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Crisaborole ointment and preparation method thereof

A technology of cleaborol and ointment, which is applied in the directions of ointment delivery, pharmaceutical formulations, active ingredients of boron compounds, etc., can solve the problem that it is difficult to avoid the chemical stability of water raw materials, it is difficult to make stable products, and the properties are uneven. and other problems, to achieve the effect of ensuring chemical stability, ensuring physical stability, easy extrusion and smearing

Pending Publication Date: 2022-07-22
北京阳光诺和药物研究股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004]But white petrolatum is a mixture of mineral esters, its composition is complex, and for unstable raw materials, its chemical stability is risky; in addition, its properties are also uneven, It is difficult to make a stable product with this excipient
However, if it is replaced with other ointment bases such as lanolin, polyethylene glycol, etc., which are hygroscopic, it is difficult to avoid the influence of the chemical stability of moisture materials

Method used

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  • Crisaborole ointment and preparation method thereof
  • Crisaborole ointment and preparation method thereof
  • Crisaborole ointment and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Example 1, preparation of creborone ointment

[0049] A 2% creborone ointment was prepared using white petrolatum within the scope of this application.

[0050] 1. Quality inspection of white vaseline

[0051] The white vaseline of this embodiment was purchased from Tianjin Hongfa Shuangsheng White Vaseline Co., Ltd. After identification, each quality inspection result conforms to the regulations in the "Chinese Pharmacopoeia 2020 Edition Four Volumes", and the specific inspection results are shown in Table 1.

[0052] Table 1, embodiment 1 white vaseline quality test result

[0053]

[0054]

[0055] Second, the prescription of criborole ointment

[0056] Table 2, the prescription of embodiment 1

[0057]

[0058]

[0059] 3. Preparation process

[0060] Prepare criborole ointment as follows:

[0061](1) Oil phase preparation: white petrolatum, paraffin, glyceryl monostearate and glyceryl monostearate are weighed and added to the container in turn, pla...

Embodiment 3

[0100] Example 3. Microscopic observation of droplet particle size

[0101] Use a microscope to observe the particle size of the droplets in the ointments prepared in Example 1, Comparative Example 1 and Comparative Example 2. The microscopically magnified 100 times observation image of Example 1 is shown in figure 1 , the comparison example 1 microscopically magnified 100 times to observe the image, see figure 2 , the comparison example 2 microscopically magnified 100 times to observe the image, see image 3 .

[0102] Depend on Figure 1-3 It can be seen that the particle size in Example 1 is all less than 16 μm, most (90%) of which are less than 12 μm, and the particle size in Comparative Example 1 is less than 25 μm, and most of them are distributed in 12-23 μm. The droplets have the phenomenon of re-agglomeration, and there are larger droplets with a particle size distribution of 30-70 μm, and the maximum can reach 64.08 μm. The droplets of Example 1 are smaller and m...

Embodiment 4

[0103] Example 4, flow curve comparison

[0104] Example 1, Comparative Example 1 and Comparative Example 2 g of Riborol ointment were respectively detected using Anton Paar MCR92, and the detection parameters are shown in Table 7.

[0105] Table 7. Flow curve detection conditions

[0106] parameter set conditions test mode Rotation mode; log sweep; linear coordinates rotor pp25 temperature(℃) 25 Holding time (s) 60 Pre-cut time (s) 0 Shear rate 0.1→100s-1 number of data points 21 change in time 10s~1s sample gap 1.0mm Add sample method Squeegee data processing model Herschel-Bulkley

[0107] Table 8. Comparison of yield stress and viscosity

[0108] sample name Yield stress (Pa) Initial viscosity (mPa.s) 50(1 / s) Viscosity (mPa.s) Comparative Example 1 715.68 5088000 34893 Example 1 292.39 1808000 20403 Comparative Example 2 46.492 530500 3722.6 ...

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Abstract

The invention discloses crisaborole ointment and a preparation method thereof. The crisaborole ointment is prepared from crisaborole, fatty alcohol, a metal chelating agent, a grease antioxidant, white vaseline, a wax hardening agent and a surfactant. The penetration of the white vaseline is 160-240 units, preferably 180-200 units, and the impurity absorbance under the wavelength of 290 nm is less than or equal to 0.07. According to the crisaborole ointment disclosed by the invention, raw material phase liquid drops are smaller and are more easily absorbed by skin; the yield stress is smaller, extrusion and smearing are easier during use, the structure can be recovered after smearing, and the original properties of the ointment are kept; the chemical stability of crisaborole can be better ensured; the preparation process is further optimized according to the properties of the raw materials, and the dispersed particle size and uniform distribution of the liquid drops can be stably maintained on the premise of ensuring the homogeneity, so that the physical stability of the ointment is ensured.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a cleaborol ointment and a preparation method thereof. Background technique [0002] Criborone, chemical name 5-(4-cyanophenoxy)-1,3-dihydro-1-hydroxy-[2,1]-benzoxaborole. Criborole is a phosphodiesterase 4 (PDE-4) inhibitor. Inhibition of PDE-4 results in increased intracellular cyclic adenosine monophosphate (cAMP) levels. The specific mechanism of action of criborole in the treatment of atopic dermatitis is not clear. [0003] Criborone is unstable in water, and it is dissolved in a non-aqueous solvent such as a polyhydric alcohol solvent and protected with a metal chelating agent, which is beneficial to reduce the influence of water on the stability of Criborone; It is easy to decompose under strong light irradiation. The raw material solution is dispersed in the oil phase matrix composed of mineral ester, wax hardener, surfactant, and grease antioxidant to make ...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K31/69A61K47/06A61K47/10A61K47/12A61K47/18A61P17/00A61P37/08
CPCA61K31/69A61K9/06A61K47/06A61K47/183A61K47/12A61K47/10A61P17/00A61P37/08
Inventor 郑柏松刘宇晶罗桓于洋孙丽张智斌
Owner 北京阳光诺和药物研究股份有限公司
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