scholarly journals Development of Salbutamol Sulphate Sustained Release Pellets Using Acrylic Polymer and Polyvinyl Acetate Polymer and Evaluation of In vitro Release Kinetics

1970 ◽  
Vol 9 (2) ◽  
pp. 109-118 ◽  
Author(s):  
Saki Sultana ◽  
Ishtiaq Ahmed ◽  
Muhammad R Islam ◽  
Md Habibur Rahman
Keyword(s):  
Sustained Release ◽  
Polyvinyl Acetate ◽  
Release Kinetics ◽  
Aqueous Dispersion ◽  
Release Mechanism ◽  
Scanning Electron Micrographs ◽  
Acrylic Polymer ◽  
Salbutamol Sulphate ◽  
Temperature Scanning

The nuclei of sustained-release pellets of salbutamol sulphate were prepared using extrusionspheronization technique followed by coating with the aqueous dispersion of methacrylic acid esters (Eudragit RS® 30 D) and commercial aqueous polyvinyl acetate dispersion (30% dispersion) (Kollicoat SR® 30 D). The coating polymers were applied to obtain a theoretical polymer load of 5%, 10%, 15%, 20% & 25 %( w/w) on the nuclei. Invitro dissolution studies of the coated pellets were performed in a USP paddle apparatus (type-2). Dissolution media was distilled water (500 ml), paddle speed was 50 rpm and it was preformed for 8 hours at 37°C (±0.5°C) temperature. Scanning Electron Micrographs (SEMs) of the nuclei & coated pellets were taken to study their surface morphology. The kinetics of the dissolution process was determined by analyzing the dissolution data using zeroorder, first order, Higuchi and Korsmeyer equations. The kinetic modeling of the dissolution profiles revealed that drug release mechanism ranged from diffusion controlled or Fickian transport to anomalous type or non-Fickian transport. T50% (MDT) and T90% values were calculated for each formulation. The higher MDT values were obtained with Eudragit® RS 30D where as Kollicoat® SR 30D showed comparatively low MDT values. MDT values were also increased with increasing polymer load on the nuclei. Key words: Salbutamol sulphate; Pellet; Aqueous dispersion; Eudragit® RS 30 D; Kollicoat® SR 30D; Extrusion spheronization; MDT. DOI: http://dx.doi.org/10.3329/dujps.v9i2.7895 Dhaka Univ. J. Pharm. Sci. 9(2): 109-118, 2010 (December)

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

1970 ◽  
Vol 8 (1) ◽  
pp. 23-30 ◽  
Author(s):  
Abul Kalam Lutful Kabir ◽  
Bishyajit Kumar Biswas ◽  
Abu Shara Shasur Rouf
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
Matrix Tablets ◽  
Angle Of Repose ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Drug Content ◽  
Compressibility Index

The objective of this study was to develop a sustained release matrix tablet of aceclofenac usinghydroxypropyl methylcellulose (HPMC K15M and HPMC K100M CR) in various proportions as release controllingfactor by direct compression method. The powders for tableting were evaluated for angle of repose, loose bulkdensity, tapped bulk density, compressibility index, total porosity and drug content etc. The tablets were subjected tothickness, weight variation test, drug content, hardness, friability and in vitro release studies. The in vitro dissolutionstudy was carried out for 24 hours using United States Pharmacopoeia (USP) 22 paddle-type dissolution apparatus inphosphate buffer (pH 7.4). The granules showed satisfactory flow properties, compressibility index and drug contentetc. All the tablets complied with pharmacopoeial specifications. The results of dissolution studies indicated that theformulations F-2 and F-3 could extend the drug release up to 24 hours. By comparing the dissolution profiles with themarketed product, it revealed that the formulations exhibited similar drug release profile. From this study, a decreasein release kinetics of the drug was observed when the polymer concentration was increased. Kinetic modeling of invitro dissolution profiles revealed the drug release mechanism ranges from diffusion controlled or Fickian transport toanomalous type or non-Fickian transport, which was only dependent on the type and amount of polymer used. Thedrug release followed both diffusion and erosion mechanism in all cases. The drug release from these formulationswas satisfactory after 3 months storage in 40°C and 75% RH. Besides, this study explored the optimum concentrationand effect of polymer(s) on acelofenac release pattern from the tablet matrix for 24 hour period.Key words: Aceclofenac; sustained release; hydrophillic matrix; HPMC; direct compression.DOI: 10.3329/dujps.v8i1.5332Dhaka Univ. J. Pharm. Sci. 8(1): 23-30, 2009 (June)

scholarly journals Evaluation of in vitro release kinetics of Capsaicin-loaded chitosan nanoparticles using DDSolver

2020 ◽  
Vol 11 (3) ◽  
pp. 4555-4559
Author(s):  
Narissara Kulpreechanan ◽  
Feuangthit Niyamissara Sorasitthiyanukarn
Keyword(s):  
Gastrointestinal Tract ◽  
Sustained Release ◽  
Release Kinetics ◽  
Chitosan Nanoparticles ◽  
Circulatory System ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Release Study ◽  
Kinetics Of

The present aim is to evaluate the release profile and its release kinetics of encapsulated capsaicin from chitosan nanoparticles using the software DDSolver. The release study was performed by using a dialysis technique in PBS solutions with different pHs (1.2, 6.8 and 7.4) to mimics the different gastrointestinal tract and circulatory system pH ranges as a releasing medium. The nanoparticles were prepared using o/w emulsification and ionotropic gelation technique under optimal condition obtained from response surface methodology (RSM) design as described in our previous study. These nanoparticles were around 180 nm in average hydrodynamic size and encapsulation efficiency percentage around 70%, respectively. In vitro drug release study suggested that the chitosan nanoparticles can potentially use to controlled and sustained release of capsaicin over at least 96. The kinetic release analysis results by DDSolver software indicated that Weibull model was suggested to be the best dynamic models with highest R2adjusted and model selection criteria (MSC) and lowest Akaike information criterion (AIC), respectively, for capsaicin loaded chitosan nanoparticles. The release mechanism of capsaicin from nanoparticles was found to be Fickian diffusion. The results suggest that the chitosan nanoparticles can be applied for the controlled and sustained release of capsaicin in the gastrointestinal tract and circulatory system.

scholarly journals DEVELOPMENT AND EVALUATION OF ORAL SUSTAINED-RELEASE RANITIDINE DELIVERY SYSTEM BASED ON BACTERIAL NANOCELLULOSE MATERIAL PRODUCED BY KOMAGATAEIBACTER XYLINUS

2020 ◽  
pp. 48-55
Author(s):  
THANH XUAN NGUYEN ◽  
MUNG VAN PHAM ◽  
CUONG BA CAO
Keyword(s):  
Sustained Release ◽  
Delivery System ◽  
Culture Media ◽  
Release Kinetics ◽  
Release Mechanism ◽  
Burst Release ◽  
Bacterial Nanocellulose ◽  
Release System ◽  
Komagataeibacter Xylinus

Objective: The short biological half-life (2-3 h) and low bioavailability (50 %) of ranitidine (RAN) following oral administration favor the development of a controlled release system. This study was aimed to develop and in vitro evaluate oral sustained-release RAN delivery system based on the bacterial nanocellulose material (BNM) produced by Komagataeibacter xylinus (K. xylinus) from selected culture media. Methods: BNMs are biosynthesized by K. xylinus in the standard medium (SM) and coconut water (CW). RAN was loaded in BNMs by the absorption method. The structural and physicochemical properties of BNMs and BNMs-RAN were evaluated via swelling behavior, FTIR, and FESEM techniques. Moreover, the effect of BNMs on RAN release profile and release kinetics was analyzed and evaluated. Results: The amount of loaded RAN or entrapment efficacy for BNM-CW is higher than for BNM-SM. The BNM-SM-RAN and BNM-CW-RAN exhibited a decreased initial burst release system followed by a prolonged RAN release up to 24 h in relation to the commercial tablets containing RAN. The RAN release from these formulations was found higher in the SGF medium than that of in SIF medium. RAN released from these formulations was found to follow the Korsmeyer-Peppas model and diffusion sustained drug release mechanism. The sustained release of RAN from BNM-SM-RAN was slower than for RAN from BNM-CW-RAN, but the mechanism of sustained RAN release was the same. Conclusion: Oral sustained-release RAN delivery system based on BNMs was successfully prepared and evaluated for various in vitro parameters. The biopolymers like BNM-SM and BNM-CW could be utilized to develop oral sustained RAN release dosage form.

scholarly journals Formulation and Evaluation of Polymer Effect on In-Vitro Kinetics of Sustained Release Matrix Tablets of Carvedilol Using Model Dependent Methods

2013 ◽  
Vol 2 (2) ◽  
pp. 70-79
Author(s):  
Umme Rahela ◽  
Md Mizanur Rahman Moghal ◽  
Sayed Masudur Rahman Dewan ◽  
Mohammad Nurul Amin
Keyword(s):  
Sustained Release ◽  
Drug Product ◽  
Release Kinetics ◽  
Matrix Tablets ◽  
Release Mechanism ◽  
Physical Parameters ◽  
Kinetics Of ◽  
In Vitro Kinetics ◽  
Polymeric Effect

The present study was designed to evaluate the polymeric effect of METHOCEL K15MCR on the sustained release drug product of Carvedilol. Carvedilol matrix tablets were formulated by direct compression method using METHOCEL K15MCR polymer in various percentages. Physical parameters were tested and the dissolution procedure was performed by using USP (II) paddle method for eight hours to examine the release kinetics. In the study, METHOCEL K15MCR polymer was found to cause the strong retardation of the drug release. The release mechanism was explored and explained with zero order, first order, Higuchi and Korsmeyer-Peppas equations. In the context, it can be suggested with a satisfactory result that this sustained release Carvedilol tablets can be marketed to treat patient ensuring proper healthcare. DOI: http://dx.doi.org/10.3329/ijpls.v2i2.15452 International Journal of Pharmaceutical and Life Sciences Vol.2(2) 2013: 70-79

scholarly journals Preparation and in vitro release kinetics of ivermectin sustained-release bolus optimized by response surface methodology

PeerJ ◽  
2018 ◽  
Vol 6 ◽  
pp. e5418 ◽  
Author(s):  
Xiangchun Ruan ◽  
Xiuge Gao ◽  
Ying Gao ◽  
Lin Peng ◽  
Hui Ji ◽  
...  
Keyword(s):  
Response Surface Methodology ◽  
Sustained Release ◽  
Response Surface ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Information Criterion ◽  
Quadratic Model ◽  
Dissolution Time ◽  
Release Mechanism

Sustained-release formulations of ivermectin (IVM) are useful for controlling parasitic diseases in animals. In this work, an IVM bolus made from microcrystalline cellulose (MCC), starch and low-substituted hydroxypropyl cellulose (LS-HPC) was optimized by response surface methodology. The bolus was dissolved in a cup containing 900 mL of dissolution medium at 39.5 °C, under with stirring at 100 rpm. A quadratic model was formulated using analysis of variance according to the dissolution time. The optimized formulation of the bolus contained 8% MCC, 0.5% starch, and 0.25% LS-HPC. The length, width, and height of the prepared IVM bolus were 28.12 ± 0.14, 16.1 ± 0.13, and 13.03 ± 0.05 mm, respectively. The bolus weighed 11.4842 ± 0.1675 g (with a density of 1.95 g/cm3) and contained 458.26 ± 6.68 mg of IVM. It exhibited in vitro sustained-release for over 60 days, with a cumulative amount and percentage of released IVM of 423.72 ± 5.48 mg and 92.52 ± 1.20%, respectively. The Korsmeyer–Peppas model provided the best fit to the dissolution release kinetics, exhibiting anR2value close to 1 and the lowest Akaike Information Criterion among different models. The parametern(0.5180) of the Korsmeyer–Peppas model was between 0.45 and 0.89. It was demonstrated that the release mechanism of the IVM bolus followed a diffusive erosion style.

scholarly journals FORMULATION DEVELOPMENT AND EVALUATION OF SUSTAINED RELEASE GASTRORETENTIVE TABLET OF EMTRICITABINE

2019 ◽  
pp. 236-240
Author(s):  
G. V. RADHA ◽  
K. TRIDEVA SASTRI ◽  
N. MANASWIN ◽  
B. LIKHITHA
Keyword(s):  
Sustained Release ◽  
Release Kinetics ◽  
Hydroxypropyl Methylcellulose ◽  
Lag Time ◽  
Transcriptase Inhibitor ◽  
Release Mechanism ◽  
Wet Granulation ◽  
Formulation Development ◽  
Weight Variation

Objective: The study aims for the design and evaluation of floating tablets of emtricitabine (EMT), post oral administration to sustain the release and enhance gastric residence time (GRT). Methods: EMT is a nucleoside reverse-transcriptase inhibitor for the prevention and treatment of human immunodeficiency virus (HIV) infection. The investigation was considered to formulate a floating tablet of EMT with various agents. The formulation included with various concentrations of hydroxypropyl methylcellulose (HPMC) k4m, ethylcellulose, microcrystalline cellulose, polyvinylpyrrolidone (PVP) by wet granulation method. Various parameters for the prepared formulations were evaluated for weight variation, thickness, hardness, friability, floating lag time (FLT), total floating time (TFT), swelling index, in vitro drug release, and fourier-transform infrared spectroscopy (FTIR) studies. Results: The best formulation F1 exhibited 88.28% release in 24 h duration, with a floating lag time of 7 min and swelling index of 52.1% and drug content was determined to be 98.27%. The release mechanism was determined to be first order with higuchi release kinetics displaying diffusion along with the dissolution of the EMT from the tablet by non fickian mechanism. Conclusion: EMT tablets showed an increased GRT with a sustained release for 24 h thereby allowing a better window for absorption consequently improve the therapeutic effect of the drug.

scholarly journals A Novel Design of Tri-Layer Membrane with Controlled Delivery of Paclitaxel and Anti-Biofilm Effect for Biliary Stent Applications

Nanomaterials ◽  
2021 ◽  
Vol 11 (2) ◽  
pp. 486
Author(s):  
Abdelrahman I. Rezk ◽  
Jeesoo Park ◽  
Joon Yeon Moon ◽  
Sunny Lee ◽  
Chan Hee Park ◽  
...  
Keyword(s):  
Sustained Release ◽  
Antibacterial Effect ◽  
Release Profile ◽  
Biliary Stent ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Dual Function ◽  
Electrospinning Technique ◽  
Layer Membrane

Here, we developed a novel biliary stent coating material that is composed of tri-layer membrane with dual function of sustained release of paclitaxel (PTX) anticancer drug and antibacterial effect. The advantages of using electrospinning technique were considered for the even distribution of PTX and controlled release profile from the nanofiber mat. Furthermore, film cast method was utilized to fabricate AgNPs-immobilized PU film to direct the release towards the tumor site and suppress the biofilm formation. The in vitro antibacterial test conducted against Gram-positive (Staphylococcus aureus) and Gram-negative (Escherichia coli) bacteria species showed excellent antibacterial effect. The in vitro drug release study confirmed the sustained release of PTX from the tri-layer membrane and the release profile fitted first order with correlation coefficient of R2 = 0.98. Furthermore, the release mechanism was studied using Korsmeyer–Peppas model, revealing that the release mechanism follows Fickian diffusion. Based on the results, this novel tri-layer membrane shows curative potential in clinical development.

Formulation and evaluation of proniosome loaded sertaconazole nitrate for topical application

2021 ◽  
Vol 1 (2) ◽  
pp. 023-037
Author(s):  
Shailaja D ◽  
Latha K ◽  
Manasa D ◽  
Shirisha A ◽  
Padmavathi R ◽  
...  
Keyword(s):  
Ex Vivo ◽  
Release Kinetics ◽  
Skin Irritation ◽  
Water Soluble ◽  
Ionic Surfactants ◽  
Release Mechanism ◽  
Stability Studies ◽  
Zero Order Release ◽  
Poorly Soluble

Proniosomal technology is a novel solution for poorly soluble drugs. Proniosomes are water-soluble carrier particles which are coated with non-ionic surfactants. Proniosomal gels were prepared by coacervation phase separation method using non-ionic surfactants, lipid carriers and cholesterol as a membrane stabilizer. FTIR compatibility studies revealed that the drug and excipients were compatible. All formulations were evaluated for pH, drug content, extrudability, spreadability, viscosity, in-vitro, ex-vivo, skin irritation and stability studies. Among formulations prepared, F80H1 has shown higher % EE (83.02) and least diffusion through dialysis membrane i.e., 17.68%. With ex-vivo studies, F80H1 formulation has shown highest skin deposition and lower flux of sertaconazole nitrate through the rat skin. F80H1 was selected as final optimized formulation. F80H1 exhibited good stability and SEM studies revealed that the vesicles were spherical in shape. The optimized formulation was found to follow zero order release kinetics and korsmeyer-peppas release mechanism. F80H1 found to be non-irritant and stable from skin irritation and stability studies.

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 and Characterization of Mucoadhesive Microcapsules of Gliclazide with Natural Gums

1970 ◽  
Vol 4 (1) ◽  
pp. 38-48 ◽  
Author(s):  
Santhosh Kumar Mankala ◽  
Nishanth Kumar Nagamalli ◽  
Ramakrishna Raprla ◽  
Rajyalaxmi Kommula
Keyword(s):  
Drug Release ◽  
Dosage Form ◽  
Guar Gum ◽  
Release Kinetics ◽  
Insulin Dependent Diabetes Mellitus ◽  
Dependent Diabetes Mellitus ◽  
Release Mechanism ◽  
Ionic Gelation ◽  
Release Formulation

Gliclazide is an oral hypoglycemic agent used in management of non-insulin dependent diabetes mellitus. Among people who are suffering from long term disorders, the major were categorized under diabetes so, a dosage form is needed to provide continuous therapy with high margin of safety & such dosage form can be achieved by microencapsulation. Gliclazide microspheres with sodium alginate (coat material, gum kondagogu, gum guar and xanthan gum (mucoadhesive agents) were prepared by orifice-ionic gelation and emulsification ionic gelation techniques varying concentrations (1:0.25, 1:0.5, 1:0.75 and 1:1). Formulations were then evaluated for surface morphology, particle shape, Carr’s index, microencapsulation efficiency, drug release, mucoadhesion studies. Compatibility studies were performed by FTIR, DSC, and XRD techniques and no interactions were found between drug and excepients used. The microspheres were found spherical and free flowing with emulsion ionic gelation technique with a size range 400-600μm. % drug content and encapsulation efficiency found in the range of 55%-68% and, 86.23%-94.46% respectively. All microspheres showed good mucoadhesive property in in-vitro wash of test. In vitro drug release studies showed that the guar gum has more potentiality to retard the drug release compared to other gums and concentrations. Drug release from the microspheres was found slow following zero order release kinetics with non-fickian release mechanism stating release depended on the coat: core ratio and the method employed. The concentration of 1:1 of SA: GG (EMG 4) found suitable for preparing the controlled release formulation of gliclazide stating emulsification gelation technique is the best among followed.   Key words: Gliclazide; Natural gums; orifice ionic gelation technique; emulsification ionic gelation technique DOI: http://dx.doi.org/10.3329/sjps.v4i1.8865 SJPS 2011; 4(1): 38-48

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