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 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: 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

Controlled Release of Metformin Hydrochloride I. In vitro Release from Physical Mixture Containing Xanthan Gum as Hydrophilic Rate Retarding Polymer

1970 ◽  
Vol 4 (1) ◽  
Author(s):  
Mashkura Ashrafi ◽  
Jakir Ahmed Chowdhury ◽  
Md Selim Reza
Keyword(s):  
Controlled Release ◽  
Xanthan Gum ◽  
In Vitro Release ◽  
Correlation Coefficients ◽  
High Ratio ◽  
Water Soluble ◽  
Metformin Hydrochloride ◽  
Model Drug ◽  
Very High

Capsules of different formulations were prepared by using a hydrophilic polymer, xanthan gum and a filler Ludipress. Metformin hydrochloride, which is an anti-diabetic agent, was used as a model drug here with the aim to formulate sustained release capsules. In the first 6 formulations, metformin hydrochloride and xanthan gum were used in different ratio. Later, Ludipress was added to the formulations in a percentage of 8% to 41%. The total procedure was carried out by physical mixing of the ingredients and filling in capsule shells of size ‘1’. As metformin hydrochloride is a highly water soluble drug, the dissolution test was done in 250 ml distilled water in a thermal shaker (Memmert) with a shaking speed of 50 rpm at 370C &plusmn 0.50C for 6 hours. After the dissolution, the data were treated with different kinetic models. The results found from the graphs and data show that the formulations follow the Higuchian release pattern as they showed correlation coefficients greater than 0.99 and the sustaining effect of the formulations was very high when the xanthan gum was used in a very high ratio with the drug. It was also investigated that the Ludipress extended the sustaining effect of the formulation to some extent. But after a certain period, Ludipress did not show any significant effect as the pores made by the xanthan gum network were already blocked. It is found here that when the metformin hydrochloride and the xanthan gum ratio was 1:1, showed a high percentage of drug release, i.e. 91.80% of drug was released after 6 hours. But With a xanthan gum and metformin hydrochloride ratio of 6:1, a very slow release of the drug was obtained. Only 66.68% of the drug was released after 6 hours. The percent loading in this case was 14%. Again, when Ludipress was used in high ratio, it was found to retard the release rate more prominently. Key words: Metformin Hydrochloride, Xanthan Gum, Controlled release capsule Dhaka Univ. J. Pharm. Sci. Vol.4(1) 2005 The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website

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 Antimicrobial Properties and Release Profile of Ampicillin from Electrospun Poly(εepsilon;-caprolactone) Nanofiber Yarns

2010 ◽  
Vol 5 (4) ◽  
pp. 155892501000500 ◽  
Author(s):  
Hang Liu ◽  
Karen K. Leonas ◽  
Yiping Zhao
Keyword(s):  
In Vitro Release ◽  
Antimicrobial Properties ◽  
Fiber Surface ◽  
Electrospun Nanofibers ◽  
Release Profile ◽  
Burst Release ◽  
Spun Yarns ◽  
Surgical Sutures ◽  
Release Model

Poly(εepsilon;-caprolactone) (PCL) electrospun fibers containing ampicillin sodium salt have been produced and twisted into nanofiber yarns. The fiber diameters and crystallinity, the in vitro antimicrobial properties of the yarns, and the in vitro release of ampicillin from yarns containing various ampicillin concentrations are studied. Decreased fiber diameters and reduced diameter variation are observed with the addition of ampicillin salt into the polymer solution. The results from the zone of inhibition test of the yarns against both gram-positive Staphylococcus aureus and gram-negative Klebsiella pneumoniae indicate that the released ampicillin retains its effectiveness after the production processes, therefore the as-spun yarns are antimicrobial active. A burst release of ampicillin from the yarns has been observed in the first hour, and the release is almost completed in 96 hours. The burst release is believed to be due to the low compatibility of ampicillin with PCL, the accumulation of ampicillin on fiber surface and the small fiber diameters. An empirical release model is developed to describe the release profile. The results indicate that the electrospun nanofibers yarns will have a great potential to be used for biomaterials, such as surgical sutures, to decrease the surgical site infection rate.

scholarly journals DESIGN AND IN VITRO/IN VIVO EVALUATION OF EXTENDED RELEASE MATRIX TABLETS OF NATEGLINIDE

2018 ◽  
Vol 7 (6) ◽  
Author(s):  
Mohini Sihare ◽  
Rajendra Chouksey
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Release Profile ◽  
Matrix Tablets ◽  
In Vivo Studies ◽  
Release Mechanism ◽  
In Vivo Evaluation

Aim: Nateglinide is a quick acting anti-diabetic medication whose potent activity lasts for a short duration. One of the dangerous side effects of nateglinide administration is rapid hypoglycemia, a condition that needs to be monitored carefully to prevent unnecessary fatalities. The aim of the study was to develop a longer lasting and slower releasing formulation of nateglinide that could be administered just once daily. Methods: Matrix tablets of nateglinide were prepared in combination with the polymers hydroxypropylmethylcellulose (HPMC), eudragits, ethyl cellulose and polyethylene oxide and the formulated drug release patterns were evaluated using in vitro and in vivo studies. Conclusion: Of the seventeen formulated matrix tablets tested, only one formulation labelled HA-2 that contained 15% HPMC K4M demonstrated release profile we had aimed for. Further, swelling studies and scanning electron microscopic analysis confirmed the drug release mechanism of HA-2. The optimized formulation HA-2 was found to be stable at accelerated storage conditions for 3 months with respect to drug content and physical appearance. Mathematical analysis of the release kinetics of HA-2 indicated a coupling of diffusion and erosion mechanisms. In-vitro release studies and pharmacokinetic in vivo studies of HA-2 in rabbits confirmed the sustained drug release profile we had aimed for. Keywords: Hydroxypropylmethylcellulose, Matrix tablets, Nateglinide, Sustained release

Drug release profile and reduction in the in vitro burst release from pectin/HEMA hydrogel nanocomposites crosslinked with titania

RSC Advances ◽  
2016 ◽  
Vol 6 (23) ◽  
pp. 19060-19068 ◽  
Author(s):  
Elisangela P. da Silva ◽  
Marcos R. Guilherme ◽  
Francielle P. Garcia ◽  
Celso V. Nakamura ◽  
Lucio Cardozo-Filho ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Profile ◽  
Burst Release ◽  
Drug Release Profile ◽  
Initial Release ◽  
Hydrogel Nanocomposites

Hydrogel nanocomposites of pectin, HEMA and titania for Vit-B12 controlled release with reduced initial release burst were prepared. A reduction of up to ca. 60% was observed.

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