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Application of saturated fatty polyol or alcoholic acid as cross-linking agent in filming gel composition

An aliphatic polyol and gel composition technology, which is applied in the directions of inactive medical preparations, drug combinations, organic inactive ingredients, etc., can solve the problems of short residence time, easy membrane rupture and shedding, etc. The effect of good capacitance, easy availability of raw materials and good flexibility

Active Publication Date: 2009-02-04
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, we have found that the local film-forming gel composition made of monoglyceryl laurate as a cross-linking agent, although the flexibility of the film is enhanced, the time of adhesion to body tissues or mucous membranes is relatively short, as in The film formed on the oral mucosa is easily eroded / dissolved by body fluids or saliva, causing the film to rupture prematurely, fall off, and even disappear, and its effective residence time on the oral mucosa is only 3 to 4 hours
The reason for the shorter residence time of the film may be related to the following reasons: (1) there are only two hydroxyl groups that can provide crosslinking on the monolaurin monoglyceride, and there are fewer crosslinkable sites; (2) monoglyceryl laurate The longer carbon chain structure (12-carbon alkyl chain) in the oil molecule may shield part of the crosslinking sites, and the longer carbon chain of lauric acid is not conducive to the tight arrangement inside the gel composition
These above factors weaken the cohesive force inside the gel composition, thereby causing the film to be more easily broken, dissolved and / or eroded, so that it disappears faster

Method used

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  • Application of saturated fatty polyol or alcoholic acid as cross-linking agent in filming gel composition
  • Application of saturated fatty polyol or alcoholic acid as cross-linking agent in filming gel composition
  • Application of saturated fatty polyol or alcoholic acid as cross-linking agent in filming gel composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～10

[0031] Embodiment 1~10 and comparative embodiment

[0032] Table 1

[0033]

[0034] Stir and dissolve the esterification agents in Examples 1-10 and Comparative Examples in Table 1 respectively in the solvent of the prescription amount, slowly add hydroxypropyl cellulose under stirring, after completely dissolving / swelling, continue stirring to form Uniform gel; Then add cross-linking agent (comparative example does not add cross-linking agent), continue to stir and make completely uniform; Replenish the solvent that can evaporate, make reach recipe quantity, stir well, degassing, obtain homogeneous is 100 grams of each film-forming gel composition of the present invention.

Embodiment 11～15

[0036] Table 2

[0037]

[0038] With benzocaine (Benzocaine), triamcinolone acetonide (Triamcinolone Acetonide), nitrate (Econazole Nitrate), amlexanox (Amlexanox) and chlorhexidine acetate (Chlorhexidine Acetate) as model drugs, the 100 grams of drug film-forming gel compositions were prepared respectively according to the preparation method in Example 1, wherein the drug was added to the solvent together with the esterifying agent.

[0039] The pharmaceutical film-forming gel compositions prepared in Table 2 can form a smooth, tough, wear-resistant, and durable hydrophobic film on the skin or mucous membrane.

[0040] The various component raw materials in the foregoing examples are conventional commercially available products.

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Abstract

The present invention discloses the application of saturated fatty polyol and / or alcoholic acid as cross-linking agent in filming gel composition. The saturated fatty polyol and alcoholic acid have the chemical general expression of CnH2n+2-m-l(OH)m(COOH)l, where n, m and l are integral number. The filming gel composition may be coated onto skin or oral mucosa to form one smooth, tough, antiwear and hydrophobic protecting film, and the film may be retained for over 5 hr in oral mucosa or 8 hr in skin.

Description

technical field [0001] The invention relates to the use of a saturated fatty polyol or alkyd or a mixture thereof as a crosslinking agent in a film-forming gel composition. Background technique [0002] Human skin, oral mucosa damage caused by cuts, abrasions, incisions and burns; inflammation caused by bacterial, fungal or viral infection; ulcers caused by various reasons and pain in local tissues caused by various reasons, etc. Common diseases in people's daily life. The topical pharmaceutical preparations clinically used to treat skin and oral mucosal diseases are usually creams, ointments, gels, tinctures, pastes, gargle sprays, etc., when these preparations are applied on human tissues or oral mucosa During local treatment, due to the normal activities of the affected area and its surrounding tissues, such as friction, sweat, saliva secretion and flushing, these agents will be dissolved and / or eroded, displaced, and shed, and the agent will remain with the affected are...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/08A61K47/36A61K9/70A61P17/02C08K5/04
Inventor 马晋隆陈志明倪旻
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT