scholarly journals Disintegration, In vitro Dissolution, and Drug Release Kinetics Profiles of k-Carrageenan-based Nutraceutical Hard-shell Capsules Containing Salicylamide

2020 ◽  
Vol 18 (1) ◽  
pp. 226-231
Author(s):  
Pratiwi Pudjiastuti ◽  
Siti Wafiroh ◽  
Esti Hendradi ◽  
Handoko Darmokoesoemo ◽  
Muji Harsini ◽  
...  
Keyword(s):  
Drug Release ◽  
Rate Constant ◽  
Release Rate ◽  
Release Kinetics ◽  
Zero Order ◽  
Dissolution Profile ◽  
Natural Polymers ◽  
Drug Release Kinetics ◽  
Hard Shell

AbstractThe release of drugs from solid drug delivery materials has been studied intently in recent years. Quantitative analyses achieved from in vitro dissolution becomes easier if a zero-order mathematical model is used. Non-gelatin nutraceutical hard-shell capsules of zero size (approximately 0.7-0.8 cm) were produced from carrageenan-based natural polymers, namely carrageenan-alginate (CA) and carrageenan-starch (CS). Disintegration, dissolution and zero-order drug release kinetics of hard-shell capsules containing 100 mg of salicylamide were studied. The disintegration time of CA and CS were observed to be less than 30 min for both CA and CS. In vitro dissolution profile showed that the percentage dissolution of CA capsules was better at pH 4.5, while that of CS was poor at pH 1.2, 4.5 and 6.8. Determination of drug release kinetics profiles of carrageenan-based hardshell capsules utilized the Noyes-Whitney and Peppas-Sahlin modification rules for zero-order. The drug release from carrageenan-based capsules followed zero-order kinetics, especially at pH 6.8, and was compared to the Higuchi model. Salicylamide in CA hard-shell capsules at a pH 6.8 had a release rate constant (kH) of 2.91 %(ppm/ ppm) min-1/2, while the release rate constant of CS was 0.36 %(ppm/ppm) min-1.

scholarly journals FORMULATION AND OPTIMIZATION OF BUOYANT IN SITU GELLING SYSTEM OF VALSARTAN USING NATURAL POLYMER

2017 ◽  
Vol 9 (10) ◽  
pp. 128
Author(s):  
S. Prasanthi ◽  
M. Vidyavathi
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Natural Polymer ◽  
Natural Polymers ◽  
Independent Variables ◽  
Drug Release Kinetics ◽  
Ftir Studies

Objective: Currently natural polymers have wide spread importance in fabrication of controlled drug delivery systems. Hence in this study ocimum basilicum mucilage, (OBM) a natural polymer used to know its effect as polymer alone and in combination with HPMC K15M and Guargum in oral in situ floating gel of Valsartan using 3 full level factorial design.Methods: FTIR studies conducted to know major drug polymer interactions. OBM, HPMC K15M and Guargum were chosen as three independent variables and examined at 3 levels for in vitro buoyancy (Y1) and drug release at 10 h (Y2) as responses. By using mathematical model approach formulation variables were quantitatively evaluated, and optimized formulation (VFIG) subjected for in vitro buoyancy, density, pH, in vitro drug release, drug content, gelling capacity and drug release kinetics. In addition VFIG studied for In vivo buoyancy and release kinetics.Results: FTIR studies revealed that excipients were compatible with drug. ANOVA results shown that independent variables have significant effect (p<0.05) on both the responses. Observed responses of optimized formulation (3 % OBM, 0.88 % HPMC and 1.25 % Guar gum) were in good agreement with the experimental values. Results of all in vitro evaluations lies within the limits and drug release kinetics followed non-fickian diffusion mechanism. In vivo buoyancy study in rabbit evidenced floatation for>8 h and in vivo pharmacokinetic study exhibited increased bioavailability of optimized formulation.Conclusion: Prepared VFIG with optimized concentrations of OBM, HPMC K15M and Guargum exploiting as a promising dosage form for enhanced gastric delivery.

Formulation Development and Characterization of controlled release core in cup matrix tablets of venlafaxine HCl

2020 ◽  
Vol 15 ◽  
Author(s):  
Balaji Maddiboyina ◽  
Vikas Jhawat ◽  
Gandhi Sivaraman ◽  
Om Prakash Sunnapu ◽  
Ramya Krishna Nakkala ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Rate ◽  
Zero Order ◽  
Water Soluble ◽  
Matrix Tablets ◽  
Drug Dissolution ◽  
Crystalline Cellulose ◽  
Hydrophobic Polymers

Background: Venlafaxine HCl is a selective serotonin reuptake inhibitor which is given in the treatment of depression. The delivery of the drug at a controlled rate can be of great importance for prolonged effect. Objective: The objective was to prepare and optimize the controlled release core in cup matrix tablet of venlafaxine HCl using the combination of hydrophilic and hydrophobic polymers to prolong the effect with rate controlled drug release. Methods: The controlled release core in cup matrix tablets of venlafaxine HCl were prepared using HPMC K5, K4, K15, HCO, IPA, aerosol, magnesium sterate, hydrogenated castor oil and micro crystalline cellulose PVOK-900 using wet granulation technique. Total ten formulations with varying concentrations of polymers were prepared and evaluated for different physicochemical parameters such FTIR analysis for drug identification, In-vitro drug dissolution study was performed to evaluate the amount of drug release in 24 hrs, drug release kinetics study was performed to fit the data in zero order, first order, Hixson–crowell and Higuchi equation to determine the mechanism of drug release and stability studies for 3 months as observed. Results: The results of hardness, thickness, weight variation, friability and drug content study were in acceptable range for all formulations. Based on the In vitro dissolution profile, formulation F-9 was considered to be the optimized extending the release of 98.32% of drug up to 24 hrs. The data fitting study showed that the optimized formulation followed the zero order release rate kinetics and also compared with innovator product (flavix XR) showed better drug release profile. Conclusion: The core-in-cup technology has a potential to control the release rate of freely water soluble drugs for single administration per day by optimization with combined use of hydrophilic and hydrophobic polymers.

Fabrication and Release Kinetics of Liposomes Containing Leuprolide Acetate

2021 ◽  
Vol 7 (1) ◽  
pp. 35-38
Author(s):  
Sudipta Das ◽  
Arnab Samanta ◽  
Koushik Bankura ◽  
Debatri Roy ◽  
Amit Nayak
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Zero Order ◽  
Leuprolide Acetate ◽  
Lipid Film ◽  
In Vitro Drug Release ◽  
Liposomal Formulations ◽  
Kinetics Of

The present work is focused on the preparation and in vitro release kinetics of liposomal formulation of Leuprolide Acetate. In this work, “Thin Lipid Film Hydration Method” was used for preparation of Leuprolide Acetate loaded liposomes. Prepared liposomal formulations of Leuprolide acetate was evaluated by drug entrapment study, in-vitro drug release kinetics and stability studies. The percentage drug entrapment of Leuprolide acetate for F1 and F2 formulations were found to be 78.14 ± 0.67 and 66.70 ± 0.81% respectively. In-vitro drug release study of liposomal formulations had shown zero order release pattern. Regression co-efficient (R2) value of Zero order kinetics for F1 and F2 formulations were 0.9912 and 0.9676 respectively. After storing formulations for 1 month, stability testing was done at 40C.It was found that all batches were stable. These liposomal formulations of Leuprolide acetate can be formulated for parenteral application to treat prostate cancer and in women, to treat symptoms of endometriosis (overgrowth of uterine lining outside of the uterus) or uterine fibroids.

Design, optimization and invitro evaluation of lovastatin nanostructures lipid carrier

2020 ◽  
Vol 6 (2) ◽  
Author(s):  
Roshan K Pawar ◽  
Kalaiselvan S ◽  
Balamurugan K
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Good Control ◽  
Kinetic Studies ◽  
Zero Order ◽  
In Vitro Drug Release ◽  
23 Factorial Design ◽  
Zero Order Release ◽  
Formulation Variables

The intention of this current study is to intensify the bioavailability of drugs which have lower bioavailability (<20 %) like Lovastatin in the form of NLC carrier and also to optimize the formulation to select perfect variables for the formulation. The Nanostructures lipid carrier was formulated using Hot Homogenization technique with some optimization by utilizing 23 factorial design with the heal of response like in-vitro drug release, % Entrapment Efϑiciency (EE%), % drug Content (%DC), Zeta potential (Zp), Polydispersity Index (PI) and Particle Size (PS) for 12 hours. The kinetic studies of in-vitro drug release was performed and the parameters of the drug in different kinetic models like higuchi kinetic, zero order, ϑirst order, peppas models were evaluated. Invitro release kinetics studies show that optimized formulation NLC (N3) obeys Super Case II kinetics transport mechanism i.e., release of drug through reduction of attractive forces between Lipid chains and Zero order release kinetics for controlled drug delivery. Hence Nanostructure lipid carrier shows a good control and predetermined rate of drug release of Lovastatin. From the obtained outcome, N3 formulation was concluded as an optimized formulation with selected formulation variables like Solid Lipid: Liquid Lipid ratio (6:4), Span 80 as Surfactant (1%) and process variables like homogenization Speed as 5000 Rotations per minute for 15 mins.><20 %) like Lovastatin in the form of NLC carrier and also to optimize the formulation to select perfect variables for the formulation. The Nanostructures lipid carrier was formulated using Hot Homogenization technique with some optimization by utilizing 23 factorial design with the heal of response like in-vitro drug release, % Entrapment Efficiency (EE%), % drug Content (%DC), Zeta potential (Zp), Polydispersity Index (PI) and Particle Size (PS) for 12 hours. The kinetic studies of in-vitro drug release was performed and the parameters of the drug in different kinetic models like higuchi kinetic, zero order, first order, peppas models were evaluated. Invitro release kinetics studies show that optimized formulation NLC (N3) obeys Super Case II kinetics transport mechanism i.e., release of drug through reduction of attractive forces between Lipid chains and Zero order release kinetics for controlled drug delivery. Hence Nanostructure lipid carrier shows a good control and predetermined rate of drug release of Lovastatin. From the obtained outcome, N3 formulation was concluded as an optimized formulation with selected formulation variables like Solid Lipid: Liquid Lipid ratio (6:4), Span 80 as Surfactant (1%) and process variables like homogenization Speed as 5000 Rotations per minute for 15 mins.

scholarly journals Design and evaluation of rectal drug delivery systems of non-steroidal anti-inflammatory drug

2012 ◽  
Vol 1 (7) ◽  
pp. 165-170 ◽  
Author(s):  
P V Swamy ◽  
Mohammed Younus Ali ◽  
Y Anand Kumar ◽  
K Prasad ◽  
N Srinivaslu
Keyword(s):  
Drug Release ◽  
Vegetable Oil ◽  
Release Rate ◽  
Diffusion Mechanism ◽  
Zero Order ◽  
Inflammatory Drug ◽  
Peg 400 ◽  
Anti Inflammatory ◽  
Hydrogenated Vegetable Oil

The aim of the present study was to design and evaluate the suppositories of aceclofenac a non-steroidal anti inflammatory drug (NSAID). Aceclofenac, rectal suppositories were developed by employing various hydrophilic and hydrophobic polymeric bases like gelatin, PEG-400 and hydrogenated vegetable oil using propylene glycol as plasticizer and beeswax as hardening agent. The in-vitro release rate data was evaluated statistically and was found that from all the formulations the drug release is by diffusion mechanism (r = 0.9547 to 0.9967) according to Higuchi’s equation. All the prepared formulations have shown zero-order release kinetics except those prepared by utilizing 15% and 20 % of PEG-400. The formulation prepared using 7.5% beeswax in hydrogenated vegetable oil has displayed zero-order drug release (r = 0.9927) and has released 99.18% of the aceclofenac within 4h, hence, this formulation is considered as a promising formulation. The stability study on the promising formulation was conducted over a period of 6 months and found that there are no significant changes in the drug content and in-vitro drug release rate (p<0.05). The result suggests that the suppositories can be prepared by employing hydrophilic and hydrophobic polymers.DOI: http://dx.doi.org/10.3329/icpj.v1i7.10810International Current Pharmaceutical Journal 2012, 1(7): 165-170

scholarly journals Development of Sustained Release Preparations of Metoclopramide Hydrochloride Based on Fatty Matrix

2013 ◽  
Vol 11 (2) ◽  
pp. 129-136 ◽  
Author(s):  
Monnujan Nargis ◽  
Md Saiful Islam ◽  
Fatima Naushin ◽  
Syed Shabbir Haider
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Rate ◽  
Release Kinetics ◽  
In Vitro Dissolution ◽  
Compression Technique ◽  
Solubility Behavior ◽  
Uptake Rates ◽  
S Model

Sustained release formulations of metoclopramide HCl (4-amino-5-chloro-N-(2-diethylaminoethyl)-2- methoxybenzamide hydrochloride) (MH) were prepared using carnauba wax (CW) and stearic acid (SA) as matrix formers. Granules were prepared by melt granulation method while direct compression technique was used to prepare the tablets. The drug release profiles of these products were studied by in-vitro dissolution testing in simulated gastric, gastrointestinal and intestinal media of pH 1.2, 4.5 and 7.5, respectively. The increase in the proportion of SA in the granules produced a concomitant decrease of the initial drug release rate but later on the release rate was enhanced in the intestinal medium. Drug release was found to be affected by compression force and stirring rate but also showed a dependency on pH of the dissolution fluid. The fastest release rate was found at pH 4.5 and the slowest at pH 1.2 which was consistent with the drug’s solubility behavior. Matrix erosion and water uptake rates were highest in the intestinal medium and lowest in the gastric medium. The drug release kinetics followed the Higuchi’s model in all cases. DOI: http://dx.doi.org/10.3329/dujps.v11i2.14563 Dhaka Univ. J. Pharm. Sci. 11(2): 129-136, 2012 (December)

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