CN101332197B - Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane - Google Patents
Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane Download PDFInfo
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- CN101332197B CN101332197B CN 200810024460 CN200810024460A CN101332197B CN 101332197 B CN101332197 B CN 101332197B CN 200810024460 CN200810024460 CN 200810024460 CN 200810024460 A CN200810024460 A CN 200810024460A CN 101332197 B CN101332197 B CN 101332197B
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- loperamide hydrochloride
- simethicone
- loperamide
- hydrochloride
- gel
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Abstract
The present invention provides a hydrochloride loperamide dimethicone composite oral instant soluble membrane, which is used for relieving diarrhea with gastroenteric turgor symptom. The hydrochloride loperamide dimethicone composite oral instant soluble membrane contains hydrochloride loperamide and dimethicone; wherein, the weight proportion of the hydrochloride loperamide and the dimethicone is 1: 60 to 65 and the optimal weight proportion is 1:62.5. The present invention also discloses a preparation method of the hydrochloride loperamide dimethicone composite oral instant soluble membrane: water-soluble components are dissolved in water except for water-soluble polymers; at least a bio-acceptable water-soluble polymer ia added into a water solution under the stirring state; a polymer gel is obtained after full stirring and dispersing; a plasticizer is added into the polymer gel and evenly stirred; finally hydrochloride loperamide, dimethicone and other components are added to obtain the hydrochloride loperamide dimethicone polymer gel; degasifying is carried out, and the gel is evenly painted on a plate, blowing is carried out for heating and drying at the temperature of 70 to 80 DEG, and cutting is carried out, thus the instant soluble membrane is obtained.
Description
Technical field
A kind of Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane of the present invention relates to a kind of loperamide hydrochloride and dimethicone compound oral instant film preparation and preparation method thereof of containing, and is used to alleviate diarrhoea and with the symptom of gastrointestinal tract flatulence.
Background technology
Loperamide hydrochloride (Loperamide Hydrochloride) is a kind of diarrhea, acts on the opiate receptor of intestinal wall, stops the release of acetylcholine and prostaglandin, thereby suppresses enterokinesia, prolongs the holdup time of intestinal contents.Can increase the tension force of anal sphincter, therefore can suppress fecal incontinence and just anxious, be used for the acute and chronic diarrhea that the various causes of disease cause.Be used for ileum fistulation patient and can reduce defecation volume and number of times, increase the thick hardness of stool.
Simethicone (Dimethicone) can change bubble surface tension force because surface tension is little, and it is broken, and therefore can eliminate the foam in the gastrointestinal tract, and the gas that is stored by foam is got rid of, thereby alleviates flatulence.Be not absorbed after entering human body, original shape is discharged.Be used for gastrointestinal tract flatulence.
Now, the oral formulations listing of existing a plurality of loperamide hydrochlorides and simethicone both at home and abroad, but because traditional oral formulations must first disintegrate under one's belt could begin to discharge medicine, onset is slow, take also inconvenient, but though oral liquid quick acting, but need soupspoon or glass when taking, take inconvenience especially under the situations such as driving, also be unfavorable for quantitatively taking, carry also inconvenient simultaneously, and preparation oral cavity disintegration tablet and oral instant-dissolving tablet preparation technology are complicated, need special installation, adopt the wet granule compression tablet prepared to exist disintegrate slow, the lyophilization prepared exists outward appearance undesirable, the shortcoming of the frangible and easy moisture absorption has influenced the application of loperamide hydrochloride and simethicone oral formulations greatly.And, for diarrhoea and with the symptom of gastrointestinal tract flatulence, no matter use the loperamide hydrochloride or the oral formulations of simethicone separately, symptoms of two aspects of reduction of patient diarrhoea and gastrointestinal tract flatulence simultaneously well all, existing known technology does not improve the suggestion of above defective yet.
Summary of the invention
The objective of the invention is provides a kind of Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane and preparation method thereof at above weak point, Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane is the oral compound preparation of a kind of loperamide hydrochloride and simethicone, this oral instant membrane is easy to carry, can under anhydrous situation, take, mouthfeel is joyful, good stability, and onset is rapid, and supplementary product consumption is little, technical process is simple, thereby resulting cost is lower, and simultaneously well the symptom of two aspects of reduction of patient diarrhoea and gastrointestinal tract flatulence has considerable economic and social benefit.
Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane is to take following scheme to realize:
A kind of Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane contains loperamide hydrochloride and simethicone, and wherein loperamide hydrochloride and simethicone weight proportion are 1: 60～65.
A kind of Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane, the chemical name of described loperamide hydrochloride is: 4-(rubigan)-4-hydroxy-n, N-dimethyl-α, α-diphenyl-1-piperidines butanamide hydrochloride, structural formula is:
Molecular formula is: C
29H
33ClN
2O
2.HCl, molecular weight is: 513.50.
A kind of Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane, described simethicone chemical name is: polydimethylsiloxane, structural formula is:
Molecular formula is: C
3H
9OSi. (C
2H
6OSi)
n.C
3H
9Si
A kind of Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane, described loperamide hydrochloride and simethicone weight proportion are 1: 62.5.
A kind of Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane contains biological acceptable water-soluble polymer as filmogen.
A kind of Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane, described water-soluble polymer are selected from a kind of or mixture in hydroxypropyl emthylcellulose, hydroxypropyl cellulose, maltodextrin, amylopectin, hydroxyethyl-cellulose, polyvinyl alcohol, pectin, chondrus ocellatus Holmes polysaccharide, sodium alginate, potassium alginate, carboxymethyl cellulose, polyvidone, elsinan, Pullulan, xanthan gum, agar, gelatin, chitosan, the chitin.
A kind of Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane, described water-soluble polymer is selected from a kind of or mixture in hydroxypropyl emthylcellulose, hydroxypropyl cellulose, the maltodextrin, the preferably mixture of hydroxypropyl emthylcellulose and maltodextrin.
A kind of Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane, described hydroxypropyl emthylcellulose be the hydroxypropyl emthylcellulose of viscosity 3～60 centipoises, the hydroxypropyl emthylcellulose of 3～15 centipoises preferably.
A kind of Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane, described hydroxypropyl emthylcellulose and maltodextrin weight proportion are 1: 0.1～2, preferably 1: 0.3～0.7.
A kind of Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane can also comprise the acceptable component of other biological:
Account for 0.1～30% at least a flavoring agent of described film weight;
Account for 0.01～5% at least a coloring agent of described film weight;
Account for 0.1～5% at least a plasticizer of described film weight;
Account for 0.1～5% at least a antiseptic of described film weight;
Account for 0.1～10% at least a saliva stimulant of described film weight;
Account for 0.1～20% at least a disintegrating agent of described film weight;
Account for 0.1～20% water of described film weight.
Described flavoring agent is selected from a kind of or mixture in aspartame, sucralose, stevioside, glycyrrhizin, saccharin sodium, glucide, mannitol, xylitol, sorbitol, fructose, sucrose, maltose, essence, spice, the sodium glutamate.
Described coloring agent is selected from FD﹠amp; A kind of or mixture in C dyestuff, color lake, the pigment.
Described plasticizer is selected from a kind of or mixture in Polyethylene Glycol, glycerol, mono glycerinate, diglyceride, the polyethylene glycol oxide sorbitol ester.
Described antiseptic is selected from a kind of or mixture in methyl hydroxybenzoate, ethyl hydroxybenzoate, sodium benzoate, the potassium sorbate.
Described saliva stimulant is selected from a kind of or mixture in citric acid, tartaric acid, lactic acid, the fumaric acid.
Described disintegrating agent is selected from a kind of or mixture in polyvinylpolypyrrolidone, low-substituted hydroxypropyl cellulose, carboxymethyl starch sodium, cross-linking sodium carboxymethyl cellulose, the pregelatinized Starch.
The water that contains film weight 0.1～20% can guarantee that Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane has the intensity and the toughness of suitable cutting packing.
A kind of preparation method of Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane:
Water soluble ingredient that will be except that water-soluble polymer is soluble in water, obtains aqueous solution;
The acceptable water-soluble polymer of at least a biology is joined in the aqueous solution under stirring, and fully dispersed with stirring obtains polymer gel;
In above-mentioned polymer gel, add plasticizer and stir;
Add loperamide hydrochloride, simethicone and other components and stir and obtain loperamide hydrochloride simethicone polymer gel;
The degassing is evenly coated loperamide hydrochloride simethicone polymer gel on the flat board;
Air blast heat drying, heat drying temperature are 70～80 ℃, and cutting obtains described Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane.
A kind of Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane contains loperamide hydrochloride and simethicone, and wherein loperamide hydrochloride and simethicone weight proportion are 1: 60～65.Also contain biological acceptable water-soluble polymer as filmogen, water-soluble polymer is preferably the mixture of hydroxypropyl emthylcellulose and maltodextrin, hydroxypropyl emthylcellulose and maltodextrin weight proportion are 1: 0.1～2, preferably 1: 0.3～0.7.The instant film of this compound oral has solved loperamide hydrochloride and the onset of simethicone common oral preparation is slow, take inconvenience, oral liquid carries inconvenience, unfavorablely quantitatively take, oral cavity disintegration tablet and oral instant-dissolving tablet preparation technology are complicated, need special installation, adopt the wet granule compression tablet prepared to exist disintegrate slow, the lyophilization prepared exists outward appearance undesirable, the shortcoming of the frangible and easy moisture absorption, easy to carry, can take under anhydrous situation, mouthfeel is joyful, and the compliance of taking medicine is good, the patient of suitable especially child old man and dysphagia takes medicine, steady quality, onset is rapid, and supplementary product consumption is little in the production, technical process is simple, resulting cost is lower, and simultaneously well the symptom of two aspects of reduction of patient diarrhoea and gastrointestinal tract flatulence has considerable economic and social benefit.
The specific embodiment
Further specify the present invention below by embodiment.Should correct understanding be: embodiments of the invention are only used for the present invention is described and provide, rather than limitation of the present invention, so, under method prerequisite of the present invention, simple modifications of the present invention is all belonged to the scope of protection of present invention.
Embodiment 1:
Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane dissolves the time limit algoscopy:
Appoint 10 of the films of getting it filled, get 1 at every turn, be about the one side that the clip of 2cm is clamped the medicine film, connect in the water-bath that clip immerses 37 ℃ together, use manual time-keeping with a folder mouth, the medicine film from immersion water to dissolving and the time of dialysis clip is and dissolves the time limit.
Embodiment 2:
Loperamide hydrochloride 1g
Simethicone 62.5g
Amylopectin 50g
Maltodextrin 10g
Stevioside 2g
Polyethylene Glycol-200 1g
Purified water 100g
Earlier that the maltodextrin and the stevioside of above-mentioned amount is soluble in water, obtain aqueous solution, amylopectin with above-mentioned amount joins in the maltodextrin aqueous solution under stirring again, fully dispersed with stirring obtains the amylopectin gel, add Polyethylene Glycol-200 again and stir, add loperamide hydrochloride and simethicone at last and stir and obtain loperamide hydrochloride simethicone gel, the degassing, uniformly with loperamide hydrochloride simethicone gel coating on flat board, 75～80 ℃ of air blast heat dryings, cutting obtains described Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane.This film is white in color, and is pliable and tough, and inlet dissolves dispersion rapidly, good mouthfeel, and it is sweet to distinguish the flavor of, and is limited to 41s when dissolving
Embodiment 3:
Loperamide hydrochloride 1g
Dimethicone compound 62.5g
Hydroxypropyl emthylcellulose (3 centipoise) 80g
Maltodextrin 40g
Sucralose 3g
Fructus Citri Limoniae essence 2g
Glycerol 1g
Ethyl hydroxybenzoate 1g
Citric acid 2g
Lemon yellow 2g
Purified water 150g
Elder generation is with the maltodextrin of above-mentioned amount, citric acid and sucralose are soluble in water, obtain aqueous solution, hydroxypropyl emthylcellulose (3 centipoise) with above-mentioned amount joins in the aqueous solution under stirring again, fully dispersed with stirring obtains the hydroxypropyl emthylcellulose gel, get the ethyl hydroxybenzoate of above-mentioned amount, stir with joining again in the hydroxypropyl emthylcellulose gel after the glycerol heating for dissolving, add loperamide hydrochloride at last, simethicone, Fructus Citri Limoniae essence and lemon yellow also stir and obtain loperamide hydrochloride simethicone gel, the degassing, uniformly with loperamide hydrochloride simethicone gel coating on flat board, 70～80 ℃ of air blast heat dryings, cutting obtains described Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane.This film is light yellow, and is pliable and tough, and inlet dissolves dispersion rapidly, and it is sweet to distinguish the flavor of, and tart flavour is moderate, and joyful citrus scented is arranged, and mouthfeel is joyful, is limited to 15s when dissolving.
Embodiment 4:
Loperamide hydrochloride 1g
Simethicone 62.5g
Hydroxypropyl emthylcellulose (15 centipoise) 80g
Maltodextrin 40g
Purified water 140g
Earlier that the maltodextrin of above-mentioned amount is soluble in water, obtain maltodextrin aqueous solution, hydroxypropyl emthylcellulose (15 centipoise) with above-mentioned amount joins in the maltodextrin aqueous solution under stirring again, fully dispersed with stirring obtains the hydroxypropyl emthylcellulose gel, add loperamide hydrochloride and simethicone again and stir and obtain loperamide hydrochloride simethicone gel, the degassing, uniformly with loperamide hydrochloride simethicone gel coating on flat board, 70～80 ℃ of air blast heat dryings, cutting obtains described Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane.This film is white in color, and is pliable and tough, and inlet dissolves dispersion rapidly, and mouthfeel is better, is limited to 39s when dissolving.
Embodiment 5:
Loperamide hydrochloride 1g
Simethicone 62.5g
Hydroxypropyl emthylcellulose (3 centipoise) 80g
Maltodextrin 40g
Sucralose 2g
Purified water 100g
Earlier that the maltodextrin and the sucralose of above-mentioned amount is soluble in water, obtain aqueous solution, hydroxypropyl emthylcellulose (3 centipoise) with above-mentioned amount joins in the aqueous solution under stirring again, fully dispersed with stirring obtains the hydroxypropyl emthylcellulose gel, add loperamide hydrochloride and simethicone again and stir and obtain loperamide hydrochloride simethicone gel, the degassing, uniformly with loperamide hydrochloride simethicone gel coating on flat board, 70～80 ℃ of air blast heat dryings, cutting obtains described Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane.This film is white in color, and toughness is general, and inlet dissolves dispersion rapidly, good mouthfeel, and it is sweet to distinguish the flavor of, and is limited to 25s when dissolving.
Embodiment 6:
Loperamide hydrochloride 1g
Simethicone 62.5g
Hydroxypropyl emthylcellulose (3 centipoise) 80g
Maltodextrin 40g
Mannitol 20g
Pregelatinized Starch 20g
Sucralose 3g
Strawberry essence 2g
Polyethylene Glycol-400 2g
Sodium benzoate 1g
Tartaric acid 2g
Purified water 200g
Elder generation is with the maltodextrin of above-mentioned amount, mannitol, sucralose, sodium benzoate and tartaric acid are soluble in water, obtain aqueous solution, hydroxypropyl emthylcellulose (3 centipoise) with above-mentioned amount joins in the aqueous solution under stirring again, fully dispersed with stirring obtains the hydroxypropyl emthylcellulose gel, add loperamide hydrochloride at last, simethicone, pregelatinized Starch and strawberry essence also stir and obtain loperamide hydrochloride simethicone gel, the degassing, uniformly the loperamide hydrochloride simethicone is coated on the flat board, 75～80 ℃ of air blast heat dryings, cutting obtains described Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane.This film is white in color, and is pliable and tough, and inlet dissolves dispersion rapidly, and it is sweet to distinguish the flavor of, and tart flavour is moderate, and with the fragrance of strong Fructus Fragariae Ananssae, mouthfeel is joyful, is limited to 17s when dissolving.
Embodiment 7:
Loperamide hydrochloride 1g
Simethicone 62.5g
Hydroxypropyl emthylcellulose (60 centipoise) 80g
Purified water 100g
Hydroxypropyl emthylcellulose (60 centipoise) with above-mentioned amount joins in the aqueous solution under stirring earlier, fully dispersed with stirring obtains the hydroxypropyl emthylcellulose gel, add loperamide hydrochloride and simethicone again and stir and obtain loperamide hydrochloride simethicone gel, the degassing, uniformly with loperamide hydrochloride simethicone gel coating on flat board, 70～80 ℃ of air blast heat dryings, cutting obtains described Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane.This film is white in color, and is pliable and tough, and inlet dissolves dispersion rapidly, and mouthfeel is general, is limited to 56s when dissolving.
Embodiment 8:
Loperamide hydrochloride 1g
Simethicone 62.5g
Hydroxypropyl emthylcellulose (6 centipoise) 70g
Maltodextrin 30g
Pregelatinized Starch 20g
Aspartame 3g
Blue berry essence 3g
Color lake (light blue) 3g
Purified water 140g
Earlier that the maltodextrin and the aspartame of above-mentioned amount is soluble in water, obtain aqueous solution, hydroxypropyl emthylcellulose (6 centipoise) with above-mentioned amount joins in the aqueous solution under stirring again, fully dispersed with stirring obtains the hydroxypropyl emthylcellulose gel, add loperamide hydrochloride at last, simethicone, pregelatinized Starch, blue berry essence and color lake (light blue) also stir and obtain loperamide hydrochloride simethicone gel, the degassing, uniformly with loperamide hydrochloride simethicone gel coating on flat board, 70～80 ℃ of air blast heat dryings, cutting obtains described Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane.It is blue, pliable and tough that this film is, and inlet dissolves dispersion rapidly, and it is sweet to distinguish the flavor of, and with the fragrance of blue berry, mouthfeel is joyful, is limited to 22s when dissolving.
Embodiment 9:
Loperamide hydrochloride 1g
Simethicone 62.5g
Hydroxypropyl emthylcellulose (3 centipoise) 90g
Maltodextrin 30g
Sorbitol 40g
Sucralose 3g
Strawberry essence 5g
Glycerol 2g
Ethyl hydroxybenzoate 1g
Citric acid 2g
The red 2g of the certain kind of berries
Purified water 150g
Elder generation is with the maltodextrin of above-mentioned amount, sorbitol, citric acid and sucralose are soluble in water, obtain aqueous solution, hydroxypropyl emthylcellulose (3 centipoise) with above-mentioned amount joins in the aqueous solution under stirring again, fully dispersed with stirring obtains the hydroxypropyl emthylcellulose gel, get the ethyl hydroxybenzoate of above-mentioned amount, stir with joining again in the hydroxypropyl emthylcellulose gel after the glycerol heating for dissolving, add loperamide hydrochloride at last, simethicone, the strawberry essence and the certain kind of berries are red and stir and obtain loperamide hydrochloride simethicone gel, the degassing, uniformly with loperamide hydrochloride simethicone gel coating on flat board, 70～80 ℃ of air blast heat dryings, cutting obtains described Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane.This film is certain kind of berries redness, and is pliable and tough, and inlet dissolves dispersion rapidly, and it is sweet to distinguish the flavor of, and tart flavour is moderate, and with the fragrance of strong Fructus Fragariae Ananssae, mouthfeel is joyful, is limited to 20s when dissolving.
Embodiment 10:
Loperamide hydrochloride 1g
Simethicone 62.5g
Hydroxypropyl cellulose 100g
Purified water 100g
Hydroxypropyl cellulose with above-mentioned amount joins in the aqueous solution under stirring earlier, fully dispersed with stirring obtains hydroxypropyl cellulose gel, add loperamide hydrochloride and simethicone again and stir and obtain loperamide hydrochloride simethicone gel, the degassing, uniformly with loperamide hydrochloride simethicone gel coating on flat board, 70～80 ℃ of air blast heat dryings, cutting obtains described Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane.This film is white in color, and is pliable and tough, and inlet dissolves dispersion rapidly, and mouthfeel is general, is limited to 54s when dissolving.
Embodiment 11:
Loperamide hydrochloride 1g
Simethicone 62.5g
Hydroxypropyl emthylcellulose (3 centipoise) 100g
Maltodextrin 35g
Sucralose 5g
Flavoring orange essence 3g
Glycerol 2g
Purified water 100g
Earlier that the maltodextrin and the sucralose of above-mentioned amount is soluble in water, obtain aqueous solution, hydroxypropyl emthylcellulose (3 centipoise) with above-mentioned amount joins in the aqueous solution under stirring again, fully dispersed with stirring obtains the hydroxypropyl emthylcellulose gel, add glycerol again and stir, add loperamide hydrochloride at last, simethicone and flavoring orange essence also stir and obtain loperamide hydrochloride simethicone gel, the degassing, uniformly with loperamide hydrochloride simethicone gel coating on flat board, 70～80 ℃ of air blast heat dryings, cutting obtains described Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane.This film is white in color, and is pliable and tough, and inlet dissolves dispersion rapidly, and it is sweet to distinguish the flavor of, and strong Fructus Citri tangerinae fragrance is arranged, and good mouthfeel is limited to 27s when dissolving.
Embodiment 12:
Loperamide hydrochloride 1g
Simethicone 62.5g
Hydroxypropyl emthylcellulose (3 centipoise) 100g
Maltodextrin 50g
Sucralose 5g
Fructus Citri Limoniae essence 5g
Glycerol 2g
Ethyl hydroxybenzoate 2g
Citric acid 5g
Purified water 200g
Elder generation is with the maltodextrin of above-mentioned amount, citric acid and sucralose are soluble in water, obtain aqueous solution, hydroxypropyl emthylcellulose (3 centipoise) with above-mentioned amount joins in the aqueous solution under stirring again, fully dispersed with stirring obtains the hydroxypropyl emthylcellulose gel, get the ethyl hydroxybenzoate of above-mentioned amount, stir with joining again in the hydroxypropyl emthylcellulose gel after the glycerol heating for dissolving, add loperamide hydrochloride at last, simethicone and Fructus Citri Limoniae essence also stir and obtain loperamide hydrochloride simethicone gel, the degassing, uniformly with loperamide hydrochloride simethicone gel coating on flat board, 70～80 ℃ of air blast heat dryings, cutting obtains described Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane.This film is white in color, and is pliable and tough, and inlet dissolves dispersion rapidly, and it is sweet to distinguish the flavor of, and tart flavour is moderate, and joyful citrus scented is arranged, and mouthfeel is joyful, is limited to 25s when dissolving.
Embodiment 13:
Loperamide hydrochloride 2g
Simethicone 125g
Maltodextrin 200g
Purified water 300g
Maltodextrin with above-mentioned amount joins in the aqueous solution under stirring earlier, fully dispersed with stirring obtains the maltodextrin gel, add loperamide hydrochloride and simethicone again and stir and obtain loperamide hydrochloride simethicone gel, the degassing, uniformly with loperamide hydrochloride simethicone gel coating on flat board, 70～80 ℃ of air blast heat dryings, cutting obtains described Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane.This film is white in color, and toughness is general, and inlet dissolves dispersion rapidly, and is little sweet, and the fragrance of corn is arranged, and good mouthfeel is limited to 31s when dissolving.
Embodiment 14:
Loperamide hydrochloride 2g
Simethicone 125g
Hydroxypropyl emthylcellulose (60 centipoise) 50g
Maltodextrin 100g
Aspartame 10g
Purified water 300g
Earlier that the maltodextrin and the aspartame of above-mentioned amount is soluble in water, obtain aqueous solution, hydroxypropyl emthylcellulose (60 centipoise) with above-mentioned amount joins in the aqueous solution under stirring again, fully dispersed with stirring obtains the hydroxypropyl emthylcellulose gel, add loperamide hydrochloride and simethicone again and stir and obtain loperamide hydrochloride simethicone gel, the degassing, uniformly with loperamide hydrochloride simethicone gel coating on flat board, 70～80 ℃ of air blast heat dryings, cutting obtains described Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane.This film is white in color, and toughness is general, and inlet dissolves dispersion rapidly, good mouthfeel, and it is sweet to distinguish the flavor of, and is limited to 38s when dissolving.
Embodiment 15:
Loperamide hydrochloride 2g
Simethicone 125g
Amylopectin 250g
Maltodextrin 50g
Stevioside 10g
Purified water 300g
Earlier that the maltodextrin and the stevioside of above-mentioned amount is soluble in water, obtain aqueous solution, amylopectin with above-mentioned amount joins in the maltodextrin aqueous solution under stirring again, fully dispersed with stirring obtains the amylopectin gel, add loperamide hydrochloride and simethicone at last and stir and obtain loperamide hydrochloride simethicone gel, the degassing, uniformly with loperamide hydrochloride simethicone gel coating on flat board, 70～80 ℃ of air blast heat dryings, cutting obtains described Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane.This film is white in color, and toughness is general, and is frangible, and inlet dissolves dispersion rapidly, good mouthfeel, and it is sweet to distinguish the flavor of, and is limited to 41s when dissolving.
Embodiment 16:
Loperamide hydrochloride 1g
Simethicone 60g
Hydroxypropyl cellulose 100g
Purified water 100g
Hydroxypropyl cellulose with above-mentioned amount joins in the aqueous solution under stirring earlier, fully dispersed with stirring obtains hydroxypropyl cellulose gel, add loperamide hydrochloride and simethicone again and stir and obtain loperamide hydrochloride simethicone gel, the degassing, uniformly with loperamide hydrochloride simethicone gel coating on flat board, 70～80 ℃ of air blast heat dryings, cutting obtains described Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane.This film is white in color, and is pliable and tough, and inlet dissolves dispersion rapidly, and mouthfeel is general, is limited to 52s when dissolving.
Embodiment 17:
Loperamide hydrochloride 2g
Simethicone 130g
Hydroxypropyl emthylcellulose (60 centipoise) 50g
Maltodextrin 100g
Aspartame 10g
Purified water 300g
Earlier that the maltodextrin and the aspartame of above-mentioned amount is soluble in water, obtain aqueous solution, hydroxypropyl emthylcellulose (60 centipoise) with above-mentioned amount joins in the aqueous solution under stirring again, fully dispersed with stirring obtains the hydroxypropyl emthylcellulose gel, add loperamide hydrochloride and simethicone again and stir and obtain loperamide hydrochloride simethicone gel, the degassing, uniformly with loperamide hydrochloride simethicone gel coating on flat board, 70～80 ℃ of air blast heat dryings, cutting obtains described Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane.This film is white in color, and toughness is general, and inlet dissolves dispersion rapidly, good mouthfeel, and it is sweet to distinguish the flavor of, and is limited to 35s when dissolving.
Claims (3)
1. Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane is characterized in that the weight of each component is:
Loperamide hydrochloride 1g
Simethicone 62.5g
3 centipoise hydroxypropyl emthylcellulose 80g
Maltodextrin 40g
Sucralose 3g
Fructus Citri Limoniae essence 2g
Glycerol 1g
Ethyl hydroxybenzoate 1g
Citric acid 2g
Lemon yellow 2g
Purified water 150g
And be prepared as follows:
Earlier with maltodextrin, citric acid and sucralose are soluble in water, obtain aqueous solution, again 3 centipoise hydroxypropyl emthylcelluloses are joined in the aqueous solution under stirring, fully dispersed with stirring obtains the hydroxypropyl emthylcellulose gel, taking ethylparaben, stir with joining again in the hydroxypropyl emthylcellulose gel after the glycerol heating for dissolving, add loperamide hydrochloride at last, simethicone, Fructus Citri Limoniae essence and lemon yellow also stir and obtain loperamide hydrochloride simethicone gel, the degassing, uniformly with loperamide hydrochloride simethicone gel coating on flat board, 70～80 ℃ of air blast heat dryings, cutting promptly gets Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane.
2. Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane according to claim 1, the chemical name that it is characterized in that loperamide hydrochloride is: 4-(rubigan)-4-hydroxy-n, N-dimethyl-α, α-diphenyl-1-piperidines butanamide hydrochloride, structural formula is:
Molecular formula is: C
29H
33ClN
2O
2.HCl, molecular weight is: 513.50.
3. Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane according to claim 1 is characterized in that described simethicone chemical name is: polydimethylsiloxane, and structural formula is:
Molecular formula is: C
3H
9OSi. (C
2H
6OSi)
n.C
3H
9Si.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200810024460 CN101332197B (en) | 2008-03-25 | 2008-03-25 | Loperamide hydrochloride dimethicone compound rapidly disintegrating oral membrane |
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| US11975097B2 (en) | 2009-10-30 | 2024-05-07 | Ix Biopharma Ltd. | Fast dissolving solid dosage form |
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| US11975097B2 (en) | 2009-10-30 | 2024-05-07 | Ix Biopharma Ltd. | Fast dissolving solid dosage form |
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