A Study of the Effect of Lipid-Based Sustained Release Formulation Techniques on Drug Release Profiles Prepared via Wet Granulation and Direct Compression

2016 ◽  
Author(s):  
Venkata Kallakunta
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Wet Granulation ◽  
Direct Compression ◽  
Release Formulation ◽  
Sustained Release Formulation ◽  
Release Profiles

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.

Development and Characterization of Glipizide Loaded Sustained Release Nanoparticles

2019 ◽  
Vol 9 (3) ◽  
pp. 232-242 ◽  
Author(s):  
Rutuja Deshmukh ◽  
Mrunal Waghulde ◽  
Satyendra Mishra ◽  
Jitendra Naik
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Drug Uptake ◽  
Sustained Drug Release ◽  
Release Formulation ◽  
Sustained Release Formulation ◽  
Fourier Transformed Infrared Spectroscopy ◽  
Wide Range ◽  
Repeated Dosing

Background: Treating the disease like diabetes is essential due to its wide range of spreading and heredity issues. Glipizide is the commonly used drug for the treatment of diabetes. Glipizide loaded sustained release nanoparticles have been developed to avoid repeated dosing. Objective: The study aimed to develop glipizide-loaded sustained release nanoparticles and characterize them for different studies. Methods: The aim of the present study was to develop glipizide-loaded sustained release nanoparticles using different polymers by the solvent evaporation method. The polymers; Eudragit (RS 100) in combination with Polycaprolactone (PCL) were used to encapsulate glipizide. Optimization of all parameters was performed as per Design Expert software by utilizing a 32 full factorial design. The developed nanoparticles were characterized using Fourier transformed infrared spectroscopy, X-ray diffraction, scanning electron microscopy and in-vitro drug release study. Results: FE-SEM showed that the surface morphology of nanoparticles was smooth and spherical as well as in an oval shape. FTIR shows there is no interaction between polymers and drug. XRD results showed that the crystallinity of pure glipizide reduced from 89.5 to 56.7% when converted into sustained release nanoparticles formulation. Sustained drug release over the period of 12 h was observed due to well encapsulation of glipizide by the polymers. Conclusion: Glipizide loaded nanoparticles were developed with good encapsulation efficiency using a combination of two different biocompatible polymers. The drug release behavior showed that they can be used to develop the sustained release formulation to reduce the side effect caused by over drug uptake as compared to the conventional formulation.

scholarly journals Liqui-Mass Technology as a Novel Tool to Produce Sustained Release Liqui-Tablet Made from Liqui-Pellets

Pharmaceutics ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 1049
Author(s):  
Matthew Lam ◽  
Nour Nashed ◽  
Ali Nokhodchi
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Tween 80 ◽  
Tween 20 ◽  
Release Formulation ◽  
Sustained Release Formulation ◽  
Eudragit Rs ◽  
Release Analysis ◽  
Insoluble Drugs ◽  
Eudragit Rs Po

The Liqui-Mass technology (also known as Liqui-Pellet technology) has shown promising results in terms of enhancing the drug release rate of water insoluble drugs in a simplistic approach. However, there is no current study on sustained-release formulation using the Liqui-Mass technology. In this study, an attempt was made to produce a sustained-release Liqui-Tablet for the first time using a matrix-based approach. The non-volatile co-solvent used in the investigation included Tween 80, Tween 20 and Kolliphor EL. The production of sustained-release propranolol hydrochloride Liqui-Tablet was successful, and data from the saturation solubility test and dissolution test did not show much difference among the mentioned non-volatile co-solvent. The best Liqui-Tablet formulation took 24 h for drug release to reach at around 100%. There seemed to be a synergistic retarding drug release effect when a non-volatile co-solvent and Eudragit RS PO were used together. The increase of Eudragit RS PO concentration increased the retardant effect. Kinetic drug release analysis suggests that the best formulation followed the Higuchi model. The flowability of pre-compressed Liqui-Tablet pellets had no issues and its size distribution was narrow. Liqui-Tablet was generally robust and most formulations passed the friability test. The study revealed that Liqui-Mass technology can be employed to sustain drug release.

STATISTICAL EXPERIMENTAL DESIGN FOR PHARMACEUTICAL DEVELOPMENT OF SUSTAINED RELEASE REGIMEN OF LINEZOLID WITH PREDICTABLE DESIGN SPACE

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (07) ◽  
pp. 30-39
Author(s):  
V. S. Gharge ◽  
◽  
R. V. Korhale ◽  
P. T. Gunjal ◽  
M. B. Shinde ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
Extracellular Fluid ◽  
Fickian Diffusion ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Statistical Experimental Design ◽  
Drug Release Profile ◽  
Sustained Release Formulation

The objective of this investigation was to develop an oral sustained release formulation of linezolid that would maximize the duration of active drug concentration in the extracellular fluid, thus assuring the therapeutic efficacy. This rationale was based on the observation that the an efficacy of linezolid depends mainly on the length of time that bacteria are exposed to antibiotic concentrations above the minimum inhibitory concentration (T>MIC). linezolid sustained release tablets were prepared by wet granulation method. A full factorial design for two-factor three levels was employed systematically to optimize drug release profile at 1, 4, 8 and 16 h. Film-coated sustained release matrix tablet exhibited fickian diffusion drug release kinetics approaching Higuchi model. The significance of the results was analyzed using analysis of non-variance (ANOVA) and P MIC for at least 24 hours.

scholarly journals Effect of Granulation Methods on Drug Release Studies in Sustained Release Matrix Tablets of a Poorly Soluble Drug prepared using Synthetic Polymers

2020 ◽  
Vol 10 (3) ◽  
pp. 76-82
Author(s):  
Lakshmi Usha Ayalasomayajula ◽  
E. Radha Rani ◽  
A.V.S. Ksheera Bhavani ◽  
A. Vyasa Murty
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Solid Dispersions ◽  
D2 Receptor ◽  
Synthetic Polymers ◽  
Solvent Evaporation ◽  
Matrix Tablets ◽  
Polymer Mixture ◽  
Wet Granulation ◽  
Direct Compression

Vomiting or emesis is the abnormal emptying of stomach and upper part of intestine through esophagus and mouth. It occurs due to stimulation of the emetic (vomiting) centre situated in the medulla oblongata. Domperidone, a D2 receptor antagonist has antiemetic and prokinetic action is used as a model drug in the present work to prepare Sustained release matrix tablets using various synthetic polymers like Eudragit and HPMC K15 M. The tablets are designed to have a pH dependent release profile in order to prevent initial drug release in the stomach to reduce the possible gastro-irritant and ulcerogenic effects of the drug. Different polymer and diluent concentrations and various compression techniques like wet granulation technique and direct compression techniques were used in order to release the contents of the tablets in a sustained manner over a certain period of time. Domperidone is BCS Class II drug and its solubility was enhanced by preparing solid dispersions using solvent evaporation technique. In the present work solid dispersions containing drug and polymer mixture in the ratio 1:1 was further formulated into tablets by incorporating various synthetic polymers in three different concentrations. The tablets were prepared using different granulating techniques. Formulation (F3) containing drug and  polymers in the ratio 1:1 prepared by wet granulation technique could sustain the drug release over a period of 12h and hence considering all the post compression parameters it was optimized as the better formulation. FTIR, DSC, X-Ray Diffraction, SEM studies were performed for optimized solid dispersion mixture and also the optimized formulation. Keywords: Solubility enhancement, Solid dispersions, Solvent Evaporation, Wet granulation, Direct Compression.

scholarly journals Implementation of time release technology in formulation development and evaluation of sustained release tablet of Lornoxicam

2014 ◽  
Vol 2 (01) ◽  
pp. 68-75 ◽  
Author(s):  
Swapnil J. Kodalkar ◽  
Rohan A. Khutale ◽  
Sachin S. Salunkhe ◽  
Sachin S. Mali ◽  
Sameer J. Nadaf
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Kinetic Studies ◽  
Release Kinetic ◽  
Matrix Tablet ◽  
Formulation Development ◽  
Release Formulation ◽  
Sustained Release Formulation ◽  
Sustained Drug Delivery

In present study, the attempts have been made to formulate sustained release tablets of lornoxicam by direct compression method. Based on viscosity grades different proportions of hydrophilic polymers (HPMC K4M, HPMC K15M, HPMC K100M) are used for preparation of lornoxicam sustained release matrix tablet. The drug excipient mixtures were subjected to preformulation studies comprising of micromeritic properties. The tablets were subjected to various studies like as physicochemical studies, in vitro drug release, kinetic studies, etc. FTIR studies shown there was no interaction between drug and polymers. The physicochemical properties of tablets were found within the limits. Lornoxicam is a first generation analgesic, inflammatory and antipyretic agent used in relieving symptoms of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, acute sciatica and low back pain. From developed formulations batch F1 have shown zero order drug release behavior and prolong drug release over a period of 12 h which was deemed as suitable and optimum formulation for sustained drug delivery. Results of the present study indicated the suitability of the low viscous polymer in the proportion of (drug:polymer) 1:1 in the preparation of sustained release formulation of lornoxicam.

scholarly journals Formulation and Evaluation of Sustained Release Verapamil Hydrochloride Using Natural Polymers

2016 ◽  
Vol 1 (02) ◽  
pp. 76-87
Author(s):  
B. Ramu ◽  
S. Ullas Kumar ◽  
G. Srikanth ◽  
Bigala Rajkamal
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Guar Gum ◽  
Release Kinetics ◽  
Natural Polymers ◽  
Release Formulation ◽  
Verapamil Hydrochloride ◽  
Sustained Release Formulation ◽  
Release Pattern ◽  
Zero Order Release

The aim of the present study was to develop sustained release formulation of Verapamil Hydrochloride to maintain constant therapeutic levels of the drug for over 12 hrs. Various grades of HPMC polymers, Guar gum, and Xanthum gum were employed as polymers. Verapamil Hydrochloride dose was fixed as 120 mg. Total weight of the tablet was considered as 400 mg. Polymers were used in the concentration of 60, 120 and 180 mg concentration. All the formulations were passed various physicochemical evaluation parameters and they were found to be within limits. Whereas from the dissolution studies it was evident that the formulation (F6) showed better and desired drug release pattern i.e.,96.10 % in 12 hours containing Guar gum polymer in the concentration of 180mg. It followed zero order release kinetics. For the optimized formulation alcohol effect has been studied by using various concentrations of alcohol in dissolution medium. As the concentration of alcohol increased the sustained action of polymer was decreased. Hence it was concluded that alcohol has significant effect on drug release pattern.

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.

Gastroretentive Floating Capsules of Risedronate Sodium: Development, Optimization, in vitro and in vivo Evaluation in Healthy Human Volunteers

2015 ◽  
Vol 8 (2) ◽  
pp. 2835-2842
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Arun Kumar Jarathi ◽  
Suresh Gande ◽  
Viswaja Medipally ◽  
Ramesh Bomma
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Zero Order ◽  
Wet Granulation ◽  
Capsule Formulation ◽  
In Vivo Evaluation ◽  
Healthy Human ◽  
X Ray ◽  
Human Volunteers

Background and the purpose of the study: Risedronate sodium inhibits osteoclast bone resorption and modulates bone metabolism. Risedronate has a high affinity for hydroxyapatite crystals in bone and is a potent antiresorptive agent. In the present investigation efforts were made to improve the bioavailability of risedronate sodium by increasing the residence time of the drug through sustained-release matrix capsule formulation via gastroretentive mechanism. Capsules were prepared by wet granulation technique. The influence of gel forming agents, amount of risedronate and total weight of capsules on physical properties, in vitro buoyancy, drug release, FTIR, DSC, X-ray studies were investigated. The release mechanisms were explored and explained by applying zero order, first order, Higuchi and Korsmeyer equations. The selected formulations were subjected to stability study at 40 °C/75% RH, 25 °C/60% RH for the period of three months. For all formulations, kinetics of drug release from capsules followed Higuchi’s square root of time kinetic treatment heralding diffusion as predominant mechanism of drug release. Formulation containing 25 mg HPMC K4M and 75 mg HPMC K100 LV (F-8) showed zero order release profile. There was no significant change in the selected formulation, when subjected to accelerated stability conditions over a period of three months. X-ray imaging in six healthy human volunteers revealed a mean gastric retention period of 5.60 ± 0.77 hrs for the selected formulation. Stable, sustained release effervescent floating capsules of risedronate sodium could be prepared by wet granulation technique.  

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