scholarly journals In Vitro Evaluation of Cocoa Pod Husk Pectin as a Carrier for Chronodelivery of Hydrocortisone Intended for Adrenal Insufficiency

2017 ◽  
Vol 2017 ◽  
pp. 1-10 ◽  
Author(s):  
Ofosua Adi-Dako ◽  
Kwabena Ofori-Kwakye ◽  
Mariam El Boakye-Gyasi ◽  
Samuel Oppong Bekoe ◽  
Samuel Okyem
Keyword(s):  
Drug Release ◽  
Adrenal Insufficiency ◽  
Aqueous Medium ◽  
Water Soluble ◽  
Hot Water ◽  
Matrix Tablets ◽  
Lag Phase ◽  
Wet Granulation ◽  
Cocoa Pod Husk

This study evaluated the in vitro potential of cocoa pod husk (CPH) pectin as a carrier for chronodelivery of hydrocortisone intended for adrenal insufficiency. FTIR studies found no drug-CPH pectin interactions, and chemometric analysis showed that pure hydrocortisone bears closer similarity to hydrocortisone in hot water soluble pectin (HWSP) than hydrocortisone in citric acid soluble pectin (CASP). CPH pectin-based hydrocortisone matrix tablets (~300 mg) were prepared by direct compression and wet granulation techniques, and the tablet cores were film-coated with a 15% HPMC formulation for timed release, followed by a 12.5% Eudragit® S100 formulation for acid resistance. In vitro drug release studies of the uncoated and coated matrix tablets in simulated gastrointestinal conditions showed that wet granulation tablets exhibit greater retardation of drug release in aqueous medium than directly compressed tablets. CASP showed greater suppression of drug release in aqueous medium than HWSP. Wet granulation HWSP-based matrix tablets coated to a final coat weight gain of ~25% w/w were optimized for chronodelivery of hydrocortisone in the colon. The optimized tablets exhibited a lag phase of ~6 h followed by accelerated drug release in the colonic region and have potential to control night time cortisol levels in patients with adrenal insufficiency.

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 Formulation and Evaluation of Sustained Release Matrix Tablets of Aceclofenac

2021 ◽  
Vol 4 (2) ◽  
pp. 99-109
Author(s):  
Priyanka Singh ◽  
Amit Kumar Shrivastava ◽  
Sachin Kumar ◽  
Manish Dhar Dwivedi
Keyword(s):  
Drug Release ◽  
Guar Gum ◽  
Polymer Concentration ◽  
Matrix Tablets ◽  
Hydrophilic Polymers ◽  
Wet Granulation ◽  
Drug Release Profile ◽  
In Vitro Drug Release ◽  
Study Results

This study aimed to improve the dissolution rate of aceclofenac and release the drug in a controlled manner over a period of 24 hours. Matrix tablets were prepared by direct compression method, using hydrophilic polymers (HPMC/guar gum). Matrix tablets were prepared by wet granulation method using different hydrophilic polymers (HPMC/guar gum). Tablets were evaluated for in vitro drug release profile in phosphate buffer with pH 6.8 (without enzymes). The thickness and hardness of prepared tablets were 3.23 ± 0.035 to 3.28 ± 0.008 mm and 3.26 ± 0.115 to 3.60 ± 0.200 kg/cm2, respectively. The friability was within the acceptable limits of pharmacopoeial specifications (0.31 to 0.71%), which indicates the good mechanical strength of the tablets. Drug release was retarded with an increase in polymer concentration due to the gelling property of polymers. The in vitro drug release from the proposed system was best explained by Higuchi’s model, indicating that drug release from tablets displayed a diffusion-controlled mechanism. The results clearly indicate that guar gum could be a potential hydrophilic carrier in developing oral controlled drug delivery systems. Based on the study results, formulations F8 was selected as the best formulation.

scholarly journals Response Surface Optimization of Sustained Release Metformin-Hydrochloride Matrix Tablets: Influence of Some Hydrophillic Polymers on the Release

2012 ◽  
Vol 2012 ◽  
pp. 1-10 ◽  
Author(s):  
Amitava Roy ◽  
Kalpana Roy ◽  
Sarbani Roy ◽  
Jyotirmoy Deb ◽  
Amitava Ghosh ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Hydroxypropyl Methylcellulose ◽  
Dissolution Kinetics ◽  
Matrix Tablets ◽  
Metformin Hydrochloride ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Response Surface Optimization

The aim of the present work was designed to develop a model-sustained release matrix tablet formulation for Metformin hydrochloride using wet granulation technique. In the present study the formulation design was employed to statistically optimize different parameters of Metformin hydrochloride tablets at different drug-to-polymer ratios employing polymers Hydroxypropyl methylcellulose of two grades K4M and K100M as two independent variables whereas the dependent variables studied were X60, X120, T50, T90, n, and b values obtained from dissolution kinetics data. The in vitro drug release studies were carried out at simulated intestinal fluids, and the release showed a non-Fickian anomalous transport mechanism. The drug release was found to reveal zero order kinetics. The granules and the tablets were tested for their normal physical, morphological, and analytical parameters and were found to be within the satisfactory levels. There were no significant drug-polymer interactions as revealed by infrared spectra. It has been found out that on an optimum increased Hydroxypropyl methylcellulose K100M concentration and decreased Hydroxypropyl methylcellulose K4M concentration the formulations were elegant in terms of their release profiles and were found to be statistically significant and generable.

scholarly journals Formulation and Evaluation of Gabapentin Sustained Release Matrix Tablet Using Hibiscus rosa sinensis Leaves Mucilage as Release Retardant

2021 ◽  
pp. 564-572
Author(s):  
P. Amsa ◽  
G. K. Mathan ◽  
S. Magibalan ◽  
E. K. Velliyangiri ◽  
T. Kalaivani ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Magnesium Stearate ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Hibiscus Rosa Sinensis

The major goal of this study was to develop and evaluate Sustained release matrix tablets of Gabapentin with Hibiscus rosa - sinensis leaves mucilage prepared by using wet granulation technique with microcrystalline cellulose as a diluents and magnesium stearate as a lubricant. Pre-compression and post-compression evaluation of physicochemical parameters were carried out and to be within acceptable limits. Drug and polymer compatibility were validated by FTIR measurements. Further, tablets were evaluated for in vitro release study. To get the sustained release of Gabapentin, the concentration of Hibiscus rosa- sinensis mucilage was tuned with a gas-generating agent. The % drug release of all formulation from F1 to F5 showed 91.24%, 80.24%, 70.53%, 62.12% and 49.83% respectively. All the dosage form release kinetics was computed using zero order, first order, Higuchi, and Korsmeyer–Peppas methods. From the above results, it is concluded that the n value of formulation F5 showed 0.78 suggesting anomalous (non-fickian) behavior of the drug. Mucilage from the leaves of Hibiscus rosa-sinensis has a great retarding effect in drug release from sustained release tablets.

scholarly journals DESIGN AND DEVELOPMENT OF TOPICAL HYDROGEL FORMULATION OF IRBISARTAN

2019 ◽  
pp. 79-83
Author(s):  
ZEESHAN SHAIKH
Keyword(s):  
Angiotensin Ii ◽  
Drug Release ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Burst Release ◽  
Angiotensin Ii Receptor ◽  
In Vitro Drug Release ◽  
Dsc Studies ◽  
Ft Ir

Objective: Irbesartan is an antihypertensive with limited bioavailability. The objective of the study was to develop controlled release matrix tablets of irbisartan drug. Methods: Tablets were prepared by wet granulation process. Result: In vitro drug release study revealed that HPMC causes initial burst release of drug hence combining HPMC sustained the action for 8 h (95.92±0.57% release). Fitting the in vitro drug release data to Korsmeyer equation indicated that diffusion along with erosion could be the mechanism for drug release. Compared to conventional tablets, the release of model drug from these HPMC matrix tablets was prolonged, leading to achieve an effective therapy with a low dosage of the drug, to reduce the frequency of medication. The pharmacological and clinical properties of irbesartan, a noncompetitive angiotensin II receptor type 1 antagonist, successfully used for more than a decade in the treatment of essential hypertension. Results: Compatibility Studies In order to investigate the possible interactions between irbesartan and distinct polymers and/or diluents, FT-IR and DSC studies were carried out. FT-IR results proved that the drug was found to be compatible with excipients as wave numbers are almost similar for pure drug and also drug excipients mixture. In picture 1 and 2. DSC studies indicate that chosen excipients for the formulation were found to be compatible with the active ingredient as the melting endothermic peaks are in the range of 250-320 °C which is same as the melting point of irbisartan. Conclusion: Irbesartan exerts its antihypertensive effect through an inhibitory effect on the pressure response to angiotensin II. Irbesartan 150–300 mg once daily confers a lasting effect over 24 h, and its antihypertensive efficacy is further enhanced by the coadministration of hydrochlorothiazide.

scholarly journals FORMULATION AND EVALUATION OF SYNTHESIZED QUINAZOLINONE DERIVATIVE FOR COLON SPECIFIC DRUG DELIVERY

2017 ◽  
Vol 10 (3) ◽  
pp. 207
Author(s):  
Vidya Viswanad ◽  
Shammika P ◽  
Aneesh Tp
Keyword(s):  
Drug Release ◽  
Guar Gum ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Scanning Calorimetry ◽  
Disintegration Time ◽  
Site Specific ◽  
The Matrix

ABSTRACTObjective: The current research deals with the formulation and evaluation of synthesized quinazolinone derivative for colon site specific delivery.Methods: The synthesized quinazolinone derivative was enteric coated 5% Eudragit L-100 with by wet granulation method using guar gum, pectin,and guar gum pectin combination as hydrophilic polymer. The prepared matrix tablet was characterized by differential scanning calorimetry andevaluated for different pre-compression and post-compression studies and drug release profiles.Results: All the matrix tablets were within the range of pharmacopeial limits with better flow properties. All the six formulations of matrix tablets haddisintegrated within 5-6 minutes. The optimized formulation selected was F6 formulation combination of guar gum and pectin with 95.79% of drugrelease than compared to the remaining formulation. The optimized matrix tablets followed zero order kinetics with Fickian diffusion.Conclusion: The results proposed that the combination of guar gum and pectin coated tablet with 5% Eudragit L-100 of synthesized quinazolinonederivative is a promising colon site specific delivery.Keywords: Quinazolinone derivative, In vitro drug release, Disintegration time, Guar gum, Pectin, 5% Eudragit L-100, Colon site-specific delivery, Wetgranulation, Compression.

scholarly journals Development and evaluation of gastroretentive norfloxacin floating tablets

2009 ◽  
Vol 59 (2) ◽  
pp. 211-221 ◽  
Author(s):  
Ramesh Bomma ◽  
Rongala Swamy Naidu ◽  
Madhusudan Yamsani ◽  
Kishan Veerabrahma
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Wet Granulation ◽  
Drug Bioavailability ◽  
Floating Tablets

Development and evaluation of gastroretentive norfloxacin floating tabletsFloating matrix tablets of norfloxacin were developed to prolong gastric residence time, leading to an increase in drug bioavailability. Tablets were prepared by the wet granulation technique, using polymers such as hydroxypropyl methylcellulose (HPMC K4M, HPMC K100M) and xanthan gum. Tablets were evaluated for their physical characteristics,viz., hardness, thickness, friability, and mass variation, drug content and floating properties. Further, tablets were studied forin vitrodrug release characteristics for 9 hours. The tablets exhibited controlled and prolonged drug release profiles while floating over the dissolution medium. Non-Fickian diffusion was confirmed as the drug release mechanism from these tablets, indicating that water diffusion and polymer rearrangement played an essential role in drug release. The best formulation (F4) was selected based onin vitrocharacteristics and was usedin vivoradiographic studies by incorporating BaSO4. These studies revealed that the tablets remained in the stomach for 180 ± 30 min in fasting human volunteers and indicated that gastric retention time was increased by the floating principle, which was considered desirable for the absorption window drugs.

scholarly journals Formulation and Evaluation of Floating Tablets of Sitagliptin with Extract of Triphala

2019 ◽  
Vol 9 (4-A) ◽  
pp. 38-47
Author(s):  
Revathi Sundaramoorthy ◽  
V Gopal ◽  
G Jeyabalan
Keyword(s):  
Drug Release ◽  
Chemical Interaction ◽  
Lag Time ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
In Vitro Drug Release ◽  
Floating Tablets ◽  
Drug Content ◽  
Soxhlet Apparatus

The aim of the present work is to formulate, optimize and evaluate hydrodynamically balanced antidiabetic system incorporated with sitagliptin and phytochemical constituents of Triphala extract for the treatment of constipation associated with diabetes.  The Triphala churna of two different ratios, 1:1:1 (TC1) and 1:2:4 (TC2) were subjected to hot percolation using Soxhlet apparatus using methanol as solvent. The floating matrix tablets of Sitagliptin with methanolic Triphala extract was prepared by wet granulation technique using HPMC K4M as polymer, starch/honey as binder and sodium bicarbonate & citric acid as effervescent agents by 24 factorial design.  The compatibility studies showed that there is no chemical interaction between the drug, polymer and the excipients used in the tablets.  The independent variables are drug & Triphala extract ratio (X1), Triphala proportion (X2), binder used for granulation (X3), and amount of effervescent excipients used (X4).  The dependent variables are hardness (Y1), buoyancy lag time (Y2), total floating time (Y3), in-vitro drug release (Y4), and T50% (Y5).  The prepared floating tablets were subjected to all post compression parameters such as hardness, friability, swelling capacity, buoyancy, total floating time, drug content & in-vitro drug release and were found to be within normal limits.  Based on drug content, buoyancy lag time and in-vitro drug release the formulations F14 and F16 were selected for in-vivo study of the formulation.  Keywords:  Triphala, Sitagliptin, honey, floating tablet. 

scholarly journals Formulation and In-Vitro Evaluation of Sustained Release Matrix Tablets of Domperidone

2020 ◽  
Vol 8 (02) ◽  
pp. 40-45
Author(s):  
Chhitij Thapa ◽  
Roma Chaudhary
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Epigastric Pain ◽  
Matrix Tablets ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Wet Granulation ◽  
In Vitro Drug Release ◽  
Weight Variation

INTRODUCTION Domperidone is a unique compound with gastro kinetic and antiemetic effects. It is used in the management of disorder by impaired motility like gastroesophageal reflux (in some instances), gastroparesis, dyspepsia, heartburn, epigastric pain, nausea, vomiting, and colonic inertia. The sustained release system is a widely accepted approach for slow drug release over an extended period to address the challenges of conventional oral delivery, including dosing frequency, drug safety, and efficacy. The study aims to formulate a domperidone sustained release tablet and compare the dissolution rate with the marketed formulations. MATERIAL AND METHODS Sustained release matrix tablets of domperidone were prepared by wet granulation method using different polymers such as HPMC K4M, ethyl cellulose, Gum acacia. Pre-compression studies like angle of repose, bulk density, tapped density, Carr's index, and Hausner’s ratio, and post-compression studies like weight variation, thickness, hardness, friability, drug content, and in-vitro drug release were evaluated.   RESULTS The release profile of domperidone sustained-release tablets was studied spectrophotometrically. The in-vitro dissolution study suggests the minimum %-cumulative drug release with 98.33% in F5. The %-cumulative drug release was maximum in F3 with 99.69%. The in-vitro drug release of all the formulations was non-significant compared to the marketed formulation (p<0.05), exhibiting the sustained-release property by all the formulations. CONCLUSION The pre-compression study concludes the better flow property of the granules of different formulations. The sustained release domperidone tablets were prepared successfully by the wet granulation method. The post-compression parameters of different formulations were within the acceptable range.

scholarly journals Study of Drug Release Kinetics from Sustained Release Matrix Tablets of Acyclovir using Natural Polymer Obtained from Colocasia Esculenta

2020 ◽  
Vol 13 (3) ◽  
pp. 172-179
Author(s):  
Dharmendra Solanki ◽  
Mohit Motiwale ◽  
Sujata Mahapatra
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
Matrix Material ◽  
Colocasia Esculenta ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
The Matrix ◽  
Release Data

Sustained-release (SR) matrix tablets of Acyclovir and polysaccharide isolated from corms of Colocasia esculenta, at different drug to polymer ratios, were prepared by using wet granulation method. The formulated tablets were also characterized by physical and chemical parameters and results were found in acceptable limits. The investigation focuses on the influence of the proportion of the matrix material on the mechanism and the release rate of the drug from the tablets. In vitro drug release appears to occur both by diffusion and a swelling-controlled mechanism, indicates the drug release from the tablet was non-Fickian super case II transport. The drug release data fit well to the Zero-order drug release Model and the Korsmeyer equation.

Sign in / Sign up

Export Citation Format

Share Document