Suppository composition

Abstract

The invention discloses a suppository composition with improved performance. The suppository composition comprises an aliphatic suppository substrate, mono-capryl-based glycerin, mono-lauroyl-based glycerin, polyoxyethylene, a suppository substrate of which the molecular structure contains polyethylene glycol and alkyl having 8 to 24 carbon atoms and a suppository medicament. The suppository composition has the advantages of improving production repeatability and retention value otherness, enhancing the function of a cavity administration retention substrate, improving stability, namely, changing melting performance, decreasing medicament releasing rate and solving or relieving problems such as scumming and the like, improving medicament releasing performance, increasing liquefaction or gelling speed and achieving stronger salt resistance and acid resistance and higher biocompatibility and the like.

Description

technical field [0001] The present invention relates to a suppository composition with improved properties. More specifically, the present invention relates to an improved suppository composition comprising an aliphatic suppository base, monocaproylglycerol, monolauroylglycerol, polyethylene oxide and molecularly structured Contains polyoxyethylene (-(CH 2 CH 2 O) n -) and a suppository base of C8-C24 alkyl and a suppository drug. technical background [0002] U.S. Patent No. 6,210,698 B1 discloses a suppository composition comprising (A) an aliphatic suppository base, (B) monocapryl glycerol, (C) monolauroyl glycerol, (D) an aliphatic insoluble Powder of the matrix and (E) a suppository drug, and (F) an "intraluminal retention matrix". The suppository maintains a melting point above body temperature in dry storage conditions and remains stable against melting during storage, when it is inserted into a body cavity, it melts or gels quickly. The "intraluminal drug reten...

AI Technical Summary

Problems solved by technology

[0004] Such as: (1), the matrix component " intracavity administration retaining matrix " in this technical suppository and the powder insoluble in aliphatic matrix have bad compatibility with aliphatic matrix, and the viscosity of molten aliphatic matrix is ​​very big, both It is not easy to mix evenly, and precipitation may occur during production and storage at higher temperatures (such as matrix melting), and some local contents are relatively high and some are relatively low. In addition, the particle size and other characteristics of the powder vary widely. These factors tend to lead to poor reproducibility of suppository composition production and differences in "lumen retention" effect, etc.

[0005] (2), the generally selected "intraluminal drug retention matrix", such as acrylic acid polymer, starch acrylate, etc., is prone to "salt poisoning" effect and "gel blocking" effect, making it "intraluminal drug retention" isotropic decline

In addition, the generally selected ionic "intraluminal drug retention matrix", such as acrylic acid polymer, starch acrylate, etc., its performance is also affected by the pH value, such as in an acidic environment such as the vagina, its performance is greatly reduced, making it Effects such as "intraluminal drug retention" have also been greatly reduced

[0006] (3) More importantly, this technology selects organic polymers with strong swelling ability in contact with water and strong mucous membrane adhesion ability, such as acrylic acid polymers (such as sodium polyacrylate), starch acrylate, etc. The high-strength water absorption capacity can make the mucous membrane in contact with the drug carrier or adjacent to the drug carrier lose water more quickly, causing a strong local "dryness", thereby causing a strong local irritation, and the patient feels local pain. Bioincompatibility issues such as strong discomfort (such as tingling)

[0007] (4) In addition, during the storage period, the suppository of this technology may have an increase in its melting point, a change in its melting performance, such as a change in its release rate at body temperature, which may affect its curative effect

Due to the transformation of the crystal form, the physical properties change, such as the melting point increases by 2-3°C, the softening time is prolonged, the melting time is prolonged (usually more than 30min), and the drug release rate slows down

[0008] (5) In addition, during the storage of the technical suppository, especially when the packaging is not perfect, under high humidity environment, the "intracavity administration retention matrix" with good hydrophilicity and poor lipophilicity in the suppository , powder insoluble in aliphatic matrix and drug powder and other components may be precipitated from the suppository, forming a layer of frost on the surface of the suppository, that is, the so-called "frosting" phenomenon, which affects its curative effect

Images