1.Application of microwave irradiation technology to the field of pharmaceutics.
Xue-Bing ZHANG ; Nian-Qiu SHI ; Zhi-Qiang YANG ; Xing-Lin WANG
Acta Pharmaceutica Sinica 2014;49(3):303-309
Microwaves can be directly transformed into heat inside materials because of their ability of penetrating into any substance. The degree that materials are heated depends on their dielectric properties. Materials with high dielectric loss are more easily to reach a resonant state by microwaves field, then microwaves can be absorbed efficiently. Microwave irradiation technique with the unique heating mechanisms could induce drug-polymer interaction and change the properties of dissolution. Many benefits such as improving product quality, increasing energy efficiency and reducing times can be obtained by microwaves. This paper summarized characteristics of the microwave irradiation technique, new preparation techniques and formulation process in pharmaceutical industry by microwave irradiation technology. The microwave technology provides a new clue for heating and drying in the field of pharmaceutics.
Chemistry, Pharmaceutical
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methods
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Drug Discovery
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instrumentation
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methods
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Microwaves
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Pharmaceutical Preparations
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administration & dosage
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chemistry
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Technology, Pharmaceutical
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methods
2.Ligand efficiency and lead optimization.
Acta Pharmaceutica Sinica 2013;48(12):1755-1762
Pharmacological activity and druggability are two pivotal factors in drug innovation, which are respectively determined by the microscopic structure and macroscopic property of a molecule. Since structural optimization consists in a molecular operation in the space with multi-dimensions, and there exists a body of uncertainties for transduction from in vitro activity into in vivo pharmacological response. It is necessary for early stage in lead optimization to evaluate compound quality or efficiency using a kind of metrics containing multi-parameters. On the basis of the describing parameters of activity and druggability, this overview deals with the roles of thermodynamic signatures and binding kinetics of drug-receptor interactions in optimizing quality of compounds, signifying the significance in optimization of microscopic structures for drug discovery.
Drug Design
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Drug Discovery
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methods
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Ligands
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Molecular Structure
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Pharmaceutical Preparations
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chemical synthesis
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chemistry
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Pharmacokinetics
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Pharmacology
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Protein Binding
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Receptors, Drug
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chemistry
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Structure-Activity Relationship
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Thermodynamics
3.Lead compound optimization strategy (1)--changing metabolic pathways and optimizing metabolism stability.
Acta Pharmaceutica Sinica 2013;48(10):1521-1531
Lead compound optimization plays an important role in new drug discovery and development. The strategies for changing metabolic pathways can modulate pharmacokinetic properties, prolong the half life, improve metabolism stability and bioavailability of lead compounds. The strategies for changing metabolic pathways and improving metabolism stability are reviewed. These methods include blocking metabolic site, reduing lipophilicity, changing ring size, bioisosterism, and prodrug.
Animals
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Biological Availability
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Drug Design
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Drug Discovery
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Drug Stability
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Half-Life
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Humans
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Metabolic Networks and Pathways
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Pharmaceutical Preparations
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chemical synthesis
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chemistry
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metabolism
4.Application of efficient synthetic techniques in drug research.
Yu ZHOU ; Lei ZHANG ; Zeng LI ; Hong LIU
Acta Pharmaceutica Sinica 2013;48(7):1014-1030
Compound libraries and chemical synthesis play important roles in drug discovery and development, and efficient synthetic techniques can greatly facilitate the drug research. This review highlights the application of some efficient synthetic techniques in drug research including microwave chemistry, click chemistry, combinatorial chemistry, cascade reactions and multicomponent reactions, as well as the construction of diverse and drug-like compound libraries.
Click Chemistry
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Combinatorial Chemistry Techniques
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methods
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Drug Discovery
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methods
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Microwaves
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Pharmaceutical Preparations
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chemical synthesis
5.National pharmaceutical company No I - development and integration
Pharmaceutical Journal 1999;282(10):11-12
For the recent 15 years, in order to change the business as new mechanism, the National pharmaceutical company No I has upgraded, perfected the technical basis, materials and facility, profession. In which the human resource was considered as a most important factor for the development and integration
growth & development
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Chemistry, Pharmaceutical
6.Some results of study on the chemical components of Da cam-Hedyotis sp. Rubiaceae
Pharmaceutical Journal 1998;272(12):12-14
Species Da cam was identified as being Hedyotis capitellata Wall. Ex G.Don var. molis Piere ex Pit. It is used as a drug in traditional medicine. Primary results on our studies of Da cam have been presented that: the of Da cam contained alkaloid, saponin, iridoid, tanin. We have extracted and isolated from the leaves caulis of Da cam Sapogenin KLD3 and determinated it was Olanaolic acid
chemistry
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Hedyotis
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Pharmaceutical Preparations
7.Designing and optimizing the formulation of tablet of malumix by the artificial intellect system (CAD/CHEM 4.6)
Pharmaceutical Journal 1999;282(10):16-19
Malumix, an antiacid uncoated tablet, contains Magaldrate as the biological active agent. Its optimal formula was established by using the artificial intelligent software CAD/CHEM 4.6, based on the experimental data of nine designed formulae. The experimental properties of the above dosage form were almost the same in comparison with its predicted ones.
Chemistry, Pharmaceutical
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Artificial Intelligence
8.Analytical process of active ingredients belonging to benzodiazepine group currently in HoChiMinh city
Pharmaceutical Journal 2004;0(9):16-18
Basing on common chemical reactions, thin layer chromato graphy, absouptive ultraviolet spectrum some parameters were determined for preparation containing benzodiazepine in HCM City. The efficiency of extraction of benzodiazepan in 6 self made sample: Rhino sweet drink, coca-cola, combined food, soya milk, 333 beer and urine. Results found 17 active substances of diazepine group in 131 specialities of commercial propriatary name in HCM City, where diazepam had accounted higher rate in narcotic intoxixation cases. In criminal cases involved in tranquillisant narcotics, the most common substance were diazepan, flunitrazepan, clonazepan, bromazepan, alprazolam, clorazepat, oxazepan and nor-diazepan
Benzodiazepines
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Pharmaceutical Preparations
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Chemistry
9.Investigation on activity of cephalosporine C acylase from some species of microcryanisms isolated in Vietnam
Pharmaceutical Journal 2003;326(6):18-22
143 bacterial strains isolated in Vietnam for the cephalosporin C acylase activity. Among them, 116 strains showed growth on the LB plates containing cephalosporin and 28 strains did not grow. From 7 strains which grew very strongly on the LB plates containing cephalosporin C, 6 strains designated as 71, 91, DT3, M6, 03 and Tb23 were selected for further cultivation in the liquid culture medium and for determination of CA activity. The cell growth curves of these strain were very similar. The cell density reached a maximum at 24-30 hours of cultivation. Among three strains 71, DT3 and Tb23 evaluated for the CA activity, DT3 showed the highest CA activity. Thus, the strain DT3 was identified as Serratia marcescens sp. DT3. This is the first report about the Serratia strain producing CA enzyme
Pharmaceutical Preparations
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pharmacy
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chemistry
10.Study on influence of manufacture on chemical composition of Salomon's seal
Pharmaceutical Journal 2004;44(12):4-6
The chemical composition of Rhizoma Polygonati (RP) after processing was investigated. The result: All 4 process methods also procedure products no causing itch, black, sweet, soft, plastic. The chemical composition of unrefined Rhizoma Polygonati contained Alcaloid, Flavonoid, Sterol, Sugar, Iridoid glycosid, Amino acid and Fat. On the thin layer chromatograph, total alcaloid of Rhizoma Polygonati processed by a way had 4 spots, total flanoid had 4 spots, 1 spots of them cleare blue. The total sugar content of Rhizoma Polygonati processed by a way is 33,4% and of unrefined Rhizoma Polygonati is 12,63%. Both unrefined RP and processed RP also have 17 acid amin, among 7 essential acid amin for the body. The content of this acid amin of processed sample is usually higher than of unrefined sample
Chemistry
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Pharmacology
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Pharmaceutical Preparations