Synthesis and Evaluation of Starch – Urea – Borate as Rate Controlling Matrix for Controlled Release

1970 ◽  
Vol 1 (2) ◽  
pp. 167-170
Author(s):  
Chowdary KPR ◽  
Murali Krishna MN
Keyword(s):  
Controlled Release ◽  
Release Rate ◽  
Guar Gum ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Drug Release Mechanism ◽  
Zero Order Kinetics ◽  
Diffusion Controlled ◽  
Controlled Release Tablets

The objective of the present investigation is to synthesize starch – urea – borate, a new starch based polymer and to evaluate its application in the design of controlled release matrix tablets of diclofenac and gliclazide. The release rate controlling efficiency of starch – urea – borate was also compared with that of known polymers. Starch – urea – borate (SUB) polymer was synthesized by gelatinization of starch in the presence of urea and borax. Matrix tablets of diclofenac (100 mg) and gliclazide (60 mg) were formulated employing starch – urea – borate polymer in different proportions of drug and polymer and the tablets were evaluated. With both diclofenac and gliclazide, release from the formulated matrix tablets was slow and spread over 24 h and depended on percent polymer in the tablet. Release was diffusion controlled and followed zero order kinetics. Non – fickian diffusion was the drug release mechanism from the formulated tablets. Diclofenac release from matrix tablets formulated employing 33 % SUB (DF3) and Gliclazide release from matrix tablets formulated employing 50 % SUB (GF4) was similar to that from the corresponding commercial SR tablets. Starch – urea – borate polymer was found suitable for the design of oral controlled release tablets of diclofenac and gliclazide. The order of increasing release rate controlling efficiency with various polymers was ethyl cellulose = guar gum > SUB > sodium CMC > HPMC. Starch – urea – borate is a better release rate controlling polymer than HPMC and sodium CMC for obtaining controlled release over    24 hours.

DESIGN AND CHARACTERIZATION OF ALFUZOSIN HCL GASTRORETENTIVE FLOATING MATRIX TABLETS EMPLOYING HPMC K 100M

INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (11) ◽  
pp. 71-73
Author(s):  
Ch. Taraka Ramarao ◽  
◽  
J Vijaya Ratna ◽  
R. B. Srinivasa
Keyword(s):  
Drug Release ◽  
Dosage Forms ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Gastric Residence Time ◽  
Drug Release Mechanism ◽  
The Matrix ◽  
Gastro Retentive

The present investigation involves developing gastro retentive drug delivery systems (GFDDS) of alfuzosin HCl using HPMCK100M a is the matrixing agent and floating enhancer. Sodium bicarbonate in the acidic environment reacts with the acid and produces carbon dioxide. The gastro retentive tablets can be formulated to increase the gastric residence time and thereby increase the oral bioavailability. From the drug release study, it was concluded that the AFTB4 formula of HPMC K 100 M matrix tablets gives the controlled release up to 12 hours by showing increased release with floating lag time 24 seconds. Non – Fickian diffusion was the drug release mechanism from the matrix tablets formulated employing HPMC K 100 M. The matrix tablets (AFTB4) formulated employing 40 % HPMC K 100 M are best suited to be used for gastro retentive dosage form of alfuzosin HCl. Finally, it can be concluded that good candidates for the preparation of gastro retentive dosage forms due its gastric stability, gastric absorption and better bioavailability.

DESIGN AND OPTIMIZATION OF ORAL BIOADHESIVE NANOCURCUMIN DELIVERY USING NOVEL HYDROPHILIC CARRIER FOR CANCER TREATMENT: AN ALTERNATIVE TO PARENTERAL CHEMOTHERAPY

INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (08) ◽  
pp. 24-36
Author(s):  
P. N Kendre ◽  
◽  
P. D. Chaudhari
Keyword(s):  
Solid Dispersion ◽  
Tablet Formulation ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Design And Optimization ◽  
Drug Release Mechanism ◽  
Zero Order Kinetics ◽  
Time Period ◽  
Two Factors ◽  
Central Composite Designs

Present study involves the design and optimization of oral bioadhesive delivery system of curcumin. Solid dispersion of curcumin was developed using novel hydrophilic carrier, Gelucire® 50/13, by melt granulation technique. Based on HPMC K 100 LV(X1) and carbopol 934P (X2), bio-adhesive tablets containing curcumin solid dispersion was developed by direct compression, using central composite designs for two factors at three levels. Tablet formulation was optimized for t50%, Rel24h and bioadhesive strength. The drug release mechanism was found to be by fickian diffusion, approaching zero-order kinetics. Average plasma uptake of curcumin was found to be 0.289μg/mL as compared to plain curcumin tablet formulation. The results were found highly significant (p<0.05). The swelling matrices behavior over the time period studied showed that the gelling layer thickness increases continuously. From this study, it may be concluded that the oral controlled bioadhesive curcumin delivery may be an alternative to parenteral chemotherapy.

scholarly journals DEVELOPMENT AND CHARACTERIZATION OF CONTROLLED RELEASE FAMOTIDINE MATRIX TABLETS CONTAINING COMPLEXES

2017 ◽  
Vol 9 (4) ◽  
pp. 38
Author(s):  
Shabnam Ain ◽  
Babita Kumar ◽  
Kamla Pathak
Keyword(s):  
Controlled Release ◽  
Polymer Blend ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
Zero Order ◽  
Matrix Tablets ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Cyclodextrin Complex ◽  
Controlled Release Tablets

Objective: The aim of the present study was to formulate the controlled release (CR) tablets of famotidine-cyclodextrin complexes to make the feasibility of complex in CR tablets and to access the kinetic of drug release mechanismMethods: In this work the solubility study of famotidine was performed in various solvents like 0.1 N HCl, phosphate buffer pH 7.4 and distilled water. Enhancement of the solubility and dissolution rate of famotidine was done by complexation with cyclodextrin before formulation into controlled release tablets. Tablets were prepared in different batches by using different concentration of HPMC K15M (hydroxy propyl methyl cellulose) and EC (ethyl cellulose) polymers and polymer blend. All batches were evaluated for pre-compression and post-compression parameters. Release kinetics was analyzed using zero order, first order, higuchi, peppas and hixon-crowell model.Results: All the formulation showed compliance with Pharmacopoeial standards. Release studies indicated that polymer blend (62%HPMCK15M and 38%EC) based matrix tablets with complexed drug was able to control the release of famotidine up to 12 h. Optimized formulation F13 containing complexed drug with same polymer blend showed zero order release and the release mechanism was predominant matrix swelling with erosion.Conclusion: Results of the present study demonstrated that the drug: β-cyclodextrin complex would be a suitable candidate for preparing controlled release tablets of famotidine to improve drug solubility, flow properties and compressibility. Thus the complex used in matrix tablet is a promising approach to achieve appropriate controlled release dosage.

Influence of Formulation Variables and Processing Techniques on Drug Release from Carbopol-971 based Matrix Tablets of Cinnarizine and Nimodipine.

2010 ◽  
Vol 2 (1) ◽  
Author(s):  
Singh K. ◽  
Pandit K. ◽  
Mishra N.
Keyword(s):  
Drug Release ◽  
Release Rate ◽  
Polymer Concentration ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Weight Variation ◽  
Diffusion Controlled ◽  
The Matrix ◽  
Processing Techniques ◽  
Formulation Variables

The matrix tablets of cinnarizine and nimodipine were prepared with varying ratio of Carbopol- 971P and co-excipients of varying hydrophilicity (i.e. dicalcium phosphate and spray dried lactose) by direct compression and wet granulation using alcoholic mucilage. The prepared tablets were evaluated for weight variation, hardness and friability. The influence of concentration of the matrix forming material and co-excipients on the release rate of the drug was studied. The release rate of Cinnarizine (more soluble drug) from tablets followed diffusion controlled mechanism whereas for nimodipine (less soluble drug), the drug release followed case-II or super case- II transport mechanism based on Korsmeyer- Peppas equation. The results indicated that the drug release from matrix tablets was increases with increase in hydrophilicity of drug and co-excipients. The release of drug also increased with thermal treatment and decreasing polymer concentration.

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 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 Development of Paroxetine Hydrochloride Single Layer Controlled-Release Tablets Based on 32 Factorial Design

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 243 ◽  
Author(s):  
Yao Yang ◽  
Zhengwei Huang ◽  
Xuan Zhang ◽  
Jinyuan Li ◽  
Ying Huang ◽  
...  
Keyword(s):  
Controlled Release ◽  
Single Layer ◽  
Suicide Mortality ◽  
Pharmacokinetic Parameters ◽  
Release Mechanism ◽  
Time Curve ◽  
Layer Separation ◽  
Significant Difference ◽  
Paroxetine Hydrochloride ◽  
Controlled Release Tablets

Major depressive disorder (MDD) is one of the main contributors to disability and suicide mortality globally. Paroxetine hydrochloride (PHH) is the most potent antidepressant used for MDD treatment. Due to its reduced side effects PAXIL® CR is a widely-used controlled-release formulation of PHH. However, the complicated double-layer production of PAXIL® CR faces the risk of layer separation. In this study, PHH enteric coating single layer controlled-release tablets (PHH-EC-SLTs) were designed as a simplified substitution of PAXIL® CR through a rational formulation screening. The optimized PHH-EC-SLTs showed similar release behaviors in vitro to PAXIL® CR and the release profiles corresponded to a zero-order release model (R2 = 0.9958). Polymer matrix erosion was the main release mechanism, according to the fitting exponents n > 1 in the Korsmeyer-Pappas model. Crucial pharmacokinetic parameters including peak-reaching time (Tmax), peak concentration (Cmax) and the area under the blood level-time curve (AUC0-48) of PHH-EC-SLTs and PAXIL® CR had no significant difference (p > 0.05) and the relative bioavailability (F = 97.97%) of PHH-EC-SLTs demonstrated their similar pharmacokinetic profiles in vivo. In view of avoiding layer separation risk and simplifying the preparation processing, the self-made PHH-EC-SLTs could be considered as a safe and economic alternative to PAXIL® CR.

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.

SUSTAINED RELEASE MATRIX TABLETS OF DICLOFENAC SODIUM EMPLOYING KOLLIDON SR, PEG 6000, LACTOSE MONO HYDRATE AND EUDRAGIT S100 IN COLON TARGET

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (10) ◽  
pp. 38-43
Author(s):  
Ch. Taraka Ramarao ◽  
◽  
B. Srinivasa Rao ◽  
J. Vijayaratana
Keyword(s):  
Drug Release ◽  
Diffusion Mechanism ◽  
Diclofenac Sodium ◽  
Zero Order ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Colon Targeting ◽  
Zero Order Kinetics ◽  
Eudragit S100 ◽  
Lag Period

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.

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