scholarly journals Effects of Humidity on the Dissolution Profiles of Controlled Release Theophylline Matrix Tablets Containing Release Enhancers Prepared By Melt Granulation and Coacervation Techniques

2020 ◽  
Vol 24 (9) ◽  
pp. 1563-1567
Author(s):  
J.A. Avbunudiogba
Keyword(s):  
Differential Scanning Calorimetry ◽  
Controlled Release ◽  
Relative Humidity ◽  
Drug Release ◽  
Chemical Properties ◽  
Modern Technology ◽  
Matrix Tablets ◽  
Scanning Calorimetry ◽  
Physical Chemical ◽  
Melt Granulation

The quantity of moisture present in tablets plays a major role in influencing the physical/chemical properties of tablets especially dissolution profiles. The purpose of the present study is to investigate the effects of relative humidity on the dissolution profiles of controlled release  theophylline matrix tablets containing release enhancer prepared by melt granulation and simple coacervation techniques. Sucrose and  microcrystalline cellulose at concentration of 3% w/w, 5% w/w, 7.5% w/w, and 10% w/w were included in the blends as release enhancers before compression into nondisintegrating matrix tablets. Resulting tablets were exposed to 0% and 75% relative humidity. Sample were withdrawn at 0, 15 days, 1 month, 2 months and 3 months and evaluated for cumulative drug release. Interactions were investigated using modern technology: Differential scanning calorimetry (DSC). Initial and maximum release were increased after exposure to 75% relative humidity. There was no drug – excipients interaction. Thus moisture increased theophylline release from both sets of tablets prepared by melt granulation and simple coacervation techniques. Keywords: Theophylline, Matrix tablets, Dissolution profiles, Release enhancers, Relative humidity

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.

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.

DESIGN AND EVALUATION OF EUDRAGIT COATED LOSARTAN POTASSIUM CONTROLLED RELEASE PELLETS BY PAN COATING TECHNIQUE

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (10) ◽  
pp. 30-38
Author(s):  
S Vidyadhara ◽  
◽  
R. L. C. Sasidhar ◽  
P Thrilochani ◽  
L. K. Lavanya
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Methyl Cellulose ◽  
Losartan Potassium ◽  
Scanning Calorimetry ◽  
Coating Agent ◽  
Coating Technique ◽  
S 100 ◽  
Eudragit S 100

The present investigation was focused on the development and evaluation of controlled release pellets of losartan potassium with Eudragit S 100 and hydroxypropyl methyl cellulose phthalate (HPMCP) by employing pan coating technique. Eudragit S 100, a high viscosity grade controlled release polymer, was mainly used as coating agent for regulating the drug release from pellets. HPMCP, an enteric coating polymer was used in the present study to regulate the drug release at varied G.I. pH conditions. The prepared pellets were evaluated for particle size, drug content, friability and for in vitro drug release. The formulations were further characterized to identify any possible interactions by FTIR spectroscopy and differential scanning calorimetry. The surface morphology of the pellets was studied by scanning electron microscopy. From the results it was observed that due to increase in the concentration of Eudragit the drug release was extended up to 12 hours. The increase in the HPMCP polymeric concentration in formulations showed initial delay in drug release.

DEVELOPMENT AND EVALUATION OF MODIFIED RELEASE MATRIX TABLETS OF MILNACIPRAN HCL USING MELT GRANULATION TECHNIQUE

INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (02) ◽  
pp. 68-71
Author(s):  
N. C Ratnakara ◽  
◽  
M. C. Gohel
Keyword(s):  
Drug Release ◽  
Matrix Tablets ◽  
Matrix Tablet ◽  
Modified Release ◽  
Independent Variables ◽  
Dependent Variables ◽  
Formulation Parameters ◽  
Predicted Values ◽  
Melt Granulation

The objective of the present study was to identify critical formulation parameters affecting the drug release from modified release wax matrix tablet of milnacipran hydrochloride employing the concept of design of experiments.The optimized amount of Compritol 888 ATO(intragranular) (X1), lactose (X2) and Compritol 888ATO (extragranular)(X3) were determined employing simplex latticedesign. The tablets were prepared using melt granulation technique. The in vitro drug release study was carried out in an acidic medium (pH 1.2) for 2 h and thereafter the dissolution study was conducted in phosphate buffer (pH 6.8).The selected dependent variables were the cumulative percentage of milnacipran hydrochloride dissolved at 1 (Y1), 8 (Y8), 16 (Y16) and 24 h (Y24). Mathematical models, correlating the independent variables with dependent variables were evolved. Optimization was performed for the three independent variables using the stated target ranges; Y1≤20%; Y8=45±5%; Y16=72±5%; Y24=100%. The optimized amounts of Compritol ATO888 (intragranular)(X1), lactose (X2) and Compritol 888ATO (extragranular)(X3), were found to be 60, 55 and 30 mg, respectively.The optimized formulation showed a release profile that was close to the predicted values. The drug was released by anomalous diffusion from the optimized formulation. Compritol 888ATO (intragranular) (X1), lactose (X2) and Compritol 888ATO(extragranular) (X3) were identified as critical variables.

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