scholarly journals Formulation and In vitro Characterization of Hydrochlorothiazide Gastroretentive Floating Drug Delivery System

2016 ◽  
Vol 14 (2) ◽  
pp. 163-170
Author(s):  
Md Asif Hasan ◽  
Sabiha Sultana ◽  
Sabiha Sultana ◽  
Md Masud Kaisar Bhuiyan ◽  
Md Selim Reza ◽  
...  

The purpose of the study was to develop and optimize floating bioadhesive gastroretentive drug delivery system (GRDDS) exhibiting a unique combination of floatation and bioadhesion to prolong residence in the stomach, using hydrochlorothiazide (HCTZ) as a model drug. Formulated matrix tablets were prepared by direct compression method with two different rate controlling polymer HPMC K4M and Carbopol 971. The formulated tablets were evaluated for physical characterization, floating lag time, swelling index and drug content uniformity. The drug release study was carried out in 0.1N HCl as the medium (pH 1.2) for 8 hours using USP type II dissolution apparatus and investigated the effects of polymers on the drug release profile. In vitro buoyancy study results found to be 10–33 sec and >8 h, floating lag time and total floating time respectively. Simulated drug release pattern in different kinetic models of Korsmeyer-Peppas release suggests that the mechanism controlling of the drug release from all formulations was the anomalous non-Fickian or anomalous release. Polymer with lower viscosity (HMPC K4M) was found to be beneficial than higher viscosity polymer (Carbopol 971) in improving the release properties of gastric floating drug delivery system. Incorporation of Carbopol in formulation also helped in maintaining buoyancy of system with desirable drug release. Further study is necessary in case of in vitro- in vivo relationship, but this study will ready to lend a hand to future scientists working in this field to successfully exploit the potential of this drug delivery system for the advantage of mankind.Dhaka Univ. J. Pharm. Sci. 14(2): 163-170, 2015 (December)

Author(s):  
SUVARNA CHITTAM ◽  
ASHOK BHOSALE

Objective: The objective is to design and optimize a floating tablet of furosemide using a novel floating agent Saccharomyces boulardii. Methods: In this study floating tablet based on principle of combination of floating and swelling prepared by direct compression technique. Saccharomyces boulardii probiotics preparation is used as a floating agent due to its bloating property i.e. production of CO2 gas and hydrophilic polymer HPMC E LV 15 used as swellable polymer. Furosemide is a BCS class IV drug selected as model drug which shows pH dependent solubility and permeability and it is better absorbed from the gastric region, hence to improve dissolution and residence at absorption site of such drug, floating drug delivery system is needed. Calcium hydroxide used as pH modifier which increase rate of dissolution of furosemide and also maintain integrity of tablet matrix. Formulation designed and developed using central composite design response surface methodology technique, so as to explore the effect of formulation variables such as amount of Saccharomyces boulardii preparation and calcium hydroxide on floating lag time and % drug release after 12h. Results: The numerical and graphical optimization technique were used to choose the optimal formulation. Floating lag time was found to be 12.6 min and 88.18% drug release for the optimized formulation. In vivo buoyancy studies depicted that formulation stay more then 6h in stomach. Conclusion: Study indicate that Saccharomyces boulardii is a promising floating agent, and the formulation containing this novel floating agent is suitable for gastro retention and it increases bioavailability of furosemide.


Author(s):  
Anand J. Patel ◽  
Deep R. Naik ◽  
Jignesh P. Raval

Floating tablets has been accepted as a process to achieve controlled drug delivery by prolonging the residence time of the dosage form at the site of absorption, thereby improving and enhancing the bioavailability of drug. The objective of present study outlines the development and characterization the floating drug delivery system of Ofloxacin to enhance its bioavailability and therapeutic efficacy, using different grades of polymer along with effervescent agent sodium bicarbonate and citric acid. Ofloxacin is a synthetic chemotherapeutic second-generation antibiotic of the fluoroquinolone class. Different tablet formulations were formulated by wet granulation technique and were evaluated for physical parameters like Tablet Thickness, Hardness, % Friability, Weight variation, Content uniformity, In vitro buoyancy, Swelling index, In vitro dissolution study and drug release mechanisms. As the concentration of the polymer in the formulations increased the release of drug decreased. Hence it was considered as suitable candidate for formulation as floating drug delivery system. Different kinetic models were applied to drug release data in order to evaluate release mechanisms and kinetics. The optimized formula F4 showed better sustained drug release with good floating properties and fitted best to be Korsmeyer-Peppas model with R2 value of 0.9575. As the n value for the Korsmeyer- Peppas model was found be more than 0.5 it follows Non-Fickian diffusion mechanism. FTIR result showed that there is no drug excipients interaction.


Drug Research ◽  
2020 ◽  
Vol 70 (12) ◽  
pp. 576-582
Author(s):  
Maninder Pal Singh ◽  
Manish Kumar ◽  
Ravi Shankar

Abstract Purpose The aim of this study was to formulate methscopolamine floating drug delivery system to increase its gastro retention for further enhancement of absorption and overall bioavailability. Method Direct compression method was used to formulate floating drug delivery system of methscopolamine bromide. Different amount of HPMC, PVP K25, and MCC were used for preparation of tablets. Result The prepared tablets were evaluated for thickness, hardness, weight variation, floating lag time, swelling index and in-vitro drug release. All the formulations showed less than 10% of weight variation. The hardness and thickness of all the formulations were within the range of 3.7−4.2 kg/cm2 and 3.63−3.83 mm respectively. Floating lag time for all the formulations was reported in seconds. The degree of swelling was reported in range of 82.10−85.83%. In vitro release was carried out for 24 h. The maximum release was shown by F1 (93.947%) while the minimum release was observed for F4 (90.420%). The best formulation was optimized on the basis of percentage cumulative drug release, floating lag time and swelling index. F1 found to be the best formulation. Further on analyzing the drug release mechanism, F1 found to exhibit korsmeyer peppas model of drug release. Conclusion Floating gastroretentive tablet of methscopolamine bromide was successfully developed using direct compression method with potential to enhance the drug absorption and effective treatment of peptic ulcer.


Author(s):  
Audumbar Digambar Mali ◽  
Ritesh Suresh Bathe

Objective: The present study was undertaken with an objective to design, develop and evaluate gastro retentive floating tablets of an antihypertensive drug, quinapril HCl, which release the drug in a sustained manner over a period of 12 h.Methods: In this research work, we used hydrophilic polymer hydroxypropyl methylcellulose (HPMC K4M), the gas generating agent sodium bicarbonate and citric acid at different ratios for the preparation of tablets. A 32 factorial design was applied systematically; the amount of HPMC K4M (X1) and the amount of citric acid (X2) were selected as independent variables. The dependent variables chosen were percentage drug release at 6 h (Q6), percentage drug release at 12 h (Q12) and floating lag time. The high concentration of HPMC K4M and citric acid gives a sustained release for quinapril HCl floating tablets. The tablets were prepared by direct compression technique and evaluated for tablet thickness, hardness, weight variation, friability, floating lag time and In vitro drug release.Results: The In vitro drug release indicated the floating dosage forms showed slower release when the concentration of HPMC K4M increases. Formulation F4 having ratio 25:8 (HPMC K4M: citric acid) was considered as an optimised formulation which shows satisfactory sustained drug release and remained buoyant on the surface of the medium for more than 12 h. It can also conclude that floating drug delivery system of quinapril HCl can be successfully formulated as an approach to increase gastric residence time and thereby improving its bioavailability.Conclusion: The developed effervescent based floating tablets are a promising floating drug delivery system for oral sustained administration of quinapril HCl.


2018 ◽  
Vol 10 (6) ◽  
pp. 65 ◽  
Author(s):  
Mirmeera Girish Niharika ◽  
Kannan Krishnamoorthy ◽  
Madhukar Akkala

The principal objective behind the writing of this article on the floating drug delivery system (FDDS) was to systematize the recent literature with the core process of floatation in acquiring gastric retention. The different strategies used in the development of FDDS by constructing the effervescent and noneffervescent type of floating tablets basis of which is buoyancy mechanism. FDDS is a method to deliver the drugs that are active locally with a narrow absorption window in the upper gastrointestinal tract, unstable in the lower intestinal environment, and possess low solubility with higher pH values. The novel methodologies in FDDS include approaches to design a single unit and multiple-unit floating systems, the physiological and formulation variability affecting gastric retention along with the use of recently invented and developed polymers. This review also focuses on various in vitro techniques and in vivo studies in view of performance and application of floating systems. Floating dosage forms can be delivered in conventional forms like tablets, capsules with the addition of suitable ingredients along with the gas generating agent. This review also throws light on different techniques used in developing floating dosage forms along with current and novel advancements.


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