Evaluation of Curcuminoids Effervescent Floating Tablets

2014 ◽  
Vol 1060 ◽  
pp. 25-28
Author(s):  
Sakonjan Treesinchai ◽  
Satit Puttipipatkhachorn ◽  
Tasana Pitaksuteepong ◽  
Srisagul Sungthongjeen
Keyword(s):  
Drug Release ◽  
Sodium Lauryl Sulfate ◽  
Hydroxypropyl Methylcellulose ◽  
Protective Layer ◽  
Lauryl Sulfate ◽  
Floating Tablets ◽  
Floating Tablet ◽  
Core Tablet ◽  
Formulation Variables ◽  
Reduced Time

The objective of this study was to develop and evaluate curcuminoids effervescent floating tablet. The system consists of a curcuminoids-containing core tablet coated with a gas forming layer (tartaric acid layer and sodium bicarbonate layer divided by a protective layer (hydroxypropyl methylcellulose)) and a gas-entrapped membrane (Eudragit® RL 30D), respectively. The floating tablets using lactose as a filler showed higher drug release than those using microcrystalline cellulose (MCC) or MCC:lactose as a filler. However, type of core tablet fillers did not affect time to float of the floating tablets in 0.1 N HCl. Increasing amount of gas forming agent reduced time to float and increased drug release from the floating tablets. The floating tablets showed good floating properties in 0.1 N HCl, however, curcuminoids released was very slow. Addition of surfactant (1%w/v sodium lauryl sulfate (SLS)) in 0.1 N HCl could improve drug release of the floating tablets but it increased time to float and caused the floating tablet ruptured. The floating properties and drug release from curcuminoids effervescent floating tablets seemed to depend on formulation variables. The higher coating level or another type of gas-entrapped membrane may be need for further study.

Design of Floating HPMC Matrix Tablets: Effect of Formulation Variables on Floating Properties and Drug Release

2011 ◽  
Vol 311-313 ◽  
pp. 1140-1143
Author(s):  
Srisagul Sungthongjeen ◽  
Pornsak Sriamornsak ◽  
Satit Puttipipatkhachorn
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Hydraulic Press ◽  
Matrix Tablets ◽  
Compression Force ◽  
Lower Viscosity ◽  
Floating Tablet ◽  
Tablet Formulations ◽  
Model Drug ◽  
Formulation Variables

Floating matrix tablets were designed and evaluated. Theophylline was used as a model drug. The system was prepared by mixing drug, matrix-forming polymer (hydroxypropyl methylcellulose, HPMC) and fillers together. The blended powder was compressed by hydraulic press. The effect of formulation variables such as type of matrix forming polymer (HPMC K100LV, HPMC K4M, HPMC K100M), amount of effervescent agent (0, 20, 30, 40% w/w) and compression force (0.5, 1 ton) on floating properties and drug release of floating matrix tablets were investigated. The results demonstrated that type of polymer affected floating properties of the floating matrix tablets. The floating matrix tablets prepared from lower viscosity HPMC (HPMC K100LV) showed faster drug release than those prepared from higher viscosity HPMC (HPMC K4M, HPMC K100M). Increasing amount of effervescent agent decreased time to float and increased drug release from the floating matrix tablets. Higher compression force did not affect time to float but decreased drug release from the floating matrix tablets. According to these results, floating properties and drug release of the floating matrix tablets could be modified by formulation variables. Some floating tablet formulations developed in this study showed good floating properties (time to float less than 15 minutes, floating time more than 8 hours) with sustained release as required. The system is promising as a carrier for gastroretentive drug delivery systems.

Preparation and Evaluation of Gemifloxacin Mesylate Floating Matrix Tablets in Healthy Human Volunteers

2017 ◽  
Vol 10 (1) ◽  
pp. 3623-3630
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Haarika B ◽  
Jyothi Sri S ◽  
K Abbulu
Keyword(s):  
Drug Release ◽  
Sodium Bicarbonate ◽  
Polymer Concentration ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
Physical Parameters ◽  
Drug Bioavailability ◽  
Floating Tablets

The purpose of present investigation was to develop floating matrix tablets of gemifloxacin mesylate, which after oral administration could prolong the gastric residence time, increase the drug bioavailability and diminish the side effects of irritating drugs. Tablets containing drug, various viscosity grades of hydroxypropyl methylcellulose such as HPMC K4M and HPMC K15M as matrix forming agent, Sodium bicarbonate as gas-forming agent and different additives were tested for their usefulness in formulating gastric floating tablets by direct compression method. The physical parameters, in vitro buoyancy, release characteristics and in vivo radiographic study were investigated in this study. The gemifloxacin mesylate floating tablets were prepared using HPMC K4M polymer giving more sustained drug release than the tablet containing HPMC K15M. All these formulations showed floating lag time of 30 to 47 sec and total floating time more than 12 h. The drug release was decreased when polymer concentration increases and gas generating agent decreases. Formulation that contains maximum concen-tration of both HPMC K15M and sodium bicarbonate (F9) showing sufficiently sustained with 99.2% of drug release at 12 h. The drug release from optimized formulation follows Higuchi model that indicates the diffusion controlled release. The best formulation (F9) was selected based on in vitro characteristics and used in vivo radiographic studies by incorporating barium sulphate as a radio-opaque agent and the tablet remained in the stomach for about 6 h.   

scholarly journals Formulation and evaluation of effervescent floating tablets of tizanidine hydrochloride

2011 ◽  
Vol 61 (2) ◽  
pp. 217-226 ◽  
Author(s):  
Komuravelly Someshwar ◽  
Kalyani Chithaluru ◽  
Tadikonda Ramarao ◽  
K. Kumar
Keyword(s):  
Drug Release ◽  
Residence Time ◽  
Release Kinetics ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
Physical Parameters ◽  
Floating Tablets ◽  
Gastric Residence Time

Formulation and evaluation of effervescent floating tablets of tizanidine hydrochloride Tizanidine hydrochloride is an orally administered prokinetic agent that facilitates or restores motility through-out the length of the gastrointestinal tract. The objective of the present investigation was to develop effervescent floating matrix tablets of tizanidine hydrochloride for prolongation of gastric residence time in order to overcome its low bioavailability (34-40 %) and short biological half life (4.2 h). Tablets were prepared by the direct compression method, using different viscosity grades of hydroxypropyl methylcellulose (HPMC K4M, K15M and K100M). Tablets were evaluated for various physical parameters and floating properties. Further, tablets were studied for in vitro drug release characteristics in 12 hours. Drug release from effervescent floating matrix tablets was sustained over 12 h with buoyant properties. DSC study revealed that there is no drug excipient interaction. Based on the release kinetics, all formulations best fitted the Higuchi, first-order model and non-Fickian as the mechanism of drug release. Optimized formulation (F9) was selected based on the similarity factor (f2) (74.2), dissolution efficiency at 2, 6 and 8 h, and t50 (5.4 h) and was used in radiographic studies by incorporating BaSO4. In vivo X-ray studies in human volunteers showed that the mean gastric residence time was 6.2 ± 0.2 h.

scholarly journals FORMULATION AND IN-VITRO EVALUATION OF THEOPHYLLINE HYDROCHLORIDE EFFERVESCENT FLOATING TABLETS: EFFECT OF POLYMER CONCENTRATION ON TABLET BUOYANCY

2019 ◽  
pp. 59-65
Author(s):  
AKPABIO E. I. ◽  
EFFIONG D. E. ◽  
UWAH T. O. ◽  
SUNDAY N. I.
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Polymer Concentration ◽  
Hydroxypropyl Methylcellulose ◽  
Controlled Drug Release ◽  
Fickian Diffusion ◽  
Wet Granulation ◽  
Floating Tablets ◽  
Swelling Characteristics

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.

scholarly journals Development and evaluation of gastroretentive norfloxacin floating tablets

2009 ◽  
Vol 59 (2) ◽  
pp. 211-221 ◽  
Author(s):  
Ramesh Bomma ◽  
Rongala Swamy Naidu ◽  
Madhusudan Yamsani ◽  
Kishan Veerabrahma
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Wet Granulation ◽  
Drug Bioavailability ◽  
Floating Tablets

Development and evaluation of gastroretentive norfloxacin floating tabletsFloating matrix tablets of norfloxacin were developed to prolong gastric residence time, leading to an increase in drug bioavailability. Tablets were prepared by the wet granulation technique, using polymers such as hydroxypropyl methylcellulose (HPMC K4M, HPMC K100M) and xanthan gum. Tablets were evaluated for their physical characteristics,viz., hardness, thickness, friability, and mass variation, drug content and floating properties. Further, tablets were studied forin vitrodrug release characteristics for 9 hours. The tablets exhibited controlled and prolonged drug release profiles while floating over the dissolution medium. Non-Fickian diffusion was confirmed as the drug release mechanism from these tablets, indicating that water diffusion and polymer rearrangement played an essential role in drug release. The best formulation (F4) was selected based onin vitrocharacteristics and was usedin vivoradiographic studies by incorporating BaSO4. These studies revealed that the tablets remained in the stomach for 180 ± 30 min in fasting human volunteers and indicated that gastric retention time was increased by the floating principle, which was considered desirable for the absorption window drugs.

scholarly journals DESIGN AND IN VITRO EVALUATION OF FLOATING DRUG DELIVERY SYSTEM OF GLIPIZIDE USING COMBINATION OF NATURAL MUCILAGES AND SYNTHETIC POLYMERS

2021 ◽  
pp. 40-48
Author(s):  
DALAPATHI GUGULOTHU ◽  
SURAJ KUMAR CHOUDHARY
Keyword(s):  
Drug Release ◽  
Guar Gum ◽  
Hydroxypropyl Methylcellulose ◽  
Lag Time ◽  
Synthetic Polymers ◽  
Time Duration ◽  
Compression Technique ◽  
Floating Tablets ◽  
Xrd Study

Objective: The objective of the study is to explore polysaccharide mucilages of Colocasia esculenta (CE), and Fenugreek (FG) as buoyancy enhancing agents, and mucoadhesive agents by developing gastroretentive floating tablets of Glipizide. Methods: Glipizide loaded floating tablets were developed with CE, and FG alone and in combination of Guar gum (GG), and Hydroxypropyl methylcellulose (HPMC) K4M using direct compression technique. The developed formulations have been subjected to evaluation of in vitro buoyancy study, in vitro drug release study (pH 1.2), and in vitro bioadhesiveness study. Therefore, the final optimized formulation was subjected to Fourier Transform Infrared Spectroscopy (FTIR), Differential scanning calorimetry (DSC), and X-ray powder diffraction (XRD) study. Results: The results of the buoyancy study for formulation F1, F2, and F5 revealed that the instant floating lag time, floating time duration of 1 h, and exhibited 100% drug release in 4 h. Therefore, the formulations developed with GG (F3), and HPMC K4M (F4) have been exhibited slow floating lag time, prolonged floating duration and drug released up to 100 % in 12 h, while; formulations F6, F7, F8, and F9 have been exhibited shortest floating lag time, longest floating time duration, the best drug released up to 12 h, and better in vitro bioadhesiveness properties. Furthermore, F7 exhibited good bioadhesive property as compared to F6, F8-F9. The results of the FTIR, DSC, and XRD study for F7 revealed that the presence of functional groups and amorphous. Conclusion: Owing to the anticipated properties like biocompatibility, biodegradability, swelling ability, and cost-effectiveness of CE; it could be the potential macromolecule for the replacement of synthetic polymers.

Influence of Hydroxypropyl Methylcellulose on Flowing and Swelling Parameters in Biomucoadhesive Tablets with Miconazole Nitrate

2017 ◽  
Vol 68 (10) ◽  
pp. 2346-2349
Author(s):  
Magdalena Birsan ◽  
Nela Bibire ◽  
Madalina Vieriu ◽  
Alina Diana Panainte ◽  
Ileana Cojocaru
Keyword(s):  
Friction Coefficient ◽  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Pharmaceutical Formulations ◽  
Direct Compression ◽  
Miconazole Nitrate ◽  
Proportionality Relationship ◽  
Formulation Variables

Original pharmaceutical formulations have been produced as oral biomucoadhesive tablets for antifungal medication. They have been obtained through direct compression using as matrix forming polymers various sorts of hydroxypropyl methylcellulose. The main goal of the study was determining the swelling index of the new mucobioadhesive formulations with miconazole nitrate in order to correctly evaluate the time of contact with mucosa, and the prolongation of drug release. For each formulation, the flowing parameters have been determined: flowing time, friction coefficient, repose angle, Haussner ratio, Carr index, and the swelling index for 6 formulations containing various sorts of hydroxypropyl methylcellulose as matrix molders, while the formulation variables studied were time and association ratio between those polymers. Though results analysis, we noticed that the values of the swelling index depended on the type and quantity of polymer, results that could also be explained by the proportionality relationship to flowing and compressibility parameters.

scholarly journals Impact of Solubility Enhancement Methods on the Dissolution Rate of Valsartan Sachet

2021 ◽  
Vol 11 (1) ◽  
pp. 63-69
Author(s):  
Anjam H. Abdalla ◽  
Anoosh B. Hagop ◽  
Dina A. Boya
Keyword(s):  
Drug Release ◽  
Sodium Lauryl Sulfate ◽  
Fourier Transforms ◽  
Critical Role ◽  
Tween 80 ◽  
Release Profile ◽  
Oral Drug ◽  
Content Uniformity ◽  
Lauryl Sulfate ◽  
Significant Difference

The oral drug delivery is the most generally used route of administration that has been explored for the delivery of drugs through various pharmaceutical products. Solubility of drug plays critical role in achieving the optimum therapeutic levels of the drug in blood and thus bioavailability. There are many drugs of various therapeutic categories fall in Biopharmaceutics Classification System Classes II and IV as they lack solubility. For all these drugs, dissolution is the big issue for the absorption process. Valsartan is an effective antihypertensive agent and it can be used for the treatment of hypertension in most cases. The objective of this study is to prepare Valsartan as an oral sachet which can be used as an alternative dosage form after improvement of drug solubility using solubilizing agents such as sodium lauryl sulfate and tween 80. Three different formulas of Valsartan sachet were prepared by conventional technique of wet granulation method named conventional formula (Fc), sodium lauryl sulfate formula (Fs), and tween 80 formula (Ft) then compared with the available marketed product of Valsartan tablet (Fd) as a reference. The preformulations studies were conducted to exclude drug excipients interaction. Evaluation was performed in terms of weight variation, dose content uniformity, and drug release study using dissolution test apparatus. Fourier Transforms Infrared Spectroscopy reveals no drug excipient interaction and the drug release profile for Fs and Ft formulas within 30 min was 100.16% and 104.16%, respectively, while for Fc only 57.55% of the drug was released. This difference in the release profile was statistically significant (P < 0.05) between Fs and Ft with Fc, but a non- significant difference (P > 0.05) was observed between Fs and Ft with the marketed Valsartan tablet (Fd). The results support the possibility of using the prepared formulas Fs and Ft as a Valsartan sachet for the oral administration alternative to conventional Valsartan tablets Fd.

Exploring the Potentials of Corn Fiber Gum in Fabricating Mucoadhesive Floating Tablet of Poorly Gastro-retainable Drug

2020 ◽  
Vol 15 ◽  
Author(s):  
Bhumika Mangla ◽  
Anurekha Jain ◽  
Deepinder Singh Malik
Keyword(s):  
Drug Release ◽  
Polymer Concentration ◽  
Storage Conditions ◽  
Corn Fiber ◽  
Compression Technique ◽  
In Vitro Drug Release ◽  
Floating Tablets ◽  
Floating Tablet ◽  
Gastro Retentive

Aim:: To formulate and preliminary evaluated polysaccharide based mucoadhesive floating tablets of Cinnarizine. Background:: Gastro-retentive drug delivery systems has proved to be a successful approach to enhance the gastric residence with site specific targeting for achieving local or generalized effect. Various patents has also been filed globally employing gastro-retentive approach. Objective:: The study is designed to explore the mucoadhesive and low density characteristics of corn fibre gum (CFG) for preparation of gastro-retentive floating tablets of cinnarizine. Methods:: Floating tablets were prepared by direct compression technique using different concentrations of CFG (45, 50, 60% w/w). The formulated floating tablet batches were evaluated for their hardness, friability, drug content, floating duration/ lag time, swelling behavior, bioadhesive strength and in vitro drug release. Results:: Mucoadhesive strength was found to increase with an increment in the polysaccharide concentration. Swelling index was found to increase both with the increase in CFG concentration and with duration for which tablet remains in medium. The in vitro drug release studies indicated decrease in drug release (91% to 77%) with the increase in polymer concentration. The release data was further fitted to various kinetic models which revealed the drug release to be in accordance with Zero-order and Higuchi models, indicating polymer to exhibit the swellable matrix forming abilities. The value of n (between 0.458 and 0.997) from Korsemeyer Peppas model depicted the possibility of drug to follow more than one mechanism of release from the formulation i.e. diffusion and erosion. Stability studies revealed the preparations to retain their integrity and pharmaceutical characteristics at variable storage conditions. Conclusion:: Thus from the research findings, CFG could be concluded to possess potential binder, release retardant and mucoadhesive characteristics which could be successfully employed for the formulation of gastro-retentive floating tablets.

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