scholarly journals Application of microcrystalline cellulose obtained from Gossypium herbaceum in direct compression of chlorpheniramine maleate tablets

2021 ◽  
Vol 15 (1) ◽  
pp. 038-048
Author(s):  
Nkemakolam Nwachukwu ◽  
Sabinus Ifeanyi Ofoefule
Keyword(s):  
Microcrystalline Cellulose ◽  
Release Kinetics ◽  
In Vitro Release ◽  
In Vitro Dissolution ◽  
Direct Compression ◽  
Chlorpheniramine Maleate ◽  
British Pharmacopoeia ◽  
Fluid Bed ◽  
Gossypium Herbaceum

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.

scholarly journals Direct Compression and in vitro Release of Chlorpheniramine Maleate from Tablets Containing Fluid Bed Dried and Lyophilized Microcrystalline Cellulose Derived from Cocos nucifera

2019 ◽  
pp. 1-15
Author(s):  
Nkemakolam Nwachukwu ◽  
Kenneth Chinedu Ugoeze ◽  
Ogbonna Okorie ◽  
Sabinus Ifeanyi Ofoefule
Keyword(s):  
Microcrystalline Cellulose ◽  
Cocos Nucifera ◽  
In Vitro Release ◽  
Mineral Acid ◽  
Chlorpheniramine Maleate ◽  
Disintegration Time ◽  
Weight Variation ◽  
Fluid Bed ◽  
Vitro Release

Aims: To investigate the mechanical and in vitro release properties of chlorpheniramine maleate (CM) tablets formulated with fluid bed dried and lyophilized microcrystalline cellulose (MCC) derived from the fruit husk of Cocos nucifera (CN). Study Design: Experimental design. Place and Duration of Study: Department of Pharmaceutical Technology and Industrial Pharmacy, University of Nigeria, Nsukka from January, 2015 to December, 2016. Methods: Chips of matured (CN) fruit husk were de-lignified by soda treatment methods to obtain alpha cellulose which was hydrolyzed with mineral acid (Hydrochloric acid) to obtain CN-MCC. A portion of the damp CN-MCC was fluid bed dried at 60°C for 2 h (coded MCCF-Cocos) and the remaining CN-MCC was lyophilized at -45°C for 3 h (coded MCCL-Cocos). The MCC powders were blended with 20, 30 and 40% w/w CM and directly compressed at 9.81 mega Pascal (mPa). The CM tablets containing MCCF-Cocos (coded CM-CF) and MCCL-Cocos (coded CM-CL) were evaluated using standard methods. Results: Both batches had tablets with minimal weight variation; CM-CL tablets were mechanically stronger (P = .037) and less friable than CM-CF tablets.  CM-CL tablets took a longer time to disintegrate than CM-CF tablets. Comparatively, CM tablets containing AVC-102 (coded CM-AV) were mechanically stronger, less friable and had a longer disintegration time than CM-CL and CM-CF tablets. The dilution potential of CM-AV was greater than CM-CL and CM-CF tablets. CM release was faster in CM-CF. There was more than 80 % release of CM from CM-CF, CM-CL and CM-AV tablets within 30 min. Although CM-CL tablets were mechanically stronger than CM-CF, the data for all batches of the tablets obtained fell within the British Pharmacopoeia set limits for uncoated tablets. Conclusion: Chlorpheniramine maleate tablets containing fluid bed dried and lyophilized microcrystalline cellulose obtained from C. nucifera had good mechanical and in vitro release properties.

scholarly journals The Mechanical and In vitro Release Properties of Diazepam from Tablets Containing Fluid Bed Dried and Lyophilized Cocos nucifera Microcrystalline Cellulose

2019 ◽  
pp. 1-14
Author(s):  
Nkemakolam Nwachukwu ◽  
Sabinus Ifeanyi Ofoefule
Keyword(s):  
Mechanical Properties ◽  
Drug Release ◽  
Microcrystalline Cellulose ◽  
Cocos Nucifera ◽  
In Vitro Release ◽  
Disintegration Time ◽  
British Pharmacopoeia ◽  
Fluid Bed ◽  
Vitro Release

Aim: This study aimed to evaluate the mechanical and in vitro release properties of diazepam from tablets containing fluid bed dried and lyophilized microcrystalline cellulose (MCC) obtained from the matured fruit husks of Cocos nucifera (CN). Study Design: Method of experiment. Place and Duration of Study: Department of Pharmaceutical Technology and Industrial Pharmacy, University of Nigeria, Nsukka from March 2015 to September, 2016 Methods:  Dried CN fruit husks were digested in sodium hydroxide to obtain alpha (α) cellulose which on hydrolysis with mineral acid (Hydrochloric acid) solution gave CN-MCC. The dry MCC obtained by either fluid bed or lyophilized drying of the wet CN-MCC were coded MCCF-Cocos and MCCL-Cocos respectively. Both MCCs were used in the formulation of diazepam tablets at 20, 30 and 40% w/w. Avicel PH 102 (AVC-102), was used as comparing standard. The tablets were evaluated for physical and dissolution properties using standard methods. Results: Results show the tablets passed the British Pharmacopoeia specifications for weight uniformity, crushing strength, disintegration time, friability and dissolution. Diazepam tablets containing MCCL-Cocos (coded DCL) were mechanically stronger than those containing MCCF-Cocos (coded DCF). Disintegration time was in the order of DCF > DCL tablets while friability was in the order of DCL < DCF tablets. Diazepam tablets containing AVC-102 (coded DAV) were mechanically stronger than DCL and DCF tablets. The dilution potential was in the order DAV > DCL > DCF. More than 80% of the diazepam content was released from DAV, DCL and DCF tablets. Conclusion: Generally, DAV, DCL and DCF tablets met the British Pharmacopoeia limits for mechanical properties and in vitro drug release with DCL tablets showing significantly (P = .05) superior mechanical properties while DCF showed faster drug release.

Gastroretentive System of Fluvastatin Sodium by Using Natural Mucilage and Synthetic Polymer

2014 ◽  
Vol 4 (2) ◽  
Author(s):  
Umamaheswara G. ◽  
Anudeep D.
Keyword(s):  
Half Life ◽  
Release Kinetics ◽  
Kinetic Studies ◽  
Diffusion Path ◽  
Synthetic Polymer ◽  
In Vitro Dissolution ◽  
Direct Compression ◽  
Drug Content ◽  
Biological Half Life

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.

scholarly journals Investigation of certain varieties of carbopol in ketorolac tromethamine hydrophilic matrix tablet formulations and evaluation of the kinetics of its in vitm release

2002 ◽  
Vol 70 (2) ◽  
pp. 189-198
Author(s):  
Genç Lütfi ◽  
Hegazy Nahed ◽  
Arica Betül
Keyword(s):  
Release Kinetics ◽  
In Vitro Release ◽  
Controlled Drug Release ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Matrix Tablet ◽  
Compression Technique ◽  
Tablet Formulations ◽  
Kinetics Of

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.

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
Keyword(s):  
Release Rate ◽  
Release Kinetics ◽  
In Vitro Dissolution ◽  
Direct Compression ◽  
Medium Ph ◽  
Kinetic Order ◽  
Dissolution Study ◽  
Tablet Matrix ◽  
Kinetics Of

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)  

scholarly journals Pullulan: an advantageous natural polysaccharide excipient to formulate tablets of alendronate-loaded microparticles

2015 ◽  
Vol 51 (1) ◽  
pp. 27-33 ◽  
Author(s):  
Luana Mota Ferreira ◽  
Aline de Arce Velasquez ◽  
Scheila Rezende Schaffazick ◽  
Letícia Cruz
Keyword(s):  
Microcrystalline Cellulose ◽  
In Vitro Release ◽  
The Other ◽  
Average Weight ◽  
Direct Compression ◽  
Compression Force ◽  
Natural Polysaccharide ◽  
Release Studies ◽  
Vitro Release

This work reports the preparation of tablets by direct compression of sodium alendronate-loaded microparticles, using pullulan as filler. The tableting properties of pullulan were compared with those of microcrystalline cellulose and lactose. Pullulan tablets showed low variations in average weight, thickness and drug content. Moreover, these tablets exhibited a higher hardness compared to the other excipients. In vitro release studies showed that only pullulan was capable to maintain gastroresistance and release properties of microparticles, due to its ability to protect particles against damage caused by compression force. Thus, pullulan was considered an advantageous excipient to prepare tableted microparticles.

scholarly journals Design and characterization of metoprolol floating matrix tablet

2017 ◽  
Vol 4 (2) ◽  
pp. 118
Author(s):  
Vasudha Bakshi ◽  
Swapna S. ◽  
Deepa Kumari Choudhary ◽  
Ch. Revanth ◽  
B. Sai KumarCh. Praveen ◽  
...  
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Release Profile ◽  
In Vitro Dissolution ◽  
Matrix Tablet ◽  
Formulation Development ◽  
Drug Release Profile ◽  
Gastric Residence Time

Objective: The objective of the present research was to develop a matrix embedded floating tablet of Metoprolol for the sustained activity and prolongation of gastric residence time to improve the bioavailability of the drug. Metoprolol was chosen as a model drug because it is better absorbed in the stomach than the lower gastro intestinal tract.Methods: The experimental work was divided into pre-formulation studies, formulation development, and evaluation. Standardization of drug and excipients confirmed the authentication of the samples. Floating test were conducted for all formulations, In vitro dissolution studies were carried out in a dissolution testing apparatus-II, FTIR study was performed to interpret the drug ,excipient interaction.Results: Floating tests were also performed for 15 formulations and among them five formulations have passed the floating tests (F1, F3, F5, F7, and F14). The In-vitro release kinetics study of this tablet indicated sustained release for Metoprolol and followed zero order release and 95% drug in 8 h in vitro. The drug release profile of formulated product was compared with marketed product Metolar. The floating tablets extended the drug release up to 8 hours. The drug-polymer interaction was evaluated by fourier transform infrared spectroscopy (FTIR).Conclusions: F3 formulation showed the best floating results. The comparative study between F3 and Metolar (Marketed Product) showed the similar in vitro drug release profile. Thus, the optimzed formulation F-3 can be successfully used for the management of hypertension.

scholarly journals Enhancement of the dissolution profile of the diuretic hydrochlorothiazide by elaboration of microspheres

2018 ◽  
Vol 83 (11) ◽  
pp. 1243-1259
Author(s):  
Oum Larbi ◽  
Haouaria Merine ◽  
Youssef Ramli ◽  
Fawzia Toumi ◽  
Kaddour Guemra ◽  
...  
Keyword(s):  
Ftir Spectroscopy ◽  
Release Kinetics ◽  
Drug Loading ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Xrd Analysis ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Scanning Calorimetry

Hydrochlorothiazide (HCTZ), which was developed and introduced in the late 1950s, is still one of the most frequently employed drugs in antihypertensive treatments. Its poor aqueous solubility is one of the reasons for its limited bioavailability after oral administration. The present paper provides details of the preparation of HCTZ-loaded microspheres by the solvent evaporation technique. A total of seven formulations were prepared using ethyl cellulose, poly(?-caprolactone) (PCL), ?-cyclodextrin (?-CD) and synthesized poly-(methyl methacrylate) (PMMA) of different molecular weights in different drug-to-carrier ratios in order to investigate their effect on the encapsulation efficiency and drug release kinetics. The prepared formulations were characterized by Fourier transform-infrared (FTIR) spectroscopy, powder X-ray diffractometry, differential scanning calorimetry, yield, drug loading, optical microscopy, surface morphology by scanning electron microscopy (SEM), and in vitro release studies in simulated gastrointestinal tract fluid. The loading efficiency was found in the range from 18?0.34 to 39?0.95 %. The microspheres were spherical, and the mean Sauter diameter (d32) of the obtained microparticles ranged from 26?0.16 to 107?0.58 ?m. The presence of the drug and polymer carriers in the microparticles was confirmed by FTIR spectroscopy and XRD analysis. In vitro dissolution studies showed that the release rate was largely affected by the characteristics of the microparticles, namely the particle size and the nature of the matrix. The release data are best fitted to the Higuchi model with high correlation coefficients (r?).

scholarly journals Formulation and evaluation of polymeric nanoparticles of an antihypetensive drug labetalol

2018 ◽  
Vol 8 (6-s) ◽  
pp. 187-191 ◽  
Author(s):  
Surendranath Betala ◽  
M. Mohan Varma ◽  
K. Abbulu
Keyword(s):  
Drug Release ◽  
Ethyl Cellulose ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Spherical Geometry ◽  
Stability Study ◽  
In Vitro Dissolution ◽  
Dissolution Time ◽  
Dissolution Medium

Labetalol is an adrenergic receptor blocking agent used in the treatment of hypertension and characterized by high solubility and high permeability which corresponds to BCS class I drug. Plasma half life ranges from 6 & bioavailability is 25%. Ethyl cellulose was used as a rate controlling polymer. Effects of addition of ethyl cellulose on in vitro dissolution were studied. Nanoparticles were formulated using different polymer ratios. In vitro drug release was carried out by using USP Type II at 50 rpm in 900 ml of acidic dissolution medium (pH 1.2) for 2 hours, followed by 900 ml alkaline dissolution medium (pH7.4) for 12 hours. Mean dissolution time is used to characterize drug release rate from a dosage form. Several kinetic models were applied to the dissolution profiles to determine the drug release kinetics. Excipients are selected by FTIR studies. Finally the nanoparticles were evaluated for various characteristics like encapsulation efficiency, percentage yield, partial size and the In vitro release for 12 hrs.  The nanoparticles were found to be discrete, spherical, and free-flowing.  The nanoparticles were uniform in size, and the microencapsulation efficiency was in the range of 52.5-81.7%. The surface morphology of prepared Labetalol nanoparticles was observed under scanning electron Microscopy. Nanoparticles had good spherical geometry. The stability study was performed at 40ºC ± 2ºC and 75 ± 5% RH for 6 months. Keywords: Nanoparticles; Labetalol, Hypertension, Ethyl Cellulose, Dissolution, entrapment efficiency.

Formulation and In vitro Release Characterization of Metoprolol Succinate Extended Release Tablets

2012 ◽  
Vol 4 (4) ◽  
pp. 1537-1543
Author(s):  
Sakthikumar T ◽  
Rajendran N N ◽  
Natarajan R
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Wet Granulation ◽  
Direct Compression ◽  
Metoprolol Succinate ◽  
Extended Release Formulations ◽  
Vitro Release

The present study was aimed to develop an extended release tablet of metoprolol Succinate for the treatment of hypertension.  Four extended release formulations F1-F4 were developed using varying proportions of hydroxylpropyl-methylcellulose K100M, sodium carboxy methyl cellulose and Eudragit L30 D55 by wet granulation. Five extended release formulations F5-F9 containing HPMC K100M and HPMC 5 cps in varying concentration were developed by direct compression. The physicochemical and in vitro release characteristics of all the formulations were investigated and compared. Two formulations, F7 and F8 have shown not more 25% drug release  in 1st h, 20%-40% drug release at 4th hour, 40%-60% drug release at 8th hour and not less than 80% at 20th hour and the release pattern conform with USP specification for 24 hours extended release formulation. It can be conclusively stated that optimum concentration of HPMC K100M (58%-65%) by direct compression method can yield an extended release of metoprolol succinate for 24 hours.

Sign in / Sign up

Export Citation Format

Share Document