Clathrate compound of periplaneta americana and cyclodextrin or cyclodextrin derivative and preparation method of clathrate compound
By preparing the inclusion compound of the American cockroach and γ-cyclodextrin, the limitations of the American cockroach extract were solved, and stability and convenience of multi-dose application were achieved.
Patent Information
- Application Number
- CN202510681010.4
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2025-05-26
- Publication Date
- 2025-08-15
AI Technical Summary
The clinical application dosage forms of the existing American cockroach extract are limited to drops, injections and capsules, and have certain defects, which limit their clinical application.
The American cockroach and γ-cyclodextrin were mixed in a certain proportion, and the inclusion compound was prepared into a powder form through the inclusion reaction. The solvent was removed by freeze-drying method to form the American cockroach/γ-cyclodextrin inclusion compound.
It realizes the stability protection of the American cockroach extract, is easy to store and transport, and can be mixed with other auxiliary materials to make various dosage forms, expanding its clinical application.
Smart Images
Figure CN120478671A_ABST
Abstract
Description
Technical Field
[0001] The invention belongs to the field of pharmaceutical preparations, and particularly relates to an inclusion compound of American cockroach and cyclodextrin or a cyclodextrin derivative and a preparation method thereof. Background Art
[0002] The American cockroach (Periplaneta americana), commonly known as the cockroach, belongs to the Blattidae family. It has a long history of medicinal use in China, and is listed as a medium-grade herb in the Shennong Bencao Jing (Shen Nong's Herbal Classic). It is described as "salty and cold in flavor, native to rivers and lakes, and used to treat blood stasis, cold and heat, resolve accumulations, throat and pharyngeal paralysis, and internal cold and infertility" (2018, Chinese Journal of Pharmaceutical Sciences). American cockroach extracts contain a large number of bioactive substances, including proteins, peptides, and alkaloids, exhibiting various biological activities, including antiviral, antitumor, and angiogenesis-promoting activities (2018, Advances in Veterinary Medicine). However, to date, the clinical application of PA is relatively limited to drops, injections, and capsules, and these formulations have certain drawbacks, which significantly restrict their clinical application.
[0003] Cyclodextrin (CD), as an excellent inclusion material, can include guest molecules of a certain size and shape and can form stable inclusion complexes with drug molecules. As a special drug carrier, the inclusion complex can encapsulate the active ingredients in the drug inside it and release the drug at the appropriate time and location through a specific release mechanism, thereby improving the bioavailability of the drug; the inclusion complex can also reduce the interaction between the drug and other substances and maintain the chemical stability of the drug. In addition, it can also reduce the accumulation of drugs in the body and reduce the damage of drugs to organs such as the liver and kidneys (2021, Chinese Modern Applied Pharmacy; 2023, Chemical Reagents).
[0004] After the American cockroach extract is prepared into an inclusion compound, it can be more conveniently mixed with other excipients to make various dosage forms of drugs, providing a reference for scientific researchers to explore new dosage forms and technologies of PA preparations to meet personalized and broader therapeutic application needs. Summary of the Invention
[0005] In view of the deficiencies in the prior art, the present invention provides an inclusion compound of American cockroach and cyclodextrin or a cyclodextrin derivative and a preparation method thereof.
[0006] The technical solutions of the present invention are as follows:
[0007] The invention discloses an inclusion compound of American cockroach and gamma-cyclodextrin, wherein the mass ratio of American cockroach to gamma-cyclodextrin is 2:1 to 2:4.
[0008] A method for preparing an inclusion compound of American cockroach and gamma-cyclodextrin comprises the following steps:
[0009] 1) Weigh an appropriate amount of American cockroach extract and add it to purified water and dissolve evenly to obtain solution A;
[0010] 2) Weigh an appropriate amount of γ-cyclodextrin and add it to purified water to dissolve it evenly to obtain solution B;
[0011] 3) Slowly dripping solution A into solution B at a mass ratio of American cockroach to γ-cyclodextrin of 2:1 to 2:4, at a certain temperature and a certain rotation speed for a certain period of time, to obtain a brown-yellow liquid C;
[0012] 4) removing the solvent from liquid C to obtain an American cockroach / γ-cyclodextrin inclusion complex.
[0013] Furthermore, in step 1), the mass concentration of solution A is 12-15% of an American cockroach aqueous solution.
[0014] Furthermore, in step 2), the mass concentration of solution B is 15-18% of γ-cyclodextrin aqueous solution.
[0015] Furthermore, the inclusion temperature during the inclusion process in step 3) is 30-60°C.
[0016] Furthermore, the inclusion time in the inclusion process of step 3) is 0.5-3h.
[0017] Furthermore, the rotation speed during the inclusion process in step 3) is 600-1700 r / min.
[0018] Furthermore, the method for removing the solvent in step 4) is freeze-drying.
[0019] The invention discloses an application of the inclusion compound of the American cockroach and gamma-cyclodextrin in the preparation of a preparation containing the American cockroach.
[0020] The beneficial effects of the present invention are as follows: the American cockroach cyclodextrin inclusion compound provided by the present invention is safe and efficient, and the preparation method is simple and quick.
[0021] The invention can convert the American cockroach extract into a powder form, which is convenient for storage, transportation and use.
[0022] The invention can protect the active ingredients in the American cockroach extract from the influence of the external environment (such as light, heat, humidity, etc.). The invention can be more conveniently mixed with other excipients to prepare medicines of various dosage forms, facilitating the development of new American cockroach preparations. BRIEF DESCRIPTION OF THE DRAWINGS
[0023] Figure 1 This is to investigate the effects of different cyclodextrins on the comprehensive score in Example 1 of the present invention. DETAILED DESCRIPTION
[0024] The following examples may enable those skilled in the art to more fully understand the present invention, but the present invention is not limited to the scope of the examples.
[0025] Example 1
[0026] This embodiment provides an inclusion compound of American cockroach and cyclodextrin and a preparation method thereof:
[0027] (1) Weigh 1.5 g of American cockroach extract and dissolve it in 10 mL of purified water until fully dissolved to prepare an American cockroach aqueous solution with a mass concentration of 15%;
[0028] (2) Weigh 1.5 g each of β-cyclodextrin, HP-β-cyclodextrin, γ-cyclodextrin, and HP-γ-cyclodextrin and dissolve them in 10 mL of purified water until fully dissolved to prepare a cyclodextrin aqueous solution with a mass concentration of 15%;
[0029] (3) Mix the two solutions in a ratio of 2:2 of American cockroach and cyclodextrin, and stir at 30°C and 600 r / min for 1 h to obtain a brown-yellow reaction solution;
[0030] (4) The reaction solution was freeze-dried and ground to obtain a brown-yellow powder of the American cockroach / γ-cyclodextrin inclusion complex.
[0031] Figure 1 The effects of different cyclodextrins on the comprehensive score in Example 1 of the present invention are shown in FIG. Figure 1 It can be seen that compared with the other three cyclodextrins, when γ-cyclodextrin is selected, the comprehensive score is the highest.
[0032] Example 2
[0033] This embodiment provides an inclusion compound of American cockroach and γ-cyclodextrin and a preparation method thereof:
[0034] (1) Weigh 1.2 g of American cockroach extract and dissolve it in 10 mL of purified water until fully dissolved to prepare an American cockroach aqueous solution with a mass concentration of 12%;
[0035] (2) Weigh 1.8 g of γ-cyclodextrin and dissolve it in 10 mL of purified water until fully dissolved to prepare a γ-cyclodextrin aqueous solution with a mass concentration of 18%;
[0036] (3) Mix the two solutions at a mass ratio of 2:1, 2:2, 2:3, or 2:4 of American cockroach and γ-cyclodextrin, and stir at 30°C and 600 r / min for 1 h to obtain a brown-yellow reaction solution;
[0037] (4) The reaction solution was freeze-dried and ground to obtain a brown-yellow powder of the American cockroach / γ-cyclodextrin inclusion complex.
[0038] Example 3
[0039] This embodiment provides a method for preparing an inclusion complex of American cockroach and γ-cyclodextrin:
[0040] (1) Weigh 1.5 g of American cockroach extract and dissolve it in 10 mL of purified water until fully dissolved to prepare an American cockroach aqueous solution with a mass concentration of 15%;
[0041] (2) Weigh 1.5 g of γ-cyclodextrin and dissolve it in 10 mL of purified water until fully dissolved to prepare a γ-cyclodextrin aqueous solution with a mass concentration of 15%;
[0042] (3) The two solutions were mixed in a ratio of 2:2 of American cockroach and γ-cyclodextrin, and stirred at 30°C and a speed of 600, 1000, 1400, and 1700 r / min for 1 h to obtain a brown-yellow reaction solution;
[0043] (4) The reaction solution was freeze-dried and ground to obtain a brown-yellow powder of the American cockroach / γ-cyclodextrin inclusion complex.
[0044] Example 4
[0045] This embodiment provides a method for preparing an inclusion complex of American cockroach and γ-cyclodextrin:
[0046] (1) Weigh 1.5 g of American cockroach extract and dissolve it in 10 mL of purified water until fully dissolved to prepare an American cockroach aqueous solution with a mass concentration of 15%;
[0047] (2) Weigh 1.5 g of γ-cyclodextrin and dissolve it in 10 mL of purified water until fully dissolved to prepare a γ-cyclodextrin aqueous solution with a mass concentration of 15%;
[0048] (3) The two solutions were mixed in a ratio of 2:2 between American cockroach and γ-cyclodextrin, and stirred at 30, 40, 50, and 60°C and a rotation speed of 600 r / min for 1 h to obtain a brown-yellow reaction solution;
[0049] (4) The reaction solution was freeze-dried and ground to obtain a brown-yellow powder of the American cockroach / γ-cyclodextrin inclusion complex.
[0050] Example 5
[0051] This embodiment provides a method for preparing an inclusion complex of American cockroach and γ-cyclodextrin:
[0052] (1) Weigh 1.5 g of American cockroach extract and dissolve it in 10 mL of purified water until fully dissolved to prepare an American cockroach aqueous solution with a mass concentration of 15%;
[0053] (2) Weigh 1.5 g of γ-cyclodextrin and dissolve it in 10 mL of purified water until fully dissolved to prepare a γ-cyclodextrin aqueous solution with a mass concentration of 15%;
[0054] (3) The two solutions were mixed in a ratio of 2:2 between American cockroach and γ-cyclodextrin, and stirred at 30°C and 600 r / min for 0.5, 1, 1.5, 2, and 3 h to obtain a brown-yellow reaction solution;
[0055] (4) The reaction solution was freeze-dried and ground to obtain a brown-yellow powder of the American cockroach / γ-cyclodextrin inclusion complex.
[0056] Example 6
[0057] This embodiment provides a method for preparing an American cockroach / γ-cyclodextrin inclusion complex:
[0058] (1) Weigh 1.2 g of American cockroach extract and dissolve it in 10 mL of purified water until fully dissolved to prepare an American cockroach aqueous solution with a mass concentration of 12%;
[0059] (2) Weigh 1.8 g of γ-cyclodextrin and dissolve it in 10 mL of purified water until fully dissolved to prepare a γ-cyclodextrin aqueous solution with a mass concentration of 18%;
[0060] (3) The two solutions were mixed in a ratio of 2:3 between American cockroach and γ-cyclodextrin, and stirred for 2 h at a reaction temperature of 50°C and a rotation speed of 1400 r / min to obtain a brown-yellow reaction solution;
[0061] (4) The reaction solution was freeze-dried and ground to obtain a brown-yellow powder of the American cockroach / γ-cyclodextrin inclusion complex.
[0062] The effects of stirring speed, reaction temperature and stirring time on the American cockroach / γ-cyclodextrin inclusion complex were studied. The specific experimental groups and results are shown in Table 1.
[0063] Inclusion rate calculation formula = amount of American cockroaches in the inclusion complex / amount of American cockroaches added when preparing the inclusion complex × 100%
[0064] Inclusion rate calculation formula = actual mass of inclusion complex / (amount of γ-cyclodextrin input + amount of American cockroach input) × 100%
[0065] The comprehensive score calculation formula = inclusion rate × 0.5 + inclusion compound yield × 0.5.
[0066] Table 1
[0067]
[0068]
[0069] The results in Table 1 show that the inclusion yield, inclusion rate and actual comprehensive score were the highest when the reaction was carried out at a rotation speed of 1700 r / min, a reaction temperature of 51°C and a stirring time of 1.5 h, indicating that this condition is the optimal condition for preparing the American cockroach / γ-cyclodextrin inclusion complex.
Claims
1. An inclusion compound of American cockroach and γ-cyclodextrin, wherein the mass ratio of American cockroach to γ-cyclodextrin is 2:1 to 2:
4.
2. A method for preparing an inclusion compound of American cockroach and γ-cyclodextrin, comprising the following steps: 1) Weigh an appropriate amount of American cockroach extract and add it to purified water and dissolve evenly to obtain solution A; 2) Weigh an appropriate amount of γ-cyclodextrin and add it to purified water to dissolve it evenly to obtain solution B; 3) Slowly dripping solution A into solution B at a mass ratio of American cockroach to γ-cyclodextrin of 2:1 to 2:4, at a certain temperature and a certain rotation speed for a certain period of time, to obtain a brown-yellow liquid C; 4) removing the solvent from liquid C to obtain an American cockroach / γ-cyclodextrin inclusion complex.
3. The preparation method according to claim 2, characterized in that In the step 1), the mass concentration of solution A is 12-15% of an American cockroach aqueous solution.
4. The preparation method according to claim 2, characterized in that In the step 2), the mass concentration of solution B is 15-18% of γ-cyclodextrin aqueous solution.
5. The preparation method according to claim 2, characterized in that The inclusion temperature during the step 3) is 30-60°C.
6. The preparation method according to claim 2, characterized in that The inclusion time in the step 3) is 0.5-3 hours.
7. The preparation method according to claim 2, characterized in that The rotation speed during the inclusion process of step 3) is 600-1700 r / min.
8. The preparation method according to claim 2, characterized in that The method for removing the solvent in step 4) is freeze drying.
9. Use of the inclusion compound of Periplaneta americana and γ-cyclodextrin according to claim 1 in the preparation of a preparation containing Periplaneta americana.