Classification and product development status of gastric retention drug delivery system

Oral administration is currently the most commonly used route of administration due to its convenience and safety

The gastric retention drug delivery system is a new type of drug that can stay in the gastric juice, extend the release time of the drug in the gastrointestinal tract, improve the absorption of the drug, or enhance the therapeutic effect of the drug in the stomach, reduce the adverse reaction and the number of medications, and improve the clinical efficacy.

1.

Physiological factors such as the patient's age, gender, posture, physical condition, emotional state, and eating conditions will affect the residence time of the drug in the stomach

2.

3.

3.

Floating gastric retention drug delivery system means that it enters the stomach after oral administration.

According to the different floating mechanisms, there are two types: effervescent and non-effervescent

3.

Bioadhesive gastric retention drug delivery system refers to the use of bioadhesive polymer materials (exogenous lectin and chitosan, etc.

3.

Expanded swelling gastric retention preparation means that the drug enters the stomach through the oral cavity in a volume available for oral administration, and then rapidly expands under the action of gastric acid to increase the volume sufficient to resist the elimination of the pyloric sphincter, thereby prolonging the drug in the stomach Detention time within

3.
4 Density gastric retention drug delivery system

Density-type gastric retention drug delivery preparation means that the drug is packed with excipients with different densities to make the preparation float or sink in the stomach, thereby changing the retention time of the drug in the stomach
.
The system is divided into high-density type and low-density type
.

The density of the high-density retention drug delivery system is higher than that of gastric juice.
After oral administration, it can quickly settle near the pylorus at the bottom of the stomach and be wrapped by gastric folds to avoid being affected by physiological conditions such as food flow in the gastrointestinal tract and gastrointestinal motility.
Excretion from the stomach prematurely, thereby increasing the gastric residence time of the drug
.
The density of the dosage form generally needs to reach 2.
5g·cm-3
.
Low-density gastroretentive drug delivery preparations are based on the direct addition of low-density materials (including cellulose acetate, polycarbonate, low-density methylhydroxypectin and agar, etc.
), air or oil to make the drug enter the gastrointestinal tract.
It quickly floats on the gastric juice and contents to achieve retention of drug delivery, which makes up for the shortcomings of the drug release time lag caused by the formation of gas and floating state in the floating drug delivery system
.

3.
5 Magnetically guided gastric retention drug delivery system

Magnetically guided gastric retention drug delivery formulations refer to drug delivery formulations that add magnetic materials to excipients and achieve retention through the action of magnetic probes close to the outside of the stomach
.
Although the effect of magnetically guided preparations is considerable, the high-precision positioning of in vitro magnetic probes, the toxicity of magnetic excipients and the compliance of patients all limit the application of such dosage forms
.

3.
6 Super porous aqueous gel drug delivery system

The super-porous hydrogel drug delivery system is a gastric retention drug delivery preparation prepared with hydrogel as a matrix
.
Superporous hydrogel is a three-dimensional hydrophilic gel molecular material.
There are many interconnected micro pores in its structure.
The diameter of the pores is about 100 μm.
After encountering water, it passes through the wetting and permeation effect of the capillary.
It swells to the target volume by absorbing water in a short time, floats on the gastric juice, and resists the action of gastric peristalsis to a certain extent, so that the drug can achieve the effect of retention and release
.

4.
Current status of gastric retention products

Due to the continuous development of related technologies, the types of gastric retention drug delivery systems have gradually become diverse
.
However, looking at the products and mechanisms of gastric retention preparations that have been on the market at home and abroad in recent years or are still in clinical research, it is not difficult to find that gastric floating preparations still occupy a large share in the market of gastric retention preparations
.
Super porous aqueous gel and magnetically guided gastric retention drug delivery system type preparations are rarely seen in the market
.

As a new dosage form developed in oral administration preparations, gastric retention drug delivery formulations play a gastric targeting role in promoting drug absorption, and provide many new methods for drug release in the stomach and the treatment of gastric diseases.

.
However, currently, there are relatively few dosage forms for gastric retention in the market, and there are many types of preparations of this type, and there are many evaluation methods in vivo and in vitro, and there is no uniform and feasible standard
.
In terms of research status and marketed products, the development prospects of floating and inflatable drug delivery systems are better, and more and more studies combine them with other gastric retention strategies to overcome their limitations to obtain longer , More stable gastric retention time
.
In recent years, the research on gastroretentive pharmaceutical preparations has continued to deepen, mainly manifested in the application of various new preparation technologies and new polymer materials in gastric retention drug delivery systems and the combination of various new preparation technologies.
It is believed that with various new With the application of excipients and new technologies, more gastric retention preparations will be used in clinical practice
.

references:

[1] Wu Tianyi, Hu Ning, Sun Shuping.
Research progress of gastric retention type sustained and controlled release drug delivery system[J].
Chinese Contemporary Medicine, 2020, 27(02): 15-17.

[2] Zhang Chungang, Yu Ziyao, Yu Chenchen, Cheng Lan, Kang Tingguo.
Research progress of gastric retention drug delivery system and its application in traditional Chinese medicine preparations[J].
China Modern Applied Pharmacy, 2020, 37(07): 877-885.

[3]Hu Manyu, Zhu Zhuangzhi, Wang Hao.
Research progress of gastric retention drug delivery system[J].
Chinese Journal of Pharmaceuticals, 2019,50(03):241-251.

[4]Huo Taotao, Tao Chun, Yao Fengfeng, Song Hongtao.
Research progress of gastric retention drug delivery system[J].
Chinese Journal of New Drugs, 2017, 26(04): 420-426.