scholarly journals Design and evaluation of a novel floating osmotic pump system

2009 ◽  
Vol 12 (1) ◽  
pp. 129 ◽  
Author(s):  
Zhihong Zhang ◽  
Bo Peng ◽  
Xinggang Yang ◽  
Chao Wang ◽  
Guangmei Sun ◽  
...  
Keyword(s):  
Drug Release ◽  
Oral Administration ◽  
In Vitro Release ◽  
Osmotic Pump ◽  
Matrix Tablets ◽  
In Vivo Evaluation ◽  
Pump System ◽  
Conventional Tablet

PURPOSE. Find a novel delivery system for oral administration of drugs that have absorption window in the upper part of gastrointestinal (GI) track. METHODS. Dipyridamole was chosen as the model drug. A novel system, which combined the osmotic pump controlled release system and the floating system, was designed; matrix tablets (MT) were prepared for compares. The effects of pH, temperature and hydrodynamic conditions on drug release and the floating behavior of floating osmotic pump system (FOP) were investigated. In vivo evaluation was performed by a three-crossover study in six Beagle dogs relative to the conventional tablet (CT). Cumulative percent input in vivo was compared with that of in vitro release profiles. RESULTS. Floating behavior of FOP, drug releases from FOP and MT were sensitive to pH of dissolution media but not sensitive to temperature; the release of dipyridamole from MT was influenced by stirring rate while drug release from FOP was not. AUC of FOP was larger than MT and CT. The linear correlations between fraction absorbed in vivo and fraction dissolved in vitro was established for FOP-a true zero-order release formula, whereas only a nonlinear correlation was obtained for MT. CONCLUTIONS. FOP could be a novel way for the oral administration for drugs like dipyridamole.

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

scholarly journals IN VIVO EVALUATION OF QUINAPRIL TRILAYERED MATRIX TABLETS

2021 ◽  
pp. 117-125
Author(s):  
ASHWIN K ◽  
RAMA MOHAN REDDY T
Keyword(s):  
Drug Release ◽  
Drug Concentration ◽  
In Vitro Release ◽  
Matrix Tablets ◽  
In Vivo Studies ◽  
Matrix Tablet ◽  
In Vivo Evaluation ◽  
Drug Content

Objective: The aim was to design, formulate, and evaluate the trilayer matrix tablets incorporated with quinapril for extend drug release. Methods: Quinapril trilayer matrix tablets were formulated using design of experiment software wherein initially 27 formulations (QF1-QF27) were designed for active layer from which one best formulation was chosen based on drug content, swelling index and in vitro release studies. The chosen formulation was formulated into extended release trilayed matrix tablet by varying proportions of polymers by direct compression and was evaluated for various physicochemical parameters, drug release. Best formulation was characterized for Fourier transform infrared (FTIR), stability, and pharmacokinetic study. Results: Out of 27 formulations highest drug release was exhibited by QF16 (98.85%) which was formulated into trilayer matrix tablets (AQF16- HQF16). Out of which EQF16 was found to exhibit highest values with 98.42% swelling index, 99.56% drug content, and 99.72% drug release in 24 h. All quinapril trilayer formulations showed zero-order and first-order for marketed product. The optimized formulation EQF16 was found to exhibit no interaction with excipients interpreted by FTIR and no significant changes were observed after loading for stability. In vivo studies conducted using optimized formulation EQF16 attained peak drug concentration (Tmax) of 4.0±0.06 and 1.0±0.03 h for the optimized and commercial formulations, respectively, while mean maximum drug concentration (Cmax) was 302.64±0.07 ng/mL and was significant (p<0.05) as compared to the quinapril marketed product formulation 358.78±0.75 ng/mL. Conclusion: Hence, quinapril was successfully formulated into trilayer matrix tablet and found to be stable.

Design, in vitro and in vivo Evaluation of Gemifloxacin Mesylate Floating Matrix Tablets

1970 ◽  
Vol 9 (1) ◽  
pp. 3143-3149
Author(s):  
Sushma Appala ◽  
Ramesh Bomma ◽  
Kishan Veerabrahma
Keyword(s):  
Helicobacter Pylori ◽  
Drug Release ◽  
Lag Time ◽  
Matrix Tablets ◽  
In Vivo Evaluation ◽  
In Vitro Drug Release ◽  
Weight Variation ◽  
Gastro Retentive

Objective of the investigation was to develop gastro retentive dosage form of gemifloxacin mesylate for local action in the stomach as it has antibacterial activity against Helicobacter pylori. Gemifloxacin mesylate is a synthetic broad-spectrum antibacterial agent for oral administration, having 7 hrs half-life and 71% oral bioavailability. In present study, gemifloxacin mesylate floating matrix tablets were prepared by direct compression method using polymers (HPMC K4M, HPMC K15M and polyox WSR 1105) and evaluated for various parameters like drug content, floating behavior (floating lag time and total floating time), in vitro drug release, swelling index, weight variation, friability, hardness and thickness. Sodium bicarbonate was incorporated as gas generating agent in all formulations. Drug-excipients compatibility was studied by Differential Scanning Calorimetry. Results have shown that the amount of polymer in the formulation affected the drug release. Optimized formulation (F8 containing polyox WSR1105 as release retarding agent) was selected based on in vitro drug release, floating lag time, floating time and other parameters. This formulation followed zero order kinetics and non-Fickian mechanism of drug release. In vivo radiographic study was conducted in healthy human volunteers using tablets containing BaSO4 as radio opaque agent. The average residence time was found to be 4.5± 0.86 h (n=3). This design of gastro retentive drug delivery system helps in increasing the local delivery of drug in patients with Helicobacter pylori infection

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 New Technology of Thermoplastic Coating for Osmotic Pump Tablets: Study on in vivo Drug Release

2020 ◽  
Vol 02 (01) ◽  
pp. e1-e10
Author(s):  
Chun Ping Yuan ◽  
Hui Min Hou ◽  
Zhi Hong Cheng ◽  
Qing Hua Ge ◽  
Ding Zhong Song ◽  
...  
Keyword(s):  
Drug Release ◽  
New Technology ◽  
In Vitro Release ◽  
Osmotic Pump ◽  
Metformin Hydrochloride ◽  
Beagle Dogs ◽  
Coating Technology ◽  
Vitro Release

Abstract Aim The in vivo pharmacokinetics of thermoplastic-coated tablets prepared by a new technology of thermoplastic coating in Beagle dogs were studied, and the correlation between in vitro release and in vivo absorption was analyzed. Methods The in vitro release profiles of metformin hydrochloride thermoplastic-coated tablets and nifedipine thermoplastic-coated tablets were investigated. The single-dose pharmacokinetic study of these tablets in Beagle dogs was performed, and the obtained results were separately compared with the data of conventional osmotic pump tablets reported in the literature. Results Metformin hydrochloride thermoplastic-coated tablets and nifedipine thermoplastic-coated tablets displayed controlled drug-release characteristics and had a good in vivo–in vitro correlation in Beagle dogs, respectively. The literature-compared results further demonstrated that both thermoplastic-coated tablets had release characteristics of osmotic pump tablets in vivo. Conclusion The thermoplastic-coated tablets could control drug release in vivo and it was further confirmed that the new thermoplastic coating technology could replace the spray coating of osmotic pump controlled-release tablets. This study provides a theoretical basis and practical support for the industrialization and clinical application of the new thermoplastic coating technology.

DEVELOPMENT AND EVALUATION OF ORAL ELEMENTARY OSMOTIC PUMP TABLETS FOR ROPINIROLE HYDROCHLORIDE

INDIAN DRUGS ◽  
2012 ◽  
Vol 49 (06) ◽  
pp. 23-30
Author(s):  
S. Patha ◽  
◽  
P. Dara ◽  
S. K Yamsani ◽  
R Thadkapally ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Osmotic Pump ◽  
In Vivo Studies ◽  
Dissolution Medium ◽  
Conventional Tablet ◽  
Peg 400 ◽  
Ropinirole Hydrochloride

The objective of the present study was to develop a sustained release once a day oral elementary osmotic tablet for ropinirole hydrochloride and evaluate its in vivo performance. The core of elementary osmotic tablet of ropinirole hydrochloride was prepared by compression of mixture consisting of drug,different concentrations of osmogens, and other tablet material. Core tablets were then coated with different concentrations of cellulose acetate and PEG-400. FTIR was used to identify if the excipients are compatible with the drug. All the tablets that were prepared were evaluated for drug release and based on the results an optimum and ideal osmotic pump composition with a zero-order drug release extended for 24 h was proposed and this was considered the optimized formulation. Surface morphology of coated formulation was studied by scanning electron microscopy. The drug release was determined in different pH media and different agitation speeds. The pharmacokinetics of the drug after oral administration of optimized osmotic pump was investigated in rabbits and the data were compared with that of a conventional tablet. In vitro in vivo correlation was determined for the optimized formulation. A suitable and simple sustained release elementary osmotic pump for ropinirole hydrochloride was developed. The release rate was independent of the pH of the dissolution medium and the agitation speeds. In vivo studies with optimized osmotic tablet formulation demonstrated that drug concentration in plasma was maintained for prolonged period and minimized fluctuation. A better in vitro in vivo correlation was achieved with the osmotic tablet. A simple once a day elementary osmotic tablet is feasible for ropinirole hydrochloride.

Preparation and In vivo Evaluation of Mucoadhesive Microspheres for Gastroretentive Delivery of Misoprostol

2017 ◽  
Vol 10 (2) ◽  
pp. 3676-3683
Author(s):  
Bhikshapathi D.V. R. N. ◽  
Ranjith Kumar K
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Gi Tract ◽  
In Vivo Evaluation ◽  
Upper Gi ◽  
Upper Gi Tract

The aim of the present investigation was to prepare and evaluate the Misoprostol mucoadhesive microspheres for gastroretentive drug delivery. Sodium alginate and sodium carboxy methyl cellulose were used as mucoadhesive polymers. Microsphere formulations were prepared using Ionotropic gelation technique. All the microspheres were characterized for particle size, scanning electron microscopy, FT-IR study, percentage yield, drug entrapment, stability studies and for in vitro release kinetics. Based on the results, the formulation M12 was selected as optimized formulation. In vitro drug release study of optimized formulation M12 showed 98.23% after 12 h in a controlled manner, which is essential for anti ulcer therapy. The marketed product shows the drug release of 95.23 within 1 h. The results of mucoadhesion study showed better retention of prepared microspheres (8) h in chic duodenal and jejunum regions of intestine. The results showed significant higher retention of mucoadhesive microspheres in upper GI tract. Pharmacokinetic study revealed that the bioavailability was found to be increased significantly when compared with marketed tablets. The drug release of Misoprostol optimized formulation M12 followed zero order, Higuchi and Korsmeyer-Peppas kinetics indicating diffusion controlled with non-Fickian (anomalous) transport thus it projected that delivered its active ingredient by coupled diffusion and erosion. Overall, the result indicated prolonged delivery with improved bioavailability of Misoprostol from mucoadhesive microspheres due to higher retention in the upper GI tract.

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.   

Fenofibrate Solid Dispersion for Improving Oral Bioavailability: Preparation, and Characterization and in vivo Evaluation

2020 ◽  
Vol 13 (5) ◽  
pp. 5102-5109
Author(s):  
Venu Madhav K ◽  
Somnath De ◽  
Chandra Shekar Bonagiri ◽  
Sridhar Babu Gummadi
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
In Vivo Evaluation

Fenofibrate (FN) is used in the treatment of hypercholesterolemia. It shows poor dissolution and poor oral bioavailability after oral administration due to high liphophilicity and low aqueous solubility. Hence, solid dispersions (SDs) of FN (FN-SDs) were develop that might enhance the dissolution and subsequently oral bioavailability. FN-SDs were prepared by solvent casting method using different carriers (PEG 4000, PEG 6000, β cyclodextrin and HP β cyclodextrin) in different proportions (0.25%, 0.5%, 0.75% and 1% w/v). FN-SDs were evaluated solubility, assay and in vitro release studies for the optimization of SD formulation. Differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM) analysis was performed for crystalline and morphology analysis, respectively. Further, optimized FN-SD formulation evaluated for pharmacokinetic performance in Wistar rats, in vivo in comparison with FN suspension.  From the results, FN-SD3 and FN-SD6 have showed 102.9 ±1.3% and 105.5±3.1% drug release, respectively in 2 h. DSC and PXRD studies revealed that conversion of crystalline to amorphous nature of FN from FT-SD formulation. SEM studies revealed the change in the orientation of FN when incorporated in SDs. The oral bioavailability FN-SD3 and FN-SD6 formulations exhibited 2.5-folds and 3.1-folds improvement when compared to FN suspension as control. Overall, SD of FN could be considered as an alternative dosage form for the enhancement of oral delivery of poorly water-soluble FN.

Design and In vivo Evaluation of Palonosetron HCl Mouth Dissolving Films in the Management of Chemotherapy-Induced Vomiting

2017 ◽  
Vol 10 (6) ◽  
pp. 3929-3936
Author(s):  
Y. Srinivasa Rao ◽  
K. Adinarayana Reddy
Keyword(s):  
Drug Release ◽  
Patient Compliance ◽  
Onset Of Action ◽  
In Vivo Evaluation ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Surface Ph ◽  
Drug Content

Fast dissolving oral delivery systems are solid dosage forms, which disintegrate or dissolve within 1 minute in the mouth without drinking water or chewing. Mouth dissolving film (MDF) is a better alternate to oral disintegrating tablets due to its novelty, ease of use and the consequent patient compliance. The purpose of this work was to develop mouth dissolving oral films of palonosetron HCl, an antiemetic drug especially used in the prevention and treatment of chemotherapy-induced nausea and vomiting. In the present work, the films were prepared by using solvent casting method with various polymers HPMC E3, E5 & E15 as a film base synthetic polymer, propylene glycol as a plasticizer and maltodextrin and other polymers. Films were found to be satisfactory when evaluated for thickness, in vitro drug release, folding endurance, drug content and disintegration time. The surface pH of all the films was found to be neutral. The in vitro drug release of optimized formulation F29 was found to be 99.55 ± 6.3 7% in 7 min. The optimized formulation F29 also showed satisfactory surface pH, drug content (99.38 ± 0.08 %), disintegration time of 8 seconds and good stability. FTIR data revealed that no interaction takes place between the drug and polymers used in the optimized formulation. In vitro and in vivo evaluation of the films confirmed their potential as an innovative dosage form to improve delivery and quick onset of action of Palonosetron Hydrochloride. Therefore, the mouth dissolving film of palonosetron is potentially useful for the treatment of emesis disease where quick onset of action is desired, also improved patient compliance.

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