Formulation and Evaluation of colon targeted drug Delivery of Diloxanide furoate Tablets using pH Dependent Polymers

Author(s):  
Pavankumar Krosuri ◽  
Ravikumar K. ◽  
Priyanka S.N. ◽  
G.Anjana Devi ◽  
Lakshmiprasanna S. ◽  
...  

Diloxanide Furoate is a Dichloroacetamide derivative utilized for the treatment of various protozoal infections like amoebiasis. Colon targeted tablets were designed using pH sensitive polymers like Eudragit S100, Eudragit L 100,Cellulose acetate phthallate at different concentrations. All the matrix,compression coated formulations showed the desired physicochemical properties as per the official limits. The drug release studies were performed according to the USP paddle method by using 0.1N HCL for 2 hours, pH 7.4 phosphate buffer for 3 hours and pH 6.8 phosphate buffer upto 18 hours. A better controlled drug release was shown for Eudragit L 100. Based on the comparative drug release studies among different Formulations F9 with Eudragit L 100 polymer showed better control drug release. The release kinetics for the Optimised Formulation F9 was calculated and “r2” value was more for Zero order kinetics i.e.,0.970 indicating that the formulation doesnot depend upon its concentration and from the Korsmeyer peppas model the diffusion exponent value “n” is > 1 indicating that it follows super case II transport mechanism. The accelerated stability studies conducted for optimised formulation F9 for 3 months have no significant variation.

1970 ◽  
Vol 8 (1) ◽  
pp. 31-38 ◽  
Author(s):  
Mohammad Nezab Uddin ◽  
Ishtiaq Ahmed ◽  
Monzurul Amin Roni ◽  
Muhammad Rashedul Islam ◽  
Mohammad Habibur Rahman ◽  
...  

The objective of this study was to design oral sustained release matrix tablets of Ranolazine usinghydroxypropyl methylcellulose (HPMC) as the retardant polymer and to study the effect of formulation factors suchas polymer proportion and polymer viscosity on the release of drug. In vitro release studies were performed usingUSP type II apparatus (paddle method) in 900 mL of 0.1N HCl at 100 rpm for 12 hours. The release kinetics wasanalyzed using the zero-order, first order, Higuchi and Korsmeyer-Peppas equations to explore and explain themechanism of drug release from the matrix tablets. In vitro release studies revealed that the release rate decreasedwith increase in polymer proportion and viscosity grade. Mathematical analysis of the release kinetics indicated thatthe nature of drug release from the matrix tablets was dependent on drug diffusion and polymer relaxation andtherefore followed non-Fickian or anomalous release. The developed controlled release matrix tablets of Ranolazineprepared with high viscosity HPMC extended release up to 12 hours.Key words: Ranolazine; Sustained release; Methocel E50 Premium LV; Methocel K100LV CR; Methocel K4M CR;Methocel K15M CR.DOI: 10.3329/dujps.v8i1.5333Dhaka Univ. J. Pharm. Sci. 8(1): 31-38, 2009 (June)


Polymers ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 691
Author(s):  
O. Sánchez-Aguinagalde ◽  
Ainhoa Lejardi ◽  
Emilio Meaurio ◽  
Rebeca Hernández ◽  
Carmen Mijangos ◽  
...  

Chitosan (CS) and poly (vinyl alcohol) (PVA) hydrogels, a polymeric system that shows a broad potential in biomedical applications, were developed. Despite the advantages they present, their mechanical properties are insufficient to support the loads that appear on the body. Thus, it was proposed to reinforce these gels with inorganic glass particles (BG) in order to improve mechanical properties and bioactivity and to see how this reinforcement affects levofloxacin drug release kinetics. Scanning electron microscopy (SEM), X-ray diffraction (XRD), swelling tests, rheology and drug release studies characterized the resulting hydrogels. The experimental results verified the bioactivity of these gels, showed an improvement of the mechanical properties and proved that the added bioactive glass does affect the release kinetics.


Author(s):  
DHARMENDER PALLERLA ◽  
SUMAN BANOTH ◽  
SUNKARI JYOTHI

Objective: The objective of this study was to formulate and evaluate the Curcumin (CUR) encapsulated sodium alginate (SA)/badam gum (BG)/kaolin (KA) microbeads for controlled drug release studies. Methods: The fabricated microbeads were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), X-ray diffraction (X-RD), and scanning electron microscopy (SEM). Dynamic swelling studies and in vitro release kinetics were performed in simulated intestinal fluid (pH 7.4) and simulated gastric fluid (pH 1.2) at 37 °C. Results: FTIR confirms the formation of microbeads. DSC studies confirm the polymorphism of CUR in drug loaded microbeads which indicate the molecular level dispersion of the drug in the microbeads. SEM studies confirmed the microbeads are spherical in shape with wrinkled and rough surfaces. XRD studies reveal the molecular dispersion of CUR and the presence of KA in the developed microbeads. In vitro release studies and swelling studies depend on the pH of test media, which might be suitable for intestinal drug delivery. The % of drug release values fit into the Korsmeyer-Peppas equation and n values are obtained in the range of 0.577-0.664, which indicates that the developed microbeads follow the non-Fickian diffusion drug release mechanism. Conclusion: The results concluded that the CUR encapsulated microbeads are potentially good carriers for controlled drug release studies.


INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (10) ◽  
pp. 38-43
Author(s):  
Ch. Taraka Ramarao ◽  
◽  
B. Srinivasa Rao ◽  
J. Vijayaratana

Matrix Tablets, each containing 50 mg of diclofenac sodium, are prepared employing Kollidon SR by direct compression method. All the tablets were found to be non-disintegrating in acidic (pH1.2) and alkaline (pH 7.4) fluids. As such, the prepared tablets were of good quality with respect to drug content, hardness and friability. As the tablets formulated were non- disintegrating in acidic fluids, they are considered suitable for colon targeting. From the drug release study, it may be concluded that the (DK2) E2 formula of diclofenac sodium matrix tablets gives the desired release profile by showing a minimal release during the lag period of 5 h and complete release at the end of 12 h. The tablets having the optimised formula (DK2)E2, having 25% Kollidon SR with 5% of channelling agent (Eudragit S100 to that of Kollidon SR) showed minimal release of 27. 4% in the lag period of 5 hours and 99.3 % of the drug was released y the end of 12 h. The diclofenac sodium matrix tablets formulated by employing Kollidon SR and various channelling agents showed non-Fickian diffusion mechanism and followed zero order kinetics. The optimized formula (DK2) E2 follows Supercase II transport as mechanism for drug release and it follows zero order kinetics. Matrix tablets (DK2) E2 formulated employing 25% Kollidon SR and 5% Eudragit S100 are best suited to be used for colon targeting of diclofenac sodium.


2018 ◽  
Vol 5 (1) ◽  
pp. 1 ◽  
Author(s):  
Jessica Oliveira ◽  
Raquel Rodrigues ◽  
Lillian Barros ◽  
Isabel Ferreira ◽  
Luís Marchesi ◽  
...  

In this study, hydrophilic magnetic nanoparticles were synthesized by green routes using a methanolic extract of Rubus ulmifolius Schott flowers. The prepared magnetic nanoparticles were coated with carbon-based shell for drug delivery application. The nanocomposites were further chemically functionalized with nitric acid and, sequentially, with Pluronic® F68 (CMNPs-plur) to enhance their colloidal stability. The resulting material was dispersed in phosphate buffer solution at pH 7.4 to study the Doxorubicin loading. After shaking for 48 h, 99.13% of the drug was loaded by the nanocomposites. Subsequently, the drug release was studied in different working phosphate buffer solutions (i.e., PB pH 4.5, pH 6.0 and pH 7.4) to determine the efficiency of the synthesized material for drug delivery as pH-dependent drug nanocarrier. The results have shown a drug release quantity 18% higher in mimicking tumor environment than in the physiological one. Therefore, this study demonstrates the ability of CMNPs-plur to release a drug with pH dependence, which could be used in the future for the treatment of cancer "in situ" by means of controlled drug release.


2018 ◽  
Vol 42 (14) ◽  
pp. 11964-11971 ◽  
Author(s):  
U. T. Uthappa ◽  
G. Sriram ◽  
Varsha Brahmkhatri ◽  
Madhuprasad Kigga ◽  
Ho-Young Jung ◽  
...  

An alternative facile approach for the surface modification of naturally available diatoms with xerogel for controlled drug release applications.


Author(s):  
AKPABIO E. I. ◽  
EFFIONG D. E. ◽  
UWAH T. O. ◽  
SUNDAY N. I.

Objective: This study was undertaken to formulate a floating drug delivery system of theophylline hydrochloride using different concentrations of a chosen polymer and then investigate how polymer concentration affects buoyancy and drug release properties of the tablets. Methods: Hydroxypropyl methylcellulose (HPMC) at different concentration levels of 15% (F1), 20% (F2) and 30% (F3) was used to form the three formulation batches of floating tablets. Wet granulation method was used for the granule preparation while Sodium bicarbonate and citric acid were used as the gas generating agent. The physical properties of the granules and the floating tablets were evaluated. Also determined were the physicomechanical properties, buoyancy and swelling characteristics of the tablets. The in vitro drug release study was carried out according to the USP I (basket method) for 8h in 900 ml 0.1N HCl at 50 rpm. Samples withdrawn at the regular predetermined time were analyzed spectrophotometrically at a wavelength of 271 nm and data obtained statistically analyzed by one-way analysis of variance (ANOVA). The differences between means were considered significant at P<0.05. Results: The result showed that polymer (HPMC) concentration significantly (p>0.05) increased swelling index and improved floating lag time, it had no significant effect on the total floating time. Percentage drug release at the end of 8 h was 100%, 98.2% and 96.13% for formulation F1, F2 and F3, respectively. All three formulations followed the Higuchi drug release kinetics model and the mechanism of drug release was the non Fickian diffusion with exponents of 0.46, 0.51 and 0.56 for the respective batch. Conclusion: Batch F3 gave a better-controlled drug release and floating properties in comparison to batch F1 and F2 thus Polymer concentration influenced the onset of floating and controlled the release of Theophylline.


2014 ◽  
Vol 2014 ◽  
pp. 1-6 ◽  
Author(s):  
Takashi Sasaki ◽  
Hiroaki Matsuura ◽  
Kazuki Tanaka

Porous polymer spheres are promising materials as carriers for controlled drug release. As a new drug-carrier material, blend particles composed of poly(L-lactic acid) (PLLA) and rifampicin were developed using the freeze-drying technique. The blend particles exhibit high porosity with a specific surface area of 10–40 m2 g−1. Both the size and porosity of the particles depend on the concentration of the original solution and on the method of freezing. With respect to the latter, we used the drop method (pouring the original solution dropwise into liquid nitrogen) and the spray method (freezing a mist of the original solution). The release kinetics of rifampicin from the blend particles into water depends significantly on the morphology of the blend particles. The results show that the release rate can be controlled to a great extent by tuning the size and porosity of the blend particles, both of which are varied by parameters such as the solution concentration and the method of freezing.


2016 ◽  
Vol 4 (23) ◽  
pp. 4156-4163 ◽  
Author(s):  
Jianmin Yang ◽  
Daisuke Katagiri ◽  
Sifeng Mao ◽  
Hulie Zeng ◽  
Hizuru Nakajima ◽  
...  

A thermoresponsive polymer microcapsule with a hollow core–porous shell structure was fabricated based on inkjet printing, which can be used to control drug release by changing the temperature at around 38 °C.


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