scholarly journals Formulation and In vitro Evaluation of Oral Floating Tablets of Salbutamol Sulphate: Comparison with Effervescent Tablets

2017 ◽  
Vol 15 (2) ◽  
pp. 203-208
Author(s):  
Md Haider Ali ◽  
Mohiuddin Ahmed Bhuiyan ◽  
Md Selim Reza ◽  
Samira Karim
Keyword(s):  
Drug Release ◽  
Oral Delivery ◽  
Dosage Form ◽  
In Vitro Dissolution ◽  
Salbutamol Sulphate ◽  
Floating Tablets ◽  
Gastric Residence Time ◽  
Usp Apparatus ◽  
Usp Apparatus 2

The aim of this research was to develop and evaluate gastric floating tablets of salbutamol sulphate. The oral delivery of anti-asthmatic salbutamol sulphate tablets were facilitated by preparing floating dosage form which could increase its absorption in the stomach by increasing the gastric residence time of the drug. Floating tablets were formulated by using different polymers like carbopol, xanthan gum, HPMC-K4 MCR and HPMC- K100 MCR with different proportions. A comparative study of normal effervescent tablets of salbutamol sulphate had also been done. The prepared tablets were evaluated for all their physicochemical properties and in vitro buoyancy study. In vitro dissolution studies of the formulations were done in pH 6.8 phosphate buffer using USP apparatus 2 (paddle method) at 50 rpm. Percent drug release of the formulations (F-1 to F-11) was from 87.34%- 99.12% after 12 hours. From the results, F-11 was selected as an optimized formulation based on 12 h drug release which showed minimal floating lag time and maximum floating time. On the other hand, 100% drug was released within 2 hours from the F-12 of effervescent salbutamol sulphate tablets in which polymer was absent while gas generating sodium bicarbonate and citric acid were present. The results of the study were consistent and may encourage formulating similar dosage form with other drugs.Dhaka Univ. J. Pharm. Sci. 15(2): 203-208, 2016 (December)

scholarly journals Release Modification of Indomethacin Controlled Release Press Coated Tablets

2016 ◽  
Vol 19 (2) ◽  
pp. 219-225 ◽  
Author(s):  
Muhammad Rashedul Islam ◽  
Md Elias Al Mamun ◽  
Md Mizanur Rahman Moghal
Keyword(s):  
Drug Release ◽  
Pharmaceutical Journal ◽  
In Vitro Dissolution ◽  
Compression Pressure ◽  
Pressure Formulation ◽  
Release Data ◽  
Usp Apparatus ◽  
Usp Apparatus 2 ◽  
Core Tablet

The study was carried out to evaluate the release modification of indomethacin press coated tablets through different polymers. Several batches of press coated tablets were prepared with indomethacin and Avicel PH 102. The core tablet was compression coated with minimal compression pressure. Formulation IX was modified by incorporating PEG 6000, sodium chloride and sodium lauryl sulphate (SLS). In vitro dissolution studies of the formulations of different excipients were done at pH 7.2 in phosphate buffer using USP apparatus 2 (paddle method) at 50 rpm and 37 ± 0.5 °C temperature. The drug release data was treated in different mathematical fashion to identify the kinetic behaviour. It was found that, drug release which was inversely proportional to the amount of xanthan gum in the coating formulations was significantly changed by the polymers used in the study. Incorporation of SLS caused the drug to be released in near zero order fashion. Drug release was found to follow Higuchi mechanism for all the formulations. The study reveals that the polymers used may be a significant factor for the discrepancy in release rate of indomethacin.Bangladesh Pharmaceutical Journal 19(2): 219-225, 2016

scholarly journals DEVELOPMENT AND IN VITRO–IN VIVO EVALUATION OF GASTRORETENTIVE FLOATING TABLETS OF AN ANTIRETROVIRAL AGENT RITONAVIR

2019 ◽  
pp. 436-443
Author(s):  
SHIREESH KIRAN R ◽  
CHANDRA SHEKAR B ◽  
NAGENDRA BABU B
Keyword(s):  
Drug Release ◽  
Residence Time ◽  
Extended Release ◽  
In Vitro Dissolution ◽  
Floating Tablets ◽  
Gastric Residence Time ◽  
Dissolution Studies ◽  
Evaluation Parameters

Objective: The present research work concerns the development of the extended release of Ritonavir floating matrix tablets, designed to prolong the gastric residence time, increase the drug bioavailability, and diminish the side effects of irritating drugs. Methods: The floating tablets of Ritonavir were prepared by direct compression method using different grades of hydroxypropyl methylcellulose (HPMC), crospovidone, Polyox WSR 303, and sodium bicarbonate, as gas generating agent. Evaluation parameters and in vivo radiographic studies were conducted in suitable model. Results: Among all formulations, F21 was chosen as optimized formulation based on evaluation parameters such as floating lag time (33 s), total floating time (>24 h), and in vitro dissolution studies. From in vitro dissolution studies, the optimized formulation F21 and marketed product were shown 98.67% and 91.46±5.02% of drug release, respectively. The main appliance of medication discharge follows zero-order kinetics and non- Fickian transport by coupled diffusion and erosion. In vivo experiments maintained the potentials in extending the gastric residence time in the fasted state in beagle dogs. The mean gastric residence time of the optimized formulation found to be 330 min±40 in the stomach, where longer gastric residence time is an important condition for prolonged or controlled drug release and also for enhanced bioavailability. Conclusion: From in vitro and in vivo radiographic studies, Ritonavir floating tablets estimated to provide novel choice for harmless, inexpensive, and extended release for the effective management of AIDS.

scholarly journals Dissolution Test for Mianserin Hydrochloride in Tablets

2019 ◽  
Vol 3 (2) ◽  
pp. 18-22
Author(s):  
Letícia Lenz Sfair ◽  
Caren Gobetti ◽  
Martin Steppe ◽  
Elfrides Schapoval
Keyword(s):  
Drug Release ◽  
In Vitro Dissolution ◽  
Dissolution Test ◽  
Dissolution Medium ◽  
Drug Release Profile ◽  
Dissolution Tests ◽  
Usp Apparatus ◽  
Usp Apparatus 2

A dissolution test for mianserin hydrochloride in coated tablets containing 30 mg was developed and validated using a fast ultraviolet spectrophotometric method. The appropriate conditions were determinate after testing sink conditions, agitation spped and dissolution medium. The sink conditions tested showed that mianserin hydrochloride was soluble in 0.01 and 0.1 M hydrochloric acid (HCl), acetate buffer pH 4.1 and 5.0 and phosphate buffer pH 6.8. Then, dissolution tests were performed to investigate the drug release in each medium. Optimal conditions to carry out the dissolution test were 900 mL 0.1 M HCl and USP apparatus 2 (paddle) at 50 rpm stirring speed. The quantification method was also adapted and validated. The UV method showed specificity, linearity, precision and accuracy. The in vitro dissolution test can be used to evaluate the drug release profile and the data was used as an aid to establish a possible correlation with in vivo data.

scholarly journals Formulation and evaluation of effervescent floating tablets of tizanidine hydrochloride

2011 ◽  
Vol 61 (2) ◽  
pp. 217-226 ◽  
Author(s):  
Komuravelly Someshwar ◽  
Kalyani Chithaluru ◽  
Tadikonda Ramarao ◽  
K. Kumar
Keyword(s):  
Drug Release ◽  
Residence Time ◽  
Release Kinetics ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
Physical Parameters ◽  
Floating Tablets ◽  
Gastric Residence Time

Formulation and evaluation of effervescent floating tablets of tizanidine hydrochloride Tizanidine hydrochloride is an orally administered prokinetic agent that facilitates or restores motility through-out the length of the gastrointestinal tract. The objective of the present investigation was to develop effervescent floating matrix tablets of tizanidine hydrochloride for prolongation of gastric residence time in order to overcome its low bioavailability (34-40 %) and short biological half life (4.2 h). Tablets were prepared by the direct compression method, using different viscosity grades of hydroxypropyl methylcellulose (HPMC K4M, K15M and K100M). Tablets were evaluated for various physical parameters and floating properties. Further, tablets were studied for in vitro drug release characteristics in 12 hours. Drug release from effervescent floating matrix tablets was sustained over 12 h with buoyant properties. DSC study revealed that there is no drug excipient interaction. Based on the release kinetics, all formulations best fitted the Higuchi, first-order model and non-Fickian as the mechanism of drug release. Optimized formulation (F9) was selected based on the similarity factor (f2) (74.2), dissolution efficiency at 2, 6 and 8 h, and t50 (5.4 h) and was used in radiographic studies by incorporating BaSO4. In vivo X-ray studies in human volunteers showed that the mean gastric residence time was 6.2 ± 0.2 h.

scholarly journals FORMULATION AND EVALUATION OF GASTRORETENTIVE TABLETS OF ANTIULCER DRUG

2016 ◽  
Vol 9 (6) ◽  
pp. 48
Author(s):  
Pranali Shivaji Salunkhe
Keyword(s):  
Drug Release ◽  
Extended Period ◽  
Lag Time ◽  
In Vitro Dissolution ◽  
Content Uniformity ◽  
In Vitro Drug Release ◽  
Gastric Residence Time ◽  
Target Drug ◽  
Weight Variation

ABSTRACTGastroretentive floating drug delivery system is utilised to target drug release in the stomach or to the upper part of intestine. Lansoprazole is proton pump inhibitor intended for oral administration used as antiulcer agent. The present investigation involved formulation and evaluation of Gastroretentive floating tablets of Lansoprazole for prolongation of gastric residence time with a view to deliver the drug at sustained and controlled manner in gastrointestinal tract. The tablets of Lansoprazole were prepared by direct compression method using gas generating agent and different polymer combinations (HPMCK4M, HPMC K100M, Psyllium husk) . The prepared tablets of Lansoprazole were evaluated for hardness, thickness, friability, weight variation, drug content uniformity, buoyancy lag time, total floating time, swelling index, in-vitro dissolution study. The varying concentration of gas generating agent and polymers were found to affect on in-vitro drug release, floating lag time and swelling index. In vitro drug release of floating Gastroretentive tablet of Lansoprazole shown that the formulation F2 was found to be the best formulation as it releases 97.9% Lansoprazole in a controlled manner for extended period of time (upto 12 hrs.)Keywords: Lansoprazole, Gastroretentive, floating tablet, total floating time.

scholarly journals Formulation and Pharmacokinetic Evaluation of Ritonavir Floating Tablets in the Management of AIDS

2018 ◽  
Vol 10 (6) ◽  
Author(s):  
R. Shireesh Kiran ◽  
B. Chandra Shekar ◽  
B. Nagendra Babu
Keyword(s):  
Drug Release ◽  
Sodium Bicarbonate ◽  
Controlled Drug Release ◽  
In Vitro Dissolution ◽  
Gastric Residence Time ◽  
Dissolution Studies ◽  
Floating Tablet ◽  
Gastro Retentive

In the current study, gastro-retentive tablets of Ritonavir was developed to increase its oral bioavailability using hydrophilic polymers HPMC K 4M, K 15M, and K 100M as release retarding agents. Polyox WSR 303 was chosen as resin, sodium bicarbonate was used as effervescent agents. The tablets were prepared by direct compression method and FTIR studies revealed that there is no interaction between the drug and polymers used for the formulation. Among all the formulations F21 containing HPMC K 100M, Crospovidone, Polyox WSR 303 and sodium bicarbonate, as gas generating agent was choosen as optimized formulation based on the evaluation parameters, floating lag time (33 sec) and total floating time (>24 h) and in vitro dissolution studies. From in vitro dissolution studies, the optimized formulation F21 and marketed product was shown 98.67% and 95.09 ± 5.01% of drug release respectively. From in vivo bioavailability studies, after oral administration of floating tablet containing 100 mg Ritonavir, the Cmax, Tmax, and AUC0–∞ of optimized gastroretentive formulation were found to be 30.11 ± 1.16μg/mL, 8.00±1.23 h and 173 ± 26.34μg*h/ml, respectively. Cmax and AUC values of optimized formulation were found to be significantly higher than of marketed product, where longer gastric residence time is an important condition for prolonged or controlled drug release and also for improved bioavailability.

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 DESIGN EXPERT SUPPORTED FORMULATION DEVELOPMENT, MATHEMATICAL OPTIMIZATION AND PREDICTABILITY STUDY OF FLOATING TABLETS OF BISOPROLOL FUMARATE

2021 ◽  
pp. 242-248
Author(s):  
SHAIKH SHAOOR AHMAD ◽  
SHAIKH SIRAJ N. ◽  
PATEL M. SIDDIK ◽  
KHALIFA MAHMADASIF YUNUS ◽  
MAKRANI SHAHARUKH I. ◽  
...  
Keyword(s):  
Drug Release ◽  
Scale Up ◽  
Mathematical Optimization ◽  
Lag Time ◽  
Stability Study ◽  
In Vitro Dissolution ◽  
Formulation Development ◽  
Floating Tablets ◽  
Design Expert

Objective: Focus of the study was to formulate Design expert Software assisted floating tablet of Bisoprolol Fumarate. Bisoprolol Fumarate is a Beta adrenergic blocking agent, used to treat cardiac diseases favorable characters to be formulated as sustained release Gastro retentive floating tablets. Methods: Floating Tablets of Bisoprolol Fumarate were prepared by using polymers such as Polyox N 12 K and Carbapol 940 P. Formulations were prepared by using direct compression method and evaluated for various parameters like Hradness, thickness, weight variations, Floating lag time Total floating time,% drug release and Stability Study etc. Results: FTIR spectroscopic study indicates no drug-excipients interaction in the prepared formulations. Hardness or crushing strength of the tablets of all the formulation was found between 5.8 and 6.5 kg/cm2. Floating lag time of all batches is in range of 1.18±2.0 to 2.43±1.6 (minutes). All other parameters of all batches are within an acceptable range. The polymer Carbopol 940 P had the significant negative effect of on the floating lag times. The In vitro dissolution profiles of optimized A3 Floating formulation of Bisoprolol Fumarate were found to sustain drug release 99.25 % up to 12 h with floating lag time of 1.45 min; Designed formulation was stable after Stability study. Optimization study was carried out by using 32 factorial designs to fabricate formulations. Conclusion: It can be conclude that reproducible results of various parameters in this developed formulation can easily scale up. Furthermore designed formulation will be very effective for controlling blood pressure.

Development of Multiple-Unit Floating Drug Delivery System of Clarithromycin: Formulation, in vitro Dissolution by Modified Dissolution Apparatus, in vivo Radiographic Studies in Human Volunteers

Drug Research ◽  
2017 ◽  
Vol 67 (07) ◽  
pp. 412-418 ◽  
Author(s):  
Arun Reddy ◽  
Narendar Reddy
Keyword(s):  
Drug Release ◽  
Residence Time ◽  
Release Kinetics ◽  
In Vitro Dissolution ◽  
Physical Parameters ◽  
Gastric Residence Time ◽  
Human Volunteers ◽  
Multiple Unit

AbstractClarithromycin (CM), a broad spectrum macrolide antibiotic used to eradicate H. pylori in peptic ulcer. Clarithromycin (CM) is well absorbed from the gastrointestinal tract, but has a bioavailability of 50% due to rapid biodegradation. The aim of this investigation was to increase the gastric residence time, and to control the drug release of clarithromycin by formulating into multiple unit floating mini-tablets. Floating tablets were prepared by using direct compression method with HPMC K4M and Polyox WSR 1105 as release retarded polymers and sodium bicarbonate as gas generating agent. The prepared mini-tablets were evaluated for thickness, weight variation, friability, hardness, drug content, in vitro buoyancy, swelling studies, in vitro dissolution studies by using modified Rossett-Rice test and in vivo radiographic studies in healthy human volunteers in fasting conditions. DSC analysis revealed that no interaction between drug and excipients. All the physical parameters of the tablets were within the acceptable limits. The optimized formulation (F6) had showed controlled drug release of 99.16±3.22% in 12 h, by zero-order release kinetics, along with floating lag time of 9.5±1.28 s and total floating time of 12±0.14 h. X-ray imaging studies revealed that in vivo gastric residence time of clarithromycin floating mini-tablet in the stomach was about 3.5 h. The results demonstrated that the developed floating mini-tablets of clarithromycin caused significant enhancement in gastric retention time along with sustained effect and increased oral bioavailability.

scholarly journals Double-layer Tablets of Lornoxicam: Validation of Quantification Method, In vitro Dissolution and Kinetic Modelling

2015 ◽  
Vol 14 (9) ◽  
pp. 1659-1666
Author(s):  
Ü Gönüllü ◽  
P Gürpınar ◽  
M Üner
Keyword(s):  
Drug Release ◽  
Double Layer ◽  
Oral Delivery ◽  
Kinetic Modelling ◽  
Uv Spectroscopy ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Dissolution ◽  
Disintegration Time ◽  
Weight Variation

Purpose: To formulate double-layer tablets of lornoxicam (LRX) prepared by direct compression method and evaluate their physical and drug release  characteristics.Methods: The outer layer of tablets, composed of microcrystalline cellulose (MCC), starch and lactose, incorporated tan initial or prompt dose of the drug (4 mg) for immediate release. Hydroxypropyl methylcellulose (HPMC), polyvinylpyrrolidone (PVP K90) and carbomer, in varying concentrations, were used to prepare the tablet cores for sustained drug delivery. Weight variation, dimensions, hardness,  tensile strength, friability and disintegration time of the tablets were evaluated. Drug release from double-layer tablets as well as kinetic models of drug release were determined after validating the method used for the quantification of the drug. The analytical method for quantification of LRX by UV spectroscopy was validated and verified for linearity, intra-day and inter-day precision, accuracy, recovery and specifity.Results: Tablet cores based on HPMC and HPMC:PVP K90 mixture displayed better compression and flow properties (good and fair to passable) than those  formulated with PVP K90 and carbomer (poor). Satisfactory results were obtained from all the tablet formulations met compendial requirements. The slowest drug release rate was obtained with tablet cores based on PVP K90 (1.21 mg%.h-1). Drug release followed Higuchi kinetic model and the tablet cores released drug by diffusion/polymer relaxation or diffusion/erosion.Conclusion: Double-layer tablet formulation of lornoxicam based on HPMC or HPMC-PVP mixture is suitable for the treatment of inflammatory and painful conditions.Keywords: Lornoxicam, Controlled release, Double-layer tablets, Non-steroidal antiinflammatory drug, Oral delivery

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