scholarly journals Development and Evaluation of Gastroretentive Floating Tablets of an Antihypertensive Drug Using Hydrogenated Cottonseed Oil

2013 ◽  
Vol 2013 ◽  
pp. 1-9
Author(s):  
Harshal Ashok Pawar ◽  
Pooja Ramchandra Gharat ◽  
Rachana Vivek Dhavale ◽  
Pooja Rasiklal Joshi ◽  
Pushpita Pankajkumar Rakshit
Keyword(s):  
Antihypertensive Drug ◽  
Methyl Cellulose ◽  
Cottonseed Oil ◽  
Lag Time ◽  
Floating Tablets ◽  
Hydrogenated Cottonseed Oil ◽  
Weight Variation ◽  
Floating System ◽  
Floating Tablet

The aim of the present work was to develop a gastroretentive floating tablet of Atenolol and investigate the effects of both hydrophilic and hydrophobic retardant on in vitro release. Atenolol is an antihypertensive drug with an oral bioavailability of only 50% because of its poor absorption from lower gastrointestinal tract. The floating tablets of Atenolol were prepared to increase the gastric retention, to extend the drug release, and to improve the bioavailability of the drug. The floating tablets were formulated using hydrophilic polymers as Hydroxy propyl methyl cellulose (HPMC K4M and HPMC K15M), hydrophobic retardant as a hydrogenated cottonseed oil (HCSO), and sodium bicarbonate as a gas generating agent to reduce floating lag time. The formulated tablets were evaluated for the quality control tests such as weight variation, hardness, friability, swelling index, floating lag time, and total floating time. The in vitro release study of the tablets was performed in 0.1 N HCl as a dissolution media. The results of the present study clearly indicates the promising potential of Atenolol floating system as an alternative to the conventional dosage and other sustained release formulations. The study also revealed the effectiveness of HCSO as retardant in combination with HPMC.

Formulation and in vitro Evaluation of Effervescent Bilayer Floating Controlled Release Tablets of Clarithromycin and Famotidine

2021 ◽  
pp. 4391-4398
Author(s):  
Murad Alam ◽  
Kifayat Ullah Shah ◽  
Kamran Ahmad Khan ◽  
Asif Nawaz ◽  
Hadia Bibi ◽  
...  
Keyword(s):  
Controlled Release ◽  
Hydroxypropyl Methylcellulose ◽  
Lag Time ◽  
Fickian Diffusion ◽  
Sustained Drug Release ◽  
Floating Tablets ◽  
Weight Variation ◽  
H Pylori ◽  
Controlled Release Tablets

The development of floating tablets with required buoyancy, lag time, and controlling release behaviour of drugs at target site is truly interesting and challenging task for researchers. Current study is concerned with the designing of effervescent floating controlled release tablets of clarithromycin and famotidine to treat peptic ulcer due to Helicobacter pylori (H. pylori) infection. Five formulations (F1-F5) were prepared, among which three formulations were of bilayered tablets while the remaining were included as plain tablets. These tablets were prepared by direct compression method using hydroxypropyl methylcellulose (HPMC) K100M, HPMC K4M and sodium bicarbonate as swelling and floating agents respectively. The qualitative tests such as thickness, hardness, weight variation, friability and uniformity of content were performed to ensure the quality of prepared tablets. The floating lag time of all formulations ranged from 14 to 20 seconds. The effervescent floating tablets with HPMC K4M (F1, F3 & F5) attained the total floating time of more than 12 hours, while tablets prepared with HPMC K100M (F2 & F4) achieved the total floating time of less than 7 hours. This difference in floating behaviour could be due to the variation in compaction and flow properties of the two polymers. The formulations with HPMC K100M (F2 & F4) have comparatively more sustained drug release properties when compared to F1, F3 and F4 using HPMC K4M as swelling and floating polymers. This could be attributed to better compaction of HPMC K100M. The prepared tablets follow non-Fickian diffusion kinetics. Overall, these floating controlled release effervescent bilayer and plain tablets may enhance the compliance and therapeutic outcomes of clarithromycin and famotidine in treatment of H. pylori.

scholarly journals In-vitro and In-vivo Relationship of Gabapentin from Floating and Immediate Release Tablets

2019 ◽  
pp. 1-12
Author(s):  
E. E. Zien El-Deen ◽  
H. A. Yassin
Keyword(s):  
Neuropathic Pain ◽  
Drug Release ◽  
Research Work ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Immediate Release ◽  
Floating Tablets ◽  
Weight Variation

Gabapentin is effective against post-traumatic spinal injury-induced neuropathic pain. It requires high dosage and frequency in the management of neuropathic pain. The present research work was an attempt to formulate and evaluate gabapentin gastro-retentive tablets to prolong gastric residence and increase drug absorption and further increase bioavailability. The floating tablets of gabapentin were prepared in two doses (300 and 600 mg) by using two polymers (hydroxyl propyl methyl cellulose and hydroxyl propyl cellulose). Immediate release tablets of gabapentin containing the same doses were prepared and used as reference formulations. The physicochemical characteristics of the prepared tablets were determined (drug content, weight variation, friability, hardness, thickness and diameter).  Drug release from the prepared tablets was followed and found that by increasing drug concentration in the tablets release rate increases. Floating tablets showed prolonged drug release (over 96%) to more than 15 hrs. Immediate release tablets showed over 97% drug release within 48 min. In-vivo results showed that plasma exposure to gabapentin in animals receiving the drug does not dose proportional and therefore may not reach therapeutically useful levels. AUC0-24 and Cmax in case of 300 mg tablets are more than those in case of 600 mg tablets. The in-vivo release of gabapentin does not correlate with the in-vitro release of the drug.

scholarly journals Development and Evaluation of Floating Tablets of Pantoprazole

2019 ◽  
pp. 452-467
Author(s):  
Sandhyarani Awatade ◽  
Ritesh Bathe ◽  
Swapna Mane
Keyword(s):  
Citric Acid ◽  
Drug Release ◽  
Research Work ◽  
Methyl Cellulose ◽  
Sustained Drug Release ◽  
Gastric Residence Time ◽  
Weight Variation ◽  
Floating Tablet ◽  
High Level

The present study was undertaken with an aim to design, develop and evaluate floating tablet of Pantoprazole, which release the drug in a sustained manner over a period of 12 hours. In this research work used hydroxy propyl methyl cellulose (HPMC K4M), gas generating agent sodium bicarbonate and citric acid. The high level of HPMC K4M and citric acid favors preparation of floating tablet Pantoprazole. The tablets were prepared by direct compression techniques and evaluated thickness, hardness, weight variation, friability, floating lag time and In-vitro drug release studies indicated that the floating dosage form showed slower release as concentration of HPMC K4M increases. Formulation F1 was considered as optimized formulation which shows satisfactory sustained drug release and remained buoyant on the surface of medium for more than 12 hrours. It can also conclude that floating drug delivery system of Pantoprazole can be successfully formulated as an approach to increase gastric residence time and thereby improving its bioavailability.

scholarly journals FORMULATION AND EVALUATION OF GASTRO RETENTIVE DRUG DELIVERY SYSTEM OF ZANAMIVIR USING DIFFERENT POLYMERS

2019 ◽  
Vol 8 (4) ◽  
Author(s):  
V. Vijaya Kumar ◽  
B. Deekshi Gladiola ◽  
C. Madhusudhana Chetty ◽  
R. E. Ugandar
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Guar Gum ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
Floating Tablets ◽  
Floating Tablet ◽  
Gastro Retentive

The objective of the present study is to develop gastro retentive drug delivery system of Zanamivir .Floating tablets of Zanamivir were developed with a gas generating agent NaHCO3 and in combination of different hydrophobic and hydrophilic polymers like xanthan gum, guar gum, HPMC and methyl cellulose .In the present work attempts have been made to prepare six formulations of Zanamivir in different ratios of drug and polymer to get a desired release profile by direct compression method .All the prepared tablets were evaluated in terms of pre compression and post compression parameters. FTIR studies revealed the absence of drug polymer interactions .Among all the formulations F5 Showed 97.4% of in vitro drug release for 10 hours and hence formulation F5 is selected as an optimized formulation. The optimized formulation F5 was found to follow Higuchi release kinetics and zero order. Further formulation F5 was subjected to accelerated stability studies for 3 months. It showed that the optimized formulation was intact without any interactions. Finally the optimized formulation F5 complying with all properties of floating tablets was found to be satisfactory Keywords: Zanamivir, floating tablet, natural gums, sodium bicarbonate, gastro retentive drug delivery systems

scholarly journals FORMULATION DEVELOPMENT, CHARACTERIZATION AND IN- VITRO EVALUATION OF FLOATING MATRIX DOSAGE FORM OF TRAMADOL HYDROCHLORIDE USING VARIOUS POLYMERS

2017 ◽  
Vol 10 (2) ◽  
pp. 281
Author(s):  
Sarada Anepu ◽  
Lohithasu Duppala ◽  
Soma Sundari M
Keyword(s):  
Methyl Cellulose ◽  
Formulation Development ◽  
Scanning Calorimetry ◽  
Tramadol Hydrochloride ◽  
Floating Tablets ◽  
Gastric Residence Time ◽  
Weight Variation ◽  
Floating Drug Delivery ◽  
Release Studies

Objective: The purpose of present study was to formulate the gastro retentive floating tablets of tramadol hydrochloride for enhancement of the gastric residence time.Methods: The floating tablets were prepared by direct compression method and evaluated for hardness, thickness, and friability of the tablets. The in vitro drug release studies were performed for different formulations and to optimize the best formulae based on the dissolution profiles.Results: Fourier transform infrared spectroscopy and differential scanning calorimetry studies revealed that there was no interaction between tramodol hydrocholride and excipients. The formulated tablets were evaluated for properties like weight variation, hardness, thickness, friability, drug content, density and floating properties, matrix integrity and complied with USP requirements. The tablets of optimized formula had floating lag time of 120, 72 and 96 seconds and the tablets remained in the floating condition for more than 12 h. The results of drug excipients compatibility studies suggest that there was no significant change in the physical appearance of these blends, when stored at 40 °C/75% RH for a period of 4 weeks.  Among various trial formulations developed with different concentration of polymer F3 (HPMC K4 M with 120mg of polymer), F5 (HPMC K15 M with 100 mg polymer), F11 (PEO WSR 303 with 100mg polymer), were chosen as the optimized formulations based on the release profile.Conclusion: Tramodol HCl floating tablets were successfully made using various polymers for the enhancement of the gastric residence time. From the present study it was concluded that hydroxy propyl methyl cellulose K 4 M can be used as effective polymer for the formulation of floating effervescent tablets of highly soluble drug indicating successful development of sustained release floating drug delivery system.Key words: Tramodol HCl, floating tablets, PEO 303 WSR, PEO N60, HPMC K 4 M, HPMC K15 M and HPMC K 100 M. 

scholarly journals FORMULATION AND IN VITRO EVALUATION OF AMLODIPINE GASTRORETENTIVE FLOATING TABLETS USING A COMBINATION OF HYDROPHILIC AND HYDROPHOBIC POLYMERS

2018 ◽  
Vol 10 (6) ◽  
pp. 119 ◽  
Author(s):  
Anas T. Alhamdany ◽  
Ali Khidher Abbas
Keyword(s):  
Hydroxypropyl Methylcellulose ◽  
Zero Order ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Order Kinetic ◽  
Floating Tablets ◽  
Hydrophobic Polymers ◽  
Weight Variation ◽  
Floating Tablet

Objective: The aim of this study was to formulate a developed floating tablet of amlodipine using different concentrations and types of hydrophilic and hydrophobic polymers to be conserved in the stomach for modulating solubility and bioavailability, diminishes drug waste and decline side effects.Methods: Through this study, eleven innovative formulations of amlodipine floating tablets were prepared [mixture of amlodipine, sodium bicarbonate (NaHCO3), hydroxypropyl methylcellulose (HPMC) E50, HPMC K100M, ethylcellulose (EC) 5 mp. a. s.] by direct compression method. The pre-compressed mixtures were then evaluated for numerous parameters such as angle of repose, bulk density, tapped density, Carr's compressibility index and Hausner's ratio. After compression, tablets were subjected to several tests like; floating behavior of tablets, tablet thickness, hardness test, friability test, weight variation, in vitro dissolution test. In addition, the optimum formulation was evaluated for Fourier transform-infrared (FT-IR) and differential scanning calorimetry (DSC) tests. Results: From in vitro dissolution tests and kinetic assessments; F8 was selected as an optimum formula, depending on the R2 value of zero order kinetics (0.9915) and (n) value of Korsmeyer-Peppas (0.9635) which indicate purely relaxation zero order kinetic with good delaying in drug release that was reached to 14 h.Conclusion: It can be concluded that the developed formulation of a certain combination of low viscosity grades of HPMC and EC was considered an efficient floating tablet.

scholarly journals Developement and Characterization of Floating Tablets of Nizatidine for Peptic Ulcer

2020 ◽  
pp. 1-12
Author(s):  
Sunil T. Galatage ◽  
Suresh G. Killedar ◽  
Rushikesh B. Katakar ◽  
Ravindra B. Kumbhar ◽  
Maya Sharma ◽  
...  
Keyword(s):  
Drug Release ◽  
Residence Time ◽  
Half Life ◽  
Research Work ◽  
Content Uniformity ◽  
Floating Tablets ◽  
Gastric Residence Time ◽  
Weight Variation ◽  
Floating Tablet

The objective of the present research work is to develop an ideal floating drug delivery system of nizatidine to increase the gastric residence time in stomach. To overcome the short half life and lower bioavailability of drug in tablet form we developed the drug in the form of effervescent floating tablet containing HPMC K100 and sodium bicarbonate by direct compression methodology. The prepared effervescent floating tablets were characterized by thickness, weight variation, hardness, friability, drug content uniformity, in vitro buoyancy time, swelling test, in vitro study and stability study and found that all formulations showed satisfactory results with enhanced half life and bioavailability that is among all formulations F1 formulation exhibited good drug release of 95.03% & has shown floating lag time 55 sec. Finally, it was concluded that formulations of nizatidine floating tablet were successfully prepared and found prolonged drug release for 12 hours thereby getting enhanced bioavailability, patient compliance by reducing dose frequency and gastric residence time.

Formulation and Evaluation of Galantamine Hydrobromide Floating Matrix Tablet

2018 ◽  
Vol 8 (2) ◽  
Author(s):  
Poreddy Srikanth Reddy ◽  
Penjuri Subhash Chandra Bose ◽  
Vuppula Sruthi ◽  
Damineni Saritha
Keyword(s):  
Sodium Alginate ◽  
Xanthan Gum ◽  
Lag Time ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Matrix Tablet ◽  
Compression Technique ◽  
Weight Variation ◽  
The Matrix

The aim of the present work was to prepare floating tablets of galantamine HBr using sodium alginate and xanthan gum as matrix forming carriers. Galantamine HBr is used for the treatment of mild to moderate Alzheimer's disease and various other memory impairments, in particular those of vascular origin. The matrix tablet formulations were prepared by varying the concentrations of sodium alginate and xanthan gum. The tablets were prepared by direct compression technique using PVP K-30 as a binder and sodium bicarbonate for development of CO2. The prepared matrix tablets were evaluated for properties such as hardness, thickness, friability, weight variation, floating lag time, compatibility using DSC and FTIR. In vitro dissolution was carried out for 12 hrs in 0.1N HCl at 37±0.5 ºC using USP paddle type dissolution apparatus. It was noted that, all the prepared formulations had desired floating lag time and constantly floated on dissolution medium by maintaining the matrix integrity. The drug release from prepared tablets was found to vary with varying concentration of the polymers, sodium alginate and xanthan gum. From the study it was concluded that floating drug delivery system for galantamine HBr can be prepared by using sodium alginate and xanthan gum as a carrier.

scholarly journals DESIGN AND EVALUATION OF INTRAGASTRIC BUOYANT TABLETS OF VENLAFAXINE HYDROCHLORIDE

2017 ◽  
Vol 10 (5) ◽  
pp. 166
Author(s):  
Parasuram Rajam Radhika ◽  
Nishala N ◽  
Kiruthika M ◽  
Sree Iswarya S
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Xanthan Gum ◽  
Hydroxypropyl Methylcellulose ◽  
Methyl Cellulose ◽  
In Vitro Drug Release ◽  
Weight Variation ◽  
Floating Drug Delivery ◽  
Venlafaxine Hydrochloride

Objective: The present study was undertaken to prolong the release of orally administered drug. The aim is to formulate, develop, and evaluate theintragastric buoyant tablets of venlafaxine hydrochloride, which releases the drug in a sustained manner over a period of 12 hrs. Different formulationswere formulated using the polymers Carbopol 934 P, xanthan gum, hydroxypropyl methylcellulose (HPMC K100M) with varying concentration ofdrug: Polymer ratio of 1:1, 1:1.5, 1:2, in which sodium bicarbonate acts as gas generating agent, and microcrystalline cellulose as a diluent.Methods: The tablets were prepared by direct compression and evaluated for tablet thickness, weight variation, tablet hardness, friability, in vitrobuoyancy test, in vitro drug release and Fourier transform infrared spectroscopy. Formulations were evaluated by floating time, floating lag time and in vitro drug release. Dissolution profiles were subjected for various kinetic treatments to analyze the release pattern of drug.Results: It was found that drug release depends on swelling, erosion, and diffusion, thus following the non-Fickian/anomalous type of diffusion.Formulation F8 was considered as an optimized formulation for gastro retentive floating tablet of venlafaxine hydrochloride. The optimizedformulation showed sustained drug release and remained buoyant on the surface of the medium for more than 12 hrs. As the concentration of HPMCK100M increases in the formulation the drug release rate was found to be decreased. The optimized formulation was subjected for the stability studiesand was found to be stable as no significant change was observed in various evaluated parameters of the formulation.Conclusion: It can be concluded that floating drug delivery system of venlafaxine hydrochloride can be successfully formulated as an approach toincrease gastric residence time, thereby improving its bioavailability.Keywords: Venlafaxine hydrochloride, Intragastric buoyant, Floating drug delivery systems, Hydroxypropyl methyl cellulose K100M, Carbopol 934 P,Xanthan gum.

scholarly journals Formulation and evaluation of bi-layer floating tablets of ziprasidone HCl and trihexyphenidyl HCl

2011 ◽  
Vol 47 (3) ◽  
pp. 545-553 ◽  
Author(s):  
Sathis Kumar Dinakaran ◽  
Santhos Kumar ◽  
David Banji ◽  
Harani Avasarala ◽  
Venkateshwar Rao
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Chemical Properties ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Floating Tablets ◽  
Ir Studies ◽  
Weight Variation ◽  
The Matrix

The purpose of this research study was to establish ziprasidone HCl NR 40 mg and trihexyphenidyl HCl SR 4mg in the form of bi-layer sustained release floating tablets. The tablets were prepared using sodium HPMC K4M / HPMC K15M as bio-adhesive polymers and sodium bicarbonate acting as a floating layer. Tablets were evaluated based on different parameters such as thickness, hardness, friability, weight variation, in vitro dissolution studies, content of active ingredient and IR studies. The physico-chemical properties of the finished product complied with the specifications. In vitro release from the formulation was studied as per the USP XXIII dissolution procedure. The formulations gave a normal release effect followed by sustained release for 12 h which indicates bimodal release of ziprasidone HCl from the matrix tablets. The data obtained was fitted to Peppas models. Analysis of n values of the Korsmeyer equation indicated that the drug release involved non-diffusional mechanisms. By the present study, it can be concluded that bi-layer tablets of ziprasidone HCl and trihexyphenidyl HCl will be a useful strategy for extending the metabolism and improving the bioavailability of Ziprasidone HCl and Trihexyphenidyl HCl.

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