scholarly journals Formulation Development and Evaluation of Drug Release Kinetics from Colon-Targeted Ibuprofen Tablets Based on Eudragit RL 100-Chitosan Interpolyelectrolyte Complexes

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Kenneth Chibuzor Ofokansi ◽  
Franklin Chimaobi Kenechukwu

Colon-targeted drug delivery systems (CTDDSs) could be useful for local treatment of inflammatory bowel diseases (IBDs). In this study, various interpolyelectrolyte complexes (IPECs), formed between Eudragit RL100 (EL) and chitosan (CS), by nonstoichiometric method, and tablets based on the IPECs, prepared by wet granulation, were evaluated as potential oral CTDDSs for ibuprofen (IBF). Results obtained showed that the tablets conformed to compendial requirements for acceptance and that CS and EL formed IPECs that showed pH-dependent swelling properties and prolonged the in vitro release of IBF from the tablets in the following descending order: 3 : 2 > 2 : 3 > 1 : 1 ratios of CS and EL. An electrostatic interaction between the carbonyl (–CO–) group of EL and amino (–) group of CS of the tablets formulated with the IPECs was capable of preventing drug release in the stomach and small intestine and helped in delivering the drug to the colon. Kinetic analysis of drug release profiles showed that the systems predominantly released IBF in a zero-order manner. IPECs based on CS and EL could be exploited successfully for colon-targeted delivery of IBF in the treatment of IBDs.

Author(s):  
Nani Tadhi ◽  
Himansu Chopra ◽  
Gyanendra Kumar Sharma

Transdermal patch is a drug delivery device in which the drugs are incorporated and is design in such a way that it releases the drug in sustained and at predetermined rate to deliver the drug through the skin to the systemic circulation painlessly. The aim of this research study was to formulate a controlled and sustained release transdermal matrix type patch of Methimazole. The matrix patch was prepared by solvent casting method using a various polymer in different concentration, HPMC (hydrophilic), Eudragit RL100 and Ethyl cellulose (hydrophobic) polymer. Total 9 prototype formulation were prepared and it was subjected for various evaluation test; weight uniformity, Folding endurance, thickness, Drug content, percent moisture content, percent Moisture uptake and In-vitro drug release study using Franz diffusion cell. The in-vitro CDR% data was fit into kinetics model to see the release kinetics from the patches. The Formulation F5 was choosen as a best formulation according to in-vitro drug release study. The in-vitro release was found 81.12 % in 12 hours, it followed zero order kinetics. The nature of polymer and concentration ratio of polymers plays a crucial role for obtaining a good transdermal patch design; therefore optimisation is very important step to formulate a desired TDDS. Therefore the result of the study encourages a further study and is hopeful that the present study would contribute to the recent pharmaceutical research for formulation development.


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.


Author(s):  
P. Amsa ◽  
G. K. Mathan ◽  
S. Magibalan ◽  
E. K. Velliyangiri ◽  
T. Kalaivani ◽  
...  

The major goal of this study was to develop and evaluate Sustained release matrix tablets of Gabapentin with Hibiscus rosa - sinensis leaves mucilage prepared by using wet granulation technique with microcrystalline cellulose as a diluents and magnesium stearate as a lubricant. Pre-compression and post-compression evaluation of physicochemical parameters were carried out and to be within acceptable limits. Drug and polymer compatibility were validated by FTIR measurements. Further, tablets were evaluated for in vitro release study. To get the sustained release of Gabapentin, the concentration of Hibiscus rosa- sinensis mucilage was tuned with a gas-generating agent. The % drug release of all formulation from F1 to F5 showed 91.24%, 80.24%, 70.53%, 62.12% and 49.83% respectively. All the dosage form release kinetics was computed using zero order, first order, Higuchi, and Korsmeyer–Peppas methods. From the above results, it is concluded that the n value of formulation F5 showed 0.78 suggesting anomalous (non-fickian) behavior of the drug. Mucilage from the leaves of Hibiscus rosa-sinensis has a great retarding effect in drug release from sustained release tablets.


2020 ◽  
Vol 10 (5) ◽  
pp. 149-158
Author(s):  
Pintu Dhar ◽  
Himangshu Sarma ◽  
Hemanta Kumar Sharma

Background: The solid oral dosage forms containing bitter drugs need improved palatability for administration. Formulation scientists have given attention to the improvement of taste masking technologies and utilised various strategies. Objective: The present work aimed to mask the bitter taste of Promethazine Hydrochloride by formulating Oral Dispersible Tablets using Okra mucilage as a taste-masking agent.  Methods: The Okra mucilage was extracted from Okra by the aqueous extraction process. An emulsion solvent diffusion technique was used for masking the bitter taste of Promethazine Hydrochloride by using Okra mucilage. The Oral Dispersible Tablet was prepared by the wet granulation method. The mucilage and the formulation were characterized and evaluated by standard methods and protocols. Results: Taste masking of the bitter drug was successfully achieved by Okra mucilage. The DSC and FTIR study revealed that the drug molecule was compatible with okra mucilage and drug entrapment efficacy was found to be 94.76%. The palatability test asserted that masking of the bitter taste of the drug.  The In vitro drug release study showed that the F7 tablet batch has a better drug release rate and followed non- fickian mechanism of drug release. Conclusion: Thus, taste masking with Okra mucilage was successful and this opens opportunities for application of common edible substances in formulation development. Keywords: Fast disintegrating tablet; Natural polymer; Mouth dissolving tablet; Promethazine Hydrochloride; Taste masking


2020 ◽  
Vol 13 (3) ◽  
pp. 172-179
Author(s):  
Dharmendra Solanki ◽  
Mohit Motiwale ◽  
Sujata Mahapatra

Sustained-release (SR) matrix tablets of Acyclovir and polysaccharide isolated from corms of Colocasia esculenta, at different drug to polymer ratios, were prepared by using wet granulation method. The formulated tablets were also characterized by physical and chemical parameters and results were found in acceptable limits. The investigation focuses on the influence of the proportion of the matrix material on the mechanism and the release rate of the drug from the tablets. In vitro drug release appears to occur both by diffusion and a swelling-controlled mechanism, indicates the drug release from the tablet was non-Fickian super case II transport. The drug release data fit well to the Zero-order drug release Model and the Korsmeyer equation.


Author(s):  
Swapna Velivela ◽  
Nikunja B Pati ◽  
B. Ravindra Babu

Temozolomide is an anti-cancer drug; it was encapsulated in liposomal intravenous application. To avoid the side effects and to target the drug to the specific site, we have formulated liposomal formulation of Temozolomide. The liposomal were prepared by dried thin film hydration technique using rotary evaporator with drug and Soya phosphatidyl choline as carrier. The prepared liposomes were characterized for size, shape, % entrapment efficiency, in-vitro drug release and physical stability. The evaluated batches showed good physicochemical characteristics. The maximum encapsulation efficiency of Temozolomide was achieved with formulation TMZ 6 with 40.19% and the in-vitro drug release is 64.94%. Based on the results it can be concluded that TMZ 6 was selected as optimized formulation and the optimized formulation Optimized formulation follows zero order release kinetics and follow super case II transport when it applied to Korsmeyer-Pepps model for mechanism of drug release.


INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (08) ◽  
pp. 67-70
Author(s):  
S. R. Baratam ◽  
◽  
V. R. Jayanthi

Gastro floating drug delivery system (GFDDS) of Levofloxacin hemihydrate (LVF), category of Quinoline antibiotic used to treat Helicobacter pylori infection. The aim of the study was to develop a Floating matrix system (FDDS) of LVF for sustained release to improve the extended retention in stomach and local site specific action in the stomach. Preparation of LVF tablets using wet granulation method using HPMC K4M with Sodium bicarbonate as effervescent agent. All formulations were developed and evaluated for Floating properties for swelling characteristics and in vitro drug release studies. In vitro drug release were performed and drug release kinetics were evaluated by using linear regression method and was found to be follow zero order release with diffusion controlled release. Optimized formula was found to be LFTA4 with 20% of polymer with 99.03% of drug release with 12 hours of Floating time and 32 seconds floating lag time. The obtained FT-IR charts indicated that there is no positive evidence for the interaction between LVF and ingredients of the optimized formula.


2021 ◽  
Vol 11 (5-S) ◽  
pp. 108-112
Author(s):  
, Sonam ◽  
Nilesh Jain ◽  
Jitendra Banveer

The goal of this study is to develop a long-acting Lansoprazole delivery system. Lansoprazole belongs to a class of antisecretory drugs known as substituted benzimidazoles, which decrease gastric acid secretion by inhibiting the (H+,K+)-ATPase enzyme system at the secretory membrane of the stomach parietal cell. Due to its mechanism of action, despite its short half-life of 1-5 hours, it can effectively block acid secretion for 24 hours. However, as his plasma concentration falls, the effect will diminish. Lansoprazole will be given as a sustained release tablet to avoid multiple dosing or to reduce the frequency of dose. Lansoprazole was produced and analysed utilizing natural and synthetic polymers such as Xanthan gum, Gellan gum, Carbopol 940 P, and Chitosan. Based on the findings of this experiment, it was determined that formulation F7 demonstrated sustained drug release for up to 12 hours in all developed formulations. Formulation (F1, F2, F3, F4, F5, and F6) were tested in vitro for drug release. For the improved formulation F7, the formulation and release kinetics were estimated. When the regression coefficient values of were evaluated, it was found that Peppas had the highest ‘r2' value, 0.952, indicating that drug release from formulations followed Peppas release kinetics. Key words: Lansoprazole, Sustain release tablets, Synthetic and Natural Polymers, formulation, evaluation


Author(s):  
D. Avinash ◽  
Madhu Gudipati ◽  
M. V. Ramana ◽  
Pallavi Vadlamudi ◽  
Rama Rao Nadendla

To formulate and evaluate the mouth dissolving tablet dosage forms of favipiravir using various superdisintegrants by using wet granulation technique. Batches of favipiravir Mouth dissolving tablets were formulated by using the wet granulation technique. The formulated granules were evaluated for their flow properties as a pre-compression parameter and the friability, hardness, disintegration, wetting ratio, wetting time, dissolution, and drug release parameters were evaluated as post-compression parameters. The effect of the varying concentrations of superdisintegrants on the formulation for disintegration time was ascertained and the results were compared. The tablet had friability and hardness values ranging from 0.60  to 0.68 % and 3.9  to 4.3 (kg/cm2). Tablet weights did not vary significantly but the disintegration time varied from 44.66  to 142.66±2.51 min and the wetting time varied from 45.33  to 144 min and the optimal batch of tablets shows a drug release of 98.8% within 60 min and first-order release kinetics of the formulations are compared.


2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Shikha Bhalla ◽  
Manju Nagpal

The aim of the current research work was to prepare and evaluate different generations of superporous hydrogels (SPH) of acrylamide and chitosan using gas blowing technique and evaluate them for swelling, mechanical properties, FTIR, SEM, XRD, and in vitro drug release. The ingredients used were acrylamide, N,N′-methylene bisacrylamide, chitosan, Pluronic F127, ammonium per sulfate-N,N,N′,N′-tetramethylenediamine, and sodium bicarbonate. All ingredients were mixed sequentially with thorough stirring. The effect of different drying conditions on properties of SPH was also evaluated. Ethanol treated batched showed maximum swelling properties due to uniform pores as indicated in SEM studies. Equilibrium swelling time was less than 10 min in all batches. Freeze drying led to lowering of density which is also supported by porosity and void fraction data. Maximum mechanical strength was found in superporous hydrogel interpenetrating networks due to crosslinked polymeric network. 70% drug was released at the end of 2 h, and further the release was sustained till the end of 24 h. In vitro drug release kinetics showed that drug release occurs by diffusion and follows Super Case II transport indicating that mechanism of drug release is not clear. Superporous hydrogel interpenetrating networks can be successfully used as sustained release gastroretentive devices.


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