Guangzhou Cellprotek Pharmaceutical Co., Ltd

Guangzhou Cellprotek Pharmaceutical Ltd.

Guangzhou Cellprotek Pharmaceuticals Ltd.

Jingxia Zhang

Guangmei Yan

Pengxin Qiu

Haiyan Hu

Suizhen Lin

Jiesi Chen

Xinhua Li

Wei Yin

Wenbo Zhu

Bingzheng Lu

Yijun Huang

Xiuhua You

Ling Li

Ning Tian

Tiandong Leng

Hanfei Sang

Shujia Zhou

Halyan Hu

Minyu Xie

Use of 5&#x3b1;-androstane-3&#x3b2;,5,6&#x3b2;-triol and analogs thereof in the preparation of a drug for the prophylaxis or treatment of an altitude sickness caused by hypobaric hypoxia is provided, so as to provide a new drug for the prophylaxis or treatment of an altitude sickness. Researches revealed that 5&#x3b1;-androstane-3&#x3b2;,5,6&#x3b2;-triol treatment can effectively reduce vasogenic edema of brain tissue ofcaused by hypobaric hypoxia, reduce the increased cerebral water content, and protect from neuronal vacuolar degeneration caused by hypobaric hypoxia, therefore it can improve neurological dysfunctions caused by hypobaric hypoxia and is useful in prophylaxis or treatment of an altitude sickness.

Neuro-protective agents and uses thereof

The present invention relates to four crystalline forms (crystalline forms A, B, C and D) of 5&#x3b1;-androstane-3&#x3b2;,5,6&#x3b2;-triol (YC-6) and preparation methods therefor. The four crystalline forms have significant difference in their lattice parameters, 2&#x3b8; values and intensity in X-ray power diffraction, and melting points, etc. The study on its polymorphism is very important for further studying its effect, bioavailability and stability.

Crystalline forms of 5&#x3b1;-androstane-3&#x3b2;,5,6&#x3b2;-triol and preparation methods therefor

The present invention discloses compound 2&#x3b2;,3&#x3b1;,5&#x3b1;-trihydroxy-androst-6-one, having the structure of formula (I). The present invention also discloses a plurality of methods for preparing the compound and a use of the compound. 

2&#x3b2;,3&#x3b1;,5&#x3b1;-trihydroxy-androst-6-one and preparation methods and use thereof

Disclosed is the use of 5&#x3b1;-androstane-3&#x3b2;,5,6&#x3b2;-triol in preparing neuroprotective drugs. The compound has significant protective effect against neuron injuries caused by cerebral ischemia, spinal cord ischemia or hypoxia and has no obvious toxic reaction within effective dose thereof.

Use of 5&#x3b1;-androstane-3&#x3b2;,5,6&#x3b2;-triol in preparation of neuroprotective drugs

A 5&#x3b1;-androstane-3&#x3b2;,5,6&#x3b2;-triol injection and its preparation are disclosed. The injection uses hydroxypropyl-&#x3b2;-cyclodextrin as a solubilizing agent and the active ingredient is present at a weight ratio of 1-20:40-500 to the hydroxypropyl-&#x3b2;-cyclodextrin. The injection may also comprise, by weight, 1-100 parts of at least one isotonic adjusting agent, 0-200 parts of at least one freeze drying filler, and 0-2000 parts of at least one solvent. The preparation method comprises dissolving hydroxypropyl-&#x3b2;-cyclodextrin solution, 5&#x3b1;-androstane-3&#x3b2;,5,6&#x3b2;-triol and at least one additional soluble excipient in water for injection in sequence to obtain a raw injection solution, and subjecting the raw injection solution to decolorization, depyrogenation, filtration and sterilization to obtain the injection. Drying the filtrate yields a solid for injection.

5&#x3b1;-androstane-3&#x3b2;,5,6&#x3b2;-triol injection and preparation method therefor

A 5&#x3b1;-androstane-3&#x3b2;,5,6&#x3b2;-triol injection and its preparation are disclosed. The injection uses hydroxypropyl-&#x3b2;-cyclodextrin as a solubilizing agent and the active ingredient is present at a weight ratio of 1-20:40-500 to the hydroxypropyl-&#x3b2;-cyclodextrin. The injection may also comprise, by weight, 1-100 parts of at least one isotonic adjusting agent, 0-200 parts of at least one freeze drying filler, and 0-2000 parts of at least one solvent. The preparation method comprises dissolving hydroxypropyl-&#x3b2;-cyclodextrin solution, 5&#x3b1;-androstane-3&#x3b2;,5,6&#x3b2;-triol and at least one additional soluble excipient in water for injection in sequence to obtain a raw injection solution, and subjecting the raw injection solution to decolorization, depyrogenation, filtration and sterilization to obtain the injection, Drying the filtrate yields a solid for injection.

5&#x3b1;-androstane (alkyl)-3&#x3b2;, 5, 6&#x3b2;-triol injection and preparation method therefor

Disclosed is the use of 5&#x3b1;-androstane(alkyl)-3&#x3b2;,5,6&#x3b2;-triol in preparing neuroprotective drugs. The compound has significant protective effect against neuron injuries caused by cerebral ischemia, spinal cord ischemia or hypoxia and has no obvious toxic reaction within effective dose thereof.

Use of 5&#x3b1;-androstane (alkyl)-3&#x3b2;,5,6&#x3b2;-triol in preparation of neuroprotective drugs

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Guangzhou, China

Jingxia Zhang