scholarly journals Formulation and evaluation of gastro-retentive floating tablets of terbinafine

2020 ◽  
Vol 13 (1) ◽  
pp. 257-266
Author(s):  
Kapil Jalodiya ◽  
Sourabh Jain ◽  
Karunakar Shukla
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Extended Period ◽  
Direct Compression ◽  
Compression Method ◽  
In Vitro Drug Release ◽  
Floating Tablets ◽  
Gastro Retentive

Gastro-retentive dosage forms enable prolonged and continuous input of the drug to the upper parts of the gastrointestinal tract and improve the bioavailability of medications those are characterized by a narrow absorption window. The purpose of this research was to develop a novel gastro retentive drug delivery system based on direct compression method for sustained delivery of active agent to improve the bioavailability, reduce the number of doses and to increase patient compliance. Gastro retentive floating tablets of terbinafine were prepared by direct compression method using altered concentrations of HPMC K4, HPMC K15 and PVP K30 as polymers. The prepared tablets of terbinafine were evaluated tablet hardness, uniformity of weight, friability, uniformity of content, in vitro buoyancy test, swelling index, in vitro dissolution study and stability study. All the compositions were resulted in adequate Pharmacopoeial limits. Compatibility studies was execution during FTIR shown that there was absence of probable chemical interaction between pure drug and excipients. The varying concentration of gas generating agent and polymers was found to affect on in-vitro drug release and floating lag time. In vitro drug release of floating gastro retentive tablet of terbinafine shown that the formulation F5 was found to be the best formulation as it releases 96.22% terbinafine in a controlled manner for an extended period of time (up to 480 min). The release data was fitted to various mathematical models such as Higuchi, Korsmeyer-Peppas, First order and Zero order to evaluate the kinetics and mechanism of the drug release. Prepared floating tablets of terbinafine may prove to be a potential candidate for safe and effective controlled drug delivery over an extended period of time for gastro retentive drug delivery system.

scholarly journals Formulation development and evaluation of gastroretentive mucoadhesive tablets of glimepiride using natural polymers

2020 ◽  
Vol 10 (4-s) ◽  
pp. 153-159
Author(s):  
Rahul Malasiya ◽  
Tarkeshwar P. Shukla
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Extended Period ◽  
Direct Compression ◽  
Compression Method ◽  
In Vitro Drug Release ◽  
Mucoadhesive Tablets ◽  
Gastro Retentive

Glimepiride, a third-generation sulfonylurea is poorly soluble anti-diabetic drug. Currently, the use of natural gums and mucilage is of increasing importance in pharmaceutical formulations as valuable drug excipients. Natural plant-based materials are economic, free of side effects, biocompatible and biodegradable. The development of mucoadhesive sustained release drug delivery system is recommended in order to enhance the bioavailability. A mucoadhesive tablets were developed using the natural polymer sodium alginate and gum tragacanth. Mucoadhesion is a complex phenomenon which involves wetting, adsorption and interpenetration of polymer chains. The tablets of glimepiride were prepared by direct compression method. Pre-compression parameters were evaluated. The tablets were evaluated for post-compression parameters such as thickness, hardness, average weight, friability and In vitro release studies. All the compositions were resulted in adequate pharmacopoeial limits. The varying concentration of polymers was found to affect on in-vitro drug release and mucoadhesive strength. In vitro drug release of gastro retentive tablet of glimepiride shown that the formulation F5 was found to be the best formulation as it releases 98.78%.  Glimepiride in a sustain release manner for an extended period of time (up to 12 hrs). The release data was fitted to various mathematical models such as higuchi, korsmeyer-peppas, first order and zero order to evaluate the kinetics and mechanism of the drug release. Prepared tablets of glimepiride may prove to be a potential candidate for safe and effective controlled drug delivery over an extended period of time for gastro retentive drug delivery system. Keywords: Glimepiride, Gastro retentive, Anti-diabetic drug, Direct compression method

scholarly journals Formulation Development and Evaluation of Sustain Release Gastroretentive Floating Tablets of Prochlorperazine Dimaleate

2019 ◽  
Vol 9 (4-s) ◽  
pp. 445-450
Author(s):  
Bharti Patle ◽  
Vivek Jain ◽  
Shradha Shende ◽  
Prabhat Kumar Jain
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Extended Period ◽  
Lag Time ◽  
In Vitro Dissolution ◽  
Compression Method ◽  
In Vitro Drug Release ◽  
Floating Tablets ◽  
Gastro Retentive

Floating drug delivery systems are the gastroretentive forms that precisely control the release rate of target drug to a specific site which facilitate an enormous impact on health care. The purpose of this research was to develop a novel gastro retentive drug delivery system based on direct compression method for sustained delivery of active agent to improve the bioavailability, reduce the number of doses and to increase patient compliance. Gastro retentive floating tablets of Prochlorperazine dimaleate (PCZ) were prepared by direct compression method using altered concentrations of HPMC K4, HPMC K15 and PVP K30 as polymers. The prepared tablets of PCZ were evaluated for hardness, thickness, friability, weight variation, drug content uniformity, buoyancy lag time, total floating time, in-vitro dissolution study, etc. All the compositions were resulted in adequate Pharmacopoeial limits. Compatibility studies was execution during FTIR shown that there was absence of probable chemical interaction between pure drug and excipients. The varying concentration of gas generating agent and polymers was found to affect on in-vitro drug release and floating lag time. In vitro drug release of floating gastro retentive tablet of PCZ shown that the formulation F9 was found to be the best formulation as it releases 98.89% in a controlled manner for an extended period of time (up to 12 hrs). The release data was fitted to various mathematical models such as Higuchi, Korsmeyer-Peppas, First order and Zero order to evaluate the kinetics and mechanism of the drug release. The optimized formulation (F9) 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.  Prepared floating tablets of PCZ may prove to be a potential candidate for safe and effective controlled drug delivery over an extended period of time for gastro retentive drug delivery system. Keywords: Prochlorperazine dimaleate, Floating tablet, Gastro retentive, Total floating time.

scholarly journals Development and Optimization of Methscopolamine Bromide Gastroretentive Floating Tablets Using 32 Factorial Design

Drug Research ◽  
2020 ◽  
Vol 70 (12) ◽  
pp. 576-582
Author(s):  
Maninder Pal Singh ◽  
Manish Kumar ◽  
Ravi Shankar
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Lag Time ◽  
Direct Compression ◽  
Compression Method ◽  
Weight Variation ◽  
Floating Drug Delivery ◽  
Floating Drug Delivery System

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.

scholarly journals Formulation and Evaluation of Floating Matrix Tablets of Sacubitril and Valsartan

2019 ◽  
Vol 9 (4-s) ◽  
pp. 298-309
Author(s):  
Sudhakar Pathak ◽  
Harish Pandey ◽  
Sunil Kumar Shah
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Lag Time ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Potential Candidate ◽  
In Vitro Drug Release ◽  
Gastric Emptying Rate ◽  
Floating Tablets

Floating Drug Delivery Systems (FDDS) have a bulk density lower than gastric fluids and thus remain buoyant in the stomach for a prolonged period of time, without affecting the gastric emptying rate. While the system is floating on the gastric contents, the drug is released slowly at a desired rate from the system. These floating tablets mainly prepared for reduction of lag time and release the drug up to 12 hours and may also increase the bioavailability of the drugs by utilizing the drug to full extent avoiding unnecessary frequency of dosing. The purpose of this research was to develop and evaluated floating matrix tablets of sacubitril and valsartan. The floating matrix tablets of sacubitril and valsartan were prepared by direct compression method using altered concentrations of HPMC K4M, HPMC K100M, sodium alginate as polymers and sodium bicarbonate, citric acid as gas generating agent. FTIR, DSC studies conformed that there was no incompatibility between the polymers and the drug. Tablet preformulation parameters were within the pharmacopoeias limit. Tablets were evaluated by different parameters such as weight uniformity, content uniformity, thickness, hardness, in vitro release studies, buoyancy determination and kinetic analysis of dissolution data. The varying concentration of gas generating agent and polymers was found to affect on in-vitro drug release and floating lag time. Tablet showed ≤ 1min lag time, continuance of buoyancy for >12 h. The in-vitro drug release pattern of sacubitril and valsartan optimized floating tablets (F16) was fitted to different kinetic models which showed highest regression (r2 = 0.9838) for Higuchi model. The Optimized formulation (F16) 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.  Prepared floating tablets of sacubitril and valsartan may prove to be a potential candidate for safe and effective controlled drug delivery over an extended period of time for gastro retentive drug delivery system.  

scholarly journals A hydrogel based quasi-stationary test system for in vitro dexamethasone release studies for middle ear drug delivery systems

2021 ◽  
Vol 7 (2) ◽  
pp. 692-695
Author(s):  
Thomas Eickner ◽  
Michael Teske ◽  
Natalia Rekowska ◽  
Volkmar Senz ◽  
Klaus-Peter Schmitz ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Drug Concentration ◽  
Drug Delivery Systems ◽  
Test System ◽  
Delivery Systems ◽  
In Vitro Drug Release

Abstract For the investigation of in vitro drug release, methods have been used in which samples of drug delivery systems are immersed in release medium. The medium is used to measure drug concentration via chromatography or photometry. These systems are suitable to investigate the drug release of different systems or to simulate tissue environments. When considering predominantly humid regions, e.g. for drug release into the cochlea through the round window membrane by a drug delivery system placed at that membrane, reproducible in vitro determination of drug release becomes particularly challenging. In this study the development of a system is reported that allows the investigation of the in vitro drug release simulating such conditions. The presented test system consists of an alginate hydrogel in glass vials simulating the biological membrane, which separates the drug delivery system from the medium filled compartment. Saline is used as release medium and injected under the hydrogel. The samples are placed on top of the hydrogel, which slightly contacts the medium surface. The drug concentration in the release medium was determined by HPLC measurements. This system allows for testing the release of dexamethasone without the samples being completely surrounded by medium. The hydrogel mediates the diffusion of the drug by ensuring the contact with the medium. Release was monitored for more than 23 days. The presented concept was successfully designed and manufactured. The system is inexpensive and can be duplicated easily. In this study, it was used to monitor the drug release of dexamethasone from PEGDA700 derived polymer. One challenge that remains to be considered is the low mechanical stability of the hydrogel, which results in a need for repeated manufacturing during the handling of the system.

scholarly journals DEVELOPMENT AND EVALUATION OF GASTRORETENTIVE FLOATING TABLETS OF A QUINAPRIL HCL BY DIRECT COMPRESSION TECHNIQUE

2017 ◽  
Vol 9 (8) ◽  
pp. 35 ◽  
Author(s):  
Audumbar Digambar Mali ◽  
Ritesh Suresh Bathe
Keyword(s):  
Drug Delivery ◽  
Citric Acid ◽  
Drug Release ◽  
Lag Time ◽  
Direct Compression ◽  
Compression Technique ◽  
Floating Tablets ◽  
Floating Drug Delivery ◽  
Floating Drug Delivery System

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.

scholarly journals DISPOSABLE CONTACT LENS-BASED OCULAR DELIVERY OF MOXIFLOXACIN : A NOVEL APPROACH

2021 ◽  
pp. 105-111
Author(s):  
UMESH KUMAR SHARMA
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Contact Lens ◽  
Drug Loading ◽  
Morphological Characteristics ◽  
Drug Release Profile ◽  
In Vitro Drug Release

Objective: In the present research, the main objective was to investigate the possibility of designing, fabricating, and optimizing a disposable ocular film-based drug delivery system. Methods: Moxifloxacin hydrochloride was loaded onto the prepared disposable ocular films by the soaking method. Results: The drug loading conditions were studied, and it was found that the maximum drug loading was achieved in 3 hours at pH 6.5 of the drug solution. It was also observed that the drug loading efficacy and in vitro drug release profile can be monitored by varying the ocular film composition. The ocular films were then characterized for thickness uniformity, size uniformity, weight uniformity, swelling index, surface pH, breaking on elongation, folding endurance, bio-adhesive strength, transparency, drug loading efficiency, moisture content, morphological characteristics, and in vitro drug release profiles. Conclusion: Based on the results, it was concluded that the developed disposable ocular films demonstrate a significant prolonged drug release within the therapeutic range of up to 12 h, which is promising as a novel disposable contact lens-based ocular drug delivery system.

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