Electrosprayed PVP/Shellac Composite Medicated Microparticles for Providing Biphasic Drug Release Profile

2014 ◽  
Vol 633-634 ◽  
pp. 562-566
Author(s):  
Yong Hui Wu ◽  
Deng Guang Yu ◽  
Qian Su ◽  
Cheng Lei Cai ◽  
Ji An Zhang ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Average Diameter ◽  
Release Profile ◽  
Vinyl Pyrrolidone ◽  
In Vitro Dissolution ◽  
Hydrophilic Polymer ◽  
Drug Release Profile ◽  
Poly Vinyl Pyrrolidone

The present study reports that a sustained release profile could be transferred into a biphasic drug release profile when a hydrophilic polymer was encapsulated into the medicated microparticles. The multiple component composite microparticles were fabricated using a single fluid electrospraying process to treat a co-dissolving solution consisting of a polymer matrix (shellac), an active ingredient (FA), and an additional hydrophilic polymer (poly vinyl pyrrolidone, PVP). FESEM results showed that the microparticles M1 consisting of shellac and FA had an average diameter of 1.27 ± 0.38 μm, whereas the microparticles M2 consisting of shellac, FA and PVP had an average diameter of 1.51 ± 0.34 μm. Both the two types of microparticles were essentially amorphous composites due to the favourable secondary interactions between the components, as demonstrated by ATR-FTIR tests. In vitro dissolution tests demonstrated that the addition of PVP in the microparticles M2 made them give a typical biphasic drug release profile, whereas the double-component microparticles provided a sustained release profile. This study shows a simple way for developing advanced drug delivery systems through tailoring the components of polymer excipients using electrospraying.

Development and In vitro Evaluation of Sustained Release Matrix Tablets of Theophylline using Hydrophilic Polymer as Release Retardant

2009 ◽  
Vol 2 (1) ◽  
pp. 450-456
Author(s):  
D. Nagasamy Venkatesh ◽  
Jawahar N. ◽  
Ganesh G.N.K. ◽  
R. Suresh Kumar ◽  
Senthil V. ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Matrix Material ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Hydrophilic Polymer ◽  
Improve Patient Compliance ◽  
In Vitro Drug Release ◽  
Improve Patient

In the present investigation, an attempt has been made to increase therapeutic efficacy, reduce frequency of administration and improve patient compliance by developing sustained release matrix tablets of theophylline. Sustained release matrix tablets of theophylline were developed by using drug and different concentrations of polymer such as 10, 20, 30, 40 and 50%. Hydroxypropylmethylcellulose (HPMC) was used as a matrix material and microcrystalline cellulose as diluent. All the lubricated formulations were compressed using 10 mm flat faced punches. Compressed tablets were evaluated for uniformity of weight, drug content, friability, hardness, thickness, in vitro dissolution and swelling index. All the formulations were found to be within pharmacopoeial standards. Among the different formulations, F1 showed sustained release of drug for 12 h with 84.23% release. The effect of release modifier (PEG 6000) on in vitro drug release was also studied. Thus, HPMC can be used as an effective matrix former, to extend the release of theophylline

scholarly journals Design and characterization of metoprolol floating matrix tablet

2017 ◽  
Vol 4 (2) ◽  
pp. 118
Author(s):  
Vasudha Bakshi ◽  
Swapna S. ◽  
Deepa Kumari Choudhary ◽  
Ch. Revanth ◽  
B. Sai KumarCh. Praveen ◽  
...  
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Release Profile ◽  
In Vitro Dissolution ◽  
Matrix Tablet ◽  
Formulation Development ◽  
Drug Release Profile ◽  
Gastric Residence Time

Objective: The objective of the present research was to develop a matrix embedded floating tablet of Metoprolol for the sustained activity and prolongation of gastric residence time to improve the bioavailability of the drug. Metoprolol was chosen as a model drug because it is better absorbed in the stomach than the lower gastro intestinal tract.Methods: The experimental work was divided into pre-formulation studies, formulation development, and evaluation. Standardization of drug and excipients confirmed the authentication of the samples. Floating test were conducted for all formulations, In vitro dissolution studies were carried out in a dissolution testing apparatus-II, FTIR study was performed to interpret the drug ,excipient interaction.Results: Floating tests were also performed for 15 formulations and among them five formulations have passed the floating tests (F1, F3, F5, F7, and F14). The In-vitro release kinetics study of this tablet indicated sustained release for Metoprolol and followed zero order release and 95% drug in 8 h in vitro. The drug release profile of formulated product was compared with marketed product Metolar. The floating tablets extended the drug release up to 8 hours. The drug-polymer interaction was evaluated by fourier transform infrared spectroscopy (FTIR).Conclusions: F3 formulation showed the best floating results. The comparative study between F3 and Metolar (Marketed Product) showed the similar in vitro drug release profile. Thus, the optimzed formulation F-3 can be successfully used for the management of hypertension.

Development and Optimization of Sustained Release Moxifloxacin Hydrochloride Loaded Nanoemulsion for Ophthalmic Drug Delivery: A 32 Factorial Design Approach

2020 ◽  
Vol 12 ◽  
Author(s):  
Sagar R. Pardeshi ◽  
Harshal A. Mistari ◽  
Rakhi S. Jain ◽  
Pankaj R. Pardeshi ◽  
Rahul L. Rajput ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Factorial Design ◽  
Water Solubility ◽  
Tween 80 ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
Bacterial Conjunctivitis ◽  
Promising Alternative

Background: Moxifloxacin is a BCS class I drug used in the treatment of bacterial conjunctivitis and keratitis. Despite its high water solubility, it possesses limited bioavailability due to anatomical and physiological constraints associated with the eyes which required multiple administrations to achieve a therapeutic effect. Objective: In order to prolong drug release and to improve antibacterial efficacy for the treatment of bacterial keratitis and conjunctivitis, moxifloxacin loaded nanoemulsion was developed. Methods: The concentration of oil (oleic acid), surfactant (tween 80), and cosurfactant (propylene glycol) were optimized by employing a 3-level 2-factorial design of experiment for the development of nanoemulsion. The developed nanoemulsion was characterized by particle size distribution, viscosity, refractive index, pH, drug content and release, transmission electron microscopy (TEM), and antibacterial study. The compatibility of the drug with the excipients was accessed by Fourier transform infrared spectroscopy (FTIR). Result: The average globule size was found to be 198.20 nm. The TEM study reveals the globules were nearly spherical and are well distributed. In vitro drug release profile for nanoemulsion shown sustained drug release (60.12% at the end of 6 h) compared to drug solution, where complete drug released within 2 h. The antibacterial effectiveness of the drug-loaded nanoemulsion was improved against S. aureus compared with the marketed formulation. Conclusion: The formulated sustained release nanoemulsion could be a promising alternative to eye drop with improved patient compliance by minimizing dosing frequency with improved antibacterial activity.

scholarly journals FORMULATION AND EVALUATION OF SUSTAINED RELEASE MATRIX TABLET OF LORNOXICAM BY DIRECT COMPRESSION METHOD

2021 ◽  
Vol 10 (5) ◽  
pp. 131-136
Author(s):  
Asim pasha ◽  
C N Somashekhar
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Prolonged Release ◽  
Matrix Tablet ◽  
Direct Compression ◽  
Dissolution Profile ◽  
Drug Content

The aim of the present work was to develop sustained release Lornoxicam matrix tablets with polymers like HPMC K15M, Ethyl cellulose, and Crospovidone as carriers in varying quantities. Direct compression was used to make matrix tablets. Various assessment parameters, such as hardness, friability, thickness, percent drug content, weight variation, and so on, were applied to the prepared formulations. In vitro dissolution studies were carried out for 24 hrs. The tablets were subjected to in-vitro drug release in (pH 1.2) for first 2 hrs. Then followed by (pH 6.8) phosphate buffer for next 22 hrs. And the results showed that among the six formulations FL3 showed good dissolution profile to control the drug release respectively. The drug and polymer compatibility were tested using FT-IR spectroscopy, which revealed that the drug was compatible with all polymers. It is also required to design an appropriate prolonged release formulation for Lornoxicam in order to maintain the drug's release. Hence by using the compatible polymers sustained release tablets were formulated and subjected for various types of evaluation parameters like friability, hardness, drug content and dissolution behaviour. Finally, the findings reveal that the prepared sustained release matrix tablets of lornoxicam have improved efficacy and patient compliance.

DEVELOPMENT AND CHARACTERIZATION OF MUCOADHESIVE PATCHES OF NICERGOLINE FOR BUCCAL DRUG DELIVERY BY USING FACTORIAL DESIGN OF EXPERIMENT (DOE)

INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (07) ◽  
pp. 52-57
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Design Of Experiment ◽  
Release Profile ◽  
Drug Release Profile ◽  
In Vitro Drug Release ◽  
Drug Release Study ◽  
Drug Content ◽  
Release Study

The aim of this research was to develop mucoadhesive buccal patches of nicergoline by using Factorial Design of Experiment, in order to provide a sustained release of drug into the systemic circulation. A 33 factorial experimental design was employed for optimization and to study the effect of formulation variables on responses R1 (% swelling index), R2 (% drug content), R3 (mucoadhesion time) and R4 (mucoadhesion strength). In vitro drug release study was performed on the optimized formulations. All the prepared formulations had good mechanical strength, mucoadhesion strength, neutral surface pH and drug content up to 98.17%. In vitro drug release study revealed that F-5 formulation showed promising sustained drug release profile (98.21%) for over 8 h and could be a potential substitute for marketed conventional formulations. The developed formulation (F5) was found to be optimized with considerably good stability and extended drug release profile.

scholarly journals In Vitro Release Kinetics Study of Different Brands of Esomeprazole Sustained Release Tablets Available in Bangladesh

1970 ◽  
Vol 2 (1) ◽  
pp. 27-31 ◽  
Author(s):  
Abul Kalam Lutful Kabir ◽  
Tasbira Jesmeen ◽  
Md Mesbah Uddin Talukder ◽  
Abu Taher Md Rajib ◽  
DM Mizanur Rahman
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
National Brand ◽  
First Order ◽  
Time Period ◽  
Esomeprazole Magnesium

Commercially available four national and four international brands of esomeprazole magnesium sustained release matrix tablets were studied in simulated gastric medium (pH 1.2) for 2 hours and simulated intestinal medium (pH 6.8) for 8 hours time period using USP reference dissolution apparatus. All the national and international brands complied with the USP in-vitro dissolution specifications for drug release in simulated gastric medium. However, one of the national brands (Code: MP-1) and one of the international brands (MP-7) failed to fulfill the official requirement of 80% drug release within 8th hour in simulated intestinal medium. Drug release of that national and international brand were 70.49% and 67.05% respectively within the specified time period, however one national brand (Code: MP-4) released 103.46 % drug within 8th hour in intestinal medium. Drug release profiles were analyzed for zero order, first order and Higuchi equation to reveal the release kinetics perspective of esomeprazole magnesium sustained release matrix tablets. It was found that zero order release kinetics was the predominant release mechanism than first order and Higuchi release kinetics for those brands (Code: MP-2, MP-3, MP-4, MP-5, MP-6 and MP-8) which complied with the USP in vitro dissolution specification for drug releases. On the other hand, first order release kinetics was predominant for one national and also one international non compliant brands (Code: MP-1 and MP-6). Key Words: In vitro dissolution; Sustained release; Market preparations; Kinetic analysis; Esomeprazole; National brand; International brand. DOI: 10.3329/sjps.v2i1.5812Stamford Journal of Pharmaceutical Sciences Vol.2(1) 2009: 27-31

scholarly journals FORMULATION AND EVALUATION OF SUSTAINED RELEASE MATRIX TABLETS OF LEVOSULPIRIDE BY USING NATURAL POLYMER

2017 ◽  
Vol 10 (5) ◽  
pp. 285
Author(s):  
S Shanmugam
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Xanthan Gum ◽  
Diffusion Mechanism ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Release Kinetic ◽  
Natural Polymers ◽  
In Vitro Drug Release

Objective: The objective of the present study was to develop sustained release matrix tablets of levosulpiride by using natural polymers.Method: The tablets were prepared with different ratios of Chitosan, Xanthan gum and Guar gum by wet granulation technique. The solubility study of the levosulpiride was conducted to select a suitable dissolution media for in vitro drug release studies.Results: Fourier transform infrared (FTIR) study revealed no considerable changes in IR peak of levosulpiride and hence no interaction between drug and the excipients. DSC thermograms showed that no drug interaction occurred during the manufacturing process. In vitro dissolution study was carried out for all the formulation and the results compared with marketed sustained release tablet. The drug release from matrix tablets was found to decrease with increase in polymer ratio of Chitosan, Xanthan gum and Guar gum.Conclusion: Formulation LF3 exhibited almost similar drug release profile in dissolution media as that of marketed tablets. From the results of dissolution data fitted to various drug release kinetic equations, it was observed that highest correlation was found for First order, Higuchi’s and Korsmeyer equation, which indicate that the drug release occurred via diffusion mechanism.  Keywords: Levosulpiride, sustained release tablets, natural polymers, in vitro drug release studies 

scholarly journals Formulation and Characterization of Aceclofenac-Loaded Nanofiber Based Orally Dissolving Webs

Pharmaceutics ◽  
2019 ◽  
Vol 11 (8) ◽  
pp. 417 ◽  
Author(s):  
Emese Sipos ◽  
Nóra Kósa ◽  
Adrienn Kazsoki ◽  
Zoltán-István Szabó ◽  
Romána Zelkó
Keyword(s):  
Oral Absorption ◽  
Vinyl Pyrrolidone ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Drug Release Profile ◽  
Scanning Calorimetry ◽  
Ft Ir ◽  
Fast Dissolution ◽  
Poly Vinyl Pyrrolidone

Aceclofenac-loaded poly(vinyl-pyrrolidone)-based nanofiber formulations were prepared by electrospinning to obtain drug-loaded orally disintegrating webs to enhance the solubility and dissolution rate of the poorly soluble anti-inflammatory active that belongs to the BCS Class-II. Triethanolamine-containing ternary composite of aceclofenac-poly(vinyl-pyrrolidone) nanofibers were formulated to exert the synergistic effect on the drug-dissolution improvement. The composition and the electrospinning parameters were changed to select the fibrous sample of optimum fiber characteristics. To determine the morphology of the nanofibers, scanning electron microscopy was used. Fourier transform infrared spectroscopy (FT-IR), and differential scanning calorimetry (DSC) were applied for the solid-state characterization of the samples, while the drug release profile was followed by the in vitro dissolution test. The nanofibrous formulations had diameters in the range of few hundred nanometers. FT-IR spectra and DSC thermograms indicated the amorphization of aceclofenac, which resulted in a rapid release of the active substance. The characteristics of the selected ternary fiber composition (10 mg/g aceclofenac, 1% w/w triethanolamine, 15% w/w PVPK90) were found to be suitable for obtaining orally dissolving webs of fast dissolution and potential oral absorption.

scholarly journals Fabrication Of Glimepiride Datura Stramonium Leaves Mucilage And Poly Vinyl Pyrrolidone Sustained Release Matrix Tablets: In Vitro Evaluation

1970 ◽  
Vol 8 (1) ◽  
pp. 63-72
Author(s):  
Abdul Ahad Hindustan ◽  
U Anand Babu ◽  
K Nagesh ◽  
D Sai Kiran ◽  
K Bindu Madhavi
Keyword(s):  
Mechanical Properties ◽  
Sustained Release ◽  
Datura Stramonium ◽  
Matrix Tablets ◽  
Vinyl Pyrrolidone ◽  
Stability Studies ◽  
Swelling Properties ◽  
Accelerated Stability ◽  
Poly Vinyl Pyrrolidone

The main purpose of the present work was to develop matrix tablets of Glimepiride with Datura stramonium leaves mucilage and Poly Vinyl Pyrrolidone and to study its functionality as a matrix forming agent for sustained release tablet formulations. Mucilage from Datura stramonium leaves was extracted, isolated, purified and characterized. Physicochemical properties of the dried powdered mucilage of Datura stramonium leaves were studied. Various formulations of Glimepiride Datura stramonium leave mucilage and Poly Vinyl Pyrrolidone were prepared. The formulated tablets were tested for mechanical properties, friability, swelling behavior, in vitro drug release pattern and the dissolution data was treated with mathematical modeling and the optimized formulation was tested for accelerated stability studies. The formulated tablets were found to have good mechanical properties, good swelling properties. The in vitro dissolution data was perfectly fitting to zero order and the release of drug from the formulation followed Higuchi’s release. The accelerated stability studies revealed that the tablets retain their characteristics even after stressed storage conditions. From this study it was concluded that the dried Datura stramonium leaves mucilage and Poly Vinyl Pyrrolidone combination can be used as a matrix forming material for making sustained release matrix tablets. DOI: http://dx.doi.org/10.3126/kuset.v8i1.6044 KUSET 2012; 8(1): 63-72

Preparation, Characterization and In Vitro Evaluation of IVM Loaded Poly(lactic-Co-Glycolic Acid) (PLGA) Microspheres

2011 ◽  
Vol 311-313 ◽  
pp. 1751-1754
Author(s):  
Gui Yu Li ◽  
Xi Hong Lu ◽  
Xue Hu Li ◽  
Lei Tao ◽  
Jian Ping Liang
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
High Performance ◽  
Glycolic Acid ◽  
Drug Release Profile ◽  
Release Formulation ◽  
Sustained Release Formulation ◽  
Drug Delivery Carrier ◽  
Drug Sustained Release

Drug was encapsulated in a novel copolymers of poly(lactic-co-glycolic acid) (PLGA) to investigate the sustained-release formulation of drug loaded polymer microspheres delivery system. Used a modified solid-in-oil-in-water (S/O/W) emulsion solvent evaporation method to prepare microspheres, its morphology and particle size distribution were estimated by scanning electron microscopy (SEM), the profile of in vitro drug release were assessed by High performance liquid chromatography (HPLC). Finally, an stable release buffer was utilized to obtain a detailed drug release profile, which was analyzed by HPLC also. Results showed that the microspheres morphology, encapsulation efficiency and the cumulative drug release efficiency were appropriate for veterinary medicine using. The modified preparation method was simple and optimized, PLGA microspheres with excellent controlled-release characteristics may serve as drug delivery carrier and may prolong the drug sustained-release effect.

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