scholarly journals Comparison of Gastro Retention Time and in vitro Release Profile studies of Ciprofloxacin HCl from Co-matrix Tablets of Hydrophilic Polymers

1970 ◽  
Vol 8 (1) ◽  
pp. 67-73 ◽  
Author(s):  
Muhammad Shahidul Islam ◽  
Kazi Rashidul Azam ◽  
Jakir Ahmed Chowdury ◽  
Md Selim Reza
Keyword(s):  
Retention Time ◽  
Xanthan Gum ◽  
Gastric Fluid ◽  
Matrix Tablets ◽  
Drug Dissolution ◽  
Simulated Gastric Fluid ◽  
Burst Release ◽  
Direct Compression ◽  
Zero Order Release

Controlled release co-matrix tablets of Ciprofloxacin HCl were prepared with different types of bioadhesivepolymers e.g. Methocel K4M, Methocel K 15M CR and Methocel K 100LV, Povidone K-30, and Xanthangum. Tablets prepared by direct compression method were subjected to in-vitro drug dissolution study for 8 hours ina simulated gastric fluid media using USP dissolution apparatus II with 50 rpm at 37±0.5ºC. The bio-adhesiveproperty was investigated in terms of retention time following in-vitro wash-off method. The concentrations ofpolymers were varied to investigate whether these variations can cause any change in release of Ciprofloxacin HClmolecule and bio-adhesion property or not. In most of the cases it is found that Methocel K4M and MethocelK100LV based co-matrix tablets release greater percentage of active drug than Methocel K15M CR based co-matrixtablets. Bio-adhesive strength of Methocel K15M CR and Xanthan gum based co-matrix tablets was proved to bemaximum followed by Methocel K4M and Xanthan gum based co-matrices. Whereas Methocel K100LV andXanthan gum based co-matrices showed little or poor muco-adhesion. Methocel K4M, K15M CR and Xanthan gumbased formulations showed nearly zero-order release, on the other hand Methocel K100LV and Xanthan gum basedformulation showed a burst release within one hour of dissolution. Finally it was revealed that Xanthan gum providedoptimum bio-adhesion functioning as a synergist in co-matrices and comply the USP specification as a most suitablecontrolled release polymer.Key words: Gastro retention time; Direct Compression; Ciprofloxacin HCl; Methocel K4M; Methocel K15M CR;Methocel K100LV; Xanthan gum.DOI: 10.3329/dujps.v8i1.5338Dhaka Univ. J. Pharm. Sci. 8(1): 67-73, 2009 (June)

scholarly journals Studies on Bio-adhesion of Matrix Tablets: I. Release Profile of Theophylline Anhydrous

1970 ◽  
Vol 5 (1) ◽  
pp. 33-37
Author(s):  
Md. Shamsuddin ◽  
Parvin Akter ◽  
Md. Ziaur Rahman Khan ◽  
Jakir Ahmed Chowdhury ◽  
Md. Selim Reza
Keyword(s):  
Controlled Release ◽  
Mucous Membrane ◽  
Xanthan Gum ◽  
In Vitro Release ◽  
Gastric Fluid ◽  
Release Profile ◽  
Matrix Tablets ◽  
Drug Dissolution ◽  
Burst Release

Controlled release matrix tablets of theophylline anhydrous were designed with different types of bioadhesive polymers. HPMC 15 cps and 50 cps, Na-CMC, Gelatin, Xanthun gum and PVP K-30 were selected to formulate matrix tablets. Tablets of theophylline were prepared by direct compression method and were subjected to in vitro drug dissolution for 8 hrs in a gastric fluid media by using thermal shaker with a shaking speed of 50 rpm at a temperature of 37 ± 0.5°C. The in vitro release study as well as retention time of bioadhesive tablets on mucous membrane were investigated to develop a bioadhesive polymer based controlled release delivery system and to evaluate the performance of such delivery device. Na-CMC, HPMC and Xanthan gum based tablets showed greater bio-adhesive strength where as gelatin and PVP K-30 based tablets showed poor bioadhesive strength. Na-CMC and Xanthun gum loaded tablets were not discharged from the mucous membrane and these tablets were fully dissolved in the gastric fluid. Xanthan gum, Na-CMC and HPMC based formulation showed nearly zero-order release. On the contrary, gelatin and PVP K-30 based formulation showed a burst release within one hour of dissolution. Key words: Bio-adhesion, Release profile, theophylline anhydrous. Dhaka Univ. J. Pharm. Sci. Vol.5(1-2) 2006 The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website

scholarly journals Studies on Bio-adhesion of Matrix Tablets: II.Comparison on Bio-adhesion Strength and Release Profiles of Theophylline Anhydrous and Its Sodium Glycinate Salt

2012 ◽  
Vol 10 (1) ◽  
pp. 1-7
Author(s):  
Md Saiful Islam ◽  
Md Ziaur Rahman Khan ◽  
Masuda Khatun ◽  
Jakir Ahmed Chowdhury ◽  
Md Selim Reza
Keyword(s):  
Xanthan Gum ◽  
Active Drug ◽  
Physical Property ◽  
Matrix Tablets ◽  
Drug Dissolution ◽  
Burst Release ◽  
Salt Form ◽  
Different Types ◽  
Zero Order Release

Controlled release matrix tablets of Theophylline anhydrous and Theophylline sodium glycinate were prepared with different types of bio-adhesive polymers e.g. HPMC 15 & 50 cps, Gelatin, PVP K-30, Na-CMC and Xanthan gum. Tablets, prepared by direct compression method were subjected to in-vitro drug dissolution for 8 hours in 0.1 N hydrochloric acid (pH 1.2) using a thermal shaker at 50 rpm at 37 ± 0.5ºC. The bio-adhesive property was investigated in terms of retention time following in-vitro wash-off method by Lehr et al. The anhydrous and corresponding salt form was used to investigate whether physical variation of Theophylline molecule can cause any change in release and bio-adhesion property or not. In most of the cases it is found that salt form releases greater percentage of active drug than its corresponding anhydrous form. Irrespective of drug’s physical property and amount of polymer, bio-adhesive strength of Xanthan gum was proved to be maximum followed by HPMC- 50 cps, Na-CMC and HPMC- 15 cps, whereas gelatin and PVP K-30 showed little or poor muco-adhesion. Xanthan gum, Na-CMC and HPMC based formulations showed nearly zero-order release; on the contrary PVP K-30 based formulation showed a burst release within one hour of dissolution.DOI: http://dx.doi.org/10.3329/dujps.v10i1.10008DUJPS 2011; 10(1): 1-7

scholarly journals Effect of Hydrophobic Polymers on the Gastro Retention Time and In vitro Release of Ciprofloxacin HCl from Co-matrix Tablets

1970 ◽  
Vol 9 (2) ◽  
pp. 97-102
Author(s):  
Muhammad Shahidul Islam ◽  
Kumar Bishwajit Sutradhar ◽  
Jakir Ahmed Chowdhury ◽  
Md Selim Reza
Keyword(s):  
Adhesive Strength ◽  
Retention Time ◽  
Xanthan Gum ◽  
Water Soluble ◽  
Matrix Tablets ◽  
Direct Compression ◽  
Eudragit Rs ◽  
Water Soluble Drug ◽  
Eudragit Rs Po

The present study was conducted to investigate the effect of different polymers on the release profile and bio-adhesive strength of a water soluble drug, ciprofloxacin HCl from different percentages of Eudragit RS PO and Kollidon SR based co-matrix tablets. Matrix formulations were prepared by direct compression method. The bioadhesive property was investigated in terms of retention time following in vitro wash-off method. The concentrations of polymers were varied to investigate whether these variations can cause any change in release of ciprofloxacin HCl molecule and bio-adhesion property or not. In most of the cases it is found that Eudragit RS PO based co-matrix tablets release greater percentage of active drug and that bio-adhesive strength of Kollidon SR and xanthan gum based co-matrix tablets were significantly better. Finally it was revealed that xanthan gum provided optimum bioadhesion functioning as a synergist in co-matrices and comply the USP specification as a most suitable controlled release polymer. Key words: Gastro retention time; direct compression; ciprofloxacin HCl; Eudragit RS PO; Kollidon SR; xanthan gum. DOI: http://dx.doi.org/10.3329/dujps.v9i2.7893 Dhaka Univ. J. Pharm. Sci. 9(2): 97-102, 2010 (December)

scholarly journals FLOATING-BIOADHESIVE MATRIX TABLETS OF HYDRALAZINE HCL MADE OF CASHEW GUM AND HPMC K4M

2017 ◽  
Vol 9 (7) ◽  
pp. 124 ◽  
Author(s):  
M. Saquib Hasnain ◽  
Poonam Rishishwar ◽  
Sadath Ali
Keyword(s):  
Ex Vivo ◽  
Diffusion Mechanism ◽  
Hydroxypropyl Methylcellulose ◽  
Gastric Fluid ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Simulated Gastric Fluid ◽  
Cashew Gum ◽  
Gastro Retentive

Objective: The objective of this paper was to prepare and evaluate floating-bioadhesive cashew gum-hydroxypropyl methylcellulose (HPMC K4M) matrix tablets for the gastro-retentive release of hydralazine HCl.Methods: The cashew gum-HPMC K4M matrix tablets of hydralazine HCl were prepared by direct compression method with the incorporation of sodium bicarbonate and citric acid as effervescent agents. Drug contents, weight variations, hardness, friability, in vitro swelling, in vitro floatation, ex vivo mucoadhesion and in vitro drug release of these matrix tablets were evaluated.Results: Drug contents, weight variations, hardness and friability of these matrix tablets were within the compendia limits. These tablets were floated well in vitro over 12 h in simulated gastric fluid (SGF, pH 1.2) with minimum lag time. The ex vivo adhesion of these matrix tablets with goat intestinal mucosa exhibited good bioadhesion in a wash off test. All these cashew gum-HPMC K4M floating-bioadhesive matrix tablets of hydralazine HCl showed in vitro sustained releases of hydralazine HCl over 12 h in SGF, pH 1.2. The in vitro hydralazine HCl followed Korsmeyer-Peppas kinetic model and anomalous (non-Fickian) diffusion mechanism. The drug-polymer compatibility analysis by FTIR spectroscopy indicated the absence of any drug-polymer interaction within this cashew gum-HPMC K4M floating-bioadhesive matrix tablets of hydralazine HCl.Conclusion: The results clearly indicate a promising potential of the use of cashew gum as matrix forming a material with HPMC K4M to prepare matrix tablets for gastro retentive delivery of hydralazine HCl through the combined approach of floatation and bioadhesion to reduce the dosing rate with better patient compliances.

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.

Development and Evaluation of Controlled Release Mucoadhesive Tablets of Captopril

1970 ◽  
Vol 9 (3) ◽  
pp. 3318-3329
Author(s):  
Kranthi Kumar Kotta ◽  
L. Srinivas
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Xanthan Gum ◽  
Diffusion Mechanism ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Content Uniformity ◽  
In Vitro Drug Release ◽  
Mucoadhesive Tablets

The present investigation focuses on the development of mucoadhesive tablets of captopril which are designed to prolong the gastric residence time after oral administration. Matrix tablets of captopril were formulated using four mucoadhesive polymers namely guar gum, xanthan gum, HPMC K4M and HPMC K15M and studied for parameters such as weight variation, thickness, hardness, content uniformity, swelling index, mucoadhesive force and in vitro drug release. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M provide slow release of captopril over period of 12 hr and were found suitable for maintenance portion of oral controlled release tablets. The cumulative % of drug release of formulation F9 and F10 were 90 and 92, respectively. In vitro release from these tablets was diffusion controlled and followed zero order kinetics. The ‘n’ values obtained from the pappas-karsemeyer equation suggested that all the formulation showed drug release by non-fickian diffusion mechanism. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M (1:1) were established to be the optimum formulation with optimum bioadhesive force, swelling index & desired invitro drug release. This product was further subjected to stability study, the results of which indicated no significant change with respect to Adhesive strength and in vitro drug release study.

Formulation Development and Characterization of controlled release core in cup matrix tablets of venlafaxine HCl

2020 ◽  
Vol 15 ◽  
Author(s):  
Balaji Maddiboyina ◽  
Vikas Jhawat ◽  
Gandhi Sivaraman ◽  
Om Prakash Sunnapu ◽  
Ramya Krishna Nakkala ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Rate ◽  
Zero Order ◽  
Water Soluble ◽  
Matrix Tablets ◽  
Drug Dissolution ◽  
Crystalline Cellulose ◽  
Hydrophobic Polymers

Background: Venlafaxine HCl is a selective serotonin reuptake inhibitor which is given in the treatment of depression. The delivery of the drug at a controlled rate can be of great importance for prolonged effect. Objective: The objective was to prepare and optimize the controlled release core in cup matrix tablet of venlafaxine HCl using the combination of hydrophilic and hydrophobic polymers to prolong the effect with rate controlled drug release. Methods: The controlled release core in cup matrix tablets of venlafaxine HCl were prepared using HPMC K5, K4, K15, HCO, IPA, aerosol, magnesium sterate, hydrogenated castor oil and micro crystalline cellulose PVOK-900 using wet granulation technique. Total ten formulations with varying concentrations of polymers were prepared and evaluated for different physicochemical parameters such FTIR analysis for drug identification, In-vitro drug dissolution study was performed to evaluate the amount of drug release in 24 hrs, drug release kinetics study was performed to fit the data in zero order, first order, Hixson–crowell and Higuchi equation to determine the mechanism of drug release and stability studies for 3 months as observed. Results: The results of hardness, thickness, weight variation, friability and drug content study were in acceptable range for all formulations. Based on the In vitro dissolution profile, formulation F-9 was considered to be the optimized extending the release of 98.32% of drug up to 24 hrs. The data fitting study showed that the optimized formulation followed the zero order release rate kinetics and also compared with innovator product (flavix XR) showed better drug release profile. Conclusion: The core-in-cup technology has a potential to control the release rate of freely water soluble drugs for single administration per day by optimization with combined use of hydrophilic and hydrophobic polymers.

scholarly journals Formulation of Quaternized Aminated Chitosan Nanoparticles for Efficient Encapsulation and Slow Release of Curcumin

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 449
Author(s):  
Ahmed M. Omer ◽  
Zyta M. Ziora ◽  
Tamer M. Tamer ◽  
Randa E. Khalifa ◽  
Mohamed A. Hassan ◽  
...  
Keyword(s):  
Slow Release ◽  
Sodium Tripolyphosphate ◽  
Chitosan Nanoparticles ◽  
Gastric Fluid ◽  
Release Profile ◽  
Simulated Gastric Fluid ◽  
Maximum Value ◽  
Structure Surface ◽  
Drug Encapsulation Efficiency

An effective drug nanocarrier was developed on the basis of a quaternized aminated chitosan (Q-AmCs) derivative for the efficient encapsulation and slow release of the curcumin (Cur)-drug. A simple ionic gelation method was conducted to formulate Q-AmCs nanoparticles (NPs), using different ratios of sodium tripolyphosphate (TPP) as an ionic crosslinker. Various characterization tools were employed to investigate the structure, surface morphology, and thermal properties of the formulated nanoparticles. The formulated Q-AmCs NPs displayed a smaller particle size of 162 ± 9.10 nm, and higher surface positive charges, with a maximum potential of +48.3 mV, compared to native aminated chitosan (AmCs) NPs (231 ± 7.14 nm, +32.8 mV). The Cur-drug encapsulation efficiency was greatly improved and reached a maximum value of 94.4 ± 0.91%, compared to 75.0 ± 1.13% for AmCs NPs. Moreover, the in vitro Cur-release profile was investigated under the conditions of simulated gastric fluid [SGF; pH 1.2] and simulated colon fluid [SCF; pH 7.4]. For Q-AmCs NPs, the Cur-release rate was meaningfully decreased, and recorded a cumulative release value of 54.0% at pH 7.4, compared to 73.0% for AmCs NPs. The formulated nanoparticles exhibited acceptable biocompatibility and biodegradability. These findings emphasize that Q-AmCs NPs have an outstanding potential for the delivery and slow release of anticancer drugs.

scholarly journals FORMULATION AND EVALUATION OF SUSTAINED RELEASE MATRIX TABLET OF LORNOXICAM BY DIRECT COMPRESSION METHOD

2021 ◽  
Vol 10 (5) ◽  
pp. 131-136
Author(s):  
Asim pasha ◽  
C N Somashekhar
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Prolonged Release ◽  
Matrix Tablet ◽  
Direct Compression ◽  
Dissolution Profile ◽  
Drug Content

The aim of the present work was to develop sustained release Lornoxicam matrix tablets with polymers like HPMC K15M, Ethyl cellulose, and Crospovidone as carriers in varying quantities. Direct compression was used to make matrix tablets. Various assessment parameters, such as hardness, friability, thickness, percent drug content, weight variation, and so on, were applied to the prepared formulations. In vitro dissolution studies were carried out for 24 hrs. The tablets were subjected to in-vitro drug release in (pH 1.2) for first 2 hrs. Then followed by (pH 6.8) phosphate buffer for next 22 hrs. And the results showed that among the six formulations FL3 showed good dissolution profile to control the drug release respectively. The drug and polymer compatibility were tested using FT-IR spectroscopy, which revealed that the drug was compatible with all polymers. It is also required to design an appropriate prolonged release formulation for Lornoxicam in order to maintain the drug's release. Hence by using the compatible polymers sustained release tablets were formulated and subjected for various types of evaluation parameters like friability, hardness, drug content and dissolution behaviour. Finally, the findings reveal that the prepared sustained release matrix tablets of lornoxicam have improved efficacy and patient compliance.

Fusion as an Approach to Enhance Dissolution Rate of a Poorly Water-Soluble Drug (Curcurmin)

2011 ◽  
Vol 393-395 ◽  
pp. 119-122
Author(s):  
Dong Hua Wan ◽  
Fen Lin ◽  
Qu Xiang Liao
Keyword(s):  
Dissolution Rate ◽  
Drug Loading ◽  
Solid Dispersions ◽  
Gastric Fluid ◽  
Molecular State ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Simulated Gastric Fluid ◽  
Scanning Calorimetry ◽  
Rate Improvement

It’s well known that curcumin is practically insoluble in water. Therefore, to improve the drug dissolution rate, fusion approach was employed to prepare curcumin solid dispersions (SDs) in the carrier Pluronic F68 with three different drug loads. The dissolution rate of curcumin from the SDs was measured at simulated gastric fluid. The concentration of the dissolved drug in the medium was determined by HPLC. The dissolution rates of the formulations were dependent on the drug loading in SDs. 92.2% CUR was dissolved in 10 min from the SDs with 8.97% drug load, whereas the amounts of drug released were 65.8% and 84.2% within 120 min from the SDs with 18.9% and 29.0% drug loads, respectively. The Fourier transform infrared spectra indicated hydrogen bond between the drug and carrier. Furthermore, their physicochemical properties were well investigated using differential scanning calorimetry and X-ray diffraction. In the dispersions containing 8.97% CUR, the drug was in the molecular state. At a composition of approximately 18.9%, CUR was dispersed as micro-fine crystals. These interesting results indicate that the physical states of the drug in the carrier, which are governed by the drug loading, can affect the dissolution rate improvement.

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