- A method for synthesizing loteprednol etabonate and a method for synthesizing intermediate (by machine translation)
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The present invention provides a method of synthesizing loteprednol etabonate, comprises the following steps: step 1: to prednisolone as raw material preparation 11 β, 17 α - dihydroxy - 3 - oxo male steroid - 1, 4 - diene - 17 β - carboxylic acid; step 2: adopts the 11 β, 17 α - dihydroxy - 3 - oxo male steroid - 1, 4 - diene - 17 β - carboxylic acid preparation 17 α - ((ethoxy-formyl) oxy) - 11 β - hydroxy - 3 - oxo male steroid - 1, 4 - diene - 17 β - carboxylic acid ethyl carbonic anhydride; step 3: the 17 α - ((ethoxy-formyl) oxy) - 11 β - hydroxy - 3 - oxo male steroid - 1, 4 - diene - 17 β - carboxylic acid ethyl carbonic anhydride adding ethanol into sodium after a period of time by adding chlorine iodine methane then will be chlorine iodine methane. In step 3 can avoid the influence of the introduction of water to the intermediate. (by machine translation)
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Paragraph 0025; 0029; 0030
(2017/05/05)
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- Loteprednol preparation method and ophthalmic composition of loteprednol
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The present invention relates to a loteprednol preparation method and an ophthalmic composition of loteprednol, particularly to a loteprednol preparation method, which comprises: dissolving a raw material loteprednol in a first organic solvent to obtain a drug-containing solution, adding a second organic solvent to the obtained solution in a dropwise manner under stirring, continuously stirring, filtering, washing the filter cake by using the second organic solvent, and drying the obtained filter cake in a vacuum oven to obtain the product. The invention further provides a loteprednol bulk drug prepared according to the method, an ophthalmic pharmaceutical composition prepared by using the prepared loteprednol as a bulk drug, and uses of the prepared loteprednol in preparation of drugs for treatment or prevention of ocular inflammations or dry eye. The method of the present invention has excellent pharmaceutical properties, wherein the prepared bulk drug and the preparation have excellent stability.
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Paragraph 0088-0090; 0103-0105; 0118-0120
(2017/09/01)
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