scholarly journals Synergistic Effect of Ultrasound and Polyethylene Glycol on the Mechanism of the Controlled Drug Release from Polylactide Matrices

Polymers ◽  
2019 ◽  
Vol 11 (5) ◽  
pp. 880
Author(s):  
Wenting Bao ◽  
Xianlong Zhang ◽  
Hong Wu ◽  
Rong Chen ◽  
Shaoyun Guo
Keyword(s):  
Polyethylene Glycol ◽  
Controlled Release ◽  
Drug Release ◽  
Synergistic Effect ◽  
In Vitro Release ◽  
Structure And Properties ◽  
Melt Extrusion ◽  
Model Drug ◽  
Vitro Release

In this paper, the synergistic effect of ultrasound and polyethylene glycol (PEG) on the controlled release of a water soluble drug from polylactide (PLA) matrices was studied. When ultrasound was used following the hot melt extrusion (HME) of the PLA/model drug release system, the release of the model drug (Methylene Blue (MB)) from the PLA when immersed in phosphate buffered saline (PBS) was affected by the variation of the parameters of ultrasound. It was found that no more than 2% PLA dissolved during the in-vitro release study, and the release of the MB from the PLA was diffusion controlled and fit well with the Higuchi diffusion model. Polyethylene glycol (PEG), which has high hydrophilicity and rapid dissolution speed, was blended with the PLA during the melt extrusion to enhance the release of the MB. The analysis of the structure and properties of the in-vitro release tablets of PLA/PEG/MB indicated that the ultrasound could improve the dispersion of MB in the PLA/PEG blends and it could also change the structure and properties of the PLA/PEG blends. Due to the dissolution of the PEG in PBS, the release of the MB from the PLA/PEG drug carrier was a combination of diffusion and erosion controlled release. Thus a new mechanism combining of diffusion and erosion models and modified kinetics model was proposed to explain the release behavior.

scholarly journals Use of hydrophilic and hydrophobic polymers for the development of controlled release tizanidine matrix tablets

2014 ◽  
Vol 50 (4) ◽  
pp. 799-818 ◽  
Author(s):  
Tariq Ali ◽  
Muhammad Harris Shoaib ◽  
Rabia Ismail Yousuf ◽  
Sabahat Jabeen ◽  
Iyad Naeem Muhammad ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
In Vitro Release ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Physical Parameters ◽  
Disintegration Time ◽  
Weight Variation ◽  
Vitro Release

The aim of the present study was to develop tizanidine controlled release matrix. Formulations were designed using central composite method with the help of design expert version 7.0 software. Avicel pH 101 in the range of 14-50% was used as a filler, while HPMC K4M and K100M in the range of 25-55%, Ethylcellulose 10 ST and 10FP in the range of 15 - 45% and Kollidon SR in the range of 25-60% were used as controlled release agents in designing different formulations. Various physical parameters including powder flow for blends and weight variation, thickness, hardness, friability, disintegration time and in-vitro release were tested for tablets. Assay of tablets were also performed as specified in USP 35 NF 32. Physical parameters of both powder blend and compressed tablets such as compressibility index, angle of repose, weight variation, thickness, hardness, friability, disintegration time and assay were evaluated and found to be satisfactory for formulations K4M2, K4M3, K4M9, K100M2, K100M3, K100M9, E10FP2, E10FP9, KSR2, KSR3 & KSR9. In vitro dissolution study was conducted in 900 ml of 0.1N HCl, phosphate buffer pH 4.5 and 6.8 medium using USP Apparatus II. In vitro release profiles indicated that formulations prepared with Ethocel 10 standard were unable to control the release of drug while formulations K4M2, K100M9, E10FP2 & KSR2 having polymer content ranging from 40-55% showed a controlled drug release pattern in the above mentioned medium. Zero-order drug release kinetics was observed for formulations K4M2, K100M9, E10FP2 & KSR2. Similarity test (f2) results for K4M2, E10FP2 & KSR2 were found to be comparable with reference formulation K100M9. Response Surface plots were also prepared for evaluating the effect of independent variable on the responses. Stability study was performed as per ICH guidelines and the calculated shelf life was 24-30 months for formulation K4M2, K100M9 and E10FP2.

Characterization and Study on In Vitro Release of Praziquantel from Poly(lactide-co-glycolide) Implants

2015 ◽  
Vol 1120-1121 ◽  
pp. 915-919
Author(s):  
Li Xia Ma ◽  
Zhi Qiang Fei ◽  
Chuan Dong Wang ◽  
Yang Liu ◽  
Xu Du ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Molecular Weight ◽  
Drug Release ◽  
In Vitro Release ◽  
Low Molecular Weight ◽  
Melt Extrusion ◽  
Polymer Erosion ◽  
Vitro Release

A series praziquantel-loaded poly(lactide-co-glycolide) implants are prepared by melt extrusion. The morphologies, structures and the in vitro releases are investigated. The results show that PZQ is dissolved or dispersed in the PLGA matrix and its crystal structure can be transformed into amorphous filament or flake-like structure. The in vitro release increased with the increase of the amount of low molecular weight PLGA0.13. The release of PZQ from the implant with a length of 20 mm is faster than that from that with a length of 10 mm. The macroscopic change and release curves of the implants reveal the drug release from the implants can be controlled by initial diffusion of drug from near the surface of implants followed by elution during polymer erosion.

scholarly journals Formulation and evaluation of almotriptan controlled release pellets

2019 ◽  
Vol 9 (1-s) ◽  
pp. 312-318
Author(s):  
Yerikala Ramesh ◽  
Abhilash Kaki Rohan ◽  
Balasaradhi Koorapati ◽  
P. Sudarsanam
Keyword(s):  
Content Analysis ◽  
Controlled Release ◽  
Drug Release ◽  
In Vitro Release ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Eudragit Rs ◽  
Drug Content ◽  
Vitro Release

Abstract: The aim of the present study was to formulate and evaluate Almotriptan pellets. Almotriptan controlled release pellets were prepared by Solution layering technique by using croscarmellose and povidone in former case and three different polymers HPMC K 100, Ethyl cellulose and Eudragit RS 100 as rate controlling polymer in three different ratios like 1:1, 1:1.5 and 1:2 to achieve desired release in later case. Evaluation was performed according to the Pharmacopoeia standards including Drug excipients compatibility, Percentage yield, Particle size distribution, Drug content analysis and in-vitro release study. The best results were found to be using Almotriptan and Eudragit RS 100 in 1:2 ratios. A broad variety of drug release pattern could be achieved by variation of polymers ratios which was optimized to match the target release profile. In comparison of in-vitro release studies for different controlled release formulations, F9 releases 98.54% of drug at the end of 12th hour and was considered as best formulation. Stability study has shown no significant change in the drug content analysis and in-vitro dissolution study of best formulation even after 6 months. Keywords: Almotriptan, Controlled release, Dissolution profile, in-vitro drug release, Stability studies.

scholarly journals Multiresponsive Poly(N-Acryloyl glycine)-Based Nanocomposite and Its Drug Release Characteristics

2019 ◽  
Vol 2019 ◽  
pp. 1-12 ◽  
Author(s):  
Nunthiya Deepuppha ◽  
Sudarat Khadsai ◽  
Boonjira Rutnakornpituk ◽  
Uthai Wichai ◽  
Metha Rutnakornpituk
Keyword(s):  
Controlled Release ◽  
In Vitro Release ◽  
Hydrodynamic Size ◽  
Magnetite Nanoparticle ◽  
Drug Controlled Release ◽  
Water Dispersibility ◽  
Release Study ◽  
Model Drug ◽  
Vitro Release

pH- and thermoresponsive nanocomposite composed of poly(N-acryloyl glycine) (PNAG) matrix and magnetite nanoparticle (MNP) was synthesized and then used for drug controlled release application. The effects of crosslinkers, e.g., ethylenediamine and tris(2-aminoethyl)amine, and their concentrations (1 and 10 mol%) on the size, magnetic separation ability, and water dispersibility of the nanocomposite were investigated. The nanocomposite crosslinked with tris(2-aminoethyl)amine (size ranging between 50 and 150 nm in diameter) can be rapidly separated by a magnet while maintaining its good dispersibility in water. It can respond to the pH and temperature change as indicated by the changes in its zeta potential and hydrodynamic size. From the in vitro release study, theophylline as a model drug was rapidly released when the pH changed from neutral to acidic/basic conditions or when increasing the temperature from 10°C to 37°C. This novel nanocomposite showed a potential application as a magnetically guidable vehicle for drug controlled release with pH- and thermotriggered mechanism.

Controlled Release of Metformin Hydrochloride I. In vitro Release from Physical Mixture Containing Xanthan Gum as Hydrophilic Rate Retarding Polymer

1970 ◽  
Vol 4 (1) ◽  
Author(s):  
Mashkura Ashrafi ◽  
Jakir Ahmed Chowdhury ◽  
Md Selim Reza
Keyword(s):  
Controlled Release ◽  
Xanthan Gum ◽  
In Vitro Release ◽  
Correlation Coefficients ◽  
High Ratio ◽  
Water Soluble ◽  
Metformin Hydrochloride ◽  
Model Drug ◽  
Very High

Capsules of different formulations were prepared by using a hydrophilic polymer, xanthan gum and a filler Ludipress. Metformin hydrochloride, which is an anti-diabetic agent, was used as a model drug here with the aim to formulate sustained release capsules. In the first 6 formulations, metformin hydrochloride and xanthan gum were used in different ratio. Later, Ludipress was added to the formulations in a percentage of 8% to 41%. The total procedure was carried out by physical mixing of the ingredients and filling in capsule shells of size ‘1’. As metformin hydrochloride is a highly water soluble drug, the dissolution test was done in 250 ml distilled water in a thermal shaker (Memmert) with a shaking speed of 50 rpm at 370C &plusmn 0.50C for 6 hours. After the dissolution, the data were treated with different kinetic models. The results found from the graphs and data show that the formulations follow the Higuchian release pattern as they showed correlation coefficients greater than 0.99 and the sustaining effect of the formulations was very high when the xanthan gum was used in a very high ratio with the drug. It was also investigated that the Ludipress extended the sustaining effect of the formulation to some extent. But after a certain period, Ludipress did not show any significant effect as the pores made by the xanthan gum network were already blocked. It is found here that when the metformin hydrochloride and the xanthan gum ratio was 1:1, showed a high percentage of drug release, i.e. 91.80% of drug was released after 6 hours. But With a xanthan gum and metformin hydrochloride ratio of 6:1, a very slow release of the drug was obtained. Only 66.68% of the drug was released after 6 hours. The percent loading in this case was 14%. Again, when Ludipress was used in high ratio, it was found to retard the release rate more prominently. Key words: Metformin Hydrochloride, Xanthan Gum, Controlled release capsule Dhaka Univ. J. Pharm. Sci. Vol.4(1) 2005 The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website

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.

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.

scholarly journals In vitro Release Kinetics Study of Ranolazine from Swellable Hydrophilic Matrix Tablets

1970 ◽  
Vol 8 (1) ◽  
pp. 31-38 ◽  
Author(s):  
Mohammad Nezab Uddin ◽  
Ishtiaq Ahmed ◽  
Monzurul Amin Roni ◽  
Muhammad Rashedul Islam ◽  
Mohammad Habibur Rahman ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
High Viscosity ◽  
Matrix Tablets ◽  
Release Studies ◽  
The Matrix ◽  
Vitro Release

The objective of this study was to design oral sustained release matrix tablets of Ranolazine usinghydroxypropyl methylcellulose (HPMC) as the retardant polymer and to study the effect of formulation factors suchas polymer proportion and polymer viscosity on the release of drug. In vitro release studies were performed usingUSP type II apparatus (paddle method) in 900 mL of 0.1N HCl at 100 rpm for 12 hours. The release kinetics wasanalyzed using the zero-order, first order, Higuchi and Korsmeyer-Peppas equations to explore and explain themechanism of drug release from the matrix tablets. In vitro release studies revealed that the release rate decreasedwith increase in polymer proportion and viscosity grade. Mathematical analysis of the release kinetics indicated thatthe nature of drug release from the matrix tablets was dependent on drug diffusion and polymer relaxation andtherefore followed non-Fickian or anomalous release. The developed controlled release matrix tablets of Ranolazineprepared with high viscosity HPMC extended release up to 12 hours.Key words: Ranolazine; Sustained release; Methocel E50 Premium LV; Methocel K100LV CR; Methocel K4M CR;Methocel K15M CR.DOI: 10.3329/dujps.v8i1.5333Dhaka Univ. J. Pharm. Sci. 8(1): 31-38, 2009 (June)

scholarly journals FABRICATION OF NANO CLAY INTERCALATED POLYMERIC MICROBEADS FOR CONTROLLED RELEASE OF CURCUMIN

2021 ◽  
pp. 206-215
Author(s):  
DHARMENDER PALLERLA ◽  
SUMAN BANOTH ◽  
SUNKARI JYOTHI
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Controlled Drug Release ◽  
Fickian Diffusion ◽  
Simulated Gastric Fluid ◽  
Release Mechanism ◽  
Release Studies ◽  
Swelling Studies ◽  
Vitro Release

Objective: The objective of this study was to formulate and evaluate the Curcumin (CUR) encapsulated sodium alginate (SA)/badam gum (BG)/kaolin (KA) microbeads for controlled drug release studies. Methods: The fabricated microbeads were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), X-ray diffraction (X-RD), and scanning electron microscopy (SEM). Dynamic swelling studies and in vitro release kinetics were performed in simulated intestinal fluid (pH 7.4) and simulated gastric fluid (pH 1.2) at 37 °C. Results: FTIR confirms the formation of microbeads. DSC studies confirm the polymorphism of CUR in drug loaded microbeads which indicate the molecular level dispersion of the drug in the microbeads. SEM studies confirmed the microbeads are spherical in shape with wrinkled and rough surfaces. XRD studies reveal the molecular dispersion of CUR and the presence of KA in the developed microbeads. In vitro release studies and swelling studies depend on the pH of test media, which might be suitable for intestinal drug delivery. The % of drug release values fit into the Korsmeyer-Peppas equation and n values are obtained in the range of 0.577-0.664, which indicates that the developed microbeads follow the non-Fickian diffusion drug release mechanism. Conclusion: The results concluded that the CUR encapsulated microbeads are potentially good carriers for controlled drug release studies.

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