Vitamin B12 Release from P(HEMA-co-THFMA) in Water and SBF: A Model Drug Release Study

2005 ◽  
Vol 58 (6) ◽  
pp. 451 ◽  
Author(s):  
Mohammad A. Chowdhury ◽  
David J. T. Hill ◽  
Andrew K. Whittaker

A model drug release study on the ingress of water and Kokubo simulated body fluid (SBF) into poly(2-hydroxyethyl methacrylate) (P(HEMA)) and its copolymers with tetrahydrofurfuryl methacrylate (THFMA) loaded with vitamin B12 was undertaken over the temperature range 298–318 K. The polymers were studied as cylinders and were loaded with either 5 or 10 wt-% of the drug. The drug release from the polymers was found to follow a Fickian diffusion mechanism in the early stages of the drug release, with higher normalized release rates at higher temperatures and higher drug loadings. The normalized release rates were also found to be higher for the SBF solution than for water. The copolymer composition was found to have a significant effect on the rate of release of the drug, with the rate falling rapidly between HEMA mole fractions of 1.0 and 0.8, but for lower mole fractions of HEMA the normalized release rate decreased more slowly. This behaviour followed the trend found for the changes in the equilibrium penetrant contents for the copolymers.

2020 ◽  
Vol 10 (3) ◽  
pp. 271-279
Author(s):  
Tran Thi Hai Yen ◽  
Nguyen Tran Linh ◽  
Vu Thi Thu Giang ◽  
Hoang Lan Anh

Objectives: Acyclovir (ACV) is an antiviral drug, which requires frequent dosing regimen because of poor oral bioavailability and short half-life. In this study, ACV nanoparticles were formulated using ammonium methacrylates copolymers such as Eudragit RS 100 (Eud RS) and Eudragit RL 100 (Eud RL) to prolong release drug, and increase bioavailability. Methods: ACV loaded nanoparticles were prepared by the solvent replacement technique and then were characterized by particle size, distribution, entrapment efficiency, differential scanning calorimeter, transmission electron microscope, and in-vitro drug release. Results: It was found that as drug:polymer ratio changed from 1:2 to1:5, particle size and drug entrapment efficiency increased significantly. ACV– Eud RS loaded nanoparticles had a larger mean diameter of 363 nm in comparison to 200 nm of ACV- Eud RL nanoparticles. DSC results showed that in the prepared ACV-Eud RS nanoparticles, the drug was presented in the amorphous phase and may have been molecularly dispersed in the polymer matrix, but in the ACV-Eud RL nanoparticles, the drug was presented in the particles and homogeneously dispersed in the polymeric matrix. The entrapment efficiency of AVC-Eud RS nanoparticles was higher than that of ACV-Eud RL nanoparticles. In vitro drug release study showed that the ratios of released drug from ACV-Eud RS nanoparticles in the range from 58±3.8 to 62.9±4.6%, which was lower than those from ACV-Eud RL nanoparticles, in the range from 73.3±4.9 to 77.9±2.9%. The release was found to follow the Weibull model with a Fickian diffusion mechanism for both ACVEud RS and ACV- Eud RL nanoparticles. Conclusion: These results suggest that ACV nanoparticles based on Eud RS100 and Eud RL100 could prolong the release of the drug.


Author(s):  
Kranthi Kumar Kotta ◽  
L. Srinivas

The present investigation focuses on the development of mucoadhesive tablets of captopril which are designed to prolong the gastric residence time after oral administration. Matrix tablets of captopril were formulated using four mucoadhesive polymers namely guar gum, xanthan gum, HPMC K4M and HPMC K15M and studied for parameters such as weight variation, thickness, hardness, content uniformity, swelling index, mucoadhesive force and in vitro drug release. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M provide slow release of captopril over period of 12 hr and were found suitable for maintenance portion of oral controlled release tablets. The cumulative % of drug release of formulation F9 and F10 were 90 and 92, respectively. In vitro release from these tablets was diffusion controlled and followed zero order kinetics. The ‘n’ values obtained from the pappas-karsemeyer equation suggested that all the formulation showed drug release by non-fickian diffusion mechanism. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M (1:1) were established to be the optimum formulation with optimum bioadhesive force, swelling index & desired invitro drug release. This product was further subjected to stability study, the results of which indicated no significant change with respect to Adhesive strength and in vitro drug release study.


Author(s):  
Nani Tadhi ◽  
Himansu Chopra ◽  
Gyanendra Kumar Sharma

Transdermal patch is a drug delivery device in which the drugs are incorporated and is design in such a way that it releases the drug in sustained and at predetermined rate to deliver the drug through the skin to the systemic circulation painlessly. The aim of this research study was to formulate a controlled and sustained release transdermal matrix type patch of Methimazole. The matrix patch was prepared by solvent casting method using a various polymer in different concentration, HPMC (hydrophilic), Eudragit RL100 and Ethyl cellulose (hydrophobic) polymer. Total 9 prototype formulation were prepared and it was subjected for various evaluation test; weight uniformity, Folding endurance, thickness, Drug content, percent moisture content, percent Moisture uptake and In-vitro drug release study using Franz diffusion cell. The in-vitro CDR% data was fit into kinetics model to see the release kinetics from the patches. The Formulation F5 was choosen as a best formulation according to in-vitro drug release study. The in-vitro release was found 81.12 % in 12 hours, it followed zero order kinetics. The nature of polymer and concentration ratio of polymers plays a crucial role for obtaining a good transdermal patch design; therefore optimisation is very important step to formulate a desired TDDS. Therefore the result of the study encourages a further study and is hopeful that the present study would contribute to the recent pharmaceutical research for formulation development.


INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (10) ◽  
pp. 38-43
Author(s):  
Ch. Taraka Ramarao ◽  
◽  
B. Srinivasa Rao ◽  
J. Vijayaratana

Matrix Tablets, each containing 50 mg of diclofenac sodium, are prepared employing Kollidon SR by direct compression method. All the tablets were found to be non-disintegrating in acidic (pH1.2) and alkaline (pH 7.4) fluids. As such, the prepared tablets were of good quality with respect to drug content, hardness and friability. As the tablets formulated were non- disintegrating in acidic fluids, they are considered suitable for colon targeting. From the drug release study, it may be concluded that the (DK2) E2 formula of diclofenac sodium matrix tablets gives the desired release profile by showing a minimal release during the lag period of 5 h and complete release at the end of 12 h. The tablets having the optimised formula (DK2)E2, having 25% Kollidon SR with 5% of channelling agent (Eudragit S100 to that of Kollidon SR) showed minimal release of 27. 4% in the lag period of 5 hours and 99.3 % of the drug was released y the end of 12 h. The diclofenac sodium matrix tablets formulated by employing Kollidon SR and various channelling agents showed non-Fickian diffusion mechanism and followed zero order kinetics. The optimized formula (DK2) E2 follows Supercase II transport as mechanism for drug release and it follows zero order kinetics. Matrix tablets (DK2) E2 formulated employing 25% Kollidon SR and 5% Eudragit S100 are best suited to be used for colon targeting of diclofenac sodium.


INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (07) ◽  
pp. 52-57

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.


2008 ◽  
Vol 136 ◽  
pp. S196
Author(s):  
Eunjung Kim ◽  
Jaemoon Yang ◽  
Jin-Suck Suh ◽  
Yong-Min Huh ◽  
Seungjoo Haam

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