scholarly journals In vitro Release Kinetic Study of Esomeprazole Magnesium from Methocel K15M and Methocel K100 LVCR Matrix Tablets

1970 ◽  
Vol 7 (1) ◽  
pp. 39-45 ◽  
Author(s):  
Bishyajit Kumar Biswas ◽  
Md Safiqul Islam ◽  
Farida Begum ◽  
Abu Shara Shamsur Rouf

In the present study esomeprazole sustained release tablet matrix was prepared by utilizing different grades of hydroxypropyl methylcellulose (HPMC) polymers such as Methocel K15M & Methocel K100 LVCR by direct compression method. Different amount of Methocel K15M was used to develop matrix builder in the seven proposed formulations (F1-F7) for the study of release rate retardant effect at 20%, 25%, 30%, 35%, 40%, 45% and 50% of total weight of tablet matrix respectively. The dissolution study of Methocel K15M based tablet matrices of those proposed formulations were carried out in the simulated gastric medium (pH 1.3) for first two hours and then in the simulated intestinal medium (pH 6.8) for 8 hours using USP dissolution apparatus II. The formulation F-5 (40%) and F-6 (45%) met the optimum release rate of esomeprazole for 10h period of in vitro dissolution study. The release kinetics of formulation F-5 and F-6 very closely followed Higuchi kinetic order than first order and zero order kinetics. Similarly Methocel K100 LVCR was used to develop matrix builder in another seven proposed formulations (F8-F14). It was found that formulations F-11 (35%), F-12 (40%) and F-13 (45%) met the desired release rate of esomeprazole for 10h period. The release kinetics of formulation F-11, F-12 and F-13 followed Higuchi kinetic order. Between these two polymers, Methocel K100 LVCR showed better release retardant effect than Methocel K15M. Key words: Esomeprazole, Direct compression, Controlled release, Methocel K15M and Methocel K100 LVCRDOI = 10.3329/dujps.v7i1.1216 Dhaka Univ. J. Pharm. Sci. 7(1): 39-45, 2008 (June)  

2015 ◽  
Vol 14 (1) ◽  
pp. 43-48 ◽  
Author(s):  
Abul Kalam Lutful Kabir ◽  
Shimul Halder ◽  
Abu Shara Shamsur Rouf

Controlled release tablet matrix of theophylline was prepared with kollidon SR, a spray dried powder grade polymer (polyvinyl acetate and povidone based matrix rate retarding hydrophobic materials) by utilizing direct compression technique. Different proportion of kollidon SR was used to develop the matrix builder in the five proposed formulations (F-1 to F-5) for the study of release rate retardant effect at 10, 12, 15, 18 and 21% of total weight of matrix tablet, respectively. The in vitro dissolution study of the matrices of those proposed tablet formulations were carried out in simulated gastric medium (pH 1.3) for first two hours and then in simulated intestinal medium (pH 6.8) for 6 hours using USP dissolution apparatus II (paddle method). The formulation F-3 (using 15% polymer) and F-4 (using 18 % polymer) met the optimum release profiles of active ingredient for 8 hr period of total study. The release kinetics for theophylline was plotted against zero order, first order and Higuchi release rate kinetics to evaluate the release mechanism of drug from the formulated tablet matrix. The release kinetics of formulation F-3 and F-4 was followed very closely by Higuchi release rate kinetic order than other kinetics such as zero order and first order kinetics which has been reflected the type of drug release from the tablet matrix by diffusion as well as erosion mechanism.Dhaka Univ. J. Pharm. Sci. 14(1): 43-48, 2015 (June)


Author(s):  
SALMA AULIA ◽  
LINA WINARTI ◽  
YUDI WICAKSONO

Objective: This study aimed to find the best SNEDDS meloxicam formula and analyze the release kinetics of meloxicam SNEDDS and non-SNEDDS using DDSolver.  Methods: Meloxicam SNEDDS was prepared using sunflower seed oil, Cremophor RH 40 as a surfactant, and polyethylene glycol (PEG) 400 as a co-surfactant.  Results: The best formula obtained subjected to the in vitro dissolution study was analyzed using DDSolver. The study shows one selected formula consists of 10% sunflower seed oil, 70% cremophor RH 40, and 20% PEG 400 with a 20.5 nm±12 nm droplet size. The dissolution study showed that SNEDDS could significantly increase the meloxicam release compared to the non-SNEDDS formulation. The kinetics of meloxicam release from SNEDDS formulations follow the Weibull release model (β = 1.00).  Conclusion: This study concludes that SNEDDS best prepared in sunflower seeds oil: Chremophor RH 40: PEG 400 ratio of 1: 7: 2 and has the potency to increase the solubility and dissolution of meloxicam.


1970 ◽  
Vol 2 (1) ◽  
pp. 37-43 ◽  
Author(s):  
Muhammad Shahidul Islam ◽  
Tasnuva Haque ◽  
Rumana Jahangir ◽  
Kanij Fatema ◽  
Mynol Islam Vhuiyan ◽  
...  

In the present study Ciprofloxacin HCl sustained release matrix tablet was prepared by utilizing different grades of hydroxypropyl methylcellulose (HPMC) polymers such as Methocel K4M CR, Methocel K4M Premium & Methocel K15M CR by direct compression method. Different amount of Methocel K15M CR was used to develop matrix builder in the three proposed formulations (F1-F3) for the study of release rate retardant effect at 5%, 6%, and 7% of total weight of tablet matrix respectively. The dissolution study of Methocel K15M CR based tablet matrices of those proposed formulations were carried out in the simulated gastric medium (pH 1.3) for 8 hours using USP dissolution apparatus II. Similarly Methocel K4M premium was used to develop matrix builder in another three proposed formulations (F4-F6). It was found that formulations F-4 (15%), F-5 (17%) and F-6 (18.3%) met the desired release rate of Ciprofloxacin HCl for 8hrs period. The release kinetics of formulation F-4, F-5 and F-6 followed Higuchi kinetic order. Again Methocel K4M premium was used for another three proposed formulations (F7-F9). It was found that formulations F-7 (6.7%), F-8 (12.3%) and F-9 (15.6%) met the desired release rate of Ciprofloxacin HCl for 8hrs period. The release kinetics of formulation F-7, F-8 and F-9 followed Higuchi kinetic order. Among these three polymers, Methocel K4M Premium showed better release retardant effect than Methocel K4M CR and Methocel K15M CR. Key Words: Ciprofloxacin HCl; Direct compression; Controlled release; Methocel K15M CR; Methocel K4M CR; Methocel K4M premium.DOI: 10.3329/sjps.v2i1.5814Stamford Journal of Pharmaceutical Sciences Vol.2(1) 2009: 37-43


Author(s):  
Umamaheswara G. ◽  
Anudeep D.

Fluvastatin sodium is a novel compound used as cholesterol lowering agent which acts through the inhibition of 3- hydroxyl-3- methyl glutaryl- coenzyme A (HMG-Co A) reductase. It has short biological half life (1-3h) in humans required a dosing frequency of 20 to 40mg twice a day. Due to its short variable biological half life it has been developed to a sustained gastroretentive system with a natural and synthetic polymer and to study how far the natural mucilage improves the sustained activity. Floating tablets were prepared by direct compression method using in combination of natural mucilage and synthetic polymer. Prior to the preparation of tablets the physical mixtures were subjected to FT IR studies and pre compression parameters. After preparation of tablets they were subjected to various tests like swollen index, drug content, In vitro dissolution and release kinetics with pcp disso software etc. The tablets prepared by direct compression shown good in thickness, hardness and uniformity in drug content, the prepared tablets floated more than 12h except FS1 and FS2 shows 9 and 11h. Swollen index studies shows with increase in concentration of polymer the swelling increases the diffusion path length by which the drug molecule may have to travel and cause lag time. In vitro results shows that on increasing the amount of hibiscus polymer the sustain activity is increased because of its integrity and forms a thick swollen mass and reduces the erosion property of the HypromelloseK100M, kinetic studies shows that FS 1, FS2, FS3 followed the Korsmeyer peppas model and the rest FS 4, FS 5, FS6 follows the zero order respectively. Based on n value indicating that the drug release followed super case II transport mechanism due to the erosion of the polymer.


2002 ◽  
Vol 70 (2) ◽  
pp. 189-198
Author(s):  
Genç Lütfi ◽  
Hegazy Nahed ◽  
Arica Betül

Matrix tablets of ketorolac trometharnine (KT) were prepared by direct compression technique and Carbopol 934, 940 and 1342 have been used as polymers in different concentrations (5-15 % ). For the quality control of tablets; physical tests as crushing strength, diameter-height ratio and fkiability, KT amount assay and in vitro dissolution techniques were performed and dissolution profiles were plotted and evaluated kinetically. The in vitro release kinetics of ten different formulations of KT matrix tablet were studied at pH 1.2 and pH 7.0 using the USP dissolution technique and apparatus with basket assembly. Dissolution results were evaluated kinetically and statistically. According to our results, different types and concentrations of carbopol to tablet formulations may effect in controlled drug release.


2013 ◽  
Vol 11 (2) ◽  
pp. 129-136 ◽  
Author(s):  
Monnujan Nargis ◽  
Md Saiful Islam ◽  
Fatima Naushin ◽  
Syed Shabbir Haider

Sustained release formulations of metoclopramide HCl (4-amino-5-chloro-N-(2-diethylaminoethyl)-2- methoxybenzamide hydrochloride) (MH) were prepared using carnauba wax (CW) and stearic acid (SA) as matrix formers. Granules were prepared by melt granulation method while direct compression technique was used to prepare the tablets. The drug release profiles of these products were studied by in-vitro dissolution testing in simulated gastric, gastrointestinal and intestinal media of pH 1.2, 4.5 and 7.5, respectively. The increase in the proportion of SA in the granules produced a concomitant decrease of the initial drug release rate but later on the release rate was enhanced in the intestinal medium. Drug release was found to be affected by compression force and stirring rate but also showed a dependency on pH of the dissolution fluid. The fastest release rate was found at pH 4.5 and the slowest at pH 1.2 which was consistent with the drug’s solubility behavior. Matrix erosion and water uptake rates were highest in the intestinal medium and lowest in the gastric medium. The drug release kinetics followed the Higuchi’s model in all cases. DOI: http://dx.doi.org/10.3329/dujps.v11i2.14563 Dhaka Univ. J. Pharm. Sci. 11(2): 129-136, 2012 (December)


2020 ◽  
Vol 10 (1) ◽  
pp. 18-23
Author(s):  
Ayan Kumar Kar ◽  
Banhishikha Kar

Quality is the most important issue in the pharmaceutical field due to the presence of a drug which is considered as safe and therapeutically active agent. In-vitro evaluation ensures their quality, bioavailability as well as optimum therapeutic activity. Paracetamol (acetaminophen) which are the active metabolites of phenacetin is commonly used for the relief of headaches and pains, and is a major ingredient in numerous cold and flu remedies. Paracetamols are available in different brands in Indian market. The main objective of the present study was to conduct the comparative in-vitro dissolution studies of various brands collected from the local market to determine whether all the formulations used were equivalent or significantly different. The calibration curve was constructed covering the concentration range of 1 to 10 mcg/ml at 268 nm by UV spectrophotometer (UV 2203 Double beam spectrophotometer, Shimadzu).  Five different brands of Paracetamol of 500 mg conventional tablets from different manufacturers were selected in the study and dissolution testing in Phosphate buffer at pH 7.4 was conducted from each brands for 90 mins by using dissolution testing apparatus USP type-II. The dissolution rate was subjected to various mathematical models like zero order, first order, Higuchi and Hixson-Crowell equations to elucidate the kinetic behavior of drug release from the test samples. Different release kinetics model of all the selected brands was assuring the quality standard of manufacturing. Keywords: Paracetamol, Marketed Tablet, In-Vitro dissolution study, Release profile.


2021 ◽  
Vol 15 (1) ◽  
pp. 038-048
Author(s):  
Nkemakolam Nwachukwu ◽  
Sabinus Ifeanyi Ofoefule

The flow, tableting and in vitro release properties of directly compressed chlorpheniramine maleate (CPM) tablets containing fluid bed dried and lyophilized microcrystalline cellulose (MCC) obtained from Gossypium herbaceum (GH) were investigated. Delignification of dried GH linters was done through the soda process to obtain alpha cellulose which was hydrolyzed with 2.0 N hydrochloric acid to get MCC. The MCC was washed with water until neutral. Drying was done by either fluid bed method or lyophilization to obtain MCC-GossF and MCC-GossL respectively. Chlorpheniramine tablets containing 20, 30 and 40% of the MCCs were prepared by direct compression method. Avicel PH102 (AVH-102) served as comparing standard. Using standard methods, evaluation of the powders and the tablets was done. The evaluated parameters of the powders and tablets conformed to the British Pharmacopoeia specifications. The CPM tablets containing MCC-GossF (coded CGF) had better flow but were not mechanically as strong as those containing MCC-GossL (coded CGL). The hardness and disintegration times of the tablets were in the order of CGF < CGL and the friability was in the order of CGF > CGL. Similar parameters of DCL compared well with CPM tablets containing AVH-102 (coded DAV). The MCC obtained from GH had dilution potential up to 40% except in CGF-4 tablets. The in vitro dissolution showed > 80% CPM release from all the batches within 30 min. The release kinetics were of mixed order while the mechanism of drug release was Fickian. The MCCs served as good directly compressible binder for chlorpheniramine maleate.


1970 ◽  
Vol 43 (3) ◽  
pp. 321-332
Author(s):  
Afsana Akhter ◽  
Monzurul Amin Roni ◽  
Mohammad Shahriarul Absar ◽  
Golam Kibria ◽  
Reza-ul Jalil

The purpose of the present study is to investigate the effect of polyvinyl acetate on the release kinetics of diltiazem hydrochloride from coated pellets prepared by solution and suspension layering technique. Kollicoat SR 30 D, an aqueous dispersion of polyvinyl acetate with different weight ratios was chosen to sustain the release of the drug. Drug was loaded with hydroxypropyl methyl cellulose on nonpareil seeds then coated with the Kollicoat SR 30 D. In vitro dissolution studies were carried out using USP dissolution apparatus Type-2. No significant difference was found in drug release from uncoated pellets and the pellets coated with 5% polymer load. With 10% polymer load, the initial release was minimized but from 2nd hour the release was quick-tempered. Better sustaining effect was found from 15- 20% polymer loaded pellets. The mean dissolution time was 2.5h and 4h while the polymer load was 15% and 20% respectively. Also these two cases 80% drug was released at 6h and 9h respectively. The physical parameters of the prepared pellets were also compared in this study. The release of drug from the coated pellets appeared to follow Higuchi's release kinetics.Key words: Diltiazem, Pellets, Kollicoat SR 30 D, Aqueous coating, Physical parameters, Release kinetics.DOI = 10.3329/bjsir.v43i3.1147Bangladesh J. Sci. Ind. Res. 43(3), 321-332, 2008


Author(s):  
SANJEEV KUMAR ◽  
AMIN MIR M ◽  
SARVESH KUMAR ◽  
ANUJ KUMAR

Objective: The main focus of the study was to investigate the marketed formulations of cinnarizine and it is marketed analogous. Methods: The study involved the analysis of basic pre-formulation studies, namely, physical properties, melting point, Fourier-transform infrared, loss on drying, assay of cinnarizine, standard curve, and partition co-efficient of various marketed tablets of cinnarizine. Results: Cinnarizine is an H1-receptor antagonist drug which is widely used for the treatment of dynamical sickness, vomiting, and vertigo. In this study, five known marketed formulations of cinnarizine were evaluated for weight variation, hardness, drug content, friability, disintegration time, and in vitro dissolution as well as the drug release kinetics of the tablets. As per the study, the drugs show low disintegration time and good hardness, also in vitro dissolution studies have shown near about 90% drug release at the end of the first 10 min and then cumulative drug release of not less than 92% in the nearby 10 min. Hence, these formulations show lower friability, acceptable taste, and shorter disintegration time which make them suitable to be accepted. Thus, the tablets are good for the use, so allow them to be marketed for the wellbeing of humans. Conclusion: It had been found that all the tablets show acceptable limits for various parameters of analysis, in a sustained manner. Thus, all the tablets are effective for usage under standard conditions.


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