Dosage forms of cyclosporine.

Cyclosporine can be given intravenously or orally, as a solution or soft gelatin capsule. Because of the drug's poor water solubility, ethoxylated plant fats and ethanol are added to the commercially available dosage forms.     

7-Aza-des-A-steroids with Antimicrobial and Cytotoxic Activity

This paper describes a convenient approach to the 7-aza-des-A-steroid (6,6a,7,8,9,9a-hexahydro-5H-cyclopenta[h]quinoline) scaffold starting from Grundmann’s ketone using two different pyridine annulation protocols. The biological evaluation of the pyridine and pyridinium products revealed that these compounds unexpectedly do not interfere with ergosterol and cholesterol biosynthesis. The pyridinium compound 6 showed significant antimicrobial and cytotoxic activities which are most likely due to its detergent-like structure.     

New Serratene Triterpenoids from Palhinhaea cernua and Their Cytotoxic Activity

Four new serratene triterpenoids, 3β,21β,24-trihydroxyserrat-14-en-24-(4'-hydroxybenzoate) (1), 3β,21α,24-trihydroxyserrat-14-en-3-(4'-hydroxybenzoate) (2), 3β,14α,15α,21α-tetrahydroxyserrat-14-en-3-(3'-methoxyl-4'-hydroxybenzoate) (3), and 3β,14α,15α,21α-tetrahydroxyserrat-14-en-21-acetyl-3-(4'-hydroxybenzoate) (4), together with two known ones, 5 and 6, were isolated from whole plants of Palhinhaea cernua. The structures of these new compounds were elucidated by spectroscopic methods. All the six compounds were tested for their in vitro cytotoxicity against three human cancer cell lines (K562, SMMC-7721, and SGC7901). Compound 5 showed cytotoxicity against the three test cell lines with IC50 values of 20.3, 34.0, and 22.5 ug/mL, respectively. Compound 1 showed slight cytotoxicity against K562 cell lines with IC50 value of 56.1 ug/mL, while no obvious inhibitory effects were detected for other compounds.     

诺氟沙星的剂型与临床应用

诺氟沙星为一氟喹诺酮类药物，在临床上广泛应用，本文就其新剂型和临床应用作的简要论述。     

固体制剂用新辅料的开发

辅料的种类和质量对药物制剂有重要影响。按辅料开发N3种方式：1）研发新的化合物或化学改性：2）对原有辅料进行物理修饰；（3）把两种或多种辅料预混处理得到新的复合辅料，归纳综述了目前固体制剂用新辅料的开发状况和趋势，着重介绍了预混辅料的研发进展。     

抗肝纤维化中药制剂的研究概况

目的：综述抗肝纤维化中药制剂的研究．说明进行其新剂型研究的意义。方法：针对中药治疗肝纤维化及中药制剂的特点，分析并阐述抗肝纤维化中药的常规制剂、缓控释制剂和靶向给药系统。结果：抗肝纤维化中药剂型各具特点，目前大多为常规制剂，新剂型的研究较少。结论：治疗肝纤维化的中药新剂型和新制剂具有很大的研究应用价值。     

Cytotoxic Activity and Quantitative Structure Activity Relationships of Arylpropyl Sulfonamides

B13 is a ceramide analogue and apoptosis inducer with potent cytotoxic activity. A series of arylpropyl sulfonamide analogues of B13 were evaluated for their cytotoxicity using MTT assays in prostate cancer PC-3 and leukemia HL-60 cell lines. Some compounds (4, 9, 13, 14, 15, and 20) showed stronger activities than B13 in both tumor cell lines, and compound (15) gave the most potent activity with IC₅₀ values of 29.2 and 20.7 µM, for PC-3and HL-60 cells, respectively. Three-dimensional quantitative structure-activity relationship (3D-QSAR) analysis was performed to build highly reliable and predictive CoMSIA models with cross-validated q² values of 0.816 and 0.702, respectively. Our results suggest that long alkyl chains and a 1R, 2R configuration of the propyl group are important for the cytotoxic activities of arylpropyl sulfonamides. Moreover, the introduction of small hydrophobic groups in the phenyl ring and sulfonamide group could increase biological activity.     

Antitumor Activity and Toxicity of Olivamide Dosage Form,a New Semi-Synthetic Olivomycin a Derivative

Pharmaceutical Chemistry Journal - Methods for selective chemical modification of the antibiotic olivomycin A (OA) were developed at G. F. Gause Institute of New Antibiotics. The compound with the...     

Development of a Dosage Form of the New Antitumor Antibiotic Olivamide

Pharmaceutical Chemistry Journal - Methods for selective chemical modification of the antitumor antibiotic olivomycin A(OA) were developed at GINA. The compound olivamide with advantages over...     

Synthesis and Cytotoxic Activity of Hydroxy-Substituted Glaucocalyxin A

Pharmaceutical Chemistry Journal - Six new glaucocalyxin A derivatives were synthesized by hydroxy substitution, their structures were elucidated on the basis of spectral analysis, and cytotoxic...     

Semisynthesis,Cytotoxic Activity,and Oral Availability of New Lipophilic 9-Substituted Camptothecin Derivatives

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银杏提取物活性成分的新剂型研究概述

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