Formulation and Evaluation of Oral Controlled Release Clarithromycin Matrix Tablets using Hydrophilic Polymer

2013 ◽  
Vol 6 (4) ◽  
pp. 2255-2259
Author(s):  
Suriyaprakash T N K ◽  
S. Lakshmana Prabu ◽  
Arumugarajan A ◽  
Sumathi A
Keyword(s):  
Phosphate Buffer ◽  
In Vitro Release ◽  
Release Profile ◽  
Matrix Tablets ◽  
Lauryl Sulfate ◽  
Dissolution Medium ◽  
Release Studies ◽  
The Matrix ◽  
Vitro Release

The objective of the present study was to develop clarithromycin tablets from polymeric hydrophilic matrices using methocel and characterization for its physic-chemical properties and in vitro release studies to optimize its release profile with the standard marketed product. Matrix tablets were prepared by wet granulation method using PVP and ethyl cellulose as binding agents. The matrix tablets were evaluated for its thickness, hardness, friability, weight variation, drug content and in vitro release studies. The drug delivery was analyzed using the paddle method in phosphate buffer pH 6.0 (dissolution medium I) and phosphate buffer pH 6.8 containing 0.5% sodium lauryl sulfate (dissolution medium II) and compared with USP dissolution limits. The dissolution release profile of formulation F9 was comparable with the market formulation and the difference factor and similarity factor f1 and f2 was found to be 2.44 and 83.18 in dissolution medium I; 1.44 and 89.71 in dissolution medium II. Stability studies were carried out as per ICH guidelines and tested for its physicochemical properties and in vitro studies. The study shows that the matrix method can be employed for preparing clarithromycin sustained release formulation using combination of hydrophilic polymers like Methocels and sodium carboxy methyl cellulose.

scholarly journals In vitro Release Kinetics Study of Ranolazine from Swellable Hydrophilic Matrix Tablets

1970 ◽  
Vol 8 (1) ◽  
pp. 31-38 ◽  
Author(s):  
Mohammad Nezab Uddin ◽  
Ishtiaq Ahmed ◽  
Monzurul Amin Roni ◽  
Muhammad Rashedul Islam ◽  
Mohammad Habibur Rahman ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
High Viscosity ◽  
Matrix Tablets ◽  
Release Studies ◽  
The Matrix ◽  
Vitro Release

The objective of this study was to design oral sustained release matrix tablets of Ranolazine usinghydroxypropyl methylcellulose (HPMC) as the retardant polymer and to study the effect of formulation factors suchas polymer proportion and polymer viscosity on the release of drug. In vitro release studies were performed usingUSP type II apparatus (paddle method) in 900 mL of 0.1N HCl at 100 rpm for 12 hours. The release kinetics wasanalyzed using the zero-order, first order, Higuchi and Korsmeyer-Peppas equations to explore and explain themechanism of drug release from the matrix tablets. In vitro release studies revealed that the release rate decreasedwith increase in polymer proportion and viscosity grade. Mathematical analysis of the release kinetics indicated thatthe nature of drug release from the matrix tablets was dependent on drug diffusion and polymer relaxation andtherefore followed non-Fickian or anomalous release. The developed controlled release matrix tablets of Ranolazineprepared with high viscosity HPMC extended release up to 12 hours.Key words: Ranolazine; Sustained release; Methocel E50 Premium LV; Methocel K100LV CR; Methocel K4M CR;Methocel K15M CR.DOI: 10.3329/dujps.v8i1.5333Dhaka Univ. J. Pharm. Sci. 8(1): 31-38, 2009 (June)

Preparation, Characterization and In vivo Evaluation of Rosuvastatin Calcium Loaded Solid Lipid Nanoparticles

2015 ◽  
Vol 8 (1) ◽  
pp. 2779-2785
Author(s):  
Kishan V ◽  
Suvarna G ◽  
Narender D
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Oral Bioavailability ◽  
Phosphate Buffer ◽  
In Vitro Release ◽  
Lipid Nanoparticles ◽  
Release Studies ◽  
First Pass ◽  
Vitro Release ◽  
Rosuvastatin Calcium

Rosuvastatin calcium (RC), is a hypolipidemic drug, and has poor oral bioavailability of about 20% due to first-pass effect. For improving the oral bioavailability of RC, solid lipid nanoparticles (SLNs) were developed using triglycerides (tristearin, tripalmitin, and trimyristin). Hot homogenization followed by ultrasonication method was used to prepare RC-SLNs. The prepared SLNs were characterized for particle size, PDI, zeta potential (ZP), entrapment efficiency (EE) and drug content. In vitro release studies were performed in 0.1N HCl and pH 6.8 phosphate buffer of by open tube method. Physical stability the SLNs was observed at refrigerated temperature and room temperature for 60 days. Pharmacokinetics of RC- SLNs after oral administration, in male Wistar rats was studied. SLNs prepared with tristearin (Dyanasan-118) having size of 207.3 ± 8.52 nm, PDI of 0.344 ± 0.084, ZP of – 20.9 ± 4.88 mV with 97.06 ± 0.210 % EE were optimized. Differential scanning calorimetric (DSC) study revealed that no interaction between drug and lipid. In vitro release studies showed that more cumulative release of RC in     pH 6.8 phosphate buffer than in 0.1NHCl during 24 hours. The lyophilized SLN formulation was used in knowing morphology of SLNs and was found to have spherical shape with increased polydispersity by Scanning electron microscopy. Pharmacokinetic studies showed the relative oral bioavailability of SLNs was 2.2 fold when compared to that of a suspension (p<0.001). Taken together, the results are indicative of SLNs as lipid based carriers for improving the oral bioavailability of this drug by minimizing first pass metabolism.

scholarly journals KINETIKA PERMEASI KLOTRIMAZOL DARI MATRIKS BASIS KRIM YANG MENGANDUNG VIRGIN COCONUT OIL (VCO)

2015 ◽  
Vol 2 (1) ◽  
pp. 14 ◽  
Author(s):  
Henny Lucida ◽  
Patihul Husni ◽  
Vinny Hosiana
Keyword(s):  
Rate Constant ◽  
In Vitro Release ◽  
Coconut Oil ◽  
Release Profile ◽  
Diffusion Cell ◽  
Virgin Coconut Oil ◽  
The Matrix ◽  
Base Matrix ◽  
Vitro Release

 ABSTRACT A kinetic study on the release of clotrimazole from a VCO containing creambase has been undertaken. The in-vitro release of the drug was studied by using a modification diffusion cell apparatus. Four formulations of clotrimazole cream were prepared, each contained either VCO or paraffin liquidum in the cream base. The amount of clotrimazole release were determined by UV spectrophotometer. Results showed that release of clotrimazole from all formulations followed Higuchi kinetics, the release rate constant from F1 (containing VCO) was significantly different than that from F1’ (containing paraffin liquidum) (p < 0.05). The rate constant of clotrimazole from F2 (containing VCO); F2’ (containing paraffin liquidum ) and F1 were not significantly different. Virgin coconut oil (VCO) was a potential cream base matrix regarding the release profile of clotrimazole from the matrix. Keywords : clotrimazol, VCO, permeation kinetic

Chronobiotic Hormone Melatonin: Comparative in vitro Release Studies from Matrix Tablets and Liposomal Formulations

2017 ◽  
Vol 14 (4) ◽  
pp. 476-480 ◽  
Author(s):  
Androniki Zampakola ◽  
Angeliki Siamidi ◽  
Natassa Pippa ◽  
Costas Demetzos ◽  
Marilena Vlachou
Keyword(s):  
In Vitro Release ◽  
Matrix Tablets ◽  
Liposomal Formulations ◽  
Release Studies ◽  
Vitro Release

scholarly journals Once Daily Sustained-Release Matrix Tablet of Naproxen: Formulation and In Vitro Evaluation

1970 ◽  
Vol 9 (1) ◽  
pp. 47-52 ◽  
Author(s):  
Muhammad Rashedul Islam ◽  
Ishtiaq Ahmed ◽  
Mohiuddin Abdul Quadir ◽  
Md Habibur Rahman
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
In Vitro Release ◽  
Matrix Tablets ◽  
Matrix Tablet ◽  
Once Daily ◽  
Weight Variation ◽  
Release Studies ◽  
The Matrix

The objective of the present study was to develop once-daily sustained-release matrix tablets of naproxen, one of the most potent non-steroidal anti-inflammatory agents used in the treatment of arthritic pain. The tablets were prepared by direct compression method using hydrophilic matrix materials like Methocel® K4M CR and Methocel® K15M CR. The tablets were subjected to measurement of thickness, diameter, weight variation, drug content, hardness and friability, the results of which were within compendial specification range. In vitro release studies were carried out by the USP basket method and were carried out at pH 7.4 buffer for ten hours. The results of dissolution studies indicated that higher polymer content in the matrix (40%) decreased the release rate of the drug as shown in formulation NMK4MF6 and NMK15MF6 (where lactose content is zero). The most successful formulations of the study, exhibited satisfactory drug release which was very close to the theoretical release profile. All the formulations exhibited diffusion-dominated drug release. Key words: Naproxen; Methocel® K4M CR; Methocel® K15M CR; Sustained release; Matrix tablets DOI: 10.3329/dujps.v9i1.7429 Dhaka Univ. J. Pharm. Sci. 9(1): 47-52 2010 (June)

Preparation and in vitro Evaluation of Bioadhesive Microparticulate System

1970 ◽  
Vol 1 (3) ◽  
pp. 257-266
Author(s):  
Nagda C. D. ◽  
Chotai N. P. ◽  
Patel S. B. ◽  
Soni T. J ◽  
Patel U. L
Keyword(s):  
Drug Loading ◽  
In Vitro Release ◽  
Phenyl Acetic Acid ◽  
Solvent Evaporation Method ◽  
Elimination Half ◽  
Release Studies ◽  
Differential Scanning Colorimetry ◽  
Polymer Interactions ◽  
Vitro Release

Aceclofenac (ACE) is NSAIDs of a phenyl acetic acid class. It is indicated in arthritis and osteoarthritis, rheumatoid arthritis, ankylosing spondylitis. It has short elimination half life of 4 hours. The objective of the study is to design, characterize and evaluate bioadhesive microspheres of ACE employing carbopol (CP) as bioadhesive polymer. Bioadhesive microspheres of ACE were prepared by solvent evaporation method. The prepared microspheres were free flowing and spherical in shape and characterized for drug loading, mucoadhesion test, infrared spectroscopy (IR), differential scanning colorimetry (DSC) and scanning electron microscopy (SEM). The in-vitro release studies were performed using pH 6.8 phosphate buffer. The drug loaded microspheres in a ratio of 1:5 showed 47% of drug entrapment; percentage mucoadhesion was 81% and 89% release in 10 h. The infrared spectra and DSC showed stable character of aceclofenac in the drug loaded microspheres and revealed the absence of drug-polymer interactions. SEM studies showed that the microspheres are spherical and porous in nature. The in vitro release profiles from microspheres of different polymer-drug ratios followed Higuchi model.

Development and In Vitro Characterization of Paclitaxel Loaded Solid Lipid Nanoparticles

2019 ◽  
Vol 9 (1) ◽  
pp. 76-85 ◽  
Author(s):  
R. Nithya ◽  
K. Siram ◽  
R. Hariprasad ◽  
H. Rahman
Keyword(s):  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
In Vitro Release ◽  
Lipid Nanoparticles ◽  
Release Profile ◽  
Mcf7 Cells ◽  
Solid Lipid ◽  
Cancerous Cells ◽  
Vitro Release

Background: Paclitaxel (PTX) is a potent anticancer drug which is highly effective against several cancers. Solid lipid nanoparticles (SLNs) loaded with anticancer drugs can enhance its toxicity against tumor cells at low concentrations. Objective: To develop and characterize SLNs of PTX (PSLN) to enhance its toxicity against cancerous cells. Method: The solubility of PTX was screened in various lipids. Solid lipid nanoparticles of PTX (PSLN) were developed by hot homogenization method using Cutina HR and Gelucire 44/14 as lipid carriers and Solutol HS 15 as a surfactant. PSLNs were characterized for size, morphology, zeta potential, entrapment efficiency, physical state of the drug and in vitro release profile in 7.4 pH phosphate buffer saline (PBS). The ability of PTX to enhance toxicity towards cancerous cells was tested by performing cytoxicity assay in MCF7 cell line. Results: Solubility studies of PTX in lipids indicated better solubility when Cutina HR and Gelucire 44/14 were used. PSLNs were found to possess a neutral zeta potential with a size range of 155.4 ± 10.7 nm to 641.9 ± 4.2 nm. In vitro release studies showed a sustained release profile for PSLN over a period of 48 hours. SLNs loaded with PTX were found to be more toxic in killing MCF7 cells at a lower concentration than the free PTX.

scholarly journals Development of nitazoxanide-loaded colon-targeted formulation for intestinal parasitic infections: centre composite design-based optimization and characterization

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Charu Bharti ◽  
Upendra Nagaich ◽  
Jaya Pandey ◽  
Suman Jain ◽  
Neha Jain
Keyword(s):  
Particle Size ◽  
Desirability Function ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
In Vitro Drug Release ◽  
Release Studies ◽  
Percentage Yield ◽  
Vitro Release ◽  
Selection Of

Abstract Background The current investigation is focused on the development and characterization of Eudragit S100 coated nitazoxanide-loaded microbeads as colon-targeted system utilizing central composite design (CCD) and desirability function. The study initiated with the selection of a BCS class II drug nitazoxanide and its preformulation screening with excipients, selection of polymer and identification of concentration for CCD, selection of optimized formulation based on desirability function, and in vitro release studies in simulated gastric and colonic media and stability studies. A two-factor, three-level CCD was employed with two independent variables, i.e. X1 (chitosan % w/v) and X2 (sodium tripolyphosphate % w/v), and three dependent variables, i.e. Y1 (particle size in micrometres), Y2 (percentage yield) and Y3 (percent entrapment efficiency), were chosen. Additionally, surface morphology, mucoadhesion and in vitro drug release studies were also conducted. Result Chitosan concentration showing maximum entrapment and optimum particle size was selected to formulate chitosan beads. The polynomial equation and model graphs obtained from the Design-Expert were utilized to examine the effect of independent variables on responses. The effect of formulation composition was found to be significant (p ˂ 0.05). Based on the desirability function, the optimized formulation was found to have 910.14 μm ± 1.03 particle size, 91.84% ± 0.64 percentage yield and 84.75% ± 0.38 entrapment efficiency with a desirability of 0.961. Furthermore, the formulations were characterized for in vitro drug release in simulated colonic media (2% rat caecal content) and have shown a sustained release of ∼ 92% up to 24 h as compared to in vitro release in simulated gastric fluid. Conclusion The possibility of formulation in enhancing percentage yield and entrapment efficiency of nitazoxanide and the utilization of CCD helps to effectively integrate nitazoxanide microbeads into a potential pharmaceutical dosage form for sustained release.

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