Development Of Mebeverine Hcl Prolonged Release Mini-Tablets By Thermoplastic Granulation Technique

Mebeverine HCl is a BCS class-I drug and thus it possesses high solubility in aqueous media across the biological pH range. The marketed reference product is a multi-unit particulate system (MUPS) containing prolonged release pellets filled in hard gelatin capsule. In conventional manufacturing process, a huge quantity of solvents (aqueous and/or organic) is used to manufacture such dosage form. Additionally, it demands more processing time and efforts. Therefore, a prolonged release capsules dosage form of Mebeverine HCl was formulated using thermoplastic (melt) granulation technique without usage of any solvent. Prolonged release minitablets sized 2 mm in diameter were developed as per quality by design principles. A 23 full-factorial design of experiment was applied to optimize levels of drug release controlling ingredients which includes a hydrophobic meltable binder (hydrogenated castor oil) cum matrixing agent, a hydrophilic meltable binder (polyethylene glycol) which may act as pore former also, and a release controlling polymer (ethyl cellulose). The optimized formulation was found stable. Dissolution profiles of the optimized formulation were found similar to the marketed reference product in different media across the physiological pH range. In conclusion, the explored solvent less process was capable to manufacture the MUPS dosage form of Mebeverine HCl prolonged-release capsules, which is stable and pharmaceutically equivalent with the reference product. The developed process is more beneficial to small and medium scale industry, as it does not require any special and costly equipment, significantly decreases manufacturing cost and increases productivity compared to conventional process, which is mentioned in literature.

Optimization of solvent-free microwave extraction for Acori Tatarinowii Rhizoma and analysis on volatile components by GC-MS / 中草药

Objective: To study the solvent-free microwave extraction for oils of Acori Tatarinowii Rhizoma and analyze the volatile components. Methods: The paper selected the best technological conditions by L9(34) orthogonal test, with the index of α-asarone, volume of volatile oils, and sum of the percentage, The essential oils in Acori Tatarinowii Rhizoma were analyzed with GC-MS. Results: The percentage of volatile oils was calculated according to peak area normalization method. The results showed similar amount of volatile oil components by two methods, and the extraction rates of α-asarone, β-asarone, and γ-asarone accounted for 4.12%, 55.11%, and 10.54% on the method of solvent-free microwave extraction, while the steam distillation was 5.39%, 47.03%, and 9.15%. To compare with two methods, solvent-free microwave extraction extracted volatile oil 0.235 mL and α-asarone 31.99 mg for 5 min, while steam distillation extracted volatile oil 0.175 mL and α-asarone 29.09 mg for 1 h. The method of solvent-free microwave extraction had the advantage of short reaction time and high yields. Conclusion: Solvent-free microwave extraction is a new method with shorter extracting time and better extracting efficiency.

Synthesis of quinolines and their In vitro antioxidant activities under solvent free conditions by using the SiO2-Zn-MgO as a novel and reusable catalyst.

The present study was aimed to determine a novel route of synthesis of quinolines and their in vitro antioxidant activities. Synthesis of quinolines is simple, economic, effective and an easy way process has been developed by using the SiO2–Zn-MgO as a novel catalyst. The quinolines antioxidative potential was evaluated using 1,1-Diphenyi-2-Picrylhydrazyl (DPPH), superoxide radical, hydroxyl radical, and hydrogen peroxide radical assay by in vitro methods. Quinolines exhibited highest level of antioxidant activities, and therefore it could be used as antioxidant that may have potential benefits in health and disease management.

One-pot synthesis of 2-ARYL-1-ARYLMETHYL-1H-1,3-benzimidazole derivatives using sulfonic acid functionlized silica (SiO2-Pr-SO3H) under solvent free conditions.

2-Aryl-1-arylmethyl-1H-1,3-benzimidazoles were synthesized by the reaction of o-phenylendiamine with different types of aromatic aldehydes in the presence of Sulfonic acid functionlized silica (SiO2-Pr-SO3H) as solid acid catalyst under solvent free condition at room temperature in good to excellent yields.