A Novel Pulsatile Release Film Coated Tablet of Zaltoprofen Loaded SNEDDS

2021 ◽  
pp. 4287-4290
Author(s):  
Rajan Kalamkar ◽  
Shailesh Wadher ◽  
Ashish Jain
Keyword(s):  
Rheumatoid Arthritis ◽  
Ethyl Cellulose ◽  
Lag Time ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Pulsatile Release ◽  
Eudragit L100 ◽  
Coated Tablet ◽  
Fast Disintegrating Tablet

The aim of the present study was to formulate pulsatile release film coated tablet of zaltoprofen for the treatment of rheumatoid arthritis. Initially solubility of zaltoprofen was enhanced by formulating self emulsifying fast disintegrating tablet of zaltoprofen. Core fast disintegrating tablet of zaltoprofen was coated with ethyl cellulose and eudragit L100 in various proportions as coating polymer. Ethanol was used as coating solvent and dibutyl phthalate as plasticizer. Film coated tablet with different coating levels were formulated and were evaluated for parameters like lag time, rupture time, in vitro dissolution etc. Amongst the nine different formulations P-4 formulation containing 3:1 ratio of ethyl cellulose and eudragit L100 with 5% coating level gives desired lag time with best drug dissolution profile. Formulated film coated tablet of zaltoprofen can be useful for chronotherapeutic treatment of rheumatoid arthritis.

scholarly journals In Silico Prediction of Plasma Concentrations of Fluconazole Capsules with Different Dissolution Profiles and Bioequivalence Study Using Population Simulation

Pharmaceutics ◽  
2019 ◽  
Vol 11 (5) ◽  
pp. 215 ◽  
Author(s):  
Marcelo Dutra Duque ◽  
Daniela Amaral Silva ◽  
Michele Georges Issa ◽  
Valentina Porta ◽  
Raimar Löbenberg ◽  
...  
Keyword(s):  
Reference Product ◽  
Plasma Concentrations ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Dissolution Behavior ◽  
Dissolution Profile ◽  
Time Data ◽  
Simulation Results ◽  
Population Simulation

A biowaiver is accepted by the Brazilian Health Surveillance Agency (ANVISA) for immediate-release solid oral products containing Biopharmaceutics Classification System (BCS) class I drugs showing rapid drug dissolution. This study aimed to simulate plasma concentrations of fluconazole capsules with different dissolution profiles and run population simulation to evaluate their bioequivalence. The dissolution profiles of two batches of the reference product Zoltec® 150 mg capsules, A1 and A2, and two batches of other products (B1 and B2; C1 and C2), as well as plasma concentration–time data of the reference product from the literature, were used for the simulations. Although products C1 and C2 had drug dissolutions < 85% in 30 min at 0.1 M HCl, simulation results demonstrated that these products would show the same in vivo performance as products A1, A2, B1, and B2. Population simulation results of the ln-transformed 90% confidence interval for the ratio of Cmax and AUC0–t values for all products were within the 80–125% interval, showing to be bioequivalent. Thus, even though the in vitro dissolution behavior of products C1 and C2 was not equivalent to a rapid dissolution profile, the computer simulations proved to be an important tool to show the possibility of bioequivalence for these products.

scholarly journals FORMULATION AND IN VITRO EVALUATION OF SALBUTAMOL SULPHATE AND THEOPHYLLINE EXTENDED-RELEASE TABLETS USING MODIFIED POLYMERS

2018 ◽  
Vol 10 (8) ◽  
pp. 67
Author(s):  
Naveen Goyal ◽  
Anil Kumar
Keyword(s):  
Ethyl Cellulose ◽  
Extended Release ◽  
Research Work ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Direct Compression ◽  
Compression Method ◽  
Salbutamol Sulphate ◽  
Modified Polymers

Objective: The main objective of this research work was to design, prepare and evaluate extended release (ER) tablets of anti-asthmatic drugs (salbutamol sulphate and theophylline) by direct compression method using diverse ratios of hydroxypropyl methylcellulose (HPMC K100M) and ethyl cellulose (EC) along with some other excipients.Methods: Extended-release matrix tablets of salbutamol sulphate and theophylline were successfully fabricated by direct compression method and coded the formulations as F1 to F7 depending on the ratios of modified polymers. The core tablets composed of hydrophilic polymers of various ratios that allow the discharge of drugs at a controlled rate after coming in contact with the aqueous medium. The designed tablets were subjected to various assessment parameters i.e. friability test, hardness test, drug content consistency and In vitro dissolution tests.Results: Prepared formulations were subjected to various assessment parameters and the findings obtained were within the prescribed limit. To perform the in vitro drug dissolution tests of fabricated tablets, the calibration plots of pure drugs using various solvents i.e. 0.1N HCl, phosphate buffer (pH 6.8) and distilled water were plotted. Dosage forms F1-F7 containing ethyl cellulose and HPMC K100M in various concentration demonstrates the prolonged medications discharge for up to 8 h, among these formulations, F6 shows 95.32±0.24 % for salbutamol sulphate and 94.19±0.39 % for theophylline release at the end of 8 h. This finding reveals that a particular window of concentrations of ethylcellulose and HPMC K100M was capable of providing prolonged drugs discharge.Conclusion: The results obtained in this research work clearly showed a promising potential of extended-release tablets containing a specific ratio of HPMC K100M and ethylcellulose as a release rate controlling polymers for effective treatment of asthma and chronic obstructive pulmonary diseases (COPD).

Effect of viscosity of hydrophilic coating polymer on lag time of atenolol pulsatile press coated tablets

2014 ◽  
Vol 1 (1) ◽  
pp. 15 ◽  
Author(s):  
Rajesh A Keraliya ◽  
Madhabhai M Patel
Keyword(s):  
Drug Delivery ◽  
Lag Time ◽  
Burst Release ◽  
Pulsatile Release ◽  
Hydrophilic Coating ◽  
Coated Tablet ◽  
Viscosity Grade ◽  
Pulsatile Drug Delivery ◽  
Pulsatile Delivery ◽  
Core Tablet

A method for the development of press coated tablet of atenolol for pulsatile delivery was investigated for chronotherapy of hypertension. Effect of viscosity of Hydroxypropylcellulose (HPC) on pulsatile release of atenlol was studied by press coating atenolol core tablet using different viscosity grade HPC and varying coat weight. L-HPC, M-HPC and H-HPC viscosity garde with 75, 100 and 150 mg coat weight were press coated over atenolol core tablets to delay release of atenolol. The batches, HP1-HP9, exhibited an increase in lag time in response to increase in viscosity and coat weight. Two of the batches HP5 and HP7 have shown a burst release of atenolol after 6.5 and 6.0 h lag time respectively, which is suitable for pulsatile drug delivery of atenolol for chronotherapy of hypertension.

scholarly journals Optimization and Prediction of Ibuprofen Release from 3D DLP Printlets Using Artificial Neural Networks

Pharmaceutics ◽  
2019 ◽  
Vol 11 (10) ◽  
pp. 544 ◽  
Author(s):  
Madzarevic ◽  
Medarevic ◽  
Vulovic ◽  
Sustersic ◽  
Djuris ◽  
...  
Keyword(s):  
Neural Network ◽  
Neural Networks ◽  
Polyethylene Glycol ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Polyethylene Glycol Diacrylate ◽  
Glycol Diacrylate ◽  
Artificial Neural

The aim of this work was to investigate effects of the formulation factors on tablet printability as well as to optimize and predict extended drug release from cross-linked polymeric ibuprofen printlets using an artificial neural network (ANN). Printlets were printed using digital light processing (DLP) technology from formulations containing polyethylene glycol diacrylate, polyethylene glycol, and water in concentrations according to D-optimal mixture design and 0.1% w/w riboflavin and 5% w/w ibuprofen. It was observed that with higher water content longer exposure time was required for successful printing. For understanding the effects of excipients and printing parameters on drug dissolution rate in DLP printlets two different neural networks were developed with using two commercially available softwares. After comparison of experimental and predicted values of in vitro dissolution at the corresponding time points for optimized formulation, the R2 experimental vs. predicted value was 0.9811 (neural network 1) and 0.9960 (neural network 2). According to difference f1 and similarity factor f2 (f1 = 14.30 and f2 = 52.15) neural network 1 with supervised multilayer perceptron, backpropagation algorithm, and linear activation function gave a similar dissolution profile to obtained experimental results, indicating that adequate ANN is able to set out an input–output relationship in DLP printing of pharmaceutics.

scholarly journals Systematic Development of Self-Nanoemulsifying Liquisolid Tablets to Improve the Dissolution and Oral Bioavailability of an Oily Drug, Vitamin K1

Pharmaceutics ◽  
2018 ◽  
Vol 10 (3) ◽  
pp. 96 ◽  
Author(s):  
Yongtao Tong ◽  
Yuli Wang ◽  
Meiyan Yang ◽  
Jiahui Yang ◽  
Lu Chen ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Soybean Lecithin ◽  
Area Under The Curve ◽  
Relative Bioavailability ◽  
Combination Method ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Vitamin K1

The purpose of this study is to improve the dissolution and oral bioavailability of an oily drug, vitamin K1 (VK1) by combination of self-nanoemulsifying and liquisolid technologies. The optimal liquid self-nanoemulsifying drug delivery systems (SNEDDS) formulation including VK1 (oil), mixture of soybean lecithin and glycocholic acid (surfactant) and Transcutol HP (cosurfactant) was obtained according to ternary phase diagrams and a central composite design. Based on compatibility, adsorption capacity and dissolution profile, liquid SNEDDS was then solidified on Fujicalin® to form solid SNEDDS by liquisolid technology and compressed directly with excipients into self-nanoemulsifying liquisolid (SNE-L) tablets. Uniform nano-emulsion suspension was formed rapidly when the SNE-L tablets disintegrated in dissolution media and higher drug dissolution was observed compared with the conventional tablets. The results of pharmacokinetic study in beagle dogs showed that the mean Cmax and the area under the curve of SNE-L tablets were remarkably higher than those of conventional tablets, which were consistent with the results of the in vitro dissolution. The relative bioavailability of SNE-L tablets and conventional tablets was approximately 200%. In conclusion, this combination method showed promise to improve the dissolution and oral bioavailability of oily drug vitamin K1.

Development and Evaluation of Floating Pulsatile Drug Delivery System Using Meloxicam

2017 ◽  
Vol 7 (04) ◽  
Author(s):  
ShirishaG. Suddala ◽  
S. K. Sahoo ◽  
M. R. Yamsani
Keyword(s):  
Rheumatoid Arthritis ◽  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Lag Time ◽  
Oral Dosage ◽  
Lag Phase ◽  
Pulsatile Drug Delivery

Objective: The objective of this research work was to develop and evaluate the floating– pulsatile drug delivery system (FPDDS) of meloxicam intended for Chrono pharmacotherapy of rheumatoid arthritis. Methods: The system consisting of drug containing core, coated with hydrophilic erodible polymer, which is responsible for a lag phase for pulsatile release, top cover buoyant layer was prepared with HPMC K4M and sodium bicarbonate, provides buoyancy to increase retention of the oral dosage form in the stomach. Meloxicam is a COX-2 inhibitor used to treat joint diseases such as osteoarthritis and rheumatoid arthritis. For rheumatoid arthritis Chrono pharmacotherapy has been recommended to ensure that the highest blood levels of the drug coincide with peak pain and stiffness. Result and discussion: The prepared tablets were characterized and found to exhibit satisfactory physico-chemical characteristics. Hence, the main objective of present work is to formulate FPDDS of meloxicam in order to achieve drug release after pre-determined lag phase. Developed formulations were evaluated for in vitro drug release studies, water uptake and erosion studies, floating behaviour and in vivo radiology studies. Results showed that a certain lag time before drug release which was due to the erosion of the hydrophilic erodible polymer. The lag time clearly depends on the type and amount of hydrophilic polymer which was applied on the inner cores. Floating time and floating lag time was controlled by quantity and composition of buoyant layer. In vivo radiology studies point out the capability of the system of longer residence time of the tablets in the gastric region and releasing the drug after a programmed lag time. Conclusion: The optimized formulation of the developed system provided a lag phase while showing the gastroretension followed by pulsatile drug release that would be beneficial for chronotherapy of rheumatoid arthritis and osteoarthritis.

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.

PERILAKU DISOLUSI KETOPROFEN DAN INDOMETASIN FARNESIL TERSALUT GEL KITOSAN-GOM GUAR

2012 ◽  
Vol 12 (1) ◽  
Author(s):  
Purwantiningsih Sugita ◽  
Bambang Srijanto ◽  
Budi Arifin ◽  
Fithri Amelia ◽  
Mahdi Mubarok
Keyword(s):  
Room Temperature ◽  
Guar Gum ◽  
Tween 80 ◽  
Chitosan Solution ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Magnetic Stirrer ◽  
Dissolution Behaviour ◽  
Shrimp Shell Waste

Chitosan, a modification of shrimp-shell waste, has been utilized as microcapsule. However, it’s fragile gel property needs to be strengthened by adding glutaraldehyde (glu) and natural hydrocolloid guar gum (gg). This research’s purposes were to study dissolution behaviour of ketoprofen and infar through optimum chitosan-guar gum microcapsule. Into 228.6 mL of 1.75% (w/v) chitosan solution in 1% (v/v) acetic acid,38.1 mL of gg solution was added with concentration variation of 0.35, 0.55, and 0.75% (w/v) for ketoprofen microcapsules and 0.05, 0.19, and 0.33% (w/v) for infar microcapsules, and stirred with magnetic stirrer until homogenous. Afterwards, 7.62mL of glu was added slowly under stirring, with concentrations varied: 3, 3.5, and 4% (v/v) for ketoprofen microcapsules, and 4, 4.5, and 5% (v/v) for infar microcapsules. All mixtures were shaked for 20 minutes for homogenization. All mixtures wereshaked for 20 minutes for homogenization. Into each  microcapsule mixture for ketoprofen, a solution of 2 g of ketoprofen in 250 mL of 96% ethanol was added, whereas solution of 100 mg of in 250 mL of 96% ethanol was added into each microcapsule mixture for infar. Every mixture was then added with 5 mL of 2% Tween-80 and stirred with magnetic stirrer for an hour at room temperature. Everymixture was then added with 5 mL of 2% Tween-80 and stirred with magnetic stirrer for an hour at room temperature. Conversion of suspension into fine powders/granules (microcapsules) was done by using spray dryer. The data of [gg], [glu], and medicine’s content from each microcapsule were treated with Minitab 14 software to obtain optimum [gg] and [glu] for microencapsulation. The dissolution behaviour of optimum ketoprofen and infar microcapsules were investigated. The result of optimization by using Minitab Release 14 software showed that among the microcapsule compositions of [gg] and [glu] were 0.35% (w/v) and 3.75% (v/v), respectively, optimum to coat ketoprofen, whereas [gg] and [glu] of 0.05% (w/v) and4.00% (v/v), respectively, optimum to coat infar, at constant chitosan concentration (1.75% [w/v]). In vitro dissolution profile showed that chitosan-guar gum gel microcapsule was more resistant in intestinal pH condition (rather basic) compared with that in gastric pH (very acidic).

The Effect of Different Superdisintegrants and their Concentrations on the Dissolution of Topiramate Immediate Release Tablets

2009 ◽  
Vol 2 (2) ◽  
pp. 531-5366
Author(s):  
V A. Vamshi Priya ◽  
G. Chandra Sekhara Rao ◽  
D. Srinivas Reddy ◽  
V. Prabhakar Reddy
Keyword(s):  
Immediate Release ◽  
Drug Dissolution ◽  
Dissolution Profile ◽  
Dissolution Medium ◽  
Lactose Monohydrate ◽  
Sodium Starch Glycolate ◽  
Tablet Disintegration ◽  
Croscarmellose Sodium ◽  
Model Drug ◽  
Usp Apparatus

The purpose of this study was to investigate the efficiency of superdisintegrants: sodium starch glycolate, croscarmellose sodium and crospovidone in promoting tablet disintegration and drug dissolution of Topiramate immediate release tablets. The efficiency of superdisintegrants was tested, by considering four concentrations, viz., like 2%, 3%, 4% and 5% in the formulations. The dissolution was carried out in USP apparatus II at 50 rpm with distilled water as a dissolution medium. The dissolution rate of the model drug topiramate was found highly dependent on the tablet disintegration, on the particle size of the superdisintegrant, on the solubility of the drug and also on the type of superdisintegrant in the dissolution medium. There was no effect of the diluent (Lactose monohydrate) on the disintegration of different concentrations of superdisintegrants. These results suggest that, as determined by the f2 metric (similarity factor), the dissolution profile of the formulation containing 4% sodium starch glycolate and lactose monohydrate as a diluent was similar to that of a marketed product.

Formulation and Evaluation of Bilayer Sustained Release Tablets of Salbutamol and Theophylline

2009 ◽  
Vol 2 (3) ◽  
pp. 638-646
Author(s):  
R. Nagaraju ◽  
Rajesh Kaza
Keyword(s):  
Ethyl Cellulose ◽  
Xanthan Gum ◽  
Dosage Forms ◽  
In Vitro Dissolution ◽  
Dissolution Studies ◽  
Sustained Release Tablets ◽  
Dissolution Apparatus ◽  
Single Dosage

Salbutamol and theophylline are available in conventional dosage forms, administered four times a day, leading to saw tooth kinetics and resulting in ineffective therapy. The combination of these two drugs in a single dosage form will enhance the patient compliance and prolong bronchodilation. Various polymers, such as hydroxy propyl methylcellulose K4M (HPMC- K4M), hydroxy propyl methylcellulose K100M (HPMC- K100M), xanthan gum, ethyl cellulose and hydroxy propyl methylcellulose phthalate (HPMC-P) were studied. HPMC-P and HPMC- K4M were found to be best in controlling the release. In-vitro dissolution studies were carried out for all the bi-layered tablets developed using USP dissolution apparatus type 2 (paddle). It was found that the tablet FB15-FW3 showed 50% release of salbutamol in first hour and the remaining was released for eight hours. However, theophylline was found to be released as per the USP specifications. The IR spectrum was taken for FB15-FW3 formulation and it revealed that there is no disturbance in the principal peaks of pure drugs salbutamol and theophylline. This further confirms the integrity of pure drugs and no incompatibility of them with excipients. Also, formulation of FB15-FW3 has shown required release pattern and complies with all the evaluated parameters and comparable to the marketed formulation.

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