Effect of coating method on release of Glimepiride from porosity osmotic pump tablets (POPTs)

2020 ◽  
pp. 37-45
Keyword(s):  
In Vitro Release ◽  
Osmotic Pump ◽  
Release Time ◽  
Once Daily ◽  
Coating Solution ◽  
Continuous Release ◽  
Red Color ◽  
Coating Method ◽  
Osmotic Agent

In this study, once-daily porosity osmotic pump tablets (POPTs) of Glimepiride were prepared using HPMC K100M (61%), osmotic agent (30% NaCl) coated using two different coating techniques spraying and dipping methods. The coating solution composed of ethyl cellulose (7.5%) w\w in ethanol (90%), castor oil (2%) as water-insoluble plasticizer and Gingo red color (0.5% w\w). In both techniques, the coating level was adjusted to give a 10% increase in the weight of the tablets. The effect of the coating by dipping technique with an increase in the weight of tablet (10 %, 20% & 50%) was also investigated to see the effect coating level on the percentage of drug release from POPTs. The results of the in vitro release of Glimepiride from tablets coated by the spraying method showed longer release time (24 hrs) than those coated with dipping method. On the other hand, increasing the coating level by dipping method retarded the release of the drug from tablets. However, the same retardation effect on release as shown with the spraying technique was only obtained by increasing the coating level with a 50% increase in the weight of the tablet. Thus, coating by spraying is more efficient to prepare POPTs to give a continuous release of Glimepiride from once daily table with the lowest increase in the total weight of the tablet.

scholarly journals FORMULATION AND EVALUATION OF FENOVERINE FLOATING TABLETS

2021 ◽  
pp. 175-180
Author(s):  
RASHMITHA V ◽  
MADHUSUDAN RAO Y ◽  
PAVANI S
Keyword(s):  
Sodium Alginate ◽  
Xanthan Gum ◽  
In Vitro Release ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Release Time ◽  
Floating Tablets ◽  
Dissolution Studies ◽  
Weight Variation

Objective: The purpose of this research was to develop a fenoverine gastroretentive drug delivery system which, following oral administration should have the ability to enhance and prolong the period of gastric residence time (GRD) with the desired in vitro release profile. Methods: In the present study, fenoverine floating tablets were prepared using an effervescent method using sodium bicarbonate and citric acid as a gas-generating agent. The tablets were formulated using direct compression technology using xanthan gum and sodium alginate as polymers. Pre-compression powders were evaluated for angle of repose, bulk density, tapped density, Carr’s index, and Hausner’s ratio, and the prepared tablets were evaluated for weight variation, thickness, diameter, hardness, friability, drug content, floating lag time, total floating time, and in vitro dissolution studies. The formulations were optimized for the different concentrations of xanthan gum, sodium alginate, and their combinations. Results: All the prepared formulations showed well in vitro buoyancy. The tablets remained buoyant for 6–12 h. The in vitro drug-release pattern of fenoverine floating tablets was adapted to different kinetic models with the highest regression to zero-order and Korsmeyer-Peppas, and the mechanism was found to be a Fickian mechanism. Conclusion: Out of all the formulations prepared, in vitro dissolution studies of the F4 formulation were found to be maximum than other batches, which exhibited desired sustained release time followed by acceptable floating properties.

scholarly journals Design and evaluation of a novel floating osmotic pump system

2009 ◽  
Vol 12 (1) ◽  
pp. 129 ◽  
Author(s):  
Zhihong Zhang ◽  
Bo Peng ◽  
Xinggang Yang ◽  
Chao Wang ◽  
Guangmei Sun ◽  
...  
Keyword(s):  
Drug Release ◽  
Oral Administration ◽  
In Vitro Release ◽  
Osmotic Pump ◽  
Matrix Tablets ◽  
In Vivo Evaluation ◽  
Pump System ◽  
Conventional Tablet

PURPOSE. Find a novel delivery system for oral administration of drugs that have absorption window in the upper part of gastrointestinal (GI) track. METHODS. Dipyridamole was chosen as the model drug. A novel system, which combined the osmotic pump controlled release system and the floating system, was designed; matrix tablets (MT) were prepared for compares. The effects of pH, temperature and hydrodynamic conditions on drug release and the floating behavior of floating osmotic pump system (FOP) were investigated. In vivo evaluation was performed by a three-crossover study in six Beagle dogs relative to the conventional tablet (CT). Cumulative percent input in vivo was compared with that of in vitro release profiles. RESULTS. Floating behavior of FOP, drug releases from FOP and MT were sensitive to pH of dissolution media but not sensitive to temperature; the release of dipyridamole from MT was influenced by stirring rate while drug release from FOP was not. AUC of FOP was larger than MT and CT. The linear correlations between fraction absorbed in vivo and fraction dissolved in vitro was established for FOP-a true zero-order release formula, whereas only a nonlinear correlation was obtained for MT. CONCLUTIONS. FOP could be a novel way for the oral administration for drugs like dipyridamole.

Preparation, Characterization and Properties Evaluation of Buprofezin Nanocomposites Obtained by Polyelectrolytes Assembly

2011 ◽  
Vol 183-185 ◽  
pp. 1677-1681 ◽  
Author(s):  
Zhe Zhang ◽  
De Fu Chi ◽  
Jia Yu
Keyword(s):  
Laser Scanning ◽  
Orthogonal Experiment ◽  
Drug Loading ◽  
In Vitro Release ◽  
Average Diameter ◽  
Laser Scanning Microscopy ◽  
Release Time ◽  
Confocal Laser ◽  
Layer By Layer

Buprofezin (BPF) microcrystals were directly encapsulated with nature polysaccharides chitosan (CHI) and sodium alginate (ALG) through layer-by-layer (LbL) self-assembly. The coated colloids were characterized using confocal laser scanning microscopy (CLSM) and scanning electron microscopy (SEM). The surface of the coated microcrystal was smoothened and the coating was uniform. Different concentrations of the ALG, CHI, BPF and CaCl2 were selected as the influencing factors, and then, the microcapsules were optimized by orthogonal experiment. The size distribution of microcapsules was determined by Laser Diffraction Size Analyzer. It showed statistically normal distribution. The average diameter of BPF was 1.5m. The encapsulation efficiency of the BPF loaded microparticles was about 67.2±0.73%. The drug loading content was about 66.7±0.31% after encapsulated. The in vitro release experiments revealed that the polyelectrolytes prolonged the release time of the encapsulated BPF microcrystals.

scholarly journals Design and Development of Controlled Porosity Osmotic Pump Tablets of Zidovudine Using Sodium Chloride as Osmogen for the Treatment of Aids

2019 ◽  
Vol 4 (1) ◽  
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Osmotic Pump ◽  
Concentration Effect ◽  
Membrane Thickness ◽  
Pore Former ◽  
Permeable Membrane ◽  
Agitation Intensity ◽  
Controlled Porosity

The present study investigates the feasibility of the design and develops controlled porosity osmotic pump (CPOP) tablets to prolong the drug release of an antiretroviral drug zidovudine of 600mg once daily. Five formulations (ZS1to ZD5) were prepared by wet granulation method using various excipients. The CPOP consisted of an osmotic core coated with a micro porous membrane made up of cellulose acetate, poly ethylene glycol and sorbitol as in situ micro pore former. The prepared tablets were evaluated for pre compression parameters, post compression parameters, in vitro drug release study, Fourier Transform Infrared Spectroscopy (FTIR) study, Differential Scanning Calorimetry (DSC) study and scanning electron microscopy (SEM) study. The formulation variables such as effect of osmogen concentration, effect of pore former concentration, effect of membrane thickness of semi permeable membrane were evaluated for drug release characteristics. For the optimized formulation (ZS4) effect of osmotic pressure, effect of pH and effect of agitation intensity was evaluated. The in vitro release kinetics were analyzed for different batches by different pharmacokinetic models such as zero order, first order, Higuchi, Korsmeyer-Peppas and Hixson-Crowell model. The result of optimized formulation releases drug up to 16 hrs in a controlled manner and follows Higuchi kinetics and which is independent of the pH and agitation intensity. The optimized formulation was found to be stable up to 3 months when tested for stability study at 40±2ºC/ 75±5% RH

Paroxetine Hydrochloride Push-pull Osmotic Pump Tablets: Designing an Innovative, Scalable Push-pull Osmotic Drug Delivery System Using QbD Approach

2020 ◽  
Vol 10 (2) ◽  
pp. 104-116
Author(s):  
Prathmesh P. Kenjale ◽  
Manjusha A. Joshi ◽  
Umesh N. Khatavkar ◽  
Vividha V. Dhapte ◽  
Varsha B. Pokharkar
Keyword(s):  
Patient Compliance ◽  
Risk Mitigation ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Osmotic Pump ◽  
Wet Granulation ◽  
Poor Patient ◽  
Poor Patient Compliance ◽  
Paroxetine Hydrochloride

Background: Paroxetine hydrochloride hemihydrate (PHH) is a serotonin reuptake inhibitor useful for the treatment of diverse psychiatric problems. Existing marketed formulations with frequent administration lead to gastrointestinal (GI) reactions and abrupt fluctuations in plasma level with poor patient compliance. These prerequisites are sufficed by controlled release push-pull osmotic pump tablets (PPOP). Objective: Objective of the present study was to develop robust and reliable PPOP formulation via Quality by design (QbD) approach to achieve desired release kinetics. Methods: PPOP was formulated using wet granulation method followed by osmotic coating. QbD strategy for defining the risk assessment of influential variables such as swelling polymers and osmogen on in vitro release kinetics of designed PPOP. Results: Presence of Polyox in push and pull layer along with osmogen controlled the drug release pattern from formulated PPOP system as depicted in 33 factorial design. These formulated optimized PPOP systems demonstrated 2 hrs lag time with zero-order kinetics, a peculiar feature of PPOPs. Conclusions: Scalable, stable PPOP tablets were fabricated by applying systematic QbD approach. The developed PPOP systems with improved concentration-independent behavior helped to address the challenges of existing marketed formulations. Risk mitigation and control strategy assured quality of the system during scalability. Application of QbD strategy in establishing the PPOP formulation would help in formulating drug candidates having gastric limitations and poor patient compliance. The present study is the detailed account of QbD based PPOP formulation, therefore it can be of potential importance from academics as well as industrial perspective.

scholarly journals Advanced flow cell design for in vitro release testing of mucoadhesive buccal films

2020 ◽  
Vol 70 (3) ◽  
pp. 359-371
Author(s):  
Blaž Grilc ◽  
Jurij Zdovc ◽  
Odon Planinšek
Keyword(s):  
In Vitro Release ◽  
Analytical Techniques ◽  
Active Pharmaceutical Ingredient ◽  
Flow Cell ◽  
Release Time ◽  
Flow Through ◽  
System Variables

AbstractFilms for buccal application are a slowly emerging new platform for drug delivery. There remains a lack of analytical techniques for the determination of in vitro active pharmaceutical ingredient release. The aim here was to develop an alternative method to the commonly used United States Pharmacopoeia (USP) 2 method, based on the flow-through cell. This system extends the release time and enables more detailed sample discrimination according to formulation. It could be used as a tool for in vivo prediction of drug release rates from buccal film formulations. The flow cell contains two chambers separated by a membrane through which the released active pharmaceutical ingredient is measured. Vital system variables and their effects on the release rate of the model active pharmaceutical ingredient are presented for formulations based on sodium alginate polymer. The method reflects the differences between films and is shown to be discriminatory for evaluation of buccal formulations.

In Vitro Characterization of Calcium Phosphate Biomaterial Loaded with Linezolid for Osseous Bone Defect Implantation

2010 ◽  
Vol 26 (7) ◽  
pp. 811-828 ◽  
Author(s):  
Hélène Gautier ◽  
Adrien Plumecocq ◽  
Gilles Amador ◽  
Pierre Weiss ◽  
Christian Merle ◽  
...  
Keyword(s):  
Calcium Phosphate ◽  
Mercury Porosimetry ◽  
In Vitro Release ◽  
Release Time ◽  
Wet Granulation ◽  
Gram Positive Bacteria ◽  
In Vitro Characterization ◽  
Vitro Release

Osteomyelitis is a severe bone infection frequently caused by Staphylococcus aureus, which shows significant resistance to methicillin. One therapeutic treatment would be to insert a bone substitute loaded to an antibiotic, which would enable the bone to be filled while the illness is being treated. Linezolid is an oxazolidinone antibiotic with a large spectrum of action. It is effective against most Gram-positive bacteria and displays a specific mode of action. The aim of this work was to study the association of linezolid with a calcium phosphate-deficient apatite matrix. Granules containing 10% and 50% linezolid were prepared by wet granulation and characterized. Porosity analyses performed by mercury porosimetry and scanning electron microscopy revealed that grain porosity with 50% linezolid was higher than that of the grains containing 10% linezolid. NMR analyses showed no change in structure of linezolid when linked to calcium-deficient apatite. These results were confirmed by studying the antibacterial activity of linezolid, which remained proportional to the quantity of loaded linezolid, proving that the antibiotic released was active. The in vitro release time varied from 9 days for granules containing 10% linezolid to 26 days for granules containing 50% linezolid.

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)

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.

scholarly journals Doxycycline and Monocaprin In Situ Hydrogel: Effect on Stability, Mucoadhesion and Texture Analysis and In Vitro Release

Gels ◽  
2019 ◽  
Vol 5 (4) ◽  
pp. 47 ◽  
Author(s):  
Venu Gopal Reddy Patlolla ◽  
William Peter Holbrook ◽  
Sveinbjorn Gizurarson ◽  
Thordis Kristmundsdottir
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Fickian Diffusion ◽  
Release Time ◽  
Release Mechanism ◽  
Oral Diseases ◽  
Zero Order Kinetics ◽  
In Situ Hydrogel

The aim of this study was to develop a stable aqueous formulation containing a combination of doxycycline and monocaprin in clinically relevant concentrations. Increase in expression of Matrix metalloproteinases (MMPs) and microbial role in oral diseases is well established and the combination of above active ingredients could be potentially beneficial in treatment of oral mucosal conditions. The hydrogels containing different concentrations of doxycycline and monocaprin in the presence and absence of stabilizing excipients were developed and their stabilities were studied at 4 °C for up to 1 year. The drug–drug interaction was evaluated using Fourier-transform infrared spectroscopy (FTIR). The addition of monocaprin on doxycycline in situ hydrogel’s mucoadhesiveness, texture properties and drug release mechanism was studied. The addition of monocaprin negatively affected the doxycycline stability and was concentration dependent, whereas monocaprin was stable up to 1 year. Doxycycline did not interfere with the anti-Candidal activity of monocaprin. Furthermore, the presence of monocaprin significantly affected the formulation hardness, compressibility and adhesiveness. Monocaprin and doxycycline release followed zero order kinetics and the release mechanism was, by anomalous (non-Fickian) diffusion. The addition of monocaprin increased the drug release time and altered the release mechanism. It is possible to stabilize doxycycline in the presence of monocaprin up to 1 year at 4 °C.

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