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Medicament and coating composition

A drug coating and composition technology, which is applied in the field of drug coating compositions whose peculiar smell is not easy to be noticed by users, can solve the problems of increasing production costs and process complexity, long residence time of coating compositions, and affecting mechanical properties of coatings, etc. problems, to achieve the effect of simplifying the coating prescription and preparation process, promoting drug dissolution, improving mechanical properties and other properties

Inactive Publication Date: 2010-12-29
钟术光
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Moreover, some alkaline modifiers mentioned in U.S. Patent US6663893B2 (or referring to EP1276470B1) and US6551617B1 also have unpleasant odors, such as L-arginine (slightly bitter taste), L-histidine (bitter taste), oleic acid Ammonium (with lard-like odor, more rancid odor after oxidation; ammonia odor), triethanolamine (slight ammonia odor), meglumine (with salty and astringent odor), trimethylamine (with ammonia odor and fish odor) wake up smell)
[0019] What needs to be pointed out is that the above-mentioned anti-"enteric coating" technology using two different polymers often has more micropores in the coating film than the same polymer, especially the compatibility of the two polymers. On bad days, the drug tends to dissolve out of the micropores, resulting in a subsequent unpleasant odor, especially if the coating composition stays in the oral cavity for a long time
[0020] If the conventional masking agent is further added to the above-mentioned coating composition, the result will not only increase the production cost and process complexity, but more importantly, will affect the mechanical properties of the coating to a greater extent, and will seriously mask the taste of the coating. The effect, because adding a large amount of other substances, especially water-soluble polar substances that are incompatible with the coating polymer, will greatly reduce the content of the polymer in the coating, and lead to a large increase in the mechanical properties of the coating. decline

Method used

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  • Medicament and coating composition
  • Medicament and coating composition
  • Medicament and coating composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0256] A coating (A) made of 60% cellulose acetate, 28% cellulose acetate diethylaminoacetate and 12% thaumatin coats the drug granules, which are Acetaminophen (APAP) Granules. Then the coated drug granules and other ingredients are mixed to form a dry suspension or compressed into tablets for pharmaceutical use. Replace 12% of Thaumatin in the paint (A) with 12% of Triethanolamine, and keep the other things unchanged, and prepare Reference Substance 1 in the same way.

Embodiment 2

[0258] Coating (B) made of 58% Eudragit NE30D, 27% Eudragit E 100, and 15% dicalcium triglycyrrhizinate coated drug particles, which were acetaminophen (APAP) particles. Then the coated drug granules and other ingredients are mixed to form a dry suspension or compressed into tablets for pharmaceutical use. Replace 15% dicalcium triglycyrrhizinate in the coating (B) with 15% triethanolamine, and prepare the reference substance 2 in the same way.

Embodiment 3

[0260] It consists of 54% ethyl cellulose, 26% Eudragit E 100, 10% calcium inosinate (38-74 μm, or 200-400 mesh) and 10% calcium guanylate (38-74 μm, or 200-400 mesh ) coating (C) made to coat the drug granules, the drug granules are sildenafil citrate granules made by dry granulation (particle content: sildenafil citrate 33.3% , microcrystalline cellulose 33%, low-substituted hydroxypropyl cellulose 14.5%, sorbitol 17.2%, silicon dioxide 0.5%, sodium stearyl fumarate 1.5%). Then the coated drug granules and other ingredients are mixed to form a dry suspension or compressed into tablets for pharmaceutical use. Replace the calcium inosinate and calcium guanylate in the paint (C) with 20% talc, and keep the other things unchanged, prepare the reference substance 3 in the same way.

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Abstract

The invention discloses a medicament and coating composition capable of preventing unpleasant peculiar smell from being perceived by users in an administration process. The composition comprises a core of medicaments with unpleasant peculiar smell, a polymer which covers outside the core and is almost water-insoluble at any pH value, a polymer which is soluble in an acidic medium and is almost insoluble in a neutral or an alkaline pH medium, and a coating which can cover or inhibit the unpleasant peculiar smell and is soluble in the alkaline compound of diluted hydrochloric acid; preferably, the two polymers is compatible or completely compatible; and more preferably, the alkaline compound is almost insoluble. Besides the original advantages, the coating composition also has the advantages of covering or inhibiting the subsequent and / or residual unpleasant peculiar smell of the medicaments and / or unpleasant peculiar smell possibly generated from an additive in the coating, improving medicament release performance, simplifying a formula and a preparation method, reducing production cost, and the like.

Description

technical field [0001] The invention relates to a drug coating composition. More specifically, the present invention relates to a drug coating composition with improved overall performance and odor that is not easily noticed by users. technical background [0002] Many active ingredients, such as antibiotics, have a strong unpleasant taste, such as bitter, spicy, astringent, etc. in the sense of taste, and foul in the sense of smell. This unpleasant odor often has multiple adverse effects. For example, the unpleasant taste of the drug can make it difficult to swallow, or cause the patient to avoid the drug treatment, thereby leading to low patient compliance. Taste of the active ingredient is usually not an issue when the medicament is formulated as a tablet or capsule to be swallowed whole, as the capsule prevents the active ingredient from coming into contact with the mouth, and the tablet can be coated to prevent the short time the tablet is in the mouth The active ing...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/38A61K47/32A61K47/42A61K47/26A61K47/24A61K47/36A61K47/30A61K9/00A61K9/06A61K9/10A61K9/14A61K9/20A61K9/48A61K9/68
Inventor 钟术光
Owner 钟术光
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