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Medicament coating composition with masked taste

A coating composition and drug coating technology, which is applied in drug delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve the problems of slow decrease in membrane permeability and decrease in drug bioavailability

Inactive Publication Date: 2013-06-12
钟术光
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

When the two different polymers have good compatibility, these micropores will slowly heal themselves during storage, which will gradually reduce the permeability of the coating film and reduce the bioavailability of the drug.

Method used

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  • Medicament coating composition with masked taste
  • Medicament coating composition with masked taste
  • Medicament coating composition with masked taste

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0179] Coating (A) Paracetamol (APAP) made of 40% cellulose acetate, 20% Eudragit E 100 and 40% zinc phosphate particles (38~74μm particle size, or 200~400 mesh) Granules (14-24 meshes, the acetaminophen granules are prepared by dry granulation, and the composition is as follows: acetaminophen (APAP) 50%, microcrystalline cellulose 30%, cross-linked carboxymethyl Sodium cellulose 17%, sodium lauryl sulfate 1%, silicon dioxide 0.5%, sodium stearyl fumarate 1.5%) for coating, after the coating process, the coating accounted for 23.08% of the entire coated granules % (weight ratio) (ie 30% increase in particle weight). Then, the coated drug granules and other ingredients are mixed in the following proportions: coated granules 40.63%, mannitol 49.37%, microcrystalline cellulose 7.5%, stearic acid 1%, silica colloid 0.5%, fragrance 1%. The final blend was then compressed into tablets having a final tablet weight of 960 mg, such tablets having a diameter of 10.5 mm, a hardness of a...

Embodiment 2

[0206] Consists of 24% ethyl cellulose, 26% diethylaminomethyl cellulose, 49.5% L-cystine particles (23-38 μm in particle size, or 400-600 mesh) and 0.5% triacetin The prepared coating (B) is applied to pipemidic acid granules (12 to 20 meshes in diameter), and the pipemidic acid granules are prepared by dry granulation, and the content of the components is as follows: Microcrystalline cellulose 34%, low-substituted hydroxypropyl cellulose 18%, fructose 8%, lactose 8%, silicon dioxide 0.5%, sodium stearyl fumarate 1.5%. After the coating process was completed, the coating accounted for 23.08% by weight of the entire coated granules (ie, 30% granule weight gain). Then, the coated drug particles and other ingredients are mixed in the following proportions: 63.73% of coated particles, 26.27% of mannitol, 7.5% of microcrystalline cellulose, 1% of stearic acid, 0.5% of silica colloid, and 1% of fragrance. The final blend was then compressed into tablets having a final tablet weigh...

Embodiment 3

[0217] Consists of 38.56% KOLLIDONE SR, 20.0% vinyldiethylamine-vinyl acetate copolymer, 11.44% EASTMAN 9-45 (acetated monoglycerides), 25% potassium hydrogen tartrate particles (particle size The coating (A) made of 38-74 μm, or 200-400 mesh) and 5% talc is applied to drug caffeine particles (40-80 mesh in particle diameter).

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Abstract

The invention discloses a medicament coating composition with improved comprehensive performance and masked taste hardly detected by a user. The medicament coating composition comprises: an outer coating, and a medicament core, wherein the outer coating contains a polymer which is not dissolved or hardly dissolved in water under any pH value, a polymer which is dissolved in an acidic medium but is not dissolved or hardly dissolved in a neutral or alkaline pH medium and a particulate matter which does not contain unpleasant odor, is not dissolved or hardly dissolved in water but can be dissolved in acidic medium and alkaline medium, and the medicament core is coated by the coating and contains unpleasant odor. The coating composition can stimulate the medicament to be released in the stomach and stimulate the medicament which is unreleased or incompletely released to enter the intestines to be released in the intestines so that the coating composition conveys the medicament contents tothe body system for more complete circulation and has higher medicament bioavailability.

Description

technical field [0001] The present invention relates to a pharmaceutical coating composition with peculiar smell not easily detected by users. Specifically, the present invention relates to a drug coating composition with improved comprehensive properties, which is difficult to be detected by the user, and the coating composition can not only promote the release of the drug in the stomach, but also promote the unreleased or unreleased drug in the stomach. The release in the intestine of the drug that enters the intestine without complete release allows the coated composition to deliver the drug component to the systemic circulation more completely, and the bioavailability of the drug is higher. technical background [0002] Many active ingredients, such as antibiotics, have strong unpleasant tastes such as bitter, spicy, astringent, etc. in terms of taste, and odor in terms of smell. Such unpleasant odors often have multiple adverse effects, for example, the unpleasant tast...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/38A61K47/36A61K47/32A61K47/02A61K47/12A61K47/16A61K47/20A61K47/22A61K47/26A61K9/00A61K9/06A61K9/10A61K9/14A61K9/20A61K9/48A61K9/68
Inventor 钟术光
Owner 钟术光