scholarly journals Development of Glyceryl Monostearate Based Ciprofloxacin Hydrochloride Sustained Release Matrix Tablet: an In vitro Study

1970 ◽  
Vol 8 (1) ◽  
pp. 81-88
Author(s):  
Susmita Laila ◽  
Tasnuva Haque ◽  
Md Mesbah Uddin Taluker ◽  
Ishtiaq Ahmed ◽  
Muhammad Rashedul Islam ◽  
...  
Keyword(s):  
Sustained Release ◽  
Release Mechanism ◽  
Physical Parameters ◽  
Matrix Tablet ◽  
Glyceryl Monostearate ◽  
Ciprofloxacin Hydrochloride ◽  
First Order ◽  
Release Pattern ◽  
First Order Kinetics

In this present study an attempt has been made to evaluate glyceryl monostearate (GMS) as a rateretarding material to sustain the release ciprofloxacin hydrochloride from the matrix tablet. The solubility ofciprofloxacin hydrochloride was studied. The physical parameters of the prepared tablets were also evaluated.Release kinetics of ciprofloxacin hydrochloride from this sustained release matrix was studied in 0.1 N HCl usingUnited States Pharmacopoeia type-II dissolution apparatus (paddle method). The effect of polymer load, drug load,hydroxylpropylmethylcellulose to compensate glyceryl monostearate (GMS) and different release modifiers wereexamined. It was observed that the release rate of drug was retarded with the increasing concentration of GMS. Therelease data were treated in different fashion to identify the release mechanism and it was revealed with fewexception that, when GMS is used as single polymer, release of active drug from the prepared matrix tablet appearedto follow the first order kinetics and showed the tendency to follow Korsmeyer model when HPMC 15 cps was usedalong with GMS. Using release enhancers the release pattern were fitted to first order kinetics. From the f2 values itcan be concluded that the release pattern of P-2, D-1, H-2 and H-3 are similar to P-1, whereas the formula of P-1, D-2and H-1 were same. MDT values were found to be increased with the increasing amount of polymer (GMS).Key words: Glyceryl monostearate; ciprofloxacin HCl; sustained release matrix; dissolution studies.DOI: 10.3329/dujps.v8i1.5340Dhaka Univ. J. Pharm. Sci. 8(1): 81-88, 2009 (June)

scholarly journals Assessment of Once Daily Sustained Release Hydrophilic Matrix Tablet of Carvedilol

2017 ◽  
Vol 16 (1) ◽  
pp. 43-53
Author(s):  
Uttom Kumar ◽  
Md Samiul Islam ◽  
Shimul Halder ◽  
Abu Shara Shamsur Rouf
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Lower Percentage ◽  
Simulated Gastric Fluid ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Lauryl Sulfate ◽  
Once Daily ◽  
Release Profiles

The objective of the present study was to design and evaluate once daily sustained release tablet of carvedilol, using two molecular weight grades of hydrophilic polymers (methocel® K4M CR and methocel®K15M CR) as release retarding materials. Two sets of formulations were prepared, where first set of four formulations (F1- F4) contained variable ratios of methocel® K4M CR and methocel® K15M CR (15% : 15%, 15% : 13%, 15% : 11% and 15% : 9%) to optimize the composition of polymers in the tablet matrices such that the drug and polymer interaction was sufficient for sustaining release up to 24 hours and second set of five formulations (F5-F9) contained variable percentages of sodium lauryl sulfate (SLS) (1.0, 1.25, 1.5, 1.75 and 2.0%) to enhance the dissolution rate of the drug from the tablet matrices because of its poor aqueous solubility. The tablets were prepared by direct compression method and evaluated for hardness, thickness, friability, weight variation and in vitro drug release. The in vitro dissolution studies were carried out in simulated gastric fluid (900 ml, pH 1.2) for 24 hours using USP type II apparatus operated at 100 rpm and 37 ± 0.05°C. The release profiles were explored and explained by zero order, first order, Higuchi, Korsmeyer-Peppas and Hixson-Crowell models. From this study, the drug release profiles for formulations F6 to F9 were found to be satisfactory and the release mechanism followed both diffusion and erosion. Due to lower percentage of SLS used, F6 was considered as the best formulation.Dhaka Univ. J. Pharm. Sci. 16(1): 43-53, 2017 (June)

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)

scholarly journals Preparation and In-vitro Characterization of Gastroretentive Floating Tablets of Domperidone

2019 ◽  
Vol 22 (2) ◽  
pp. 170-175 ◽  
Author(s):  
Ikramul Hasan ◽  
Tushar Saha ◽  
Md Selim Reza
Keyword(s):  
Pharmaceutical Journal ◽  
Release Mechanism ◽  
Physical Parameters ◽  
First Order ◽  
In Vitro Characterization ◽  
Time Determination ◽  
Acidic Dissolution

The present investigation was design for domperidone floating table preparation and in-vitro characterization. The ultimate target was increasing gastric retention by means of floatability of the tablet. Hydrophilic cellulosic polymers, Methocel K15M and Methocel K100M were used in this experiment for achieving release controlling property. Sodium bicarbonate played the key role of floatation by generating gas. Direct compression was the method of choice for preparing the tablets. The tablets were evaluated for physical parameters, buoyancy study, total floating time determination and dissolution study. Acidic dissolution medium (0.1N HCl), mimicking the environment of the stomach, was used in USP II apparatus for 12 hours to find out the pattern of drug release. The release mechanism was analyzed by exploring the zero order, first order, Higuchi and Korsmeyer equations. All the physical parameters were within acceptable range and Methocel K100M showed more floating lag time and sustained release property than Methocel K15M. All the formulations showed more than 12 hours floating time. Fourier Transform Infrared Spectroscopy (FTIR) study confirmed the compatibility of the drug with the excipients. Bangladesh Pharmaceutical Journal 22(2): 170-175, 2019

scholarly journals Formulation and Evaluation of Polymer Effect on In-Vitro Kinetics of Sustained Release Matrix Tablets of Carvedilol Using Model Dependent Methods

2013 ◽  
Vol 2 (2) ◽  
pp. 70-79
Author(s):  
Umme Rahela ◽  
Md Mizanur Rahman Moghal ◽  
Sayed Masudur Rahman Dewan ◽  
Mohammad Nurul Amin
Keyword(s):  
Sustained Release ◽  
Drug Product ◽  
Release Kinetics ◽  
Matrix Tablets ◽  
Release Mechanism ◽  
Physical Parameters ◽  
Kinetics Of ◽  
In Vitro Kinetics ◽  
Polymeric Effect

The present study was designed to evaluate the polymeric effect of METHOCEL K15MCR on the sustained release drug product of Carvedilol. Carvedilol matrix tablets were formulated by direct compression method using METHOCEL K15MCR polymer in various percentages. Physical parameters were tested and the dissolution procedure was performed by using USP (II) paddle method for eight hours to examine the release kinetics. In the study, METHOCEL K15MCR polymer was found to cause the strong retardation of the drug release. The release mechanism was explored and explained with zero order, first order, Higuchi and Korsmeyer-Peppas equations. In the context, it can be suggested with a satisfactory result that this sustained release Carvedilol tablets can be marketed to treat patient ensuring proper healthcare. DOI: http://dx.doi.org/10.3329/ijpls.v2i2.15452 International Journal of Pharmaceutical and Life Sciences Vol.2(2) 2013: 70-79

scholarly journals RATIONAL DESIGNING OF SUSTAINED RELEASE MATRIX FORMULATION OF ETODOLAC EMPLOYING HYPROMELLOSE, CARBOMER, EUDRAGIT AND POVIDONE

2017 ◽  
Vol 9 (12) ◽  
pp. 92
Author(s):  
Nilesh N. Mahajan ◽  
Pooja Wadhavane ◽  
Debarshi Kar Mahapatra
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Stability Study ◽  
Release Mechanism ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Toxic Substances ◽  
Drug Release Profile ◽  
Matrix Formulation

Objective: The existing investigation represents a challenge in formulating etodolac oral controlled release tablets employing five most prominent hydrophilic release rate retardant polymers like HPMC K100M, HPMC K4M, Carbopol 934P, Eudragit RS100, and Polyvinyl pyrrolidone K90 which are USFDA approved non-toxic substances, cost-effective, and easily available.Methods: The tablets were manufactured by wet granulation method along with talc, anhydrous lactose, and magnesium stearate. The pre-compression attributes of the produced granules and the post-compression characteristics were assessed according to the specified protocols. The formulations were accessed for their ability to release the drug in the simulated gastric media and the obtained results were fitted into various kinetic models to determine the probable drug release mechanism(s). A short-term stability study (for 90 days duration) was also performed.Results: The prepared granules demonstrated superior flow properties and packing ability, whereas the fabricated sustained release matrix batches showed excellent mechanical characteristics. The in vitro drug release profile of the hypromellose, carbomer, eudragit and povidone based sustained release matrix tablet formulations expressed drug release for the period of 12 hr following the diffusion cum erosion mechanism(s) (termed as anomalous diffusion) and illustrated comparable drug release with that of marketed formulation (Etogesic®-ER 600 mg). The produced formulations revealed splendid reproducibility and stability under accelerated conditions.Conclusion: The judiciously planned fabrication of the matrix formulations possess the ability to decrease the frequency of drug administration to twice-daily along with minimizing the blood level fluctuations, which ultimately leads to enhanced patient compliance and better therapeutic regimens.

scholarly journals In vitro Release Kinetic Study of Theophylline from Kollidon SR Polymer Based Matrix Tablet

2015 ◽  
Vol 14 (1) ◽  
pp. 43-48 ◽  
Author(s):  
Abul Kalam Lutful Kabir ◽  
Shimul Halder ◽  
Abu Shara Shamsur Rouf
Keyword(s):  
Release Rate ◽  
Release Kinetics ◽  
Zero Order ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Medium Ph ◽  
First Order ◽  
Tablet Matrix

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)

Effects of release modifier on Carvedilol release from Kollidon SR based matrix

2012 ◽  
Vol 1 (8) ◽  
pp. 186 ◽  
Author(s):  
Urmi Das ◽  
Mohammad Salim Hossain
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Microcrystalline Cellulose ◽  
Matrix Tablets ◽  
Dissolution Time ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Weight Variation ◽  
The Matrix ◽  
Tablet Formulations

<p>Sustained release Carvedilol matrix tablets constituting Kollidon SR were developed in this study in an attempt to investigate the effect of release modifiers on the release profile of Carvedilol from matrix. Three matrix tablet formulations were prepared by direct compression of Kollidon SR in combination with release modifier (HPMC and Microcrystalline Cellulose) and magnesium stearate. Tablets containing only Kollidon SR with the active ingredient demonstrated a rapid rate of drug release. Incorporation of HPMC in the matrix tablet prolonged the release of drug but incorporation of Microcrystalline Cellulose showed superimposable release pattern with an initial burst effect as confirmed by mean dissolution time and Higuchi release rate data. After 7 hours of dissolution, Carvedilol release from the matrix systems were 91.42%, 83.41%, from formulation F1 and F2 respectively. Formulation F3 exhibited 100 % release at 4 hours. All the tablet formulations showed acceptable pharmaco-technical properties and complied with the in-house specifications for tablet weight variation, friability, hardness, thickness, and diameter. Prepared tablets also showed sustained release property for carvedilol. The drug release mechanism from the matrix tablets of F1 and F2 was found to be followed by Fickian and F3 by Non-Fickian mechanism.</p><p>DOI: <a href="http://dx.doi.org/10.3329/icpj.v1i8.11095">http://dx.doi.org/10.3329/icpj.v1i8.11095</a></p> <p>International Current Pharmaceutical Journal 2012, 1(8): 186-192</p>

In-vitro Kinetic Hydrolysis Study of Metronidazole Derivatives with Carvacrol and Eugenol Using Validated RP-HPLC Method

2020 ◽  
Vol 16 ◽  
Author(s):  
M. Alarjah
Keyword(s):  
Half Life ◽  
Hplc Method ◽  
Hydrolysis Rate ◽  
First Order ◽  
First Order Kinetics ◽  
Rp Hplc ◽  
Pharmacokinetic Properties ◽  
Pseudo First Order ◽  
Kinetic Hydrolysis

Background: Prodrugs principle is widely used to improve the pharmacological and pharmacokinetic properties of some active drugs. Much effort was made to develop metronidazole prodrugs to enhance antibacterial activity and or to improve pharmacokinetic properties of the molecule or to lower the adverse effects of metronidazole. Objective: In this work, the pharmacokinetic properties of some of monoterpenes and eugenol pro metronidazole molecules that were developed earlier were evaluated in-vitro. The kinetic hydrolysis rate constants and half-life time estimation of the new metronidazole derivatives were calculated using the validated RP-HPLC method. Method: Chromatographic analysis was done using Zorbbax Eclipse eXtra Dense Bonding (XDB)-C18 column of dimensions (250 mm, 4.6 mm, 5 μm), at ambient column temperature. The mobile phase was a mixture of sodium dihydrogen phosphate buffer of pH 4.5 and methanol in gradient elution, at 1ml/min flow rate. The method was fully validated according to the International Council for Harmonization (ICH) guidelines. The hydrolysis process carried out in an acidic buffer pH 1.2 and in an alkaline buffer pH 7.4 in a thermostatic bath at 37ºC. Results: The results followed pseudo-first-order kinetics. All metronidazole prodrugs were stable in the acidic pH, while they were hydrolysed in the alkaline buffer within a few hours (6-8 hr). The rate constant and half-life values were calculated, and their values were found to be 0.082- 0.117 hr-1 and 5.9- 8.5 hr., respectively. Conclusion: The developed method was accurate, sensitive, and selective for the prodrugs. For most of the prodrugs, the hydrolysis followed pseudo-first-order kinetics; the method might be utilised to conduct an in-vivo study for the metronidazole derivatives with monoterpenes and eugenol.

scholarly journals A Novel Design of Tri-Layer Membrane with Controlled Delivery of Paclitaxel and Anti-Biofilm Effect for Biliary Stent Applications

Nanomaterials ◽  
2021 ◽  
Vol 11 (2) ◽  
pp. 486
Author(s):  
Abdelrahman I. Rezk ◽  
Jeesoo Park ◽  
Joon Yeon Moon ◽  
Sunny Lee ◽  
Chan Hee Park ◽  
...  
Keyword(s):  
Sustained Release ◽  
Antibacterial Effect ◽  
Release Profile ◽  
Biliary Stent ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Dual Function ◽  
Electrospinning Technique ◽  
Layer Membrane

Here, we developed a novel biliary stent coating material that is composed of tri-layer membrane with dual function of sustained release of paclitaxel (PTX) anticancer drug and antibacterial effect. The advantages of using electrospinning technique were considered for the even distribution of PTX and controlled release profile from the nanofiber mat. Furthermore, film cast method was utilized to fabricate AgNPs-immobilized PU film to direct the release towards the tumor site and suppress the biofilm formation. The in vitro antibacterial test conducted against Gram-positive (Staphylococcus aureus) and Gram-negative (Escherichia coli) bacteria species showed excellent antibacterial effect. The in vitro drug release study confirmed the sustained release of PTX from the tri-layer membrane and the release profile fitted first order with correlation coefficient of R2 = 0.98. Furthermore, the release mechanism was studied using Korsmeyer–Peppas model, revealing that the release mechanism follows Fickian diffusion. Based on the results, this novel tri-layer membrane shows curative potential in clinical development.

scholarly journals Bleaching of chlorophylls by UV irradiation in vitro: The effects on chlorophyll organization in acetone and n-hexane

2008 ◽  
Vol 73 (3) ◽  
pp. 271-282 ◽  
Author(s):  
Jelena Zvezdanovic ◽  
Dejan Markovic
Keyword(s):  
Uv Irradiation ◽  
Photosynthetic Pigments ◽  
Energy Input ◽  
First Order ◽  
First Order Kinetics ◽  
Uv Photons ◽  
The Stability ◽  
Major Factors

The stability of chlorophylls toward UV irradiation was studied by Vis spectrophotometry in extracts containing mixtures of photosynthetic pigments in acetone and n-hexane. The chlorophylls underwent destruction (bleaching) obeying first-order kinetics. The bleaching was governed by three major factors: the energy input of the UV photons, the concentration of the chlorophylls and the polarity of the solvent, implying different molecular organizations of the chlorophylls in the two solvents.

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