Optimization and Evaluation of Solubility-Modulated Gastroretentive Floating Matrix Tablet of Furosemide

2014 ◽  
Vol 7 (3) ◽  
pp. 2581-2589
Author(s):  
Anita Lalwani ◽  
D Bhalodiya ◽  
C Patel ◽  
L Panchal ◽  
P Shelat
Keyword(s):  
Experimental Design ◽  
Drug Release ◽  
Sodium Bicarbonate ◽  
Delivery System ◽  
Solid Dispersion ◽  
Lag Time ◽  
Storage Conditions ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Scanning Calorimetry

The objective of the present study was to prepare delivery system for furosemide which has poor solubility and has specific absorption in stomach. Solid dispersion of furosemide (SD) was prepared in polyethylene glycol 6000 and characterized using differential scanning calorimetry. Floating gastroretentive tablets of the prepared solid dispersion were then prepared by wet granulation technique, using polymer Methocel K100M CR (HPMC) and sodium bicarbonate. A 32 factorial design was applied systematically to study the effect of the amount of HPMC (X1) and sodium bicarbonate (X2) on the floating lag time (YFLT) and amount of drug release at the end of 1st hr (Y60), 6th hr (Y360) and 12th hr (Y720). The solubility of SD was higher than that of drug alone and the physical mixture. The results of multiple regression analysis, when applied to responses obtained for experimental design batches, indicated that low level of HPMC and high level of sodium bicarbonate decreased the floating lag time, while the amount of drug released at all time points decreased with increase in level of HPMC. Swelling behavior of experimental design batches was studied and its relationship with mechanism of drug release was interpreted.  Batch D3 came close to satisfying the drug release and floating criteria. Drug compatibility with the excipients used was ascertained using FTIR. Stability studies were carried out at recommended storage conditions and the tablets were found to be stable. Delivery system could be developed for furosemide which addressed the solubility and site specificity issues of drug.  

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 Formulation and Development of Gastroretentive Drug Delivery System of Efavirenz

2019 ◽  
Vol 11 (05) ◽  
Author(s):  
Monica RP Rao ◽  
Pooja B. Karanjkar
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Solid Dispersion ◽  
In Vitro Release ◽  
Lag Time ◽  
Intrinsic Dissolution ◽  
Drug Content

Efavirenz, a non-nucleotide reverse transcriptase inhibitor is an important drug for treating patients with Human Immunodeficiency Virus infections. It belongs to BCS class II have low solubility and poor intrinsic dissolution rate. It is highly basic (pKa 10.2) which makes it suitable candidate for floating dosage form for continuous delivery in stomach.The study was aimed to improve the solubility by solid dispersion technique.Saturation solubility study and drug content were evaluated for solid dispersion preparation. Saturation solubility shows 8 fold increases in 0.1 N HCL compared to plain drug and drug content was found to be between 95%-102%. Further effervescent floating gastroretentive drug delivery system was prepared by 32 full factorial design with independent variables i.e., concentration of HPMC K100 as matrix forming agent and citric acid as gas generating agent. Lag time, floating time, percent drug release were studied as responses. The optimized batch exhibited floating lag time of 40 sec and the in vitro release studies showed 89.5% drug release in 9 h and tablet remained floating for greater than 8 h. The study thus demonstrated that solubility is increased by solid dispersion technique and floating delivery systems may increase solubility and bioavailability of Efavirenz.

scholarly journals FORMULATION AND OPTIMIZATION OF FLOATING TABLETS OF CLOPIDOGREL BISULPHATE USING DESIGN OF EXPERIMENTS

2018 ◽  
Vol 10 (6) ◽  
pp. 126
Author(s):  
Sanjeevani S. Deshkar ◽  
Arvind S. Pawara ◽  
Satish V. Shirolkar
Keyword(s):  
Drug Release ◽  
Sodium Bicarbonate ◽  
Factorial Design ◽  
Water Uptake ◽  
Lag Time ◽  
Matrix Tablets ◽  
Lower Percentage ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Bicarbonate Concentration

Objective: The present study aimed at designing of floating matrix tablet of clopidogrel bisulphate by design of experiments.Methods: The tablets were prepared by direct compression technique using hydroxypropyl methylcellulose K15 (HPMC) as a matrix polymer and sodium bicarbonate as a gas generating agent. In order to optimize the concentration of HPMC (X1) and sodium bicarbonate (X2), a 32 full factorial design was employed. The tablet formulations were evaluated for floating lag time (Y1), floating or buoyancy time (Y2), percent water uptake, and differential scanning calorimetry (DSC) and in vitro drug release (Y3).Results: The formulation variables, HPMC concentration, and sodium bicarbonate concentration exerted a significant effect on floating behavior and drug release characteristics of the tablet. The optimized formulation, with 15% sodium bicarbonate concentration and 30 % HPMC concentration resulted in 5±2.6 sec of floating lag time, 22.0±0.6 h of floating time and 42.0±0.99% of clopidogrel bisulphate release in 8 h of dissolution study. The drug release mechanism was identified as nonfickian. The water uptake studies revealed that with an increase in HPMC concentration, there was an increase in swelling index of tablet whereas higher sodium bicarbonate concentration supported the faster erosion of matrix tablets. DSC study revealed no interaction of drug and polymers. The lower percentage error between predicted and observed responses of the optimized formulation validated the design.Conclusion: The study demonstrated successful designing of floating clopidogrel bisulphate tablet with factorial design.

scholarly journals FORMULATION AND EVALUATION OF GASTRORETENTIVE FLOATING TABLETS OF LAFUTIDINE

2018 ◽  
Vol 8 (5) ◽  
pp. 393-399
Author(s):  
Ramdas T. Dolas ◽  
Shalindra Sharma ◽  
Madhuraj Sharma
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Active Agent ◽  
Lag Time ◽  
In Vitro Dissolution ◽  
Wet Granulation ◽  
Floating Tablets

The purpose of this research was to develop a novel gastroretentive drug delivery system based on wet granulation technique for sustained delivery of active agent. Quick GI transit could result in incomplete drug release from the drug delivery system above the absorption zone leading to decreased efficacy of the administered dose and thus less patient compliance. Gastroretentive floating tablets, which was designed to provide the desired sustained and complete release of drug for prolonged period of time. Gastroretentive floating tablets of lafutidine were prepared by wet granulation technique using different concentrations of Gum Kondagagu, Gum olibanum and Locust bean Gum. The optimized formulation (LF14) exhibited 99.54% drug release in 12 hrs, while the buoyancy lag time was 33 sec. In-vitro drug release kinetics was found to follow both the Zero order and the possible mechanism of lafutidine release from the optimized formulation might be attributed to super case II transport mechanism. The Optimized formulation (LF14) showed no significant change in physical appearance, drug content, floating lag time, in vitro dissolution studies after 75%±5% RH at 40±20C relative humidity for 6 months. Keyword: Wet granulation, Floating lag Time, Gastroretentive, Lafutidine

Development and Evaluation of Floating Pulsatile Drug Delivery System Using Meloxicam

2017 ◽  
Vol 7 (04) ◽  
Author(s):  
ShirishaG. Suddala ◽  
S. K. Sahoo ◽  
M. R. Yamsani
Keyword(s):  
Rheumatoid Arthritis ◽  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Lag Time ◽  
Oral Dosage ◽  
Lag Phase ◽  
Pulsatile Drug Delivery

Objective: The objective of this research work was to develop and evaluate the floating– pulsatile drug delivery system (FPDDS) of meloxicam intended for Chrono pharmacotherapy of rheumatoid arthritis. Methods: The system consisting of drug containing core, coated with hydrophilic erodible polymer, which is responsible for a lag phase for pulsatile release, top cover buoyant layer was prepared with HPMC K4M and sodium bicarbonate, provides buoyancy to increase retention of the oral dosage form in the stomach. Meloxicam is a COX-2 inhibitor used to treat joint diseases such as osteoarthritis and rheumatoid arthritis. For rheumatoid arthritis Chrono pharmacotherapy has been recommended to ensure that the highest blood levels of the drug coincide with peak pain and stiffness. Result and discussion: The prepared tablets were characterized and found to exhibit satisfactory physico-chemical characteristics. Hence, the main objective of present work is to formulate FPDDS of meloxicam in order to achieve drug release after pre-determined lag phase. Developed formulations were evaluated for in vitro drug release studies, water uptake and erosion studies, floating behaviour and in vivo radiology studies. Results showed that a certain lag time before drug release which was due to the erosion of the hydrophilic erodible polymer. The lag time clearly depends on the type and amount of hydrophilic polymer which was applied on the inner cores. Floating time and floating lag time was controlled by quantity and composition of buoyant layer. In vivo radiology studies point out the capability of the system of longer residence time of the tablets in the gastric region and releasing the drug after a programmed lag time. Conclusion: The optimized formulation of the developed system provided a lag phase while showing the gastroretension followed by pulsatile drug release that would be beneficial for chronotherapy of rheumatoid arthritis and osteoarthritis.

A Comparative Study of Matrix Tablets Designed by Different Methods

2017 ◽  
Vol 10 (2) ◽  
pp. 3645-3652
Author(s):  
Tulsi Bisht ◽  
Rishishwar Poonam
Keyword(s):  
Drug Release ◽  
Comparative Study ◽  
Guar Gum ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Once Daily ◽  
Gum Acacia ◽  
Weight Variation ◽  
Evaluation Parameters

The aim of present work was to develop once daily sustained release matrix tablet of aceclofenac by wet granulation technique using natural gums i.e.: gum acacia, guar gum and Xanthan gum. In this present study matrix tablets were prepared using three different methods and a comparative study was done. Aceclofenac sodium being the newer derivative of diclofenac having short biological half life (4hrs.), so it requires more than one dose per day to maintain therapeutic dose. The prepared tablets were evaluated for various parameters like weight variation, hardness, swelling index, friability, percent drug release and various release profile like zero order, first order, Higuchi's, and Koshemeyrs-peppa. All the evaluation parameters met pharmacopoeial specifications and through dissolution studies it was matrix tablets prepared with method 2 shows heighest percent drug release and matrix tablet prepared by method 3 showed lowest percent drug release at the end of 8 hrs. (Shown in fig. 8, comparative release study of all three formulations). Matrix tablet of aceclofenac were successfully prepared and evaluated and it can be concluded that matrix tablet prepared with natural gums showed release rate for a prolonged time and can be of great importance for “once daily” tablet to reduce side effects and toxicity related with NSAIDs.  

Preparation and Evaluation of a Gas Formation-based Multiple-Unit Gastro-Retentive Floating Delivery System of Dipyridamole

2012 ◽  
Vol 5 (1) ◽  
pp. 1607-1616
Author(s):  
Y. Madhusudan Rao ◽  
Katakam V V ◽  
S Reddy ◽  
J M Somagoni ◽  
P K Panakanti ◽  
...  
Keyword(s):  
Drug Release ◽  
Delivery System ◽  
Polymeric Membrane ◽  
Wet Granulation ◽  
Physical Parameters ◽  
Gastric Residence Time ◽  
Gas Formation ◽  
Multiple Unit ◽  
Model Drug

The aim of this study was to prepare mini tablets to be filled into a capsule that is designed to float on the gastric contents based on gas formation technique. The drug-containing core mini-tablets were prepared by wet granulation method followed by a coating of the core units with seal coating, an effervescent layer and a gas-entrapping polymeric membrane (Eudragit RS30D, RL30D). Dipyridamole, which is predominantly absorbed in the upper part of GI tract and unabsorbed/insoluble at the lower intestine, was used as a model drug. The effect of the preparative parameters like amount of the effervescent agent layered onto the seal coated units, type and coating level of the gas-entrapping polymeric membrane, floating ability and drug release properties of the multiple-unit FDDS were evaluated. The formulations were evaluated for pharmacopoeial quality control tests. Physical parameters were found to be within the acceptable limits. The system using Eudragit® RL30D as a gas-entrapping polymeric membrane exhibited floating properties. The time to float decreased as amount of the effervescent agent increased and coating level of gas-entrapping polymeric membrane decreased. The optimum system exhibited complete floating within 3 minutes and maintained that buoyancy over a period of 8 hours. The drug release was sustained and linear with the square root of time. Increasing the coating level of the gas-entrapping polymeric membrane decreased drug release. Both the rapid-floating and sustained-release properties were achieved in the multiple-unit floating delivery system developed in this study. The in vivo gastric residence time was examined by radiograms and it was found that the units remained in the stomach for about 6 hours. The analysis of the dissolution data after storage at 40°C and 75% RH for 6 months showed no significant change indicating good stability.

Development, Characterization and Optimization of Mucoadhesive Tablet for Buccal Delivery of Domperidone

2019 ◽  
Vol 9 (1) ◽  
pp. 37-49
Author(s):  
Jagdale Sachin ◽  
Panbude Aishwarya ◽  
Navasare Priya
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Research Work ◽  
Wet Granulation ◽  
Buccal Delivery ◽  
Scanning Calorimetry ◽  
Mucoadhesive Polymers ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Background and Objective: Upon oral administration domeperidone is rapidly absorbed, but subjected to the first pass effect which lowers systemic bioavailability to 15%. Mucoadhesive tablet can remain attached to buccal mucosa and becomes capable of bypassing hepatic first-pass metabolism to improve absorption directly into systemic circulation. The present research work was carried with an aim to develop, evaluate and optimize mucoadhesive tablet containing domperidone (DOME) for buccal delivery using different bio-adhesive polymeric combinations. </P><P> Methods: The buccal tablets were formulated by wet granulation method using isopropyl alcohol. The preliminary formulations were prepared using combinations of HPMC K4, HPMC K15, HPMC K100, HPMC E5 as mucoadhesive polymers. 32 full factorial design was applied to determine the effect of independent variables like concentration of mucoadhesive polymers (HPMC K15 and HPMC K100) over dependent variables like mucoadhesive properties (swelling index, bioadhesive strength and in vitro drug release). The prepared mucoadhesive tablets were evaluated for their tablet properties and mucoadhesive properties. The interactions between drug and polymers were studied by Fourier Transform Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC). </P><P> Results: All formulations of factorial design showed satisfactory physicochemical, mechanical and bioadhesive characteristics. The formulation F9 exhibited maximum cumulative drug release, mucoadhesive strength and swelling index. Conclusion: The developed buccal tablet of domperidone might prove alternative to bypass the hepatic first pass metabolism and to avoid degradation which in turn may result in reducing the frequency of administration. Thus, mucoadhesive tablet of domeperidone may become viable alternative overcoming the side effects; achieving greater therapeutic effectiveness and improving the patient compliance.

scholarly journals Development and Optimization of Gastro-Retentive Formulation of Hydralazine HCl

2016 ◽  
Vol 8 (05) ◽  
Author(s):  
Himanshu Acharya ◽  
Rakesh Patel
Keyword(s):  
Drug Release ◽  
Sodium Bicarbonate ◽  
Methyl Cellulose ◽  
Optimization Procedure ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Wet Granulation ◽  
Floating Tablets ◽  
Hydralazine Hydrochloride ◽  
Predicted Values

Hydralazine hydrochloride has a half-life of 2 to 4 hours with an oral bioavailability of 26-50%. Since hydralazine has a demethylating effect on various suppressor genes, it can be used in various types of cancer to support chemotherapy. The purpose of this study was to optimize and evaluate floating tablets of hydralazine hydrochloride designed to prolong the gastric residence time and to provide controlled release of the drug for 24 h. The floating tablets of hydralazine hydrochloride were prepared by the wet granulation method. Polymers of hydroxy propyl methyl cellulose (HPMC K100M), HPMC K15M, carbopol 940 and sodium bicarbonate were used as the release retarding agents. This study investigated utility of a 3-factor, 3-level Box-Behnken design and optimization process for floating tablet of Hydralazine with 5 replicates of center points. Amount of HPMC K4 (Hydroxy Propyl Methyl cellulose), amount of sodium bicarbonate were selected as the independent variables whereas total floating time (TFT), T90, % cumulative drug release at 24 hours, and T20, Q1 were selected as dependent variables. Non-Fickian diffusion release transport was confirmed as the release mechanism for the optimized formulation and the predicted values agreed well with the experimental values. Drug excipient compatibility studies were investigated by FTIR, DSC and XRD. The produced tablets exhibited good floating time and controlled drug release over a period of 24 h. The resultant data were critically analyzed to locate the composition of optimum formulations. All predicted values of response variables of optimized formulation demonstrated close agreement with the experimental data during optimization procedure.

scholarly journals A REVIEW ON DISINTEGRATION CONTROL MATRIX TABLETS

2018 ◽  
Vol 8 (5) ◽  
pp. 19-22
Author(s):  
Pralhad K. Kanke ◽  
Pankaj Sawant ◽  
Ajit Jadhav ◽  
Md. Rageeb Md. Usman
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Solid Dispersion ◽  
Gastrointestinal Transit ◽  
Matrix Tablets ◽  
Surface Erosion ◽  
Matrix Tablet ◽  
Control Matrix ◽  
Dispersion Technique ◽  
Wax Coating

A number of sustained release formulations are available in the market which successfully sustained the drug release over a prolonged period of time by different mechanisms. The new approach for sustaining the drug release is disintegration control matrix tablet which sustained the drug release up to 24hrs by controlling the disintegration rate of tablet. Disintegration control matrix tablet (DCMT) mainly forms the granules containing drug and disintegrating agent such as low substituted hydroxyl propyl cellulose by various methods such as solid dispersion technique. The sustained release of drug is maintained by increasing the wax coating or decreasing the amount of disintegrants. The release of drug from tablet is uniform throughout till all the drug releases from tablet as it involves drug release by diffusion, dissolution and surface erosion mechanism. DCMT increases the solubility of drug and improves the bioavailability without disturbing gastrointestinal transit. BCS Class II, III, IV drugs are the best candidate for DCMT formulations. Keywords: Disintegration control matrix tablet (DCMT), Wax, Disintegrating agent, Solid dispersion.

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