Montmorillonite suspension for treating acute diarrhea, and preparation method thereof

Abstract

The invention belongs to the technical field of medicinal preparations, and especially relates to a montmorillonite suspension for treating acute diarrhea, and a preparation method thereof. Sodium carboxymethyl cellulose contains sodium cations, which can switch with some calcium cations in montmorillonite, so that partial CMC-Na can enter the interlayer or surface of the montmorillonite; when theconcentration of the CMC-Na and the exchangeable calcium cations on the surface of the montmorillonite can reach a balance state, deflocculation effects can be achieved, so that the settlement volumeratio of the formed montmorillonite suspension can be qualified and stabilized, and easy re-dispersion can be realized; and two bacteriostatic agents which are methyl hydroxybenzoate and propyl hydroxybenzoate can have antibacterial activity when pH is 4-8, can give protons with the increasing of the pH, so that anions of phenol groups can be formed, and bacteriostatic effects can decrease with the increasing of the pH. The composition formula of the montmorillonite suspension is in a balanced deflocculation state, so that the montmorillonite suspension with stable settlement volume ratio reliable in dispersing and qualified in bacteriostatic effect can be obtained.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to a montmorillonite suspension for treating acute diarrhea and a preparation method thereof. Background technique [0002] Montmorillonite is a dioctahedral layered structure composed of silicon-oxygen tetrahedrons and aluminum-oxygen octahedrons, with a general structural formula of (K, Na, Ca, Mg) y (Al, Mg) 2 (Si,Al) 4 o 10 (OH) 2 xH2O, where (K, Na, Ca, Mg) y For interlayer exchangeable cations, (Al, Mg) 2 is the cation in the octahedron, (Si, Al) 4 It is a cation in the tetrahedron. The random substitution of A1 and Mg for Si and Al in the structure causes an imbalance of charge, making it have the characteristics of charging and ion exchange. It is called "the king of mycotoxin adsorption". The mechanism is to rely on its uniform distribution to cover the digestive tract mucosa, which can combine with mucus glycoproteins, increase mucus volume, impr...

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Problems solved by technology

[0003] Montmorillonite powder, as a solid dosage form, has the advantages of being easy to carry and store, but its clinical application has many requirements. If the medication is not standardized, the curative effect will be poor, and there are the following problems: (1) when taking it, pour 1 bag into 50mL warm Stir well in boiling water and take it. First, the temperature should not be controlled. When cold water is added, the montmorillonite powder is difficult to infiltrate, resulting in uneven dispersion; hot water, especially children, resists it, and when the temperature drops, the montmorillonite precipitates and aggregates. Many patients report that it is difficult to swallow, just like lime powder, which is difficult to swallow; (2) If the montmorillonite powder is not completely dispersed evenly, it will lead to uneven distribution of montmorillonite on the mucous membrane of the digestive tract, especially for gastritis and colitis 1. Patients with diarrhea caused by irritable bowel syndrome. Patients with such diseases are often accompanied by mucosal erosion and bleeding. If montmorillonite is unevenly distributed in the digestive tract mucosa, it will affect the curative effect

[0006] (1) The composition does not contain a suspending agent. Although montmorillonite has the characteristics of swelling and dispersing in water, forming a negatively charged plate surface and a positively charged edge suspension, this suspension state is unstable, from montmorillonite It can be seen that the stone powder will precipitate soon after adding water and stirring well in clinical use. Only relying on the expansion of montmorillonite itself, the dispersion characteristics cannot be effectively guaranteed.

[0007] At the same time, we used a homogenizer to crush montmorillonite in multiple batches, and found that when the particle size reached D90=16μm, it was difficult to reduce the particle size of montmorillonite with existing equipment no matter how long the time was or the crushing intensity was increased.

According to the results, it is found that if the particle size of the montmorillonite suspension without suspending agent is too large, its sedimentation volume is difficult to meet the requirements, which will bring the risk of redispersibility and inhomogeneous distribution in the body; if the montmorillonite suspension is reduced The particle size removal method is the main method, but it is difficult to achieve crushing to about 10 μm with existing equipment; in addition, it is difficult to achieve the uniformity of each batch and each bottle of samples with existing equipment and processes, so only montmorillonite itself The expansion and dispersion of the suspension cannot meet the requirements for the sedimentation volume ratio of the suspension

[0008] If glycerin is used as a suspending agent, oral administration of glycerin will bring the risk of diarrhea to patients, and it will lead to excessive viscosity of the product and poor redispersibility. Due to the high viscosity, it is difficult to accurately divide the dosage and the taste is poor, so the existing suspending agent cannot be used method to improve its stability

[0009] (2) the antibacterial agent selected in the existing montmorillonite suspension is sodium benzoate, and sodium benzoate is an acid preservative, and has no bactericidal, bacteriostatic effect in alkaline medium

It is disclosed in the existing literature that under the condition of pH=7.0, the commonly used oral preservatives benzoic acid and its salts, sorbic acid and its salts hardly have antiseptic effect, and it is stated that paraben preservatives and montmorillonite The stone has incompatibility, and the joint use will be absorbed by the montmorillonite and lose the antiseptic effect

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