Latest ArticlesCompound amino acid injection, as the source of nitrogen in parenteral nutrition, is administrated to patients with compromised gastrointestinal function or those whose nutritional needs cannot be met through gastrointestinal tract. Therefore, compound amino acid injection plays an important role in nutritional therapy and support. The active pharmaceutical ingredients of compound amino acid injection are complicated, and some amino acids are sensitive to light, heat, and oxygen, etc., which brings certain challenges to the research and development of such drugs. Based on literature research and evaluation experience in recent years, this paper discusses some issues which may need to consider during the development of generic drugs of compound amino acid injection from the aspects of API quality control, formulation design, manufacturing process development, quality research and control, selection of container enclosure system and stability studies in order to provide reference for researchers in this field.
In order to improve the oral bioavailability of curcumin, curcumin nanocrystalline suspension (Cur-NCS) was prepared by the high-pressure homogenization method in "top-down" method. Its physical properties, in vitro release, in vivo bioavailability and anti-inflammatory activity were studied.
The prescription and process parameters were optimized using particle size and zeta potential as evaluation indexes; the sample morphology was characterized by transmission electron microscopy, the in vitro release of curcumin nanocrystallines suspension was determined by HPLC, and the blood concentration of curcumin in rats was measured by LC-MS/MS; the anti-inflammatory activity was investigated in RAW264.7 inflammatory cell model, and curcumin was investigated in a mouse model of bronchial asthma airway inflammation nanosuspension on the therapeutic effect of curcumin on airway inflammation in mice.
Preparation process: curcumin was sheared at high speed for 2 min at 16 000 r·min-1 and cycled 40 times at 800 bar. Prescription: curcumin dosage was 0.2%, TPGS dosage was 0.20% and soy lecithin dosage was 0.16%; the cumulative drug release of API and Cur-NCS was 11.67% and 27.44%, respectively. After gavage in rats, Cur-NCS bioavailability was increased by 1.86-fold after gavage in rats. In an in vitro inflammatory cell model and in vivo bronchial asthma mouse model, Cur-NCS significantly inhibited the expression of inflammatory factors NO, IL-6, TNF-α and the levels of MDA, IgE and ICAM-1, and increased the expression of IL-10 and the level of SOD.
The identified preparation process and prescription can meet the preparation requirements of curcumin nanosuspension, and the in vitro release, in vivo bioavailability and anti-inflammatory activity are significantly better than those of API, and curcumin nanosuspension can provide ideas for subsequent dosage form studies.
Clinical trials is a scientific experimental activity that needs thorough plan and strict execution. Investigators often expect to complete the trial according to the study plan. However, due to the uncertainty of disease mechanisms, the diversity of patients, and the complexity of interventions, trials usually cannot be executed exactly according to the established protocols. A comprehensive review of the implementation of registered clinical trials reveals that such situations are not uncommon and commonly include: the aim of the clinical trials is apparent inability to complete thus requiring termination of the trials; unexpected events, such as adverse reactions, policy changes, etc., leading to suspend the trial and adjust the trial protocol. However, research on this issue is limited, and there is no definite answer on the scientific understanding, reason analysis, and plan design. In this paper, we comprehensively review the factors related to the suspension and termination of clinical trials and try to propose a solution.
The phosphorylation of serine 209 of eukaryotic translation initiation factor 4E (eIF4E) by mitogen-activated protein kinase-interacting kinase (MNK) is closely related to the process of translation initiation of tumor-related mRNA, and this process plays an important role in tumor occurrence and metastasis. Since MNK has gradually become an important antitumor target, the development of MNK small-molecule inhibitors has attracted the attention of researchers in recent years. Therefore, we reviewed the research progress of MNK small-molecule inhibitors by summarizing the structure and signal transduction mechanism of MNK.
To prepare photothermal lipid membrane coated Escherichia coli and study the properties.
The photothermal lipid membrane (LMI) was prepared by thin film dispersion method, and the electrostatic adsorption method was used to coat Escherichia coli with the lipid membrane (LMI@Ec). The size and potential of LMI@Ec were analyzed by laser scattering particle size analyzer, the morphology of E.coli and LMI@Ec was observed by transmission electron microscopy and laser confocal microscopy, and plate counting method was used to detect cell viability of LMI@Ec. In addition, the effect of protein expression of LMI@Ec was evaluated by polyacrylamide gel electrophoresis, and the photothermal effect of LMI@Ec was detected by Infrared Photothermal Imager.
LMI@Ec had a smooth surface with the average particle size of (1 990.5±132) nm and the potential of -(5.09±0.52) mV. The coating of the lipid membrane had little effect on the activity of E.coli. Although the bacterial activity decreased after laser irradiation, the growth curve recovered to the same level as wild bacteria after 10 h of temperature gradient culture in LB medium. LMI@Ec had well photothermal properties and can normally express protein. In vitro cytotoxicity experiments showed that LMI@Ec under 808 nm laser irradiation presented enhanced antitumor effect on B16F10 and HepG2 cells.
The successful preparation of LMI@Ec provides a new research direction for the subsequent in-depth study of bacteria-mediated disease treatment.
Salt-inducible kinases (SIKs) belong to the AMP-activated protein kinase (AMPK) family, which mainly regulates the cytosolic-cytoplasmic distribution of cAMP-response element binding protein transcriptional coactivators (CRTCs). They exert regulatory effect on the synthesis of CRTC-CREB complexes, which indirectly affect the transcription and expression of CREB target genes and various physiological processes, such as energy metabolism, cell cycle progression and apoptosis. Previous researches related to SIKs have focused on peripheral system diseases, including tumors, hypertension and gluconeogenesis. In recent years, increasing studies have begun to explore the link between SIKs and central nervous system diseases with abnormal levels of SIKs present in diseases such as depression, sleep disturbance, epilepsy and Alzheimer's disease. It suggests that dysregulation of SIKs signaling is involved in the pathological processes of these diseases and has the potential to become new therapeutic targets in these diseases. This article reviews the role and regulatory mechanisms of SIKs in depression, sleep disturbance and other neurological diseases.
Different levels of genotoxic impurities 1-methyl-4-nitroso piperazine (MNP) and 1-methyl-4-nitroso piperazine (CPNP) were detected in rifampicin and rifapentine capsules. In this study, the nitrite ions in rifampicin and rifapentine capsules were determined by solid phase extraction-ion chromatography to explore the relationship between the content of nitrite ions and the formation of above genotoxic impurities.
The method of solid phase extraction-ion chromatography used for nitrite determination was established and validated.
Nitrite ion was not detected in rifampicin and rifapentine capsules with different levels of MNP and CPNP.
It is speculated that the origin of MNP and CPNP in rifampin and rifapentine capsules was not from nitrite ion, but derived from oxidative degradation of API.
Histopathology data of toxicology studies during nonclinical safety evaluation of drugs are critical during the drug discovery and development process that is necessary for regulatory bodies to assess drug-related toxicity in laboratory animals and its impact on human safety in clinical trials. Artificial intelligence (AI) has been widely used in clinical medical practice with progress in the whole slide image (WSI), digital pathology and algorithms. However, the progress of machine learning (ML)-in particular, deep learning (DL)-has been rather slow in toxicologic pathology of nonclinical toxicology studies. This paper briefly reviews the role of toxicologic pathology in drug discovery and development, overview of AI and approaches of DL, applications of approaches of DL in toxicologic pathology, as well as the challenges in implementation of approaches of DL in toxicologic pathology, in order to provide reference for implementation of approaches of DL in toxicologic pathology for toxicology studies during nonclinical safety evaluation of drugs in China.
The establishment of impurity limits is one of the key factors in the establishment of drug product specifications. Reasonable impurity limits are very important for the safety and controllability, and closely related to the drug quality. Taking several typical impurities as examples, this paper systematically expounds and demonstrates the determination approach of the maximum daily exposure dose (PDE), the conversion method in specific drugs, and the limit determination of impurities in products, which can help better understand and implement ICH-related guidelines. This paper provides reference for drug developers to formulate product specification.
In recent years, with the aging of the global population and the general improvement of consumer awareness, disease prevention and early intervention have been paid more and more attention, and the traditional Chinese medicine (TCM) industry, which has the unique advantage of "preventive treatment of disease", has ushered in a huge development opportunity. Especially under the special background of the global COVID-19 pandemic, TCM has played an important role and provided a good opportunity for its industrial development. With the promulgation of a series of policies in China, the inheritance and innovative development of TCM have been accelerated. In this paper, we investigated the TCM's domestic and foreign market, research and development investment of enterprises, approval trend of innovative drugs, and internationalization and the layout of patents in the past 20 years, analyzed the current situation of TCM innovation and development, and looked forward to the future trend, with a view to provide inspiration for the future inheritance and innovation of TCM.
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