scholarly journals Development and in vitro Characterization of Gastro Retentive Raft Forming Stavudine Tablets

2017 ◽  
Vol 9 (01) ◽  
Author(s):  
Mahendar Rupavath ◽  
K. S. K Rao
Keyword(s):  
Drug Release ◽  
Matrix Tablets ◽  
Drug Dissolution ◽  
Release Mechanism ◽  
Compatibility Study ◽  
Drug Bioavailability ◽  
Drug Content ◽  
Weight Variation

The objective of the present investigation was to identify a suitable raft forming agent and to develop raft forming stavudine matrix tablets using different rate controlling natural, semi-synthetic and synthetic polymers to achieve prolonged gastric residence time, leading to an increase in drug bioavailability and patient compliance. Various raft forming agents were used in preliminary screening. Raft forming floating tablets were developed using pullulan gum as natural rate controlling polymer, and directly compressible grades of hydroxypropyl methylcellulose (Benecel K4M DC) as semi synthetic, and Carbopol 71G as synthetic rate controlling polymers respectively and optimum concentrations of sodium-bicarbonate as gas generating agent to generate optimum buoyancy by direct compression method. Raft forming tablets were evaluated for weight variation, thickness, hardness, friability, drug content, in vitro drug release, floating buoyancy and raft strength. Drug-excipients compatibility study showed no interaction between drug and excipients. Raft forming tablets showed satisfactory results when evaluated for weight variation, thickness, hardness, friability, drug content, and raft strength. The optimized formulation was selected based on physicochemical characteristics and in vitro drug dissolution characteristics. Further, the optimized formulation was evaluated for in vivo radiographic studies by incorporating BaSO4 as radio opaque substance. Optimized formulation showed controlled and prolonged drug release profiles while floating and raft formation over the dissolution medium. Diffusion followed by erosion with raft forming drug release mechanism was observed for the formulation, indicating that dissolution media diffusion and polymer erosion played an essential role in drug release. In vivo radiographic studies revealed that the raft forming formulations remained in the stomach for 240 30 min in rabbits and indicated that gastric retention time was increased by the floating and raft forming principle, which was considered and desirable for absorption window drugs.

scholarly journals Formulation, Optimization and in vitro Characterization of Stavudine Gastro Retentive Floating Matrix Tablets

2016 ◽  
Vol 8 (03) ◽  
Author(s):  
Mahendar Rupavath ◽  
Kranthi G. ◽  
Chinna Palem ◽  
K. S. K. Patnaik
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
Release Mechanism ◽  
Wet Granulation ◽  
Drug Bioavailability ◽  
In Vitro Drug Release ◽  
Weight Variation

The aim of the present investigation was to develop floating matrix tablets of stavudine to achieve prolong gastric residence time, leading to an increase in drug bioavailability and patient compliance. Floating tablets were prepared by wet granulation technique, using hydroxypropyl methylcellulose (HPMC K15M) as synthetic, pullulan gum as natural rate controlling polymers and optimum amounts of sodium-bicarbonate and citric acid as gas generating agents in suitable ratios to generate optimum buoyancy. Developed formulations were evaluated for weight variation, thickness, hardness, friability, drug content, in vitro drug release, floating lag time and floating buoyancy. All the formulations exhibited acceptable physical properties and the best formulation (F3) was selected based on in vitro characteristics. Further, the optimized formulation was evaluated for in vivo radiographic studies by incorporating BaSO4 as radio opaque substance. All the formulations were studied for in vitro drug release characteristics for 16 h. Optimized formulation showed controlled and prolonged drug release profiles while floating over the dissolution medium. Diffusion followed by erosion drug release mechanism was observed for the formulation, indicating that water diffusion and polymer erosion played an essential role in drug release. In vivo radiographic studies revealed that the tablets remained in the stomach for 8 ± 0.5 h in fasting human volunteers and indicated that gastric retention time was increased by the floating principle, which was considered and desirable for absorption window drugs.

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.

Preparation and Evaluation of Gemifloxacin Mesylate Floating Matrix Tablets in Healthy Human Volunteers

2017 ◽  
Vol 10 (1) ◽  
pp. 3623-3630
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Haarika B ◽  
Jyothi Sri S ◽  
K Abbulu
Keyword(s):  
Drug Release ◽  
Sodium Bicarbonate ◽  
Polymer Concentration ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
Physical Parameters ◽  
Drug Bioavailability ◽  
Floating Tablets

The purpose of present investigation was to develop floating matrix tablets of gemifloxacin mesylate, which after oral administration could prolong the gastric residence time, increase the drug bioavailability and diminish the side effects of irritating drugs. Tablets containing drug, various viscosity grades of hydroxypropyl methylcellulose such as HPMC K4M and HPMC K15M as matrix forming agent, Sodium bicarbonate as gas-forming agent and different additives were tested for their usefulness in formulating gastric floating tablets by direct compression method. The physical parameters, in vitro buoyancy, release characteristics and in vivo radiographic study were investigated in this study. The gemifloxacin mesylate floating tablets were prepared using HPMC K4M polymer giving more sustained drug release than the tablet containing HPMC K15M. All these formulations showed floating lag time of 30 to 47 sec and total floating time more than 12 h. The drug release was decreased when polymer concentration increases and gas generating agent decreases. Formulation that contains maximum concen-tration of both HPMC K15M and sodium bicarbonate (F9) showing sufficiently sustained with 99.2% of drug release at 12 h. The drug release from optimized formulation follows Higuchi model that indicates the diffusion controlled release. The best formulation (F9) was selected based on in vitro characteristics and used in vivo radiographic studies by incorporating barium sulphate as a radio-opaque agent and the tablet remained in the stomach for about 6 h.   

scholarly journals DESIGN AND IN VITRO/IN VIVO EVALUATION OF EXTENDED RELEASE MATRIX TABLETS OF NATEGLINIDE

2018 ◽  
Vol 7 (6) ◽  
Author(s):  
Mohini Sihare ◽  
Rajendra Chouksey
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Release Profile ◽  
Matrix Tablets ◽  
In Vivo Studies ◽  
Release Mechanism ◽  
In Vivo Evaluation

Aim: Nateglinide is a quick acting anti-diabetic medication whose potent activity lasts for a short duration. One of the dangerous side effects of nateglinide administration is rapid hypoglycemia, a condition that needs to be monitored carefully to prevent unnecessary fatalities. The aim of the study was to develop a longer lasting and slower releasing formulation of nateglinide that could be administered just once daily. Methods: Matrix tablets of nateglinide were prepared in combination with the polymers hydroxypropylmethylcellulose (HPMC), eudragits, ethyl cellulose and polyethylene oxide and the formulated drug release patterns were evaluated using in vitro and in vivo studies. Conclusion: Of the seventeen formulated matrix tablets tested, only one formulation labelled HA-2 that contained 15% HPMC K4M demonstrated release profile we had aimed for. Further, swelling studies and scanning electron microscopic analysis confirmed the drug release mechanism of HA-2. The optimized formulation HA-2 was found to be stable at accelerated storage conditions for 3 months with respect to drug content and physical appearance. Mathematical analysis of the release kinetics of HA-2 indicated a coupling of diffusion and erosion mechanisms. In-vitro release studies and pharmacokinetic in vivo studies of HA-2 in rabbits confirmed the sustained drug release profile we had aimed for. Keywords: Hydroxypropylmethylcellulose, Matrix tablets, Nateglinide, Sustained release

scholarly journals Crushed Tablets: Does the Administration of Food Vehicles and Thickened Fluids to Aid Medication Swallowing Alter Drug Release?

2014 ◽  
Vol 17 (2) ◽  
pp. 207 ◽  
Author(s):  
Yady Juliana Manrique-Torres ◽  
Danielle J Lee ◽  
Faiza Islam ◽  
Lisa M Nissen ◽  
Julie A.Y. Cichero ◽  
...  
Keyword(s):  
Drug Release ◽  
Orange Juice ◽  
Immediate Release ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Simulated Gastric Fluid ◽  
Drug Bioavailability ◽  
Thickening Agents

Purpose. To evaluate the influence of co-administered vehicles on in vitro dissolution in simulated gastric fluid of crushed immediate release tablets as an indicator for potential drug bioavailability compromise. Methods. Release and dissolution of crushed amlodipine, atenolol, carbamazepine and warfarin tablets were tested with six foods and drinks that are frequently used in the clinical setting as mixers for crushed medications (water, orange juice, honey, yoghurt, strawberry jam and water thickened with Easythick powder) in comparison to whole tablets. Five commercial thickening agents (Easythick Advanced, Janbak F, Karicare, Nutilis, Viscaid) at three thickness levels were tested for their effect on the dissolution of crushed atenolol tablets. Results. Atenolol dissolution was unaffected by mixing crushed tablets with thin fluids or food mixers in comparison to whole tablets or crushed tablets in water, but amlodipine was delayed by mixing with jam. Mixing crushed warfarin and carbamazepine tablets with honey, jam or yoghurt caused them to resemble the slow dissolution of whole tablets rather than the faster dissolution of crushed tablets in water or orange juice. Crushing and mixing any of the four medications with thickened water caused a significant delay in dissolution. When tested with atenolol, all types of thickening agents at the greatest thickness significantly restricted dissolution, and products that are primarily based on xanthan gum also delayed dissolution at the intermediate thickness level. Conclusions. Dissolution testing, while simplistic, is a widely used and accepted method for comparing drug release from different formulations as an indicator for in vivo bioavailability. Thickened fluids have the potential to retard drug dissolution when used at the thickest levels. These findings highlight potential clinical implications of the addition of these agents to medications for the purpose of dose delivery and indicate that further investigation of thickened fluids and their potential to influence therapeutic outcomes is warranted. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

scholarly journals Formulation and Evaluation of Fast Dissolving Film of Losartan Potassium

2021 ◽  
Vol 68 (1) ◽  
Author(s):  
Bhageerathy A ◽  
Sandhya Murali ◽  
eny Sara Thomas ◽  
Sigi Vasanthkumar ◽  
Prasanth V V
Keyword(s):  
Drug Release ◽  
Physical Stability ◽  
Losartan Potassium ◽  
In Vivo Studies ◽  
Disintegration Time ◽  
Drug Content ◽  
Weight Variation ◽  
Significant Difference

A total of nine formulations of fast dissolving films of Losartan Potassium were developed by solvent casting method using film forming polymers such as HPMC E5, E15 and E50 and other film modifiers. The appearances of films were transparent, thin, flexible, elastic, smooth and transparent. The weight variation ranged between 16.14 ± 0.192 and 17.31 ± 0.313 and showed that there was no significant difference in the weight of individual formulations. All the formulations showed more than 150 of folding endurance. The drug content was found to be in an acceptable range for all the formulations which indicated uniform distribution of drug. A rapid dissolution of all the film was observed by the dissolution test, in which above 90% of Losartan Potassium was released within 5 min. The formulation F1 showed maximum drug release (98.73) within 5 minutes. Based on the in vitro drug release, drug content and in vitro disintegration time it is found that F1 was selected as the best formulation. The formulations showed satisfactory physical stability at 40°C at 75 % RH. Losartan Potassium (LOSAR-25) is shown in Figure 4. From the results of comparative studies of marketed product and it found that F1 showed 98.73% release within 5 min and LOSAR 25 showed 90.76% release in 30 min. In vitro studies indicate that this potential drug delivery system has considerably good stability and release profile. Nevertheless, further in vivo studies are warranted to confirm these results.

scholarly journals Design, Fabrication and Evaluation of Drug Release Kinetics from Aceclofenac Matrix Tablets using Hydroxypropyl Methyl Cellulose

1970 ◽  
Vol 8 (1) ◽  
pp. 23-30 ◽  
Author(s):  
Abul Kalam Lutful Kabir ◽  
Bishyajit Kumar Biswas ◽  
Abu Shara Shasur Rouf
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
Matrix Tablets ◽  
Angle Of Repose ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Drug Content ◽  
Compressibility Index

The objective of this study was to develop a sustained release matrix tablet of aceclofenac usinghydroxypropyl methylcellulose (HPMC K15M and HPMC K100M CR) in various proportions as release controllingfactor by direct compression method. The powders for tableting were evaluated for angle of repose, loose bulkdensity, tapped bulk density, compressibility index, total porosity and drug content etc. The tablets were subjected tothickness, weight variation test, drug content, hardness, friability and in vitro release studies. The in vitro dissolutionstudy was carried out for 24 hours using United States Pharmacopoeia (USP) 22 paddle-type dissolution apparatus inphosphate buffer (pH 7.4). The granules showed satisfactory flow properties, compressibility index and drug contentetc. All the tablets complied with pharmacopoeial specifications. The results of dissolution studies indicated that theformulations F-2 and F-3 could extend the drug release up to 24 hours. By comparing the dissolution profiles with themarketed product, it revealed that the formulations exhibited similar drug release profile. From this study, a decreasein release kinetics of the drug was observed when the polymer concentration was increased. Kinetic modeling of invitro dissolution profiles revealed the drug release mechanism ranges from diffusion controlled or Fickian transport toanomalous type or non-Fickian transport, which was only dependent on the type and amount of polymer used. Thedrug release followed both diffusion and erosion mechanism in all cases. The drug release from these formulationswas satisfactory after 3 months storage in 40°C and 75% RH. Besides, this study explored the optimum concentrationand effect of polymer(s) on acelofenac release pattern from the tablet matrix for 24 hour period.Key words: Aceclofenac; sustained release; hydrophillic matrix; HPMC; direct compression.DOI: 10.3329/dujps.v8i1.5332Dhaka Univ. J. Pharm. Sci. 8(1): 23-30, 2009 (June)

Design, in vitro and in vivo Evaluation of Gemifloxacin Mesylate Floating Matrix Tablets

1970 ◽  
Vol 9 (1) ◽  
pp. 3143-3149
Author(s):  
Sushma Appala ◽  
Ramesh Bomma ◽  
Kishan Veerabrahma
Keyword(s):  
Helicobacter Pylori ◽  
Drug Release ◽  
Lag Time ◽  
Matrix Tablets ◽  
In Vivo Evaluation ◽  
In Vitro Drug Release ◽  
Weight Variation ◽  
Gastro Retentive

Objective of the investigation was to develop gastro retentive dosage form of gemifloxacin mesylate for local action in the stomach as it has antibacterial activity against Helicobacter pylori. Gemifloxacin mesylate is a synthetic broad-spectrum antibacterial agent for oral administration, having 7 hrs half-life and 71% oral bioavailability. In present study, gemifloxacin mesylate floating matrix tablets were prepared by direct compression method using polymers (HPMC K4M, HPMC K15M and polyox WSR 1105) and evaluated for various parameters like drug content, floating behavior (floating lag time and total floating time), in vitro drug release, swelling index, weight variation, friability, hardness and thickness. Sodium bicarbonate was incorporated as gas generating agent in all formulations. Drug-excipients compatibility was studied by Differential Scanning Calorimetry. Results have shown that the amount of polymer in the formulation affected the drug release. Optimized formulation (F8 containing polyox WSR1105 as release retarding agent) was selected based on in vitro drug release, floating lag time, floating time and other parameters. This formulation followed zero order kinetics and non-Fickian mechanism of drug release. In vivo radiographic study was conducted in healthy human volunteers using tablets containing BaSO4 as radio opaque agent. The average residence time was found to be 4.5± 0.86 h (n=3). This design of gastro retentive drug delivery system helps in increasing the local delivery of drug in patients with Helicobacter pylori infection

Formulation and in vitro Evaluation of Matrix tablets containing Repaglinide

2021 ◽  
pp. 4429-4434
Author(s):  
C.C. Patil ◽  
J. Vekatesh ◽  
S. R Karajgi ◽  
Vijapure Vitthal ◽  
Ashwini G. ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Fourier Transforms ◽  
Methyl Cellulose ◽  
Matrix Tablets ◽  
Differential Scanning Calorimetric ◽  
Content Uniformity ◽  
Drug Content ◽  
Weight Variation

The aim of this project was to develop sustained release matrix tablets of Repaglinide. Sustained release matrix tablets of Repaglinide were prepared by the wet granulation method using polymers like Hydroxy propyl methyl cellulose, Microcrystalline cellulose, Eudragit RS-100 in different ratios. The matrix tablets of Repaglinide were evaluated for hardness, weight variation, friability, drug content uniformity, and in-vitro drug release. In order to determine the drug release mechanisms and kinetics, the data was subjected to zero order, first order, and higuchi and peppas diffusion model. Twelve batches of sustained release matrix tablets of Repaglinide were developed. Among these formulations F4, F8 and F12 formulation showed satisfactory physicochemical properties and drug content uniformity and sustained release of drug for 12 hours with maximum release of 86.95%, 84.91% and 84.91%. The optimized formulations were characterized for Differential scanning calorimetric analysis; Fourier transforms infrared spectroscopy and scanning electron microscopic studies. IR spectroscopic studies indicated that there were no drug-excipient interactions. The prepared sustained release matrix tablets of Repaglinide were successfully developed and evaluated.

scholarly journals Formulation and Evaluation of Bilayer Matrix Tablets of Nebivolol Hydrochloride and Valsartan

2019 ◽  
Vol 9 (4-s) ◽  
pp. 82-93
Author(s):  
Selvi Arunkumar ◽  
L. Srinivas ◽  
D. Satyavati ◽  
C. Emmanuel
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Immediate Release ◽  
Matrix Tablets ◽  
Pharmacokinetic Studies ◽  
Drug Content ◽  
Bilayer Tablets ◽  
Nebivolol Hydrochloride

The present study is an attempt to develop bilayer matrix tablets of Nebivolol Hydrochloride and Valsartan with immediate release for Nebivolol Hydrochloride and sustained release for Valsartan. Superdisintegrants such as sodium starch glycolate and Crosscarmellose sodium were evaluated for immediate release of Nebivolol Hydrochloride and polymers HPMC K100M and K4M for sustained release of Valsartan. Preformulation studies were performed prior to compression. The compressed bilayer tablets were evaluated for weight variation, thickness, hardness, friability, drug content and in vitro drug release using USP dissolution apparatus type 2 in 0.01N HCl and phosphate buffer pH 6.8. All the pre and post compression parameters were found to be within the acceptable limits. The results of dissolution show that the formulations B3 was the best of all immediate and sustained release layer batches. The release kinetics of Valsartan was subject to curve fitting analysis in order to identify the best fit kinetic model. The regression analysis proves that the best formulations follow zero order release and drug release by diffusion process based on Fick’s law of diffusion. The data for stability studies infer no considerable change in drug content and dissolution rates as per ICH guidelines. The best formulation B3 was subjected to in vivo pharmacokinetic studies in rabbit model. In vitro, In vivo correlation (IVIVC) showed considerable linearity. Hence a novel bilayer tablet formulation of Nebivolol Hydrochloride and Valsartan was successfully developed by combining both immediate (IR) and sustained (SR) release layers. Keywords: Bilayer tablets, fixed unit dosage form, Nebivolol hydrochloride, Valsartan, LC-MS analysis.

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