scholarly journals Drug Release from the Water-in-Oil-in-Water Multiple Emulsion in Vitro. II. Effects of the Addition of Hydrophilic Surfactants to the Internal Aqueous Compartment on the Release Rate of Secretin.

1993 ◽  
Vol 41 (4) ◽  
pp. 741-746 ◽  
Author(s):  
Takayuki OHWAKI ◽  
Masahiro NAKAMURA ◽  
Hiroshi OZAWA ◽  
Yoshiaki KAWASHIMA ◽  
Tomoaki HINO ◽  
...  
Keyword(s):  
Drug Release ◽  
Release Rate ◽  
Multiple Emulsion ◽  
Oil In Water

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.

scholarly journals Development and In Vitro-In Vivo Evaluation of a Novel Sustained-Release Loxoprofen Pellet with Double Coating Layer

Pharmaceutics ◽  
2019 ◽  
Vol 11 (6) ◽  
pp. 260 ◽  
Author(s):  
Dongwei Wan ◽  
Min Zhao ◽  
Jingjing Zhang ◽  
Libiao Luan
Keyword(s):  
Citric Acid ◽  
Drug Release ◽  
Sustained Release ◽  
Release Rate ◽  
Diffusion Rate ◽  
Immediate Release ◽  
Pharmacokinetic Studies ◽  
Release Tablet

This study aimed to develop a novel sustained release pellet of loxoprofen sodium (LXP) by coating a dissolution-rate controlling sub-layer containing hydroxypropyl methyl cellulose (HPMC) and citric acid, and a second diffusion-rate controlling layer containing aqueous dispersion of ethyl cellulose (ADEC) on the surface of a LXP conventional pellet, and to compare its performance in vivo with an immediate release tablet (Loxinon®). A three-level, three-factor Box-Behnken design and the response surface model (RSM) were used to investigate and optimize the effects of the citric acid content in the sub-layer, the sub-layer coating level, and the outer ADEC coating level on the in vitro release profiles of LXP sustained release pellets. The pharmacokinetic studies of the optimal sustained release pellets were performed in fasted beagle dogs using an immediate release tablet as a reference. The results illustrated that both the citric acid (CA) and ADEC as the dissolution- and diffusion-rate controlling materials significantly decreased the drug release rate. The optimal formulation showed a pH-independent drug release in media at pH above 4.5 and a slightly slow release in acid medium. The pharmacokinetic studies revealed that a more stable and prolonged plasma drug concentration profile of the optimal pellets was achieved, with a relative bioavaibility of 87.16% compared with the conventional tablets. This article provided a novel concept of two-step control of the release rate of LXP, which showed a sustained release both in vitro and in vivo.

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.

STUDY OF THE DIFFERENT RELEASE CHARACTERISTICS OF ANTIBIOTICS FROM PATIENTS: A DYNAMIC ELUTING SYSTEM TO INVESTIGATE DRUG RELEASE FROM ANTIBIOTIC-IMPREGNATED CALCIUM SULFATE DELIVERY

2015 ◽  
Vol 15 (01) ◽  
pp. 1550012
Author(s):  
YANG ZHANG ◽  
RENJIE WU ◽  
YING HU ◽  
YU DONG ◽  
LIFENG SHEN ◽  
...  
Keyword(s):  
Drug Release ◽  
Delivery System ◽  
Release Rate ◽  
Calcium Sulfate ◽  
Fickian Diffusion ◽  
Release Behavior ◽  
Cumulative Release ◽  
In Vivo Release

Background: Antibiotic-impregnated calcium sulfate delivery systems (ACDS) are commonly used to treat chronic osteomyelitis. Our research is to investigate drug release in vitro over a longer period, as a cautious predictor of in vivo release. Methods: The local release behavior of antibiotic in vitro was simulated. The consecutive dynamic eluting experiment was performed based on the pro-operative characteristic of osteomyelitis patients and the determined results of drug concentration in the human drainage tissue fluid (DTF). The concentration of each drug in the receiving solution was detected by ultra-performance liquid chromatography-tandem quadrupole detector mass spectrometry. The ACDS was reviewed by scanning electronic microscopy (SEM) after 48 h, and prepared to be eluted for another examination after 33 days. The mechanism of antibiotic release was analyzed by using the Ritger–Peppas and Weibull equations. Results: The cumulative release rate of vancomycin in a vancomycin-calcium sulfate delivery system (VCDS) was 77.50 % (3.0 mm diameter) and 72.43 % (4.8 mm diameter), while that of the tobramycin in a tobramycin-calcium sulfate delivery system (TCDS) was 88.0 % (3.0 mm diameter) and 84.55 % (4.8 mm diameter). At the 15th day, approximately 27.92% of vancomycin was and 29.35% of tobramycin was released from the local implant in vivo. Using SEM, numerous vancomycin and tobramycin particles were found to be attached to the columnar calcium sulfate crystals at the start of the experiment. The release behavior of the two antibiotics followed a combination of Fickian diffusion and Case II transport mechanisms within the first 48 h, and a Fickian diffusion mechanism during the subsequent time period. The correlation coefficient of tobramycin and vancomycin in vivo and in vitro was 0.9704–0.9949 and 0.9549–0.9782, respectively. Conclusion: A good correlation of the in vivo and in vitro cumulative release rates was observed by comparing the cumulative release rate of drugs in vitro by means of the dynamic eluting model, and in the DTF. Therefore, our study has proved that it is possible to use the dynamic eluting model as a cautious predictor of in vivo release.

Effects of Four Mesostructures on their Drug Release Properties

2013 ◽  
Vol 645 ◽  
pp. 125-128
Author(s):  
Wei Zeng
Keyword(s):  
Drug Release ◽  
Mesoporous Materials ◽  
Release Rate ◽  
Drug Efficacy ◽  
Drug Release Rate ◽  
Ordered Mesoporous Materials ◽  
Ordered Mesoporous ◽  
Fast Release ◽  
Mcm 41

Five ordered mesoporous materials, SBA-1, MCM-48, SBA-7, MCM-41 and SBA-15, were prepared and tested as mesophase drug delivery systems with an anti-inflammatory drug, ibuprofen. The results of these mesostructures on in vitro ibuprofen delivery indicated that the mesoporous materials with cage-like structure, SBA-1 and SBA-7, had unfavorable load and release properties. MCM-48 also showed fast release rate due to its opening channel. However, the hexagonal mesostructure in MCM-41 and SAB-15 was advantageous for extending drug release rate although a little difference existed between them. Compared with commercial ibuprofen capsule, the release system based on MCM-41 materials displayed the drug efficacy in a longer time.

Development of Acrylic Matrix Type Ketoprofen Patch

2012 ◽  
Vol 506 ◽  
pp. 533-536
Author(s):  
Nanthida Wonglertnirant ◽  
S. Tipwichai ◽  
Praneet Opanasopit ◽  
Theerasak Rojanarata ◽  
Suwannee Panomsuk ◽  
...  
Keyword(s):  
Drug Release ◽  
Release Rate ◽  
Pressure Sensitive Adhesive ◽  
Drug Release Rate ◽  
Matrix Type ◽  
Adhesive Matrix ◽  
Pressure Sensitive ◽  
Transdermal Patches ◽  
Significant Difference

Ketoprofen transdermal patches (KTPs) were fabricated using an acrylic pressure sensitive adhesive (PSA) polymer. The influence of different factors (amount of PSA, drug content, and pressure applying on the backing membrane during preparation) on the characteristics of ketoprofen patch (thickness, W/A ratio, and adhesiveness of matrix film) and in vitro drug release behavior were investigated. The results revealed the successful fabrication and a good physical appearance of KTPs using acrylic PSA. Microscopic observations, FTIR spectra, and DSC thermograms were permitted to demonstrate that the drug was dispersed molecularly in the polymer. As the amount of PSA in the adhesive matrix was increased, the release rate of ketoprofen was decreased. Contrarily, the drug release rate was increased corresponding to the increase of ketoprofen content in the adhesive matrix. There was no significant difference in the release rate when the pressure applying on the backing membrane was varied. The kinetic of ketoprofen release from acrylic matrix type transdermal patches followed the Higuchis diffusion model.

Influence of Vertical Diffusion Cell Set-Up on In Vitro Silver Sulfadiazine Drug Release from Thermo-Responsive Cellulose Hydrogel

2021 ◽  
Vol 1030 ◽  
pp. 19-26
Author(s):  
Maha Mohammad Al-Rajabi ◽  
Teow Yeit Haan
Keyword(s):  
Drug Release ◽  
Release Rate ◽  
Silver Sulfadiazine ◽  
Diffusion Cell ◽  
Vertical Diffusion ◽  
In Vitro Drug Release ◽  
Cellulose Hydrogel ◽  
Membrane Type ◽  
Set Up

In-vitro drug release is used to measure the release of the silver sulfadiazine (SSD) from thermo-responsive cellulose hydrogel using a vertical diffusion cell (VDC). However, selected VDC set-up used by researchers are random, and the studies are lacking in information on the challenging sink conditions during in-vitro drug release study. The objective of this study is to examine the influence of VDC set-up on the in-vitro SSD drug release from thermo-responsive cellulose hydrogel. VDC set-up including receptor medium composition, membrane type, and stirring speed were studied. The results depicted that SSD release rate increased with increasing ammonia percentage in phosphate buffer solution. On the other hand, membrane type do not influence SSD release rate. While, increasing stirring speed results in forming vortex or air bubble entrapment underneath the membrane. 0.25 v/v% ammonia receptor medium, cellulose membrane or polysulfone membrane, and 600 rpm stirring speed are the optimum VDC set-up, confirming sink condition and discriminating ability of this optimum VDC set-up. This work has successfully studied the influence of VDC set-up on in-vitro SSD drug release from thermo-responsive cellulose hydrogel, and the optimum VDC set-up was selected.

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

Sign in / Sign up

Export Citation Format

Share Document