阅读说明：本技术 氧化环糊精在制备崩解剂中的应用 (Application of oxidized cyclodextrin in preparation of disintegrating agent ) 是由 魏星跃 王星敏 于 2019-12-06 设计创作，主要内容包括：本发明涉及氧化环糊精在制备崩解剂中的应用,属于医药技术领域,通过控制环糊精氧化的程度,可以控制以该氧化环糊精作为崩解剂药物的崩解时间。通过试验发现,崩解时间随着环糊精氧化程度的增加而减少,当减少到一定程度后不再减少而趋于稳定,因此,也可以根据目标药物所需的崩解时间来选择可以满足该要求的氧化环糊精作为崩解剂,从而缩短寻找合适崩解剂的时间。(The invention relates to an application of oxidized cyclodextrin in preparing a disintegrant, belonging to the technical field of medicines, and the disintegration time of a medicament taking the oxidized cyclodextrin as the disintegrant can be controlled by controlling the oxidation degree of the cyclodextrin. Tests show that the disintegration time is reduced along with the increase of the oxidation degree of the cyclodextrin, and the cyclodextrin is not reduced to a certain degree and tends to be stable, so that the oxidized cyclodextrin meeting the requirement can be selected as a disintegrant according to the disintegration time required by a target drug, and the time for searching a proper disintegrant is shortened.)

1. Use of oxidized cyclodextrin in the preparation of a disintegrant.

2. The use of claim 1, wherein the oxidized cyclodextrin is prepared by a process comprising:

dissolving cyclodextrin in water, adding hydrogen peroxide, carrying out oscillation reaction at room temperature until the hydrogen peroxide is completely consumed, taking out reaction liquid, carrying out suction filtration and washing to obtain a solid phase, and drying the solid phase to obtain oxidized cyclodextrin.

3. The use of claim 2, wherein the amount of hydrogen peroxide is positively correlated to the number of hydroxyl groups on the glucose unit in the cyclodextrin.

4. The use of claim 2, wherein the cyclodextrin is but not limited to one of β -cyclodextrin, α -cyclodextrin, γ -cyclodextrin, acetylated β -cyclodextrin, acetylated α -cyclodextrin, or acetylated γ -cyclodextrin.

5. The use of claim 4, wherein the mass-to-volume ratio of β -cyclodextrin to hydrogen peroxide is 5:0.2-3.4, and the unit of the mass-to-volume ratio is g: mL.

6. The use according to any one of claims 2 to 5, wherein the shaking reaction is carried out in a shaker at a rotation speed of 300 and 350r/min and a shaking amplitude of 20 to 30 mm.

7. The use as claimed in any of claims 2 to 5, wherein the suction filtration washing is carried out 3 to 5 times with ice water as the washing liquid.

8. The use according to any one of claims 2 to 5, wherein the drying is in particular an oven drying at 105 ℃ and 110 ℃ for 3 to 4 hours.

Technical Field

The invention belongs to the technical field of medicines, and particularly relates to application of oxidized cyclodextrin in preparation of a disintegrating agent.

Background

In recent years, with the development of new technologies in the medical field, especially in the aspect of polymer industry, the appearance of a large number of new drugs will promote the development and application of pharmaceutic adjuvants, including a key adjuvant, namely a high-efficiency disintegrating agent. The disintegrating agent is an important auxiliary material in the process of producing tablets, is used for overcoming pressure and physical force required by a binding agent, and accelerating the disintegration of the tablets in gastrointestinal fluid into fine particles, so that the tablets meet the requirement of disintegration within a specified time, and the dissolution speed and the bioavailability of the medicine are improved.

β -cyclodextrin (β -CD) has truncated cone shape, each glucose unit in the molecule adopts an untwisted chair type conformation as a glucopyranose unit, the 4C1 conformation structure β -cyclodextrin molecule has all primary hydroxyl groups located on one side of the ring, namely, 6-hydroxyl group of the glucose unit forms a main face (narrower end) of the truncated cone-shaped structure of cyclodextrin, and all secondary hydroxyl groups located on the other side of the ring, namely, 2-hydroxyl group and 3-hydroxyl group form a secondary face (broader face) of the truncated cone-shaped structure of cyclodextrin, the inner wall of cyclodextrin is composed of hydrogen atoms pointing to cavities C3 and C5 and glycosidic bond oxygen atoms, so that the inner part of the cavity has higher electron cloud density and shows certain hydrophobicity, the secondary hydroxyl group of cyclodextrin makes the large end and the outer wall of the cavity hydrophilic, in addition, because 6-methylene exists, the main face also shows certain hydrophobicity, therefore, the cyclodextrin molecule has a circular truncated cone-shaped molecular structure of 'external hydrophilic and internal hydrophobic', the β -cyclodextrin molecule has a plurality of shielding performance, and can form a plurality of organic and inorganic complexes, even can be used for a plurality of active food molecules, and can be used for mutual control, even for a plurality of organic and a plurality of active food.

Currently, sodium methyl starch, low-substituted propyl cellulose, crospovidone, microcrystalline cellulose, croscarmellose sodium, pregelatinized starch, and the like are used for preparing disintegrants, and related studies on cyclodextrin-based disintegrants are less.

Disclosure of Invention

In view of the above, an object of the present invention is to provide an application of oxidized cyclodextrin in the preparation of a disintegrant.

In order to achieve the purpose, the invention provides the following technical scheme:

1. use of oxidized cyclodextrin in the preparation of a disintegrant.

Preferably, the oxidized cyclodextrin is prepared as follows:

dissolving cyclodextrin in water, adding hydrogen peroxide, carrying out oscillation reaction at room temperature until the hydrogen peroxide is completely consumed, taking out reaction liquid, carrying out suction filtration and washing to obtain a solid phase, and drying the solid phase to obtain oxidized cyclodextrin.

Preferably, the dosage of the hydrogen peroxide is positively correlated with the number of hydroxyl groups on a glucose unit in the cyclodextrin.

Preferably, the cyclodextrin is, but not limited to, one of β -cyclodextrin, α -cyclodextrin, γ -cyclodextrin, acetylated β -cyclodextrin, acetylated α -cyclodextrin, or acetylated γ -cyclodextrin.

Preferably, the mass-to-volume ratio of the β -cyclodextrin to the hydrogen peroxide is 5:0.2-3.4, and the unit of the mass-to-volume ratio is g: mL.

Preferably, the oscillation reaction is carried out in a shaking table with the rotation speed of 300-350r/min and the shaking amplitude of 20-30 mm.

Preferably, the washing with suction filtration is carried out 3-5 times by using ice water as a washing liquid.

Preferably, the drying is specifically drying at 105-110 ℃ for 3-4 h.

The invention has the beneficial effects that: the invention provides an application of oxidized cyclodextrin in preparing a disintegrant, and the disintegration time of a medicament taking the oxidized cyclodextrin as the disintegrant can be controlled by controlling the oxidation degree of the cyclodextrin. Tests show that the disintegration time is reduced along with the increase of the oxidation degree of the cyclodextrin, and the cyclodextrin is not reduced to a certain degree and tends to be stable, so that the oxidized cyclodextrin meeting the requirement can be selected as a disintegrant according to the disintegration time required by a target drug, and the time for searching a proper disintegrant is shortened.

Additional advantages, objects, and features of the invention will be set forth in part in the description which follows and in part will become apparent to those having ordinary skill in the art upon examination of the following or may be learned from practice of the invention. The objectives and other advantages of the invention may be realized and attained by the means of the instrumentalities and combinations particularly pointed out hereinafter.

Detailed Description

The embodiments of the present invention are described below with reference to specific embodiments, and other advantages and effects of the present invention will be easily understood by those skilled in the art from the disclosure of the present specification. The invention is capable of other and different embodiments and of being practiced or of being carried out in various ways, and its several details are capable of modification in various respects, all without departing from the spirit and scope of the present invention.