scholarly journals Development and Characterization of Controlled Porosity Osmotic Pump Tablets of Captopril

2020 ◽  
Vol 1 (2) ◽  
pp. 54-59
Author(s):  
Paniz Mahjoub ◽  
Amid Morshedlu
Keyword(s):  
Drug Release ◽  
Cellulose Acetate ◽  
Osmotic Pump ◽  
Polyethylene Glycol 400 ◽  
In Vitro Drug Release ◽  
Coating Solution ◽  
The Core ◽  
Peg 400 ◽  
Controlled Porosity

Background: The objective of the present study was to design a porous osmotic pump-based drug delivery system for the controlled release of captopril (Cap) which can maintain a constant therapeutic concentration, thus reducing dose-related side effects and dosing frequency. Methods: The study evaluated in vitro drug release for the controlled porosity osmotic pump tablet (CPOPT) of Cap. This in vitro drug release study investigated the influence of the tablet formulation variables such as the amount of mannitol, hydroxypropylmethylcellulose K4M (HPMCK4M), and polyvinyl pyrrolidone (PVP K-30) in the core and the concentration of cellulose acetate and polyethylene glycol 400 (PEG-400) in the coating solution. Results: It was found that the drug release was mostly affected by the amount of mannitol, HPMCK4M, and PVP K-30 in the core and the amount of cellulose acetate and PEG-400 in the coating solution. Conclusion: In general, the objective of the study was established by coating the core tablet containing osmotic and pore-forming agents. Therefore, the CPOPT of Cap could be a safe, effective, stable, and promising preparation in the future.

scholarly journals FORMULATION AND EVALUATION OF CHLOROTHALIDONE LOADED MOUTH DISSOLVING FILM-A BIOAVAILABILITY ENHANCEMENT APPROACH USING MULTILEVEL CATEGORIC DESIGN

2020 ◽  
pp. 34-41
Author(s):  
SHUBHAM BIYANI ◽  
SARANG MALGIRWAR ◽  
RAJESHWAR KSHIRSAGAR ◽  
SAGAR KOTHAWADE
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Aqueous Dispersion ◽  
Onset Of Action ◽  
Polyethylene Glycol 400 ◽  
Bioavailability Enhancement ◽  
Disintegration Time ◽  
Peg 400 ◽  
Folding Endurance

Objective: The intension of the present study includes fabrication and optimization of mouth dissolving film loaded with Chlorothalidone by solvent evaporation techniques using two components and their three levels as multilevel Categoric design. Methods: Major problem associated with the development of film loaded with BCS class II drug is to increase its solubility. Here the Chlorothalidone solubility achieved by co-solvents, such as methanol. After dissolving the drug in co-solvent, this drug solution is poured into an aqueous dispersion of Hydroxypropyl Methylcellulose E5 (HPMC E5) and Polyethylene glycol 400 (PEG 400). The two independent variables selected are factor A (concentration of HPMC E5) and factor B (concentration of PEG 400) was selected on the basis of preliminary trials. The percentage drug release (R1), Disintegration time in sec (R2) and folding endurance (R3) were selected as dependent variables. Here HPMC E5 used as a film former, PEG 400 as plasticizer, mannitol as bulking agent, Sodium starch glycolate as a disintegrating agent, tween 80 as the surfactant, tartaric acid as saliva stimulating agent, sodium saccharin as a sweetener and orange flavour etc. These fabricated films were evaluated for physicochemical properties, disintegration time and In vitro drug release study. Results: The formulation F6 has more favorable responses as per multilevel categoric design is % drug release about 98.95 %, average disintegration time about 24.33 second and folding endurance is 117. Thus formulation F6 was preferred as an optimized formulation. Conclusion: The present formulation delivers medicament accurately with good therapeutic efficiency by oral administration, this mouth dissolving films having a rapid onset of action than conventional tablet formulations.

scholarly journals FORMULATION AND IN VITRO–IN VIVO PHARMACOKINETIC EVALUATION OF CARDIOVASCULAR DRUG-LOADED PULSATILE DRUG DELIVERY SYSTEMS

2021 ◽  
pp. 144-151
Author(s):  
KUMAR BABU PASUPULETI ◽  
VENKATACHALAM A. ◽  
BHASKAR REDDY KESAVAN
Keyword(s):  
Drug Release ◽  
Ethyl Cellulose ◽  
Release Kinetic ◽  
In Vitro Drug Release ◽  
The Core ◽  
Coated Tablet ◽  
Tablet Formulations ◽  
Core Tablet

Objective: This study is to formulate Nebivolol into a Pulsatile liquid, solid composite compression coated tablet, which will delay the release of the drug in early morning hypertension conditions. Methods: The liquid, solid composite tablet was formulated and compressed with the ethylcellulose coating polymer. The percent in vitro drug release of the liquid solid composite compressed tablet was tested. Based on disintegration time and wetting time, the LCS2, LCS3, LSC6, LCS7 and LCS12 formulations were found to be the optimized solid-liquid compacts fast-dissolving core tablet formulations, which may be excellent candidates for further coating with polymer to transfer into press coated pulsatile tablet formulations. Coating the core tablet with varying ethyl cellulose concentrations resulted in five different formulations of the pulsatile press-coated tablet (CT1, CT2, CT3, CT4, CT5). In vitro drug release, in vitro release, kinetic studies, in vivo pharmacokinetic and stability tests were all performed for the prepared pulsatile press coated tablet. Results: CT3 tablets are coated with ethyl cellulose polymer, which shows maximum controlled drug release from the core tablet i.e. 96.34±1.2% at 8th h. It shows there was an efficient delay in drug release form core tablet i.e. up to 3 h, followed by the maximum amount of drug release of 96.34±2.4 at 8h. Which shows the core drug will be more efficiently protected from the gastric acid environment 1.2 pH, duodenal environment 4.0 pH and release drug only in the small intestine. Conclusion: According to the findings, CT3 Pulsatile press-coated tablet increased the bioavailability of Nebivolol by 3.11 percent.

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

scholarly journals FORMULATION DEVELOPMENT AND EVALUATION OF CHRONOMODULATED DRUG DELIVERY SYSTEM BY ZAFIRLUKAST

2021 ◽  
pp. 211-220
Author(s):  
N. SHIVA KRISHNA ◽  
B. JAYANTHI ◽  
A. MADHUKAR
Keyword(s):  
Drug Release ◽  
Lag Time ◽  
Early Morning ◽  
Release Profile ◽  
Locust Bean Gum ◽  
In Vitro Drug Release ◽  
The Core ◽  
Locust Bean ◽  
Core Tablet

Objective: The main objective of the present study was to formulate and evaluate a time-controlled single-unit oral pulsatile drug delivery system containing Zafirlukast for the prevention of nocturnal asthma attacks. To provide time-scheduled drug release for Asthma disease. It is used for preventing asthmatic attacks at early morning. Pulsatile release dosage form is increasing patient compliance by reducing the dosing frequency, especially in the early morning. Methods: Core tablets were prepared by incorporating different concentrations of natural and synthetic super disintegrants. Drug-containing core tablets (ZC1-ZC15) with different compositions of natural super disintegrants (Plantago ovata seed powder, Locust bean gum) synthetic super disintegrants (Sodium starch glycolate (SSG), Cross carmellose sodium (CCS), Crospovidone (CP)) were prepared by direct compression technique. The core tablets were subjected to pre-formulation, physicochemical and In vitro drug release studies. The fast disintegrating core tablet formulation was selected and press-coated tablets (P1-P11) were prepared with different compositions of hydrophobic polymers Eudragit RS100, Eudragit RL 100, Ethylcellulose and hydrophilic polymers Hydroxypropyl methylcellulose K4M, K100M. The optimized formulation was selected and quantified based on in vitro drug release profile in simulated gastric and intestinal fluids. Results: The pre and post-compression parameters of tablets were also found to be within limits. Formulation ZC5 with 16 mg of Locust bean gum showed the least disintegrating time, i.e., 22.13 sec, and was selected as the best immediate release core tablet. The press-coated tablet formulation P8 having 62.5 mg Eudragit RS100 and 62.5 mg of HPMC K4M in ratio 1:1 over the core tablet ZC5 showed rapid and drug release nearly after 4 h lag time and 98.86 % up to 12 h. Accelerated stability studies of the optimized formulation P8 indicated no significant difference in release profile after 3 mo. Conclusion: The in vitro dissolution study showed that lag time before drug release was highly affected by the coating amount level and nature of coating polymer used. Time-controlled pulsatile release tablets can be prepared using press-coating techniques.

scholarly journals New Technology of Thermoplastic Coating for Osmotic Pump Tablets: Study on in vitro Drug Release

2019 ◽  
Vol 01 (01) ◽  
pp. e1-e10
Author(s):  
Chunping Yuan ◽  
Huimin Hou ◽  
Shuyun Ou ◽  
Shujing Zhao ◽  
Yongjian Gao ◽  
...  
Keyword(s):  
Drug Release ◽  
New Technology ◽  
Spray Coating ◽  
Osmotic Pump ◽  
Release Mechanism ◽  
Membrane Thickness ◽  
In Vitro Drug Release ◽  
Coating Technology ◽  
Release Profiles

Aim The in vitro drug release profiles of metformin hydrochloride thermoplastic coated tablets and nifedipine thermoplastic coated tablets were studied. Methods By measuring the in vitro release profiles of the thermoplastic coated tablets of model drugs, the effects of membrane thickness, polyethylene glycol-1,500 (PEG1500) content, number of orifice, stirring speed, and release medium on the drug release were investigated, and the rule and mechanism of drug release were also analyzed by comparing with the osmotic pump tablets (OPTs). Results Thermoplastic coated tablets with single- or double-chamber construction performed the same function of controlling the drug release, operated under the same release mechanism (osmotic pressure drove the drug release), and exhibited the same release characteristics (zero-order release, unaffected by release medium, and stirring speed) and release rule (release rate was inversely proportional to the membrane thickness but proportional to the PEG1500 content) as compared with OPTs prepared by the common spray coating technology. Conclusion Thermoplastic coated tablets have the same release characteristics in vitro as OPTs. The new technology of thermoplastic coating can replace the spray coating technology of OPTs. This study provides theoretical basis and practical support for the industrialization and clinical application of thermoplastic coating technology.

DEVELOPMENT AND EVALUATION OF ORAL ELEMENTARY OSMOTIC PUMP TABLETS FOR ROPINIROLE HYDROCHLORIDE

INDIAN DRUGS ◽  
2012 ◽  
Vol 49 (06) ◽  
pp. 23-30
Author(s):  
S. Patha ◽  
◽  
P. Dara ◽  
S. K Yamsani ◽  
R Thadkapally ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Osmotic Pump ◽  
In Vivo Studies ◽  
Dissolution Medium ◽  
Conventional Tablet ◽  
Peg 400 ◽  
Ropinirole Hydrochloride

The objective of the present study was to develop a sustained release once a day oral elementary osmotic tablet for ropinirole hydrochloride and evaluate its in vivo performance. The core of elementary osmotic tablet of ropinirole hydrochloride was prepared by compression of mixture consisting of drug,different concentrations of osmogens, and other tablet material. Core tablets were then coated with different concentrations of cellulose acetate and PEG-400. FTIR was used to identify if the excipients are compatible with the drug. All the tablets that were prepared were evaluated for drug release and based on the results an optimum and ideal osmotic pump composition with a zero-order drug release extended for 24 h was proposed and this was considered the optimized formulation. Surface morphology of coated formulation was studied by scanning electron microscopy. The drug release was determined in different pH media and different agitation speeds. The pharmacokinetics of the drug after oral administration of optimized osmotic pump was investigated in rabbits and the data were compared with that of a conventional tablet. In vitro in vivo correlation was determined for the optimized formulation. A suitable and simple sustained release elementary osmotic pump for ropinirole hydrochloride was developed. The release rate was independent of the pH of the dissolution medium and the agitation speeds. In vivo studies with optimized osmotic tablet formulation demonstrated that drug concentration in plasma was maintained for prolonged period and minimized fluctuation. A better in vitro in vivo correlation was achieved with the osmotic tablet. A simple once a day elementary osmotic tablet is feasible for ropinirole hydrochloride.

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.

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