scholarly journals Inward release polymer matrix covered by a permeable membrane: a possible zero-order controlled release device

2005 ◽  
Vol 60 (21) ◽  
pp. 5803-5808 ◽  
Author(s):  
Bo-Tau Liu ◽  
Jyh-Ping Hsu
Author(s):  
Nirmala Rangu ◽  
Gande Suresh

The present study was aimed to develop once-daily controlled release trilayer matrix tablets of nelfinavir to achieve zero-order drug release for sustained plasma concentration. Nelfinavir trilayer matrix tablets were prepared by direct compression method and consisted of middle active layer with different grades of hydroxypropyl methylcellulose (HPMC), PVP (Polyvinyl Pyrrolidine) K-30 and MCC (Micro Crystalline Cellulose). Barrier layers were prepared with Polyox WSR-303, Xanthan gum, microcrystalline cellulose and magnesium stearate. Based on the evaluation parameters, drug dissolution profile and release drug kinetics DF8 were found to be optimized formulation. The developed drug delivery system provided prolonged drug release rates over a period of 24 h. The release profile of the optimized formulation (DF8) was described by the zero-order and best fitted to Higuchi model. FT-IR studies confirmed that there were no chemical interactions between drug and excipients used in the formulation. These results indicate that the approach used could lead to a successful development of a controlled release formulation of nelfinavir in the management of AIDS.


2020 ◽  
Vol 15 ◽  
Author(s):  
Balaji Maddiboyina ◽  
Vikas Jhawat ◽  
Gandhi Sivaraman ◽  
Om Prakash Sunnapu ◽  
Ramya Krishna Nakkala ◽  
...  

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.


2018 ◽  
Vol 19 (7) ◽  
pp. 3277-3286 ◽  
Author(s):  
Ling Gong ◽  
Yanyan Sun ◽  
Miao Yu ◽  
Ying Gao ◽  
Meijuan Zou ◽  
...  

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 233 ◽  
Author(s):  
Pradeep Kumar ◽  
Yahya Choonara ◽  
Lisa du Toit ◽  
Neha Singh ◽  
Viness Pillay

This study aimed to develop a prolonged-release device for the potential site-specific delivery of a neuroprotective agent (nicotine). The device was formulated as a novel reinforced crosslinked composite polymeric system with the potential for intrastriatal implantation in Parkinson’s disease interventions. Polymers with biocompatible and bioerodible characteristics were selected to incorporate nicotine within electrolyte-crosslinked alginate-hydroxyethylcellulose gelispheres compressed within a release rate-modulating external polymeric matrix, comprising either hydroxypropylmethylcellulose (HPMC), polyethylene oxide (PEO), or poly(lactic-co-glycolic) acid (PLGA) to prolong nicotine release. The degradation and erosion studies showed that the produced device had desirable robustness with the essential attributes for entrapping drug molecules and retarding their release. Zero-order drug release was observed over 50 days from the device comprising PLGA as the external matrix. Furthermore, the alginate-nicotine interaction, the effects of crosslinking on the alginate-hydroxyethycellulose (HEC) blend, and the effects of blending PLGA, HPMC, and PEO on device performance were mechanistically elucidated using molecular modelling simulations of the 3D structure of the respective molecular complexes to predict the molecular interactions and possible geometrical orientation of the polymer morphologies affecting the geometrical preferences. The compressed polymeric matrices successfully retarded the release of nicotine over several days. PLGA matrices offered minimal rates of matrix degradation and successfully retarded nicotine release, leading to the achieved zero-order release for 50 days following exposure to simulated cerebrospinal fluid (CSF).


Author(s):  
Shamo Zokhrab Tapdiqov

Doxycycline was loaded with synthesized micelles composed of methyl Poly (ethylene glycol-block-poly (L-alanine–co–L-aspartate), or mPEG–Ala–Asp, and then characterized as a drug delivery carrier. The synthesis of the temperature-sensitive mPEG–Ala–Asp block copolymer was carried out by two-step ring-opening polymerization: firstly, the mPEG reacts with L-alanine N-carboxylic anhydride, and secondly the resulting mPEG–Ala reacts with benzyl aspartate N-carboxylic anhydride. The molecular structure of the copolymers obtained was determined by FT-IR and NMR spectroscopy methods and the micelles were characterized by SEM, TEM and DLS, respectively. The controlled release of Dox from hydrogel in the presence of PBS (8 to 9% by weight) lasts 6 to 7 days exhibiting stable release rates. The drug release mechanisms were studied: Higuchi and zero order models. The results and correlation coefficients applied to the Higuchi and zero-order models. The findings show the potential use of mPEG–Ala–Asp as an effective depot matrix to deliver anthracycline class drugs.


2000 ◽  
Author(s):  
Rupak K. Banerjee ◽  
Robert J. Lutz ◽  
Keyvan Keyhani ◽  
Robert L. Dedrick ◽  
Brian King ◽  
...  

Abstract Due to physiological barriers within the eye, which limit penetration of many drugs from the systemic circulation into the vitreous, the most common method of treating retinal disease is direct intravitreal injection. However, this common procedure may be inappropriate for a wide range of drugs as it may lead to highly variable concentrations potentially causing higher toxicity for tissues inside the eye and limiting therapeutic effect. A recent procedure is to use surgically implanted drug release device, called implant here, in the vitreous of the eye that allow controlled release of drug over a sustained period of time. For constant release of drug over 15 hours, a substantial reduction in peak drug concentration is predicted near the retina. When compared with the implant, a doubling of drug concentration would be expected for more than 3 hours near the retina for the intravitreal injection.


2020 ◽  
Vol 8 (3) ◽  
pp. 960-972 ◽  
Author(s):  
Zhi Wei Kenny Low ◽  
Yifei Luo ◽  
Kangyi Zhang ◽  
Qianyu Lin ◽  
Cally Owh ◽  
...  

On-demand controllable drug delivery systems enable the administration of precise dosages and thus have the potential to improve overall healthcare.


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