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 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.

scholarly journals Design and Evaluation of Polymeric Controlled Release Natamycin Ocular Inserts

1970 ◽  
Vol 6 (1) ◽  
pp. 108-115 ◽  
Author(s):  
A Rajasekaran ◽  
V Sivakumar ◽  
K Karthika ◽  
J Padma Preetha ◽  
T Abirami
Keyword(s):  
Drug Release ◽  
Transmission Rate ◽  
In Vitro Release ◽  
Zero Order ◽  
Release Kinetic ◽  
Permeable Membrane ◽  
Zero Order Kinetics ◽  
Zero Order Release ◽  
S 100

The main aim of this study is to develop ocular drug delivery system for Natamycin; a polyeneantibiotic is highly useful for the treatment of conjunctivitis and keratitis. The ocuserts were preparedusing different polymers such as eudragit L-100, eudragit S-100, eudragit RL-100, hydroxy propylmethyl cellulose phthalate and cellulose acetate phthalate at various proportion and combinationsusing PEG-400 as plasticizer. The prepared ocuserts were evaluated for their physicochemicalparameters like drug content, weight uniformity, folding endurance, thickness, % moistureabsorption and water vapour transmission rate. The in vitro drug release from the formulations wasstudied using commercial semi permeable membrane and the in vitro release kinetic datas weretreated according to the diffusion models proposed by Higuchi and Peppas in order to access themechanism of drug release from the formulations, which were following zero order kinetics. All theformulations showed no change in the physical appearance and the FTIR studies indicated nopossibility of interaction between drug and polymer. The expected zero order release for one day wasobserved in the formulation D1 (3% Eudragit RL100 and 1% Eudragit L100)Keywords: Ocular Insert; Ocular Delivery; NatamycinDOI: 10.3126/kuset.v6i1.3318 Kathmandu University Journal of Science, Engineering and Technology Vol.6(1) 2010, pp108-115

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.

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

2020 ◽  
Vol 02 (01) ◽  
pp. e1-e10
Author(s):  
Chun Ping Yuan ◽  
Hui Min Hou ◽  
Zhi Hong Cheng ◽  
Qing Hua Ge ◽  
Ding Zhong Song ◽  
...  
Keyword(s):  
Drug Release ◽  
New Technology ◽  
In Vitro Release ◽  
Osmotic Pump ◽  
Metformin Hydrochloride ◽  
Beagle Dogs ◽  
Coating Technology ◽  
Vitro Release

Abstract Aim The in vivo pharmacokinetics of thermoplastic-coated tablets prepared by a new technology of thermoplastic coating in Beagle dogs were studied, and the correlation between in vitro release and in vivo absorption was analyzed. Methods The in vitro release profiles of metformin hydrochloride thermoplastic-coated tablets and nifedipine thermoplastic-coated tablets were investigated. The single-dose pharmacokinetic study of these tablets in Beagle dogs was performed, and the obtained results were separately compared with the data of conventional osmotic pump tablets reported in the literature. Results Metformin hydrochloride thermoplastic-coated tablets and nifedipine thermoplastic-coated tablets displayed controlled drug-release characteristics and had a good in vivo–in vitro correlation in Beagle dogs, respectively. The literature-compared results further demonstrated that both thermoplastic-coated tablets had release characteristics of osmotic pump tablets in vivo. Conclusion The thermoplastic-coated tablets could control drug release in vivo and it was further confirmed that the new thermoplastic coating technology could replace the spray coating of osmotic pump controlled-release tablets. This study provides a theoretical basis and practical support for the industrialization and clinical application of the new thermoplastic coating technology.

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.

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.

Formulation and In vitro Release Characterization of Metoprolol Succinate Extended Release Tablets

2012 ◽  
Vol 4 (4) ◽  
pp. 1537-1543
Author(s):  
Sakthikumar T ◽  
Rajendran N N ◽  
Natarajan R
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Wet Granulation ◽  
Direct Compression ◽  
Metoprolol Succinate ◽  
Extended Release Formulations ◽  
Vitro Release

The present study was aimed to develop an extended release tablet of metoprolol Succinate for the treatment of hypertension.  Four extended release formulations F1-F4 were developed using varying proportions of hydroxylpropyl-methylcellulose K100M, sodium carboxy methyl cellulose and Eudragit L30 D55 by wet granulation. Five extended release formulations F5-F9 containing HPMC K100M and HPMC 5 cps in varying concentration were developed by direct compression. The physicochemical and in vitro release characteristics of all the formulations were investigated and compared. Two formulations, F7 and F8 have shown not more 25% drug release  in 1st h, 20%-40% drug release at 4th hour, 40%-60% drug release at 8th hour and not less than 80% at 20th hour and the release pattern conform with USP specification for 24 hours extended release formulation. It can be conclusively stated that optimum concentration of HPMC K100M (58%-65%) by direct compression method can yield an extended release of metoprolol succinate for 24 hours.

Design, Synthesis and Studies on Novel Polymeric Prodrugs of Erlotinib for Colon Drug Delivery

2020 ◽  
Vol 20 ◽  
Author(s):  
Sahil Kumar ◽  
Bandna Sharma ◽  
Tilak R. Bhardwaj ◽  
Rajesh K. Singh
Keyword(s):  
Drug Delivery ◽  
Colon Cancer ◽  
Drug Release ◽  
Anticancer Agents ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Specific Treatment ◽  
Drug Conjugates ◽  
Polymer Drug Conjugates

Aims: In the present study, polymer-drug conjugates were synthesized based on azo-bond cleavage drug delivery approach for targeting erlotinib as anticancer drug specifically to the colon for the proficient treatment of colon cancer. Background: Colon cancer (CC) is the third commonly detected tumor worldwide and it make up about 10 % of all cases of cancers. Most of the chemotherapeutic drugs available for treating colon cancer are not only toxic to cancerous cells but also to the normal healthy cells. Among the various approaches to get rid of the adverse effects of anticancer agents, prodrugs are one of the most imperative approaches. Objective: The objective of the study is to chemically modify the erlotinib drug through azo-bond linkage and suitable spacer which will be finally linked to polymeric backbone to give desired polymer linked prodrug. The azo reductase enzyme present in colon is supposed to cleave the azo-bond specifically and augment the drug release at the colon. Methods: The synthesized conjugates were characterized by IR and 1H-NMR spectroscopy. The cleavage of aromatic azobond resulted in a potential colon-specific liberation of drug from conjugate studied in rat fecal contents. In vitro release profiles of polyphosphazene-linked conjugates of erlotinib have been studied at pH 1.2, pH 6.8 and pH 7.4. The stability study was designed to exhibit that free drug was released proficiently and unmodified from polyphosphazene-erlotinib conjugates having aromatic azo-bond in artificial colon conditions. Results: The synthesized conjugates were demonstrated to be stable in simulated upper gastro-intestinal tract conditions. The drug release kinetics shows that all the polymer-drug conjugates of erlotinib follow zero-order release kinetics which indicates that the drug release from the polymeric backbone is independent of its concentration. Kinetic study of conjugates with slope (n) shows the anomalous type of release with an exponent (n) > 0.89 indicating a super case II type of release. Conclusion: These studies indicate that polyphosphazene linked drug conjugates of erlotinib could be the promising candidates for the site-specific treatment of colon cancer with least detrimental side-effects.

Formulation and Characterization of Glimepiride Nanoparticles for Dissolution Enhancement

2020 ◽  
Vol 10 (5) ◽  
pp. 649-663
Author(s):  
Reena Siwach ◽  
Parijat Pandey ◽  
Harish Dureja
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
Oral Absorption ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Class Ii ◽  
Dissolution Enhancement ◽  
In Vitro Drug Release ◽  
Bcs Class Ii

Background: The rate-limiting step in the oral absorption of BCS class II drugs is dissolution. Their low solubility is one of the major obstacles in the process of drug development. Dissolution rate can be increased by decreasing the particle size to the nano range, eventually leading to increased bioavailability. Objective: : In the present study, glimepiride loaded nanoparticles were prepared to enhance the dissolution rate. The aim of the work was to examine the effect of polymer-drug ratio, solvent-antisolvent ratio and speed of mixing on in vitro release of glimepiride. Methods: Glimepiride is an antidiabetic drug belonging to the BCS class II drugs. The polymeric nanoparticles were formulated according to Box-Behnken Design (BBD) using nanoprecipitation technique. The prepared nanoparticles were evaluated for in vitro drug release, loading capacity, entrapment efficiency, and percentage yield. Result: It was found that NP-8 has maximum in vitro drug release and was selected as an optimized batch. Analysis of Variance (ANOVA) was applied to the in vitro drug release to study the fitness and significance of the model. The batch NP-8 showed 70.34 ± 1.09% in vitro drug release in 0.1 N methanolic HCl and 92.02 ± 1.87% drug release in phosphate buffer pH 7.8. The release data revealed that the nanoparticles followed zero order kinetics. Conclusion: The study revealed that the incorporation of glimepiride into gelucire 50/13 resulted in enhanced dissolution rate.

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.

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