English oral delivery of drug was the commonly used modality because of patient compliance and ease of administration. After oral administration of any drug, its bioavailability is affected by its residence time in stomach. Recently, gastroretentive drug delivery systems (GRDDS) have gained wide acceptance for drugs with a narrow absorption window, decreased stability at high alkaline pH, and increased solubility at low pH. This approach develops a drug delivery system, which gets retained within gastric fluid, thereby releasing its active principles in the stomach. Some methods used to achieve gastric retention of drugs include the use of effervescence agents, mucoadhesive polymers, magnetic material, bouncy enhancing excipient, and techniques that form plug-like devices that resist gastric emptying. This review provides a concise account of various attributes of recently developed approaches for GRDDS.
A potent non-sulfhydryl prodrug, trandolapril is transformed into the active substance, trandolaprilat, in the liver. For obese individuals with mild-to-moderate essential hypertension, Trandolapril is effective and safe. The elimination t1/2 of trandolapril and trandolaprilat are approximately 6 hours and 16–24 hours, respectively. The goal of present work is to develop the Trandolapril immediate release tablet using various superdisintegrants. Crospovidone, Sodium starch glycolate and Croscarmellose sodium in concentrations of 2%, 4%, and 6% were used as superdisintegrating agents for the optimization. Direct compression technique was used to make nine formulations (IRTR 1 to IRTR 9). The powder blends of all batches were evaluated for different parameters to know the powder flow characteristics and it was found that the powder blend had excellent flow and compressibility characteristics. Then, compressed tablets were tested for quality control parameters as per the IP. In formulation IRTR1-IRTR9, disintegration time was observed 30.23 to 71.67 Sec and more than 70% drug was released in 30 min. Thus, based on evaluation results, it is concluded that formulation of immediate release (IR) tablets of Trandolapril were successfully developed. Minimum disintegration time 30.23 seconds 90.56% drug release in 30 min was obtained with IRTR3. KEYWORDS: Trandolapril, Immediate release, Crospovidone, Sodium starch glycolate, crocarmellose sodium
Objective: To develop a Verapamil hydrochloride controlled release gastro-retentive (CRGR) tablet for once-daily dosing using the response surface Box-Behnken Design (BBD) approach for the improvement of bioavailability and reduction in dosing frequency to overcome the issues related to the conventional tablet formulation. Methods: For the optimization, 33Box-Behnken design was used. The independent variables were selected, the amount of Compritol 888 ATO (A), HPMC K15M (B), and Sodium bicarbonate (C). The dependent variables were Cumulative % drug release in 1.5 h (Q1.5), 8 h (Q8), 24 H (Q24) and floating lag time (FLT). Flow properties of pre-compressed powder, physical characteristics, drug content, floating lag time, total floating time and in vitro dissolution study of all formulation were assessed. In vitro dissolution study of optimized formulation that was prepared experimentally was performed and compared with predicted data obtained from the software. Drug release kinetics of the optimized formulation was also assessed to know the mechanism of drug release from the CRGR tablets. Results: Responses of experimental runs were found as Q1.5: 12.78-33.62 (%), Q8: 43.03-64 (%), Q24: 78.77 to 103.57 (%) and floating lag time as 3.01 min to 5.08 min. The predicted optimized formula with the highest desirability value of 0.963 containing amount 126.030 mg, 160.00 mg and 80.955 mg of Compritol 888 ATO, HPMC K15M and Sodium biarbonate respectively was prepared and evaluated. The experimental values from optimized formulation were obtained as Q1.5: 23.397%, Q8; 57.744%, Q24: 97.150% and FLT: 3.12 min. Predicted and experimental results were found comparable for all the responses. The release data from the optimized formulation were best fitted in the Higuchi (r2 = 0.999) and the Korsmeyer-Peppas ((r2 = 0.998, n=0.54) model. The in vitro drug release studies indicated that the Verapamil hydrochloride gastroretentive tablet releases the drug in controlled manner for 24 h. Conclusion: This study found that using Box-Behnken Design with the response and variable relation, it is possible to achieve an optimum formulation with desirable characteristics. This study also established the suitability of Compritol 888 ATO-HPMC K15M combination with Sodium bicarbonate to increase the gastric residence time tablet formulation had once-daily dosing of the Verapamil Hcl with improved bioavailability for effective management of hypertension.
The researchers are doing much work to give eco-friendly solutions for the pollution and toxicity caused by most of the organic solvents. Maheshwari has given a nice concept, known as mixed-solvency concept by the application of which, innumerable solvent systems can be developed. Maheshwari is of the opinion that each substance possesses solubilizing power. He has given several eco-friendly methods in the area of drug estimations and formulations precluding the use of toxic organic solvents. The present research work also provides an eco-friendly method to estimate spectrophotometrically, the metronidazole drug in tablet formulations without the help of organic solvent. The present investigation is an attempt to show that solids can also be wisely used to act as solvent precluding the use of organic solvents. The main objective of the present study is to demonstrate the solvent action of solid. Solid excipients can nicely be employed as solubilizers in the development of pharmaceutical dosage forms in solution form of poorly soluble drugs (mixed solvency concept). Present study describes the application of solvent character of eutectic liquid consisting of phenol and niacinamide in 25:10 ratio (PNM 2510) on the weight basis for spectrophotometric estimation of metronidazole tablets. Solubility of metronidazole in distilled water was found to be 7.28 mg/ml at room temperature. More than 80 mg of metronidazole dissolves in 1 ml of PNM 2510. In the present investigation, PNM 2510 was utilized to extract out (dissolve) the drug from tablet powder of metronidazole tablets. Distilled water was used for dilution purpose. Absorbance was noted at 320 nm against reagent blank to calculate the amount of drug in the tablets. Proposed method is novel, eco-friendly, rapid, free from toxicity of organic solvent, accurate and reproducible. Recovery studies and statistical data proved the accuracy, reproducibility and precision of the proposed method. The presence of phenol, niacinamide and tablet excipients did not interfere in the spectrophotometric estimation of metronidazole at 320 nm. Phenol and niacinamide do not interfere above 300 nm in spectrophotometric analysis.
The recent study's objective was to prepare and evaluate the Repaglinide (RG) solid dispersion. RG is poorly water soluble, BCS class II drug. Repaglinide solid dispersion (RG-SD) was prepared by solvent evaporation method using different proportion of PVP K30. The prepared RG-SD was evaluated for solubility studies, drug content, in vitro dissolution, DSC studies and XRD studies. DSC and XRD studies results indicate that RG exists in amorphous form in solid dispersion. The solubility of pure RG was enhanced from 34.41±0.68 to 370.3±1.52 μg/mL in distilled water at 370 C. RG-SD (RG:PVP K30) (1:10) showed high burst release (65%) in the first 30 min. Current research concludes that Repaglinide solid dispersions using PVP-K30 (1:10) as a carrier in solid dispersions showed promising results in enhancement of repaglinide properties. KEYWORDS: Repaglinide, Solid Dispersion, PVK K30, Dissolution Rate, Solvent evaporation
Objective: The recent study's objective was to optimize and formulate a controlled-release gastro-retentive floating tablet of RG using a central composite design, which provides continuous release of Repaglinide for up to 24 h. Methods: Repaglinide gastro-retentive floating tablet (RG-GRF Tablet) was prepared by direct compression method. The optimization was carried out using a three-factor and three-level Central Composite design. The amount of Eudragit RSPO (A), HPMC K-100M (B) and Sodium bicarbonate (C) were selected as independent variables and the Cumulative % drug release in 1.5 h (DR1.5), Cumulative % drug release in 8 h (DR8), Cumulative % drug release in 24 h (DR24) and Floating lag time (FLT) were used as dependent variables. Results: CCD analysis results shows that predicted and experimental values for optimized formulation were found to be almost similar. Optimized amounts of Eudragit RSPO, HPMC K-100M, and NaHCO3 were 14.351 mg, 44.438 mg, and 10 mg, respectively, with the highest possible desirability value of 0.898. The experimental values at optimized preparation conditions were found to be DR1.5 is 30.68%, DR8 is 64.90%, DR24 is 96.54%, and FLT is 4.41 min. The release data from the optimized formulation were closely matched with the Korsmeyer-Peppas model and in vitro drug release studies indicated that the RG-GRF Tablet continuously releases the drug for 24 h in a controlled manner. Conclusion: Current research concludes that RG-GRF Tablets provide drug release for up to 24 h, and the derived central composite design can be used for forecasting the DR1.5, DR8 and DR24 as well. RG can also be made more bioavailable by extending the gastric residence time.
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