scholarly journals PHYSICO-MECHANICAL AND RELEASE PROPERTIES OF SUSTAINED RELEASE ARTESUNATE TABLETS IN HYDROXYPROPYL METHYLCELLULOSE MATRIX

2018 ◽  
Vol 10 (1) ◽  
pp. 103 ◽  
Author(s):  
Musiliu Adedokun ◽  
Benjamin Onah ◽  
Anthony Attama
Keyword(s):  
Sustained Release ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Angle Of Repose ◽  
Simulated Gastric Fluid ◽  
Release Mechanism ◽  
Average Weight ◽  
Significant Difference ◽  
Vitro Release

Objective: This work was aimed at formulating artesunate tablets with hydroxypropyl methylcellulose (HPMC)-a hydrophilic polymer for the purpose of achieving a sustained release profile of the drug and evaluating their properties.Methods: The solubility profile of artesunate was determined in water, methanol, ethanol, ethanol/water mixtures (50/50, 40/60 v/v), simulated intestinal fluid (SIF) without enzymes (pH 7, 7.2 and 8), simulated gastric fluid (SGF) without enzymes (pH 1.2), 0.1N hydrochloric acid (HCI), 0.1N sodium hydroxide (NaOH), 0.1N acetic acid and phosphate buffer solution, PBS (pH 7, 7.2 and 8). Four batches of oral sustained release artesunate tablets intended for once-daily dosing were formulated with 10%, 20%, 25% and 30% w/w concentrations of HPMC using wet granulation method. Evaluation of granule properties was done by determining the angle of repose, flow rate, bulk density, tapped density, Carr’s index and Hausner’s quotient. The compressed tablets were also evaluated using official and non-official parameters. Absolute drug contents were determined in 0.1N NaOH, ethanol and methanol. In vitro release was studied in different media and release kinetics mechanism elucidated. In vivo studies were carried out using healthy Wistar rats.Results: Artesunate was observed to exhibit solubility at varying degrees depending on solvents or media employed as well as the pH of the media. All the granule batches have Hausner’s quotient value of approximately 1.2. The values for Carr’s index for all the batches ranged between 30 and 40. The angle of repose, Carr’s index and Hausner’s quotient values indicate good flow properties of the granules for all the batches. All the tablet batches conformed to official standard in terms of weight uniformity as no single tablet deviated beyond 5% from the average weight in each batch with no significant difference in the values (p>0.05). Values of hardness increased insignificantly from batches A to D (p>0.05). Friability values were very low and follows no specific pattern among the batches but the difference in the values was significant (p<0.05). Absolute drug content reduced while in vitro release times increased as hardness increased, indicating the probable progressive reduction in the tendency of the matrix to release the drug as the concentration of HPMC increased from batches A to D. n values obtained from analysis of release mechanism were above 0.89 for each batch.Conclusion: The release mechanism was shown to be complex and the release involved zero order, first order, and Higuchi model kinetics. The biological half-life of artesunate was shown to be 1.05 hr, and metabolites which bear resemblance to artesunate in absorbance seem to be encountered. In this work, HPMC matrix yielded high-quality tablets indicating its usefulness in sustained released product development.

Formulation and Evaluation of Sustained Release Dosage Forms of Norfloxacin

2018 ◽  
Vol 11 (6) ◽  
pp. 4331-4337
Author(s):  
C Suja ◽  
Sismy C
Keyword(s):  
Sustained Release ◽  
Guar Gum ◽  
In Vitro Release ◽  
Angle Of Repose ◽  
Prolonged Release ◽  
Weight Variation ◽  
Sustained Release Tablets ◽  
Release Study ◽  
Vitro Release

The goal of this study was to formulate and evaluate norfloxacin sustained release tablets. Norfloxacin sustained release tablets were prepared by wet granulation method using two polymers such as HPMC K 100 M (hydrophilic polymer) and guar gum (natural polymer) and with three polymer ratios (0.5, 1.0 and 1.5). The prepared granules were evaluated to preformulation studies such as angle of repose, bulk density, tapped density, bulkiness, compressibility index and Hauser’s ratio. All the parameters shows that the granules having good flow properties. Then the formulated tablets were taken to evaluation studies such as hardness, weight variation, friability, drug content and thickness. All the parameters were within the acceptable limits. IR spectral analysis showed that there was no interaction between the drug and polymers. The in vitro release study was performed in phosphate buffer pH 7.4 at 293 nm. The in vitro release study showed that if the polymer ratio is increased, then the release of the drug is prolonged. HPMC K 100M shows a prolonged release when compared to guar gum.

scholarly journals FABRICATION OF NANO CLAY INTERCALATED POLYMERIC MICROBEADS FOR CONTROLLED RELEASE OF CURCUMIN

2021 ◽  
pp. 206-215
Author(s):  
DHARMENDER PALLERLA ◽  
SUMAN BANOTH ◽  
SUNKARI JYOTHI
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Controlled Drug Release ◽  
Fickian Diffusion ◽  
Simulated Gastric Fluid ◽  
Release Mechanism ◽  
Release Studies ◽  
Swelling Studies ◽  
Vitro Release

Objective: The objective of this study was to formulate and evaluate the Curcumin (CUR) encapsulated sodium alginate (SA)/badam gum (BG)/kaolin (KA) microbeads for controlled drug release studies. Methods: The fabricated microbeads were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), X-ray diffraction (X-RD), and scanning electron microscopy (SEM). Dynamic swelling studies and in vitro release kinetics were performed in simulated intestinal fluid (pH 7.4) and simulated gastric fluid (pH 1.2) at 37 °C. Results: FTIR confirms the formation of microbeads. DSC studies confirm the polymorphism of CUR in drug loaded microbeads which indicate the molecular level dispersion of the drug in the microbeads. SEM studies confirmed the microbeads are spherical in shape with wrinkled and rough surfaces. XRD studies reveal the molecular dispersion of CUR and the presence of KA in the developed microbeads. In vitro release studies and swelling studies depend on the pH of test media, which might be suitable for intestinal drug delivery. The % of drug release values fit into the Korsmeyer-Peppas equation and n values are obtained in the range of 0.577-0.664, which indicates that the developed microbeads follow the non-Fickian diffusion drug release mechanism. Conclusion: The results concluded that the CUR encapsulated microbeads are potentially good carriers for controlled drug release studies.

scholarly journals Formulation and Evaluation of Microsponge Based Nicorandil Sustained Released Tablet

2017 ◽  
Vol 9 (3) ◽  
pp. 285-296
Author(s):  
S. S. Patel ◽  
M. R. Patel ◽  
M. J. Patel
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Fickian Diffusion ◽  
Diffusion Method ◽  
P Value ◽  
Once Daily ◽  
Release Studies ◽  
Significant Difference ◽  
Vitro Release

The aim of the present work was to develop once-daily sustained release microsponges formulations of Nicorandil, a potent potassium channel opener used in cardiovascular diseases and it has low oral bioavailability (70%) and half-life 1 h. So, it is good candidate for sustained release formulations based on microsponge technology. The microsponges were prepared by using quasi-emulsion solvent diffusion method. Scanning Electron Microscopy (SEM) revealed that the microsponges of nicorandil with Eudragit - RSPO and HPMC K100M were smooth, porous, glossy and discrete spherical. The actual drug content and encapsulation efficiency of batch M1 to M9 were obtained in range of 62.05 ± 0.31 to 80.69 ± 0.43 and 64.41 ± 1.71 to 70.58 ± 1.12, respectively. The microsponges formulations were subjected to in-vitro release studies and the results were evaluated kinetically and statically. The best fitted model was found to be Korsmeyer - Peppas model (R2 = 0.9992) for M6 batch.  The ‘n’ value for Korsmeyer - Peppas model was between 0.5 and 1.0 which is indicative of non-Fickian diffusion. Statistical analysis using ANOVA yielded a p value of 0.572 for all the formulations, indicating that there was no significant difference among them.

Formulation and Evaluation of Mefloquine Hydrochloride Nanoparticles

2014 ◽  
Vol 7 (1) ◽  
pp. 2377-2386
Author(s):  
Dilip Kumar Gupta ◽  
B K Razdan ◽  
Meenakshi Bajpai
Keyword(s):  
Particle Size ◽  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Taste Masking ◽  
Diffusion Method ◽  
Drug Entrapment Efficiency ◽  
Resistant Strains ◽  
Vitro Release

The present study deals with the formulation and evaluation of mefloquine hydrochloride nanoparticles. Mefloquine is a blood schizonticidal quinoline compound, which is indicated for the treatment of mild-to-moderate acute malarial infections caused by mefloquine-susceptible multi-resistant strains of P. falciparum and P. vivax. The purpose of the present work is to minimize the dosing frequency, taste masking toxicity and to improve the therapeutic efficacy by formulating mefloquine HCl nanoparticles. Mefloquine nanoparticles were formulated by emulsion diffusion method using polymer poly(ε-caprolactone) with six different formulations. Nanoparticles were characterized by determining its particle size, polydispersity index, drug entrapment efficiency, drug content, particle morphological character and drug release. The particle size ranged between 100 nm to 240 nm. Drug entrapment efficacy was >95%. The in-vitro release of nanoparticles were carried out which exhibited a sustained release of mefloquine HCl from nanoparticles up to 24 hrs. The results showed that nanoparticles can be a promising drug delivery system for sustained release of mefloquine HCl.

Formulation and Evaluation of Itopride Hydrochloride Floating Beads for Gastroretentive Delivery

2013 ◽  
Vol 6 (4) ◽  
pp. 2269-2280
Author(s):  
Nagratna Dhople ◽  
P N Dandag ◽  
A P Gadad ◽  
C K Pandey ◽  
Masthiholimath V S
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Sustained Release Formulation ◽  
Prokinetic Drug ◽  
Drug Entrapment Efficiency ◽  
Itopride Hydrochloride ◽  
Vitro Release

A gastroretentive sustained release system of itopride hydrochloride was formulated to increase the gastric residence time and modulate its release behavior. Itopride hydrochloride is a prokinetic drug used in the treatment of gastroeosophageal reflux disease, Non-ulcer dyspepsia and as an antiemetic. Hence, itopride hydrochloride beads were prepared by emulsion gelation method by employing low methoxy pectin and sodium alginate as sustained release polymers in three different ratios alone and in combination and sunflower oil was used to enable floating property to the beads. The effect of variation in polymer and their concentration was investigated. The beads were evaluated for production yield, particle size, swelling index, density measurement, buoyancy, drug content, drug entrapment efficiency, in vitro release characteristics and release kinetic study. Based on drug entrapment efficiency, buoyancy, swelling and in vitro release, F9 was selected as the optimized formulation. F9 was further subjected to surface morphology by SEM, in vitro release comparison with marketed formulation, in vivo floating study in rabbits and stability study for 90 days. In vitro release follows zero order and fitted in Korsmeyer peppas model (Non-Fickian release). Therefore, the rate of drug release is due to the combined effect of drug diffusion and polymer swelling. The in vivo X-ray studies revealed that the beads were floating in the rabbit stomach up to 10 hours. Thus, it was concluded that the sustained release formulation containing itopride hydrochloride was found to improve patient compliance, minimize the side effects and decrease the frequency of administration.

Formulation and Evaluation of Atorvastatin Calcium-Poly-ε-Caprolactone Nanoparticles Loaded Ocular Inserts for Sustained Release and Antiinflammatory Efficacy

2020 ◽  
Vol 21 (15) ◽  
pp. 1688-1698
Author(s):  
Germeen N.S. Girgis
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Pluronic F127 ◽  
In Vivo Study ◽  
Average Weight ◽  
Drug Release Profile ◽  
Atorvastatin Calcium ◽  
Anti Inflammatory

Purpose: The work was performed to investigate the feasibility of preparing ocular inserts loaded with Poly-ε-Caprolactone (PCL) nanoparticles as a sustained ocular delivery system. Methods: First, Atorvastatin Calcium-Poly-ε-Caprolactone (ATC-PCL) nanoparticles were prepared and characterized. Then, the optimized nanoparticles were loaded within inserts formulated with Methylcellulose (MC) and Polyvinyl Alcohol (PVA) by a solvent casting technique and evaluated physically, for in-vitro drug release profile. Finally, an in-vivo study was performed on the selected formulation to prove non-irritability and sustained ocular anti-inflammatory efficacy compared with free drug-loaded ocuserts. Results: The results revealed (ATC-PCL) nanoparticles prepared with 0.5% pluronic F127 were optimized with 181.72±3.6 nm particle size, 0.12±0.02 (PDI) analysis, -27.4± 0.69 mV zeta potential and 62.41%±4.7% entrapment efficiency. Nanoparticles loaded ocuserts manifested compatibility between drug and formulation polymers. Moreover, formulations complied with average weight 0.055±0.002 to 0.143±0.023 mg, and accepted pH. ATC-PCL nanoparticles loaded inserts prepared by 5% MC showed more sustained, prolonged in-vitro release over 24h. In-vivo study emphasized non-irritability, ocular anti-inflammatory effectiveness represented by smaller lid closure scores, and statistically significant lowering in PMN count after 3h. Conclusion: These findings proposed a possibly simple, new and affordable price technique to prepare promising (ATC-PCL) nanoparticles loaded inserts to achieve sustained release with prolonged antiinflammatory efficacy.

Preparation, evaluation, and in vitro release of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules

2020 ◽  
pp. 1-9
Author(s):  
Yunhong Wang ◽  
Rong Hu ◽  
Yanlei Guo ◽  
Weihan Qin ◽  
Xiaomei Zhang ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Rate ◽  
Orthogonal Design ◽  
Drug Loading ◽  
In Vitro Release ◽  
Core Material ◽  
Evaluation Indexes ◽  
Vitro Release

OBJECTIVE: In this study we explore the method to prepare tanshinone self-microemulsifying sustained-release microcapsules using tanshinone self-microemulsion as the core material, and chitosan and alginate as capsule materials. METHODS: The optimal preparation technology of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules was determined by using the orthogonal design experiment and single-factor analysis. The drug loading and entrapment rate were used as evaluation indexes to assess the quality of the drug, and the in vitro release rate was used to evaluate the drug release performance. RESULTS: The best technology of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules is as follows: the concentration of alginate is 1.5%, the ratio of tanshinone self-microemulsion volume to alginate volume to chitosan mass is 1:1:0.5 (ml: ml: g), and the best concentration of calcium chloride is 2.0%. To prepare the microcapsules using this technology, the drug loading will be 0.046%, the entrapment rate will be 80.23%, and the 24-hour in vitro cumulative release rate will be 97.4%. CONCLUSION: The release of the microcapsules conforms to the Higuchi equation and the first-order drug release model and has a good sustained-release performance.

Formulation and Evaluation of Sustained Release Bilayer Matrix Tablet of Glimepiride and Metformin Hydrochloride

2021 ◽  
pp. 273-279
Author(s):  
Mayuri B. Patil ◽  
Avish D. Maru ◽  
Jayshree S. Bhadane
Keyword(s):  
Sustained Release ◽  
Type Ii Diabetes ◽  
In Vitro Release ◽  
Angle Of Repose ◽  
Metformin Hydrochloride ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Type Ii ◽  
Weight Variation

The aim of the present study was to design and evaluate bilayer tablets of metformin hydrochloride as sustained release form for the treatment of Type-II diabetes mellitus. The basic aim of any Bi-layer tablet formulation is to separate physically or chemically incompatible ingredients and to produce repeat action or prolonged action of tablet. They are many drugs for treating type-II diabetes. Sulphonyl urea and biguanides are used commonly by a wide section of patients. Melt granulation process was used for the formulation of sustained comprising metformin layer and wet granulation of immediate comprising layer of glimepiride. The precompression studies like bulk density, tapped density, angle of repose, compressible index and post formulation studies includes weight variation, hardness, thickness, friability and dissolution study. The in-vitro release profile of Glimepiride was dissolved within 45 min, and Metformin Hydrochloride was able to release more than 12 hrs. They all the formulation was optimized formula due to its higher rate of dissolution and collate all other parameters with the official specifications.

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)

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