Doxycycline hydrochloride solution and preparation method thereof
A technology of doxycycline hydrochloride and doxycycline, applied in the direction of tetracycline active ingredients, antibacterial drugs, etc., can solve the preparation and application of doxycycline hydrochloride instability constraints, no obvious improvement in drug oxidative discoloration, metal Solve problems such as low solubility of ion complexes, achieve high practical value, reduce drug loss, and simplify the administration process
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Embodiment 1
[0037] Example 1 Screening of polysesthetic solution hydrochloride solution
[0038] The present invention found in the pre-experimental screening, although 10%, 20% concentration of hydrochloride solution can be prepared in a suitable excipient combination, but it is more difficult to prepare a high concentration of properties (30%) Western hydrochloride solution. Accordingly, the present invention is intended to prepare a high concentration (30%) hydrochloride polycyclo solution in which properties stabilized, and then dose adjustment at a high concentration (30%), and screens 10% and 20% concentration.
[0039] In order to provide a polysestyloxin solution having a concentration height (30%) and stable properties, that is, after a long-term placement, the solution is not reduced and the solution color does not deeperate, and the preparation of a well-affected hydrochloride solution is carried out. A large number of explorations and attempts. Some pre-selection prescriptions wer...
Embodiment 2
[0052] Example 2 Optimization of hydrochloride solution prescription
[0053] 1. Single factor screening of polysestylin solution hydrochloride solution
[0054] In order to further enhance the stability of the Doublestiplin solution of the present invention, the present invention is found in the original prescription by measuring the drug content and color of the prepared hydrochloride solution after analyzing the prepared hydrochloride solution. The antioxidants and complexing agents are added to make the stability of the polysestylcyclic solution made of hydrochloride solutions. Among them, the antioxidant is a butylhydroxy anisole (BHA), dibutylhydroxytol (BHT), and tert-butyl phenol (TBHQ), or no mercynin (PG), the complexing agent Citric acid or L-tartaric acid. The specific prescription is shown in Table 4:
[0055] Table 4
[0056] Prescription Prescription Prescription Prescription four DOX DOX DOX DOX BHA, BHT, TBHQ BHA, BHT, TBHQ No mercyl ester...
Embodiment 3
[0103] Example 3 Preparation and Acceleration Test of Polycyclo Solution of Hydrochloride
[0104] In order to further verify the stability of the polysestylcyclic solution of the present invention, the present invention has been formulated by 10%, 20%, and 30%, respectively, of the accelerated test and content measurement.
[0105] The process of the doxycycline solution is shown in Table 13, and the amount of DOX in the table is as a westheninometer.
[0106] Table 13 Hydrochloride solution
[0107]
[0108] Preparation method: Under a nitrogen, apply an appropriate amount of 1,2-propylene glycol in the beaker, add absolute ethanol, and then add no saladate and citric acid, slow heating to 50 ~ 65 ° C, and after all reagents are fully dissolved, Keep the temperature, adding hydrochloride polycyclosin, thoroughly stirring dissolved, cooling, and displays the solvent to 100 mL, filtrate, and poured into the container in the container. Nitrogen.
[0109] The nitrogen environment ...
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