Zhongguo ying yong sheng li xue za zhi = Zhongguo yingyong shenglixue zazhi = Chinese journal of applied physiology最新文献

Objective: Bosutinib (BST) is a Biopharmaceutics Classification System Class II drug having very low solubility and high permeability. Low aqueous solubility and poor dissolution of BST lead to poor bioavailability, Thus, limited aqueous solubility is the bottleneck for the therapeutic outcome of BST. Animal data suggest that the absolute bioavailability of BST is about 14-34% due to an extensive first-pass effect. To overcome hepatic first-pass metabolism and to enhance oral bioavailability, lipid-based drug delivery systems such as solid lipid nanoparticles (SLNs) can be used.

Methods: SLNs are submicron colloidal carriers having a size range of 50-1000 nm. These are prepared with physiological lipid and dispersed in water or aqueous surfactant solution. BST can be conveniently loaded into SLNs to improve the oral bioavailability by exploiting the intestinal lymphatic transport. An optimal system was evaluated for bioavailability study in rats compared with that of BST suspension (SUS).

Results: An in vitro cytotoxicity study was done by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay method through ATCC cell lines; the percent inhibition was more in SLN when compared with SUS. The pharmacokinetics of BST-SLNs after oral administration in male Wistar rats was studied. The bioavailability of BST was increased by 2.28 fold when compared with that of a BST SUS.

Conclusion: The results are indicative of SLNs as suitable lipid-based carrier system for improving the oral bioavailability of BST.

Introduction: Incorporating rare and threatened healing plants from Traditional Chinese Medicine (TCM) into modern medicine is a hopeful way to expand treatment choices and encourage the long-term use of plant resources. These plants have been used in Traditional Chinese Medicine for a long time. They have powerful healing properties, including the ability to reduce inflammation and fight cancer. They also protect nerves and the heart.

Method: A thorough study of all the scientific studies, clinical trials, ethnobotanical surveys, and conservation reports that were found were all looked at in relation to rare and threatened medical plants used in TCM. We looked through databases like PubMed, Scopus, and Web of Science for relevant pieces. Studies published in peer-reviewed journals, reports from reputable conservation organisations, and written down traditional knowledge were all considered to be relevant.

Results: Key results show that plants like Dendrobium, Panax notoginseng, Taxus chinensis, and Cistanche deserticola can be used as medicines and that there are good ways to protect them. Some of the conservation methods that have been named are agroforestry, community-based management, current breeding techniques, and sustainable gathering. Collaboration in research, clinical trials, personalised medicine, regulatory harmonisation, and public education programs are all part of the integration with modern medicine. These programs try to solve problems like scientific proof, protection, and cultural integration.

Conclusion: When rare and threatened medical plants from Traditional Chinese Medicine (TCM) are used in modern medicine, it can improve health and help protect wildlife. Using both old information and new science discoveries together can lead to new treatments and long-term uses for these plant materials. Large-scale clinical studies, new ways of growing plants, and looking into how TCM herbs and regular drugs can work together should be the main topics of future study. For global healthcare to improve and for these important plant resources to be used in the long term, academics, healthcare workers, lawmakers, and local communities must work together.

The main issue with Hypertension therapy is quick commencement of effect. The creation of suitable dose forms may help address the issue of medications having a delayed beginning of effect. Oral Antihypertensive medication treatment is best suited for and has seen a rise in popularity with fast-disintegrating tablets. In terms of patient compliance, quick start of action, precise dosage, strong chemical stability, ease of self-administration, and compactness, they are superior to other traditional methods. As a popular hypertension medication, Propranolol HCl is a strong candidate for development into Fast Dissolving Tablets (FDTs). Because to first pass metabolism, it has a limited bioavailability. Therefore, the primary goal of the research was to create Propranolol HCl fast-dissolving tablets in order to increase the drug's bioavailability and dissolution rate. Microcrystalline cellulose used to make fast-dissolving Propranolol HCl tablets, together with varying concentrations of super disintegrates such as Chia Seed mucilage and sodium starch glycolate. Each batch was made by compressing it directly. Three formulation variables were combined, and the combined impact was examined using a 23 Full Factorial design. Here, the disintegration time is examined as a dependent parameter and the concentrations of chia seed mucilage, Sodium Starch Glycolate, and Microcrystalline Cellulose were considered as independent variables, X1, X2, and X3, respectively. The program Design Expert is used to depict the data.

Background: Following the COVID-19 pandemic, microvascular and macrovascular thrombotic problems emerged that required anticoagulants. Apixaban (RN) is a factor Xa inhibitor that treats deep vein thrombosis and the two forms of artery diseases (coronary artery disease and peripheral artery disease).

Materials and methods: The study objective was to create fast-disintegrating Apixaban Oral Thin Films (OTF) with the help of various super disintegrants to shorten disintegration time and enhance drug release in order to assist patients who have difficulty in swallowing conventional dosage forms and increase bioavailability. OTF was created using the solvent casting method. A 22 factorial design was employed in Design-Expert® software to develop an ideal formula.

Results: The optimized film formula pH, drug content, disintegration time, folding endurance, and dissolution rate were estimated, and the film was subjected to a short-term stability study. The optimized formula exhibited a cumulative drug release of 93.47% in 60 sec.

Conclusion: The drug's in vitro release pattern shows first-order kinetics and fickian diffusion was the mechanism of drug release. These findings supported that Apixaban OTFs offer a quick release of the medication from the administration site into the systemic circulation.

The burgeoning field of nanotechnology has ushered in innovative Novel drug delivery systems (NDDS) that enhance the efficacy, safety, and patient compliance of pharmaceutical treatments. This study explores the synthesis and application of silver nanoparticles (AgNPs) using green chemistry approaches, specifically leveraging plant extracts as reducing agents. AgNPs, known for their unique physical and chemical properties, including antimicrobial capabilities, offer significant potential in modern drug delivery. This study investigates the potential of using Allium cepa peel waste for the green synthesis of silver nanoparticles. This study also revealed the resultant formation of silver nanoparticles through microscopy and UV spectroscopy, which were further analyzed by Scanning Electron Microscopy. This green synthesis method not only aligns with environmentally friendly practices but also provides a cost-effective and scalable approach to nanoparticle production. We formulated a hair dye incorporating these AgNPs and evaluated its physicochemical parameters, demonstrating enhanced performance compared to control formulations without nanoparticles. This work underscores the promise of green-synthesized nanoparticles in developing advanced drug delivery systems, offering insights into future applications in anticancer and antimicrobial treatments. Our findings advocate for the broader adoption of sustainable nanotechnology in pharmaceutical sciences, potentially revolutionizing the treatment landscape with safer and more effective therapeutic options.

Introduction: The traditional medicinal system of India, Ayurveda, has mentioned Cordia Dichotoma as a potential treatment for various ailments. In the current research, the extracts of Cordia Dichotoma was examined to evaluate their antidepressant potential.

Materials and methods: Here, green leaves of Cordia Dichotoma were used to prepare chloroform, ethanol, and aqueous extracts (referred to as CdCe, CdEe, and CdAe respectively). The research focused on investigating the antidepressant effects of these extracts using behavioral models in experimental animals. Additionally, locomotor activity was assessed as part of the evaluation process.

Results: Immobility time was reduced with CdEe Cordia Dichotoma rFST & mTST when at 200 mg/kg and 400 mg/kg body weight. The CdAe showed reduction in immobility time in the repeated rFST) at 400 mg/kg, while in the mTST, significant effects were observed at 200 and 400 mg/kg. Regarding the chloroform extract, it only exhibited a significant reduction in immobility time in the modified Tail Suspension Test (mTST) at a low dose of 200 mg/kg. However, no noticeable change in motor dysfunction was observed with CCl4 and aqueous extracts at doses of 200 and 400 mg/kg. It is worth noting that the chloroform extract (CdCe) did lead to a significant decrease in locomotor activity at the same dosage level. Taken together, these findings suggest that extracts obtained from Cordia Dichotoma leaves may possess antidepressant properties.

A simple, Accurate, precise method was developed for the estimation of the Lorlatinib in API form and Marketed pharmaceutical dosage form by RP-HPLC. Chromatogram was run through Hypersil C18 (4.6mm×150mm, 5µm) Particle size Column and Mobile phase containing Methanol and Water taken in the ratio of 25: 75% v/v was pumped through column at a flow rate of 1.0 ml/min. Temperature was maintained at 38ºC. Optimized wavelength selected was 310 nm. Retention times of Lorlatinib were found to be 3.513 minutes respectively. The %RSD for the Repeatability and Intermediate Precision of the Lorlatinib were found to be within limits. %Recovery was obtained 98.96% and it was found to be within the limits for Lorlatinib respectively. The LOD, LOQ values obtained from regression equations of Lorlatinib were 0.332µg/ml and 1.0078 µg/ml respectively. Regression equation of Lorlatinib was found to be y = 39948x + 16821 respectively. The Retention times was decreased and run time was decreased, so the method developed was simple and economical that can be adopted in regular Quality control test in Industries.

Background and objectives: Nanosponges are one of the most innovative ways to use the newest developments in nanodrugs delivery. Nanosponges can catch drugs that dissolve in water or ones that don't. This work uses statistical design to find the best nanosponges for drugs that don't dissolve easily and make them.

Material and methods: It was looked into how to statistically make the most of the effects of independent factors. The ethyl cellulose ratio and stirring rate were chosen based on how they affected the dependent variables, such as particle size and how well they were trapped. FTIR, SEM, zeta potential, entrapment efficiency, and particle size data were used to test the nanosponges that were made. Using carbopol, the best lot of nanosponges was added to the gel.

Results: Using ethyl cellulose and polyvinyl alcohol as stabilizers in the emulsion liquid diffusion method, it was possible to make drug-loaded nanosponges. It was possible to make the nanosponges composition work better by using Central Composite Design. It has been seen that making drug-filled nanosponges improves stability.

Conclusion: The study showcased the enhanced capacity of a formulation with decreased particle size and high entrapment efficiency to disseminate effectively.

Objective: This work is aimed to Formulate, Optimize and Evaluate Gastro-Retentive Microspheres of Antidiabetic Agent by Full Factorial Design.

Methods: Microspheres were prepared using Emulsification-cross linking technique. To this HPMC-K4M and Carbopol was dissolved in 250 ml of water and allowed to swell for 24 hr at room temperature. And separately chitosan was dissolved in 3% (v/v) glacial acetic acid and this also kept for 24 h to swell or dissolve properly. After 24hr this swelled mixture was mixed under magnetic stirrer (Remi, India) at specific stirring rate for 1hr in order to find homogeneous mass of both the gum. Then slurry of chitosan also was homogenized for half an hour. The drug, Glipizide (1g) was then added to the chitosan solution and mixed homogenesously.

Results: The aim of the study was to formulate and evaluate microspheres, for Gastro-Retentive Microspheres of the chosen drug. The EE of microspheres was found to be 91.52%, maximum . Buoyancy property observed was 93.82% for Optimized formulation F-9, Drug release 57.34% till 8 h. The work also aims to study various parameters affecting the behaviour of microspheres in oral dosage form.

Conclusion: Drugs with short half-life that are absorbed from the gastrointestinal tract (GIT) are eliminated rapidly from the blood flow. To avoid this, the oral SR Gastro-retentive was developed as this formulation released the drug slowly into the GIT and maintained a stable drug concentration in the serum for a longer duration of time.

An analytical, accurate, precise, specific, efficient and simple Ultra-Performance Liquid Chromatography method has been developed and validated for the determination of Pazopanib in bulk and was applied on marketed Pharmaceutical Dosage form. The mobile phase used for the chromatographic runs consisted of 0.1% OPA Buffer and Acetonitrile in the ratio of 30:70% v/v. The separation was achieved on a BHEL UPLC column using isocratic mode. Pazopanib Drug peak were well separated and were detected by a PDA detector at 256 nm. The developed method was linear at the concentration range 6-14 μg/ml for Pazopanib. The method has been validated according to ICH guidelines with respect to system suitability, specificity, precision, accuracy and robustness. The LOD and LOQ for the Pazopanib were found to be 0.5853 µg/ml and 1.7738µg/ml respectively. The developed method is simple, precise, specific, accurate and rapid, making it suitable for estimation of Pazopanib in bulk and marketed pharmaceutical dosage form dosage form.