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 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 Formulation, Optimization and in vitro Characterization of Stavudine Gastro Retentive Floating Matrix Tablets

2016 ◽  
Vol 8 (03) ◽  
Author(s):  
Mahendar Rupavath ◽  
Kranthi G. ◽  
Chinna Palem ◽  
K. S. K. Patnaik
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
Release Mechanism ◽  
Wet Granulation ◽  
Drug Bioavailability ◽  
In Vitro Drug Release ◽  
Weight Variation

The aim of the present investigation was to develop floating matrix tablets of stavudine to achieve prolong gastric residence time, leading to an increase in drug bioavailability and patient compliance. Floating tablets were prepared by wet granulation technique, using hydroxypropyl methylcellulose (HPMC K15M) as synthetic, pullulan gum as natural rate controlling polymers and optimum amounts of sodium-bicarbonate and citric acid as gas generating agents in suitable ratios to generate optimum buoyancy. Developed formulations were evaluated for weight variation, thickness, hardness, friability, drug content, in vitro drug release, floating lag time and floating buoyancy. All the formulations exhibited acceptable physical properties and the best formulation (F3) was selected based on in vitro characteristics. Further, the optimized formulation was evaluated for in vivo radiographic studies by incorporating BaSO4 as radio opaque substance. All the formulations were studied for in vitro drug release characteristics for 16 h. Optimized formulation showed controlled and prolonged drug release profiles while floating over the dissolution medium. Diffusion followed by erosion drug release mechanism was observed for the formulation, indicating that water diffusion and polymer erosion played an essential role in drug release. In vivo radiographic studies revealed that the tablets remained in the stomach for 8 ± 0.5 h in fasting human volunteers and indicated that gastric retention time was increased by the floating principle, which was considered and desirable for absorption window drugs.

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.

Formulation and Evaluation of Isabgol and Liquorice Based Nutraceuticals Floating Tablets for Management of Gastric Ulcer

2020 ◽  
Vol 01 ◽  
Author(s):  
Ritesh Kumar Tiwari ◽  
Lalit Singh ◽  
Shashi Verma ◽  
Vijay Sharma
Keyword(s):  
Drug Release ◽  
Sodium Bicarbonate ◽  
Magnesium Stearate ◽  
Gastric Ulcers ◽  
Physical Parameters ◽  
Floating Tablets ◽  
Zero Order Kinetics ◽  
Liquorice Extract ◽  
Tablet Formulations

Background: Floating tablets extend drug residence time, enhance bioavailability and promote the delivery of local drugs to the stomach. With this objective, floating tablets were prepared for the treatment of gastric ulcers containing aqueous extract of liquorice and Isabgol. Methods: Tablets containing HPMC K100M (hydrophilic polymer), liquorice extract, sodium bicarbonate (gas generating agent), talc, and magnesium stearate were prepared using direct compression method. Physical parameters of formulations such as diameter, thickness, hardness, friability, weight uniformity, drug content, buoyancy time, dissolution, and mechanism for drug release, were assessed. The formulations have been optimized based on buoyancy time and in- vitro drug release. Results: The diameter of all formulations was in the range 11.310-11.833 mm; thickness was in the range 4.02-4.071 mm. The hardness ranged from 3.1 to 3.4 kg/cm. All formulations passed the USP requirements for friability and uniformity of weight. All tablet formulations had a buoyancy period of less than 5 min and throughout the research, the tablet stayed in floating condition. All tablet formulations were accompanied in drug discharge by zero-order kinetics and model Korsemeyer-Peppas. Conclusion: It was discovered that the optimized formulation was F7, which released 98.5 percent of the drug in 8 hr. invitro, while the buoyancy time was 3.5 min. For gastroretentive drug delivery systems, formulations containing Isabgol, sodium bicarbonate and HPMC K100 M in combination may be promising.

scholarly journals Development and in vitro Characterization of Gastro Retentive Raft Forming Stavudine Tablets

2017 ◽  
Vol 9 (01) ◽  
Author(s):  
Mahendar Rupavath ◽  
K. S. K Rao
Keyword(s):  
Drug Release ◽  
Matrix Tablets ◽  
Drug Dissolution ◽  
Release Mechanism ◽  
Compatibility Study ◽  
Drug Bioavailability ◽  
Drug Content ◽  
Weight Variation

The objective of the present investigation was to identify a suitable raft forming agent and to develop raft forming stavudine matrix tablets using different rate controlling natural, semi-synthetic and synthetic polymers to achieve prolonged gastric residence time, leading to an increase in drug bioavailability and patient compliance. Various raft forming agents were used in preliminary screening. Raft forming floating tablets were developed using pullulan gum as natural rate controlling polymer, and directly compressible grades of hydroxypropyl methylcellulose (Benecel K4M DC) as semi synthetic, and Carbopol 71G as synthetic rate controlling polymers respectively and optimum concentrations of sodium-bicarbonate as gas generating agent to generate optimum buoyancy by direct compression method. Raft forming tablets were evaluated for weight variation, thickness, hardness, friability, drug content, in vitro drug release, floating buoyancy and raft strength. Drug-excipients compatibility study showed no interaction between drug and excipients. Raft forming tablets showed satisfactory results when evaluated for weight variation, thickness, hardness, friability, drug content, and raft strength. The optimized formulation was selected based on physicochemical characteristics and in vitro drug dissolution characteristics. Further, the optimized formulation was evaluated for in vivo radiographic studies by incorporating BaSO4 as radio opaque substance. Optimized formulation showed controlled and prolonged drug release profiles while floating and raft formation over the dissolution medium. Diffusion followed by erosion with raft forming drug release mechanism was observed for the formulation, indicating that dissolution media diffusion and polymer erosion played an essential role in drug release. In vivo radiographic studies revealed that the raft forming formulations remained in the stomach for 240 30 min in rabbits and indicated that gastric retention time was increased by the floating and raft forming principle, which was considered and desirable for absorption window drugs.

scholarly journals GASTRO-FLOATING TABLETS OF REPAGLINIDE: PREPARATION AND IN VIVO EVALUATION

2018 ◽  
Vol 11 (7) ◽  
pp. 291
Author(s):  
Poornima P ◽  
Abbulu K ◽  
Mukkanti K
Keyword(s):  
Hydroxypropyl Methylcellulose ◽  
In Vitro Dissolution ◽  
Effective Management ◽  
Drug Bioavailability ◽  
In Vivo Evaluation ◽  
Floating Tablets ◽  
Gastric Residence Time ◽  
Evaluation Parameters

Objective: Current research concerns the expansion of repaglinide matrix floating tablets, which are designed to prolong the gastric residence time, increase the drug bioavailability, and diminish the side effects.Methods: Different formulations of repaglinide floating tablets were prepared with different grades of hydroxypropyl methylcellulose (HPMC) and other agents. Evaluation parameters and in vivo bioavailability studies were conducted in the suitable model.Results: Among all the formulations, F21 containing HPMC K1500 PH PRM, Polyox WSR 303, and sodium bicarbonate, as gas generating agent was selected as optimized formulation based on physicochemical properties, floating lag time (36 s), and total floating time (>24 h). From in vitro dissolution studies, the optimized formulation F21 showed drug release of 98.92±5.19% within 24 h whereas 95.09±5.01% of the drug was released from the marketed product within 1 h.Conclusion: From in vitro and in vivo bioavailability studies repaglinide floating tablets expected to give a new choice for safe, economical, and increased bioavailability for effective management of diabetes mellitus.

Development and In Vitro – In Vivo Evaluation of Gastro-retentive Floating Tablets Containing Repaglinide

2018 ◽  
Vol 11 (2) ◽  
pp. 4026-4036
Author(s):  
Poornima P ◽  
Abbulu K ◽  
Mukkanti K
Keyword(s):  
Drug Release ◽  
Residence Time ◽  
Chemical Properties ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Drug Bioavailability ◽  
In Vivo Evaluation ◽  
Gastric Residence Time

The present investigation concerns the development of the repaglinide floating matrix tablets, which after oral administration are designed to prolong the gastric residence time, increase the drug bioavailability and diminish the side effects of irritating drugs. FTIR studies revealed that there is no interaction between the drug and polymers used for the formulation. Among all the formulations F21 containing HPMC K1500 PH PRM, Polyox WSR-303 and Sodium bicarbonate, as gas generating agent was selected as optimized formulation based on physico chemical properties, floating lag time (36 sec) and total floating time (>24 h). From in vitro dissolution studies, the optimized formulation F21 showed drug release of 98.92±5.19% within 24h whereas 95.09±5.01% of the drug was released from the marketed product within 1h. The major mechanism of drug release follows zero order kinetics and non-Fickian transport by coupled diffusion and erosion. In vivo experiments supported the expectations in prolonging the gastric residence time in the fasted state in beagle dogs. The mean gastric residence time for the tested tablets was 270 min±60. This result is encouraging, because a longer gastric residence time is an important condition for higher bioavailability of the drugs included in the prolonged or controlled release dosage forms.

scholarly journals IN SITU GEL AS PLATFORM FOR KETOCONAZOLE SLOW RELEASE DOSAGE FORM

2018 ◽  
Vol 10 (5) ◽  
pp. 76
Author(s):  
Methaq Hamad Sabar ◽  
Iman Sabah Jaafar ◽  
Masar Basim Mohsin Mohamed
Keyword(s):  
Drug Release ◽  
Guar Gum ◽  
Polymer Concentration ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
High Viscosity ◽  
In Situ Gel ◽  
Alginate Concentration

Objective: The aim of this study was to formulate ketoconazole (keto) as oral floating in situ gel to slow the release of keto in the stomach.Methods: Sodium alginate (Na alginate) was used as a primary polymer in the preparation of the in situ gel and was supported by the following polymers: guar gum (GG), hydroxypropyl methylcellulose (HPMC) K4M, K15M and carbapol 940 as viscosity enhancing agents. As a consequence, and to complete the gelation process of above formulations was by adding the calcium carbonate (CaCO3). The in situ gels were investigated by the following tests: floating lag time, floating duration, viscosity, drug content, in vitro gelling studies and in vitro release study.Results: The study showed that the faster release was obtained with F1 which contained Na alginate alone. Additionally, reduction in Na alginate concentration resulted in significant increase in drug release. It was also noted that the increase in GG (viscosity enhancing polymer) concentration resulted in non-significant decrease in percent drug release and the reduction in CaCO3 concentration led to significant increase in drug release. Moreover, the release of drug was also affected by grade of viscosity enhancing polymer, the faster release was observed with the formula which contained a polymer of low viscosity (HPMC K4M) and an opposite result was with the high viscosity polymer (HPMCK15M).Conclusion: This study showed the formulation of Na alginate with GG and CaCO3, led to gain floating in situ gel and a sustained release of keto. 

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

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