- Preparation method of hydrocortisone sodium succinate
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The invention discloses a preparation method of hydrocortisone sodium succinate. The method comprises the steps of preparing hydrocortisone succinic acid monoester by using succinic anhydride and hydrocortisone as raw materials; and performing a reaction by using the hydrocortisone succinic acid monoester as a raw material at a low temperature, and after the reaction is completed, performing treatment on the reaction liquid by adopting acetone with a temperature of about -20 DEG C to obtain the hydrocortisone sodium succinate. The process conditions adopted in the method provided by the invention are as follows: the sodium salt is generated at the low temperature, then the reaction liquid is added into a large amount of acetone, filtering is performed, the filter cake is washed by using the acetone and water, and finally vacuum drying is performed to remove the acetone; the process of high-temperature steaming is avoided, so that the product is stable, and has a high yield and a good state; the purity can reach 97% or more during reaction, and after purification, the product is in full compliance with the Chinese Pharmacopoeia standard; and the acetone can be recycled, so that theproduction costs are saved; therefore, the solution is suitable for industrial production, and the product quality is good.
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Paragraph 0042-0044; 0046-0048; 0050-0052; 0054-0056
(2019/10/02)
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- Production process of hydrocortisone hemisuccinate
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The invention discloses a production process of hydrocortisone hemisuccinate. The production process comprises a step of enabling hydrocortisone to react with succinic anhydride in an acetone solventby using triethylamine as a catalyst, wherein a mass ratio of the hydrocortisone and the succinic anhydride is 1 to (0.7 to 1.1), a mass ratio of the hydrocortisone and the acetone is 1 to (3 to 5), and a mass ratio of the hydrocortisone and the triethylamine is 1 to (0.2 to 0.5). According to the production process of the hydrocortisone hemisuccinate disclosed by the invention, the effects that the yield is greatly increased and the environment is friendly are also achieved while the hydrocortisone hemisuccinate uses pyridine or dimethyl sulfoxide as the solvent at the same time.
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Paragraph 0012-0016
(2019/01/20)
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- Magnetic particle-based hydrocortisone chemiluminescence immune assay method and kit
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The invention discloses a fully-automatic magnetic particle-based hydrocortisone chemiluminescence immune assay method and application thereof. Immunomagnetic beads are coated by goat anti rabbit, antigen is detected by a chemiluminescent marker, a specific antibody of hydrocortisone is applied, a competitive response mode is established, a fully-automatic chemiluminescence immune assay serves asa detection tool, and the hydrocortisone is quantitatively detected according to the measured luminous value. According to the established method, the maximal detection range of the hydrocortisone reaches to 0.42 to 72.27 ng/mL, the detection limit is 0.12 ng/mL, the sensitivity can reach to 5.57 ng/mL and the recovery rate is 84.3 to 102.3 percent. According to the method, the detection process can realize full automation, the influence by professional testing personnel is not considered, the whole detection process is rapid and can be completed only by about 40 minutes, the detection limit is low, the sensitivity is high, the linear range is wide, the market requirement is met and good market application prospect is achieved.
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Paragraph 0015; 0054-0056
(2018/07/30)
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- Design and synthesis of furoxan-based nitric oxide-releasing glucocorticoid derivatives with potent anti-inflammatory activity and improved safety
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A series of furoxan-based nitric oxide-releasing glucocorticoid derivatives was synthesized. The pharmacological assays indicated that three compounds, including I4, I5, and I6, had anti-inflammatory activity. Furthermore compared with the leading compound hydrocortisone the safety of I6 was greatly improved. Due to releasing NO in vivo the side effects of glucocorticoids, including hypertension and osteoporosis, were effectively avoided.
- Fang, Lei,Zhang, Yihua,Lehmann, Jochen,Wang, You,Ji, Hui,Ding, Dayong
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p. 1062 - 1066
(2007/10/03)
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- The synthesis and immunosuppressive activities of steroid-urotoxin linkers
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The urotoxins (Glu-Asp-Gly-OH, His-Gly-Glu-OH, His-Gly-Lys-OH, and His-Gly-Lys-NHNH2) were introduced into the convenient sites of hydrocortisone and prednisolone via the amidation or condensation reactions to form the corresponding linkers 7a-d, 8a-d, 9a,b, and 10a,b in acceptable yields. The bioassays such as prolongation of heterotopic transplanted cardiac tissue survival in vivo, inhibitory effects on phagocytosis of mouse peritoneal macrophages and concanavalin (ConA) or lipopolysaccharide (LPS) induced proliferation of mouse spleen lymphocytes in vitro show that at the comparable concentrations the immunosuppressive activities of the steroid-urotoxin linkers 7a-d, 8a-d, 9a,b, and 10a,b were higher than that of hydrocortisone, prednisolone, and the urotoxins alone, as well as significantly higher than that of the mixture of hydrocortisone and urotoxins or prednisolone and urotoxins. The so-called 'permissive action' may be responsible for the enhancement of the mentioned bioactivities of the steroid-urotoxin linkers 7a-d, 8a-d, 9a,b, and 10a,b.
- Wang, Chao,Zhao, Ming,Qiu, Xuecai,Peng, Shiqi
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p. 4403 - 4421
(2007/10/03)
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- Preparation of europium-labeled derivatives of cortisol for time-resolved fluoroimmunoassays
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Cortisol 3-(O-carboxymethyl)oxime, 6- and 21-hemisuccinoxycortisol, and Cortisol 7-carboxyethyl thioether were synthesized. These carboxyl derivatives were labeled using a described general labeling method with a europium chelate. The labeled steroids were tested in a competitive time-resolved fluoroimmunoassay using antibodies raised against cortisol. Only the site-homologous antigen-antibody pairs underwent immunoreaction and gave satisfactory calibration curves.
- Mikola, Heikki,Miettinen, Paeivi
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