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

Active Publication Date: 2022-02-11
SOUTH CHINA AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are three major difficulties in the preparation of doxycycline hydrochloride solution: one, the groups such as phenolic hydroxyl group, enol group and amido group contained in the doxycycline hydrochloride structure are easily oxidized and hydrolyzed, resulting in doxycycline hydrochloride in the Under heating condition, or easily oxidize and decompose in solution, very easily cause phenomena such as solution system discoloration, drug content to reduce; Its two, under conditions such as light, easily generate isomer (comprising in doxycycline hydrochloride solution) 4-epidoxycycline, 6-epidoxycycline, etc.), or become the main reason for the deepening of the color of its solution system; third, although studies have shown that the complexation of doxycycline hydrochloride and metal ions can be used Make it form a complex to improve the stability of doxycycline hydrochloride, but further research shows that the complex formed by metal ions and doxycycline does not significantly improve the problem of drug oxidative discoloration
At the same time, because tetracycline drug molecules contain many hydroxyl groups, enol hydroxyl groups and carbonyl groups, the metal ion complexes formed have low solubility, which will affect the absorption of drugs when used as oral solutions.
The instability of doxycycline hydrochloride restricts the preparation and application of the drug solution dosage form

Method used

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  • Doxycycline hydrochloride solution and preparation method thereof
  • Doxycycline hydrochloride solution and preparation method thereof
  • Doxycycline hydrochloride solution and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

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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Abstract

The invention provides a doxycycline hydrochloride solution and a preparation method thereof. According to the invention, the highest concentration of doxycycline in the doxycycline hydrochloride solution is 30%, the doxycycline hydrochloride solution can be diluted with water in any proportion to be used as a doxycycline hydrochloride oral solution, the solution has good stability, the stability is good after the solution is mixed with water, and the palatability is not influenced; and the doxycycline hydrochloride solution overcomes the phenomena that existing doxycycline hydrochloride soluble powder is prone to generating precipitates, uneven in dissolution and the like during high-concentration dissolution, solves the problem of high-concentration dissolution of doxycycline hydrochloride, and is suitable for being used in actual production and high in practical value.

Description

Technical field [0001] The invention belongs to the technical field of veterinary drug preparation. More specifically, it relates to a polysethytic solution of hydrochloride and a preparation method thereof. Background technique [0002] According to the "2019 Chinese Antibacterial Pharmacies", the beast antibacterial drug is administered mainly by mixed feeding pathway, accounting for 61.81%, and the drinking water is given by 17.64%. However, in 2019, the Ministry of Agriculture issued an announcement No. 194, requiring all of the promotion of all promoting growth drug feed additives in addition to traditional Chinese medicine from 2020, while livestock bacterial diseases remains currently in scale and individuals. Common diseases in breeding in breeding process. Therefore, in the case where the traditional feed dosage mode is limited by the forbidden prevention, the drinking water administration is simple, fast, stress, and quick start, less labor, and large groups of drugs. W...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/65A61P31/04
CPCA61K31/65A61P31/04
Inventor 黄显会刘子瑶崔璨李欣龚炯舟于洋张云晓邓竞增
Owner SOUTH CHINA AGRI UNIV
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