scholarly journals Interpolymer Complex of Chitosan and Eudragit L-100: Preparation, Characterization and Drug Release Behavior

2021 ◽  
pp. 115-127
Author(s):  
Shrikant Bute ◽  
Saurabh Gupta ◽  
Kamlesh Wadher ◽  
Nikita Naidu ◽  
Milind Umekar
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Diclofenac Sodium ◽  
Matrix Tablets ◽  
Interpolymer Complex ◽  
Interpolyelectrolyte Complex ◽  
Eudragit L100 ◽  
Interpolyelectrolyte Complexes ◽  
Release Drug ◽  
Model Drug

Aims: The aim of the present investigation was to prepare interpolymer complex between Chitosan and Eudragit L100, and to evaluate its performance as a matrix for controlled release of drugs, using Diclofenac sodium as a model. Methodology: Interpolymer complex were prepared by combining different % chitosan solutions with different % Eudragit L100 solutions in different ratios. The formation of interpolyelectrolyte complexes (IPEC) between carbopol and Chitosan was investigated, using turbidimetry and viscosity measurement. The structure of the prepared IPEC was investigated using FTIR spectroscopy and DSC. A Rotary compression press was used to formulate matrix tablets of diclofenac sodium using polymers in physical mixture and IPECs.The amount of Diclofenac Sodium released in the dissolution medium was determined spectrophotometrically at 276 nm. Results: The results of the present investigation confirmed the formation of an interpolyelectrolyte complex between Chitosan and Eudragit L 100. The release of the model drug Diclofenac sodium was significantly controlled from tablets made up of the IPEC as compared with polymers alone and in combination. Release profiles were represented by a mathematical model, which indicates that the prepared system releases drug in a zero-order manner by changing the ratio of the IPEC in the tablets. Conclusion: Controlled release drug delivery systems designed to manipulate the drug release to achieve specific clinical objectives that are unattainable with conventional dosage forms.

scholarly journals Comparative Evaluation of HPMC, PVA and Gelatin as Matrices for Controlled Release Drug Delivery

1970 ◽  
Vol 2 (1) ◽  
pp. 51-55
Author(s):  
Mohammad Anwarul Basher ◽  
Abul Kalam Lutful Kabir ◽  
Mohammad Musarraf Hussain ◽  
Mir Mohammad Abdullah Al Mamun
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Diclofenac Sodium ◽  
Magnesium Stearate ◽  
Matrix Tablets ◽  
Matrix Tablet ◽  
Pharmaceutical Sciences ◽  
Drug Release Profile ◽  
Compression Process ◽  
Model Drug

The present study was undertaken to compare three different polymeric gums- HPMC, PVA and gelatin as controlled release matrices. Diclofenac sodium, a potent analgesic, was used as the model drug. Different ratio of HPMC, PVA and gelatin were incorporated into the lactose loaded Diclofenac tablet to explore their impact on drug release. Matrix tablets of Diclofenac were prepared by using individual polymer with magnesium stearate and aerosil by direct compression process at 5 ton pressure. The release of drug from these matrices was studied over 2 hrs in acidic media where insignificant release was observed. Then, the same formulations were studied over 8 hours in buffer media of pH 6.8 at a temperature of 37± 0.5°C. Statistically significant differences in drug release profile was found among the tablets prepared from different matrices. The study revealed that the average % release of drug from different types of polymer loaded matrix tablet varied with the ratio of different polymers. Among the three polymers, PVA showed best dissolution pattern. A comparison of Higuchi curve and bi-exponential curve was also performed. Key words: HPMC; PVA; Gelatin; Controlled release; Diclofenac DOI: 10.3329/sjps.v2i1.5816Stamford Journal of Pharmaceutical Sciences Vol.2(1) 2009: 51-55

Preparation and Evaluation of Ternary Polymeric Blends for Controlled Release Matrices Containing Weakly Basic Model Drug

2020 ◽  
Vol 17 ◽  
Author(s):  
Wasfy M. Obeidat ◽  
Shadi F. Gharaibeh ◽  
Abdolelah A. Jaradat ◽  
Osama Abualsuod
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Sodium Alginate ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Sustained Drug Release ◽  
Basic Drug ◽  
Basic Model ◽  
Polymeric Compositions ◽  
Model Drug

Objective: The objective of this study was to evaluate the suitability of ternary mixture of smart polymers comprised of Eudragit®E100, Eudragit®L100, and sodium alginate to serve as a carrier for sustained drug release for weakly basic drugs. The model drug chosen in this part of the study is Metronidazole. Methods: Matrix tablets formulations were prepared by either direct compression or by wet granulation. Dissolution studies were conducted using USP XXΠ rotating paddle apparatus in three different consecutive stages (pH 1.2, 4.8 and 6.8). Tablets made of low to intermediate proportions of sodium alginate and an approximately equal proportions of Eudragit®E100 and Eudragit®L100 were found to have significant modification of drug release rates. Result: Thus, indicating a potential for controlling the drug release for 12 hours depending on polymers ratios in the formulation. The ratio of sodium alginate to total Eudragit® polymers and the ratio of Eudragit®E100 to Eudragit®L100 within the ternary polymeric composition were found critical in determining the controlled release performance. Conclusion: Results of swelling studies were in agreement with the dissolution behaviors of the tablets. The findings suggest the significance of the ternary polymeric compositions in controlling the release of weakly basic drug.

Development and Evaluation of Controlled Release Mucoadhesive Tablets of Captopril

1970 ◽  
Vol 9 (3) ◽  
pp. 3318-3329
Author(s):  
Kranthi Kumar Kotta ◽  
L. Srinivas
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Xanthan Gum ◽  
Diffusion Mechanism ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Content Uniformity ◽  
In Vitro Drug Release ◽  
Mucoadhesive Tablets

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.

Formulation and Evaluation of Nelfinavir Extended Release Trilayer Matrix Tablets by Design of Experiment

2018 ◽  
Vol 11 (5) ◽  
pp. 4259-4268
Author(s):  
Nirmala Rangu ◽  
Gande Suresh
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Magnesium Stearate ◽  
Zero Order ◽  
Matrix Tablets ◽  
Drug Dissolution ◽  
Crystalline Cellulose ◽  
Dissolution Profile ◽  
Release Formulation

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.

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.

Pectin-Chitosan Multilayer Coated Microbeads of Diclofenac Sodium Prepared by Layer-by-Layer Technique

2014 ◽  
Vol 1060 ◽  
pp. 45-49
Author(s):  
Kamonrak Cheewatanakornkool ◽  
Pornsak Sriamornsak
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Diclofenac Sodium ◽  
Gastric Fluid ◽  
Layer By Layer ◽  
Release Behavior ◽  
Freeze Dried ◽  
Layer Technique ◽  
Calcium Pectinate ◽  
Layer By Layer Technique

The main objective of this study was to fabricate biopolymer-based microbeads, providing enteric properties and controlled release of diclofenac sodium, using layer-by-layer technique. The calcium pectinate microbeads have been designed and coated with chitosan and pectin multilayers. Drug release was performed in simulate gastric fluid (pH 1.2) for 2 hours, followed by pH 6.8 buffer for 8 hours. The effects of chitosan concentration, number of layer and drying technique on drug release were investigated. The results showed that the calcium pectinate microbeads could be simply prepared by ionotropic gelation and then coated with chitosan and pectin solutions using layer-by-layer procedure. The diameter of the microbeads ranged from 800 to 1000 μm for air-dried samples and from 1 to 2 mm for freeze-dried samples. The freeze-dried microbeads had a rough surface and many pores inside, as observed by SEM. The microbeads coated with 4% chitosan/4% pectin revealed a slower drug release than those coated with 1% chitosan/4% pectin and demonstrated a controlled release pattern. Moreover, different drying techniques and numbers of layer also influenced drug release behavior of the prepared microbeads.

scholarly journals Fabrication and In Vitro Evaluation of pH-Sensitive Polymeric Hydrogels as Controlled Release Carriers

Gels ◽  
2021 ◽  
Vol 7 (3) ◽  
pp. 110
Author(s):  
Muhammad Suhail ◽  
Chih-Wun Fang ◽  
Arshad Khan ◽  
Muhammad Usman Minhas ◽  
Pao-Chu Wu
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Acrylic Acid ◽  
Chondroitin Sulfate ◽  
Diclofenac Sodium ◽  
Research Work ◽  
Controlled Delivery ◽  
Scanning Calorimetry ◽  
Release Studies

The purpose of the current investigation was to develop chondroitin sulfate/carbopol-co-poly(acrylic acid) (CS/CBP-co-PAA) hydrogels for controlled delivery of diclofenac sodium (DS). Different concentrations of polymers chondroitin sulfate (CS), carbopol 934 (CBP), and monomer acrylic acid (AA) were cross-linked by ethylene glycol dimethylacrylate (EGDMA) in the presence of ammonium peroxodisulfate (APS) (initiator). The fabricated hydrogels were characterized for further experiments. Characterizations such as Scanning electron microscopy (SEM), Thermogravimetric analysis (TGA), Differential scanning calorimetry (DSC), Powder X-ray diffractometry (PXRD), and Fourier transform infrared spectroscopy (FTIR) were conducted to understand the surface morphology, thermodynamic stability, crystallinity of the drug, ingredients, and developed hydrogels. The swelling and drug release studies were conducted at two different pH mediums (pH 1.2 and 7.4), and pH-dependent swelling and drug release was shown due to the presence of functional groups of both polymers and monomers; hence, greater swelling and drug release was observed at the higher pH (pH 7.4). The percent drug release of the developed system and commercially available product cataflam was compared and high controlled release of the drug from the developed system was observed at both low and high pH. The mechanism of drug release from the hydrogels followed Korsmeyer–Peppas model. Conclusively, the current research work demonstrated that the prepared hydrogel could be considered as a suitable candidate for controlled delivery of diclofenac sodium.

scholarly journals Optimizing the Role of Polymer Blend in the Preparation of Acyclovir Controlled-Release Tablets: An Approach for Better Patient Compliance

2018 ◽  
Author(s):  
Barkat Khan ◽  
Faheem Haider ◽  
Kifayat Shah ◽  
Bushra Uzair ◽  
Kaijian Hou ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Kinetics ◽  
Immediate Release ◽  
Matrix Tablets ◽  
Release Mechanism ◽  
In Vitro Drug Release ◽  
Solubility Study ◽  
Release Data

This study was carried out to formulate and evaluate controlled release (CR) matrix tablets of Acyclovir using combination of hydrophilic and hydrophobic polymers. Acyclovir is a guanine derivative and is its half-life is short hence administered five times a day using immediate release tablets. Six formulations (F1-F6) were developed using Ethocel and Carbopol in equal combinations at drug-polymer (D:P) ratio of 10:5, 10:6, 10:7, 10:8, 10:9 and 10:10. Solubility study was performed using six different solvents. The compatibility studies were carried out using FTIR and DSC. According to USP, Quality Control and dimensional tests (hardness, friability, disintegration and thickness) were executed. In-vitro drug release studies of Acyclovir was carried out in dissolution apparatus using using 0.1 N HCl medium at constant temperature of 37 ± 0.5 ºC. In order to analyze the drug release kinetics, five different mathematical models were applied to the release data. The results showed that there was no incompatibility between drug and polymers. Physical QC tests were found within limits of USP. The release was retarded upto 24 hrs and non-fickian in-vitro drug release mechanism was found. A formulation developed using blend of polymers, showed excellent retention and desired release profiles thus providing absolute control for 24 hrs.

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