants and sublimating agents in the TLM-FDTs formula, the three-factor, three-level full factorial design is a suitable tool. TLM-FDTs are a possible drug delivery system for enhancing TLM bioavailability and could be used to treat rheumatoid arthritis.

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Design, Fabrication and Evaluation of Drug Release Kinetics from Aceclofenac Matrix Tablets using Hydroxypropyl Methyl Cellulose

Cited by 8 publications

References 8 publications

The effect of hydrophilic and hydrophobic polymers on release profiles of diclofenac sodium from matrix tablets

The effect of hydrophilic and hydrophobic polymers on release profiles of diclofenac sodium from matrix tablets

An Improvement of Efficacy of Moxifloxacin HCl for the Treatment of Bacterial Keratitis by Formulation of Ocular Mucoadhesive Microspheres

Tolmetin Sodium Fast Dissolving Tablets for Rheumatoid Arthritis Treatment: Preparation and Optimization Using Box-Behnken Design and Response Surface Methodology

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