Tetracaine hydrochloride crystal, composition containing tetracaine hydrochloride and preparation method thereof

A technology of tetracaine hydrochloride and its composition, which is applied in the field of local anesthetics, can solve problems such as increased adverse reactions, reduced drug efficacy, and unfavorable purity levels, so as to improve stability and drug safety, reduce the use of excipients, and reduce the Effects of Security Risks

Active Publication Date: 2015-04-29
李宏 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

This patented technology allows creating pure tetraacylammonia (TAA) with improved properties such as increased water content or lowered melting point compared to other methods like evaporation techniques. These new forms also have fewer harmful chemicals added during manufacturing process. They may even help make certain types more stable but less effective at producing them due to their low concentration levels. Overall, this method provides an efficient way to produce these important molecules while reducing environmental concerns associated with traditional ways of making it.

Problems solved by technology

The technical problem addressed in this patents relating to preparing stable crystalline forms of tacrolimus hydrochioride (TCLH), such as those described above, is finding suitable methods to achieve desired levels of impurities during manufacturing processes while maintaining their bioavailability over time without compromising its effects on patient health outcomes due to potential side effects caused from excessive exposure to certain substances like other drugs commonly found within the same class called nitrated caffeine analogs.

Method used

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  • Tetracaine hydrochloride crystal, composition containing tetracaine hydrochloride and preparation method thereof
  • Tetracaine hydrochloride crystal, composition containing tetracaine hydrochloride and preparation method thereof
  • Tetracaine hydrochloride crystal, composition containing tetracaine hydrochloride and preparation method thereof

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Embodiment 1

[0033] The preparation of embodiment 1 tetracaine hydrochloride crystal

[0034] Take by weighing 300 grams of tetracaine hydrochloride, add 6 liters (L), 20 ℃ of water stirring and dissolving under nitrogen protection, be made into the tetracaine hydrochloride solution that concentration is 5%;

[0035] Under a sound field with a frequency of 25KHz and an output power of 10W, under stirring at 50 rpm (r / min), add a mixture of n-butanol and n-hexane at a rate of 20 ml / min (mL / min) at 10°C Solvent (the volume ratio of n-butanol and n-hexane is 2:1) 12L, stop the sound field after adding, let stand to grow crystals for 3 hours; filter after the crystals are precipitated, wash with absolute ethanol, and vacuum dry for 5 hours to obtain tetracaine hydrochloride Because of the crystals, the weight is 267.3g, and the yield is 89.1%.

[0036] The crystal that obtains tetracaine hydrochloride is tested, and the following examples all adopt this test method, and the follow-up will not...

Embodiment 2

[0043]The preparation of embodiment 2 tetracaine hydrochloride crystals

[0044] Take by weighing 300 grams of tetracaine hydrochloride, add 1.5 L, 25 ℃ of water under the protection of nitrogen, stir and dissolve, and be made into the tetracaine hydrochloride solution that concentration is 20%;

[0045] Under the sound field that the frequency is 30KHz and the output power is 70W, under stirring at 100r / min, add the mixed solvent of n-butanol and n-hexane at 2°C at a rate of 60mL / min (the volume ratio of n-butanol and n-hexane is 4 : 1) 4.5L, stop the sound field after adding, leave standstill to grow crystal 4 hours; Filter after crystal precipitation, wash with dehydrated alcohol, vacuum-dry 10 hours, obtain the crystal of tetracaine hydrochloride, weight is 272.1g, yield was 90.7%.

[0046] The X-ray powder diffraction pattern obtained by measuring the crystalline compound using Cu-Kα rays is as follows: figure 1 shown. Detected by high performance liquid chromatography...

Embodiment 3

[0047] The preparation of embodiment 3 tetracaine hydrochloride crystals

[0048] Take by weighing 300 grams of tetracaine hydrochloride, add 3 L, 22 ℃ of water under the protection of nitrogen, stir and dissolve, and make the tetracaine hydrochloride solution that concentration is 10%;

[0049] Under the sound field that frequency is 30KHz, output power is 50W, under 160r / min stirring, add the mixed solvent of n-butanol and n-hexane of 8 ℃ (the volume ratio of n-butanol and n-hexane is 10 with the dripping speed of 40mL / min : 1) 15L, stop the sound field after adding, leave standstill to grow crystal 6 hours; Filter after crystal is separated out, wash with dehydrated alcohol, vacuum-dry 7 hours, obtain the crystal of tetracaine hydrochloride, weight is 258.0g, yield is 86.0%.

[0050] The X-ray powder diffraction pattern obtained by measuring the crystalline compound using Cu-Kα rays is as follows: figure 1 shown. Detected by high performance liquid chromatography, its pu...

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Abstract

The invention relates to a tetracaine hydrochloride crystal and a preparation method thereof, and a composition containing tetracaine hydrochloride and a preparation method thereof. The tetracaine hydrochloride crystal has characteristic peaks in the X-ray powder diffractogram at the following 2theta diffraction angles: 6.7 degrees, 11.0 degrees, 13.5 degrees, 14.2 degrees, 14.7 degrees, 17.4 degrees, 18.6 degrees, 19.7 degrees, 20.2 degrees, 21.0 degrees, 21.8 degrees, 23.2 degrees, 23.8 degrees, 24.4 degrees, 24.9 degrees, 26.1 degrees, 27.1 degrees, 28.9 degrees, 30.5 degrees, 32.2 degrees, 33.6 degrees, 34.1 degrees, 34.8 degrees, 35.8 degrees, 38.9 degrees, 39.4 degrees and 40.0 degrees. The crystal purity is 99.8% above, and no organic solvent resides; and the composition prepared from the crystal has the advantages of favorable dissolvability, high stability and high medical safety.

Description

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Claims

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Application Information

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Owner 李宏
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