CN1634061A - Pharmaceutical formulation of pseudoephenrine hydrochloride and its preparing process - Google Patents
Pharmaceutical formulation of pseudoephenrine hydrochloride and its preparing process Download PDFInfo
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- CN1634061A CN1634061A CN 200410040852 CN200410040852A CN1634061A CN 1634061 A CN1634061 A CN 1634061A CN 200410040852 CN200410040852 CN 200410040852 CN 200410040852 A CN200410040852 A CN 200410040852A CN 1634061 A CN1634061 A CN 1634061A
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Abstract
Disclosed is a pharmaceutical formulation of pseudoephenrine hydrochloride and its preparing process, which is prepared from acetaminopher, d-pesudoephedrine hydrochloride, waterless Dextromethorphan Hydrobromide, and right amount of base material. The invention also discloses the process for preparing the medicament. By preparing into the form of gel type, children are willing to take the preparation, it has good effects for controlling children's virus infection of upper respiratory tract and treating children's common cold.
Description
Technical field: the present invention is the pseudo-anaesthetic thing of a kind of bis-phenol preparation and preparation method thereof, and particularly pseudo-numb gel preparation of bis-phenol and other preparation method belong to technical field of medicaments.
Technical background: flu also claims acute upper respiratory tract infection, is commonly encountered diseases and the frequently-occurring disease that influences human health.Cold virus has nearly 200 kinds, and children's is because health defensive enginery immaturity also, and a little less than the resistance against diseases, so that all must catch 6-7 time every year, Kai Fa children coryza medicine kind increases gradually in recent years, and dosage form is different; As: disclosed number of patent application is " 02110056 " in the Chinese patent communique, patent application, number of patent application that name is called " Rationed fenmameimin drops " are called the patent application of " U.S.A pounces on pseudo-numb dry suspension and processing technology " for " 00136032 ", name; They all are to be used for active drug that infantile common cold is prevented and treated; But antihistamine composition chlorphenamine maleate has all been used in two parts of applications, the effect of this composition is secretions drying and the thickness that makes lower respiratory tract, reduces sneeze and secretion Rhinorrhea, has slight sedation simultaneously, the patient is easily drowsiness, is unfavorable for the work and study on daytime.And the product that has gone on the market: the pseudo-sesame candy slurry of bis-phenol, adopted acetaminophen, selectivity to shrink the pseudoephedrine hydrochloride of upper respiratory tract blood capillary, the dextromethorphan hydrobromide of maincenter antitussive effect with antipyretic-antalgic, though product has good antipyretic-antalgic, antitussive, alleviates the congested curative effect of nasal mucosa, but be the dosage form kind at the children characteristics, infant uses existing product that certain difficulty, displeased acceptance are arranged.In the real life, child patient quantity is huge, and is poor to the ability to accept of general formulation, and the outward appearance of medicine, mouthfeel directly influence the application and the curative effect of medicine; Infantile common cold is a kind of commonly encountered diseases that has a strong impact on child health, the dosage form of selecting suitable prescription control children's upper respiratory tract viral infection and being suitable for child administration is setting about a little of research and development children coryza medicine, in view of the develop rapidly of medical science and these situations that deepen continuously that cold virus is studied, need exploitation effective medicine preparation that a kind of market prospect is wide, the child takes like a shot, the treatment of infantile common cold is reached a new high, thereby infantile common cold patient's quality of life is further improved.
Summary of the invention: the objective of the invention is to: the pseudo-anaesthetic thing of a kind of bis-phenol preparation and preparation method thereof is provided; The present invention is made into fruit jelly or the soft sweet type gel that liked by the child, and children's extremely is ready to take, and has reduced the adult and has advised the trouble of feeding, and is not only tasty, and therapeutical effect is good, has enriched the dosage form kind, and market prospect is very wide; And, select feasible substrate and technology rationally, product appearance, good mouthfeel at the pharmaceutical properties of ambroxol hydrochloride.
The present invention constitutes like this: the pseudo-anaesthetic thing of bis-phenol preparation: calculate according to weight, it is to be made into gel, injection by acetaminophen 1000～2000mg, pseudoephedrine hydrochloride 100～200mg, anhydrous dextromethorphan hydrobromide 20～80mg and appropriate amount of auxiliary materials, comprising: injection, powder pin, freeze-dried powder, dispersible tablet, soft capsule, drop pill, slow releasing preparation.Specifically: the pseudo-anaesthetic thing of this bis-phenol preparation: calculate according to weight, it is prepared into gel fruit jelly or soft sweet type gel oral formulations by acetaminophen 1000～2000mg, pseudoephedrine hydrochloride 100～200mg and anhydrous dextromethorphan hydrobromide 20～80mg and an amount of substrate, and wherein: substrate is one or more compositions of carrageenan, agar, carbomer, gelatin, sodium carboxymethyl cellulose or arabic gum.Specifically: the gel preparation that the substrate that the gel preparation of this product is mixed to obtain by 1: 2 part by weight by acetaminophen 1600mg, pseudoephedrine hydrochloride 150mg and anhydrous dextromethorphan hydrobromide 50mg and Konjac glucomannan, carrageenan is prepared into is semifluid or solid gel shape.The gel preparation of indication of the present invention can also be by acetaminophen 1600mg, pseudoephedrine hydrochloride 150mg and anhydrous dextromethorphan hydrobromide 50mg and carrageenan: agar: Konjac glucomannan: gelatin: sodium carboxymethyl cellulose: arabic gum=1: 1: 0.5: 1: 3: 1 part by weight mixes the substrate that obtains and is prepared from, the gel preparation that obtains, its shape that is translucent.The preparation method of the pseudo-anaesthetic thing of bis-phenol preparation: will be to acetyl-amino phenol, pseudoephedrine hydrochloride and anhydrous hydrobromic acid right U.S. husky and substrate mix homogeneously, after the sterilization promptly.Specifically: the gel in the described preparation prepares like this: by beta-schardinger dextrin-: acetaminophen is that 3: 1 part by weight takes by weighing beta-schardinger dextrin-, beta-schardinger dextrin-is dissolved in 30 ℃ of thermostatted water solution, add corresponding acetaminophen separately, after the 250rmin magnetic agitation 4 hours, drop to room temperature gradually, the clathrate suspension that forms was left standstill in refrigerator 24 hours, sucking filtration, discard filtrate, drain back 50 ℃ of cold drying with distilled water wash, must be to acetyl-amino phenol clathrate; Konjac glucomannan, carrageenan are pressed 1: 2 part by weight mix homogeneously; under stirring condition; 0.8% mixed-matrix is put into cold water; make it to disperse; soak 20～30min, make the abundant water absorption and swelling of substrate, stir then, heat; filter; filter the back and add under condition of stirring acetyl-amino phenol clathrate, pseudoephedrine hydrochloride, anhydrous dextromethorphan hydrobromide, mix homogeneously joins rapidly in the disinfecting container; seal; sterilization is cooled to about 30 ℃ condensation rapidly; drying, promptly.
Gel in the preparation of the present invention can also prepare like this: by beta-schardinger dextrin-: acetaminophen is that 3: 1 part by weight takes by weighing beta-schardinger dextrin-, beta-schardinger dextrin-is dissolved in 30 ℃ of thermostatted water solution, add corresponding acetaminophen separately, after the 250rmin magnetic agitation 4 hours, drop to room temperature gradually, the clathrate suspension that forms was left standstill in refrigerator 24 hours, sucking filtration, discard filtrate, drain back 50 ℃ of cold drying with distilled water wash, must be to acetyl-amino phenol clathrate; With carrageenan: agar: Konjac glucomannan: gelatin: sodium carboxymethyl cellulose: arabic gum=1: 1: 0.5: 1: 3: 1 part by weight mix homogeneously; under stirring condition; 0.8% mixed-matrix is put into cold water;, make it to disperse, soak 20～30min; make the abundant water absorption and swelling of substrate; stir then; heating is filtered, and filters the back and adds under condition of stirring acetyl-amino phenol clathrate; pseudoephedrine hydrochloride; anhydrous dextromethorphan hydrobromide; mix homogeneously; join rapidly in the disinfecting container, seal, sterilization; be cooled to rapidly about 30 ℃; condensation, drying, promptly.In preparation process, allow to add materials such as suitable flavoring agent or food coloring, with the color and luster that improves product, local flavor etc.
Compared with prior art, the application will have preparation now and change system into fruit jelly or the soft sweet type gel that liked by the child, children's extremely is ready to take, reduce the adult and advised the trouble of feeding, not only tasty, product has enriched the dosage form kind for control children's upper respiratory tract viral infection, treatment children's's flu function well, and market prospect is very wide.
The applicant finds in development process, the acetaminophen poor solubility, if directly make gel, the dissolubility of medicine, dissolution, bioavailability are all poor than liquid preparation; The more important thing is in the gel environment of humidity to be hydrolyzed into p-aminophenol that oxidation further takes place then, and color is pulverize redness, brown gradually, becomes black at last; And the kind of gel-type vehicle and consumption have played crucial effects to outward appearance, stability, the curative effect of product; As a kind of novel form, the release of medicine, to absorb whether desirable, gelling or the like be key problem in technology problem of the present invention.
The applicant has carried out a series of experiments, select to adopt beta-schardinger dextrin-at last: 3: 1 part by weight of acetaminophen, 6 hours mixing time, 30 ℃ temperature, technical conditions such as parcel acetaminophen etc., improved greatly medicine dissolution, improved the stability of product; The composite substrate of weight ratio that adopts Konjac glucomannan, carrageenan to press 1: 2, the product stability that makes, gel strength ideal, outward appearance is good, selects the supplementary product kind of preparation technology, use of pharmaceutical preparation provided by the invention and consumption, ratio etc., can guarantee its science, reasonable, feasible; The preparation that obtains has effective therapeutic effect.
Experimental example 1: acetaminophen clathrate technical study
(1) technical study
Group medicine: beta-schardinger dextrin-mixing time enclose temperature ℃ clathrate weight g clathrate content %
1 1∶8 6 50 6.44 11.2
2 1∶8 6 40 6.19 9.3
3 1∶8 6 30 5.38 8.7
4 1∶6 3 40 7.37 21.3
5 1∶6 3 30 7.42 16.8
6 1∶6 3 50 8.02 14.6
7 1∶3 1 30 10.29 38.5
8 1∶3 1 50 10.35 30.2
9 1∶3 1 40 10.08 22.3
The result shows that the clathrate optimum process condition of preparation is: beta-schardinger dextrin-: 3: 1 part by weight of acetaminophen, 6 hours mixing time, 30 ℃ temperature.
(2) release experiment
With 30 livers, the normal male rat of renal function (age about 3 months, 200～250g), be divided into 3 groups at random: the pseudo-numb syrup group of bis-phenol, do not prepare clathrate gel group, gel group of the present invention, 10 every group.Behind every group of rat fasting 12h, difference single-dose ambroxol hydrochloride sheet, ambroxol hydrochloride capsule and gel group of the present invention (dosage is 0.6mg), 2h advances unified feedstuff after the administration, in the back 0.5,1,2 of taking medicine, 5,10h extracts ulnar vein blood 2-3ml, and centrifugal 10min gets serum and places-20 ℃ of cryopreservation to measuring.Measurement result sees Table 3.
(* 10 for table 3 blood drug level-time data
-9G/ml)
Group 0.5h 1h 2h 5h 10h
The pseudo-numb syrup group 3.5 of bis-phenol ± 1.8 4.8 ± 1.1 3.8 ± 0.7 1.3 ± 0.5 0.3 ± 0.2
Do not prepare clathrate gel group 3.6 ± 1.1 4.0 ± 1.4 4.1 ± 1.0 3.6 ± 0.9 2.5 ± 0.5
Gel group 4.2 of the present invention ± 1.3 5.2 ± 3.4 4.1 ± 0.6 1.3 ± 0.4 0.5 ± 0.9
The result shows: after cyclodextrin and medicine form clathrate, the physicochemical property of acetaminophen changes to some extent, suppress hydrolysis, oxidation, improve dissolubility, the blood drug level of product of the present invention last stage after advancing medicine all is not less than liquid preparation, show gel of the present invention is entered the internal energy rapid absorption of body, reach valid density.
Experimental example 2: Study on Forming
(1) selection of matrix species
The ambroxol hydrochloride gel clarity of gel relatively
Substrates quantity % gel strength (g/cm
2)
Carrageenan 0.8 1665.2
Konjac glucomannan 0.8 1557.4
Carrageenan+Konjac glucomannan 0.8 1101.3
(2) screening of substrate composition and consumption
Konjac glucomannan: carrageenan consumption % mouthfeel
1: 1 0.6 crisp, difference of hardness, poor toughness, no bite
1: 1 0.8 crisp, difference of hardness, poor toughness, no bite
1: 1 1.0 crisp, difference of hardness, poor toughness, no bite
Hardness was moderate in 1: 2 0.6, and tough elasticity is relatively poor, and bite is arranged
Hardness was moderate in 1: 2 0.8, and tough good springiness has bite
Hardness was big in 1: 2 1.0, and tough elasticity is strong
Hardness was big in 1: 3 0.6, and tough elasticity is strong
Hardness was big in 1: 3 0.8, and tough elasticity is strong
Hardness was big in 1: 3 1.0, and tough elasticity is strong
The result shows: the best composite condition of substrate is a Konjac glucomannan: the part by weight of carrageenan=1: 2, consumption is 0.8%.
(3) study on the stability
0 month 6 months March December
The group color indicates content % color and indicates content % color sign content % color sign content %
Do not wrap up gel yellowish 99.8 yellowish 99.7 brown 98.0 dark brown 97.5
Gel of the present invention yellowish 99.9 yellowish 99.8 yellowish 99.6 yellowish 99.6
The result shows: after cyclodextrin and medicine formed clathrate, the physicochemical property of acetaminophen changed to some extent, suppressed hydrolysis, oxidation, had improved preparation stability.
Experimental example 3: pharmacodynamic experiment
The experimentation of antipyretic effect
The experiment material animal: healthy New Zealand large ear rabbit, body weight (2.4 ± 0.3) kg, male and female have concurrently; Medicine: medicine A: according to method preparation of the present invention, medicine B: the pseudo-sesame candy slurry of bis-phenol; Instrument: computer numeral clinical thermometer.
Experimental technique: get 24 of health large ear rabbits, 3d before the experiment, at room temperature 22-25 ℃, humidity is that every interval was surveyed animal anus temperature in 1 hour 1 time totally 4 times under the 55%-65% ventilated environment, animal is adapted to, and the animal of selection body temperature fluctuation range in 0.4 ℃ of scope is standby.During experiment animal is divided into 4 groups at random by the body weight size, is respectively normal saline group, A group, B group.Survey rabbit anus temperature 1 time every 30min with the computer digital clinical thermometer, survey altogether 3 times, ask for its meansigma methods and be this animal basal body temperature.Press 1ml/kg administration rabbit ear edge intravenous injection deactivation escherichia coli pyrogenicity, and before pyrogenicity 30 minutes gastric infusions at twice after 30min and the pyrogenicity.After pyrogenicity 30,60,120,240 and 360min survey rabbit anus temperature respectively 5 times, calculate the difference respectively organize rabbit day part treatment back anus temperature and basal body temperature, processing takes statistics.
Each different period body temperature situation of change in treated animal treatment back
The group treatment back time (min)
30 60 120 240 360
Normal saline group 0.47 ± 0.39 1.33 ± 0.24 2.20 ± 0.05 1.58 ± 0.15 0.84 ± 0.14
Treatment A group 0.34 ± 0.17 0.82 ± 0.47 0.92 ± 0.47 0.51 ± 0.18 0.33 ± 0.15
Treatment B group 0.37 ± 0.29 0.84 ± 0.29 0.99 ± 0.24 0.55 ± 0.23 0.44 ± 0.27
The result shows: the A group has obvious antipyretic effect to escherichia coli pyrogenicity rabbit, and its effect of bringing down a fever is not less than and is better than the B group, and antipyretic effect is lasting than the B group.
Concrete embodiment:
Embodiments of the invention 1:
Acetaminophen 2000mg, pseudoephedrine hydrochloride 200mg, anhydrous dextromethorphan hydrobromide 80mg
By beta-schardinger dextrin-: acetaminophen is that 3: 1 part by weight takes by weighing beta-schardinger dextrin-, beta-schardinger dextrin-is dissolved in 30 ℃ of thermostatted water solution, add corresponding acetaminophen separately, after the 250rmin magnetic agitation 4 hours, drop to room temperature gradually, the clathrate suspension that forms was left standstill in refrigerator 24 hours, sucking filtration, discard filtrate, drain back 50 ℃ of cold drying with distilled water wash, must be to acetyl-amino phenol clathrate; With Konjac glucomannan; carrageenan is pressed 1: 2 part by weight mix homogeneously; under stirring condition; 0.8% mixed-matrix is put into cold water; make it to disperse, soak 20～30min, make the abundant water absorption and swelling of substrate; stir then; heating; filter, filter the back and under condition of stirring, add acetyl-amino phenol clathrate; pseudoephedrine hydrochloride; anhydrous dextromethorphan hydrobromide, mix homogeneously; join rapidly in the disinfecting container; seal, sterilization is cooled to rapidly about 30 ℃; condensation; drying promptly gets gel, this product oral; three times on the one; each 2 bags; every bag 10 gram.
Embodiments of the invention 2:
Acetaminophen 1000mg, pseudoephedrine hydrochloride 100mg, anhydrous dextromethorphan hydrobromide 20mg
By beta-schardinger dextrin-: acetaminophen is that 3: 1 part by weight takes by weighing beta-schardinger dextrin-, beta-schardinger dextrin-is dissolved in 30 ℃ of thermostatted water solution, add corresponding acetaminophen separately, after the 250rmin magnetic agitation 4 hours, drop to room temperature gradually, the clathrate suspension that forms was left standstill in refrigerator 24 hours, sucking filtration, discard filtrate, drain back 50 ℃ of cold drying with distilled water wash, must be to acetyl-amino phenol clathrate; With carrageenan: agar: Konjac glucomannan: gelatin: sodium carboxymethyl cellulose: arabic gum=1: 1: 0.5: 1: 3: 1 part by weight mix homogeneously; under stirring condition; 0.8% mixed-matrix is put into cold water; make it to disperse; soak 20～30min, make the abundant water absorption and swelling of substrate, stir then; heating; filter; filtering the back adds under condition of stirring acetyl-amino phenol clathrate; pseudoephedrine hydrochloride; anhydrous dextromethorphan hydrobromide, mix homogeneously joins rapidly in the disinfecting container; seal; sterilization is cooled to about 30 ℃ condensation rapidly; drying promptly gets gel.
Embodiments of the invention 3:
Acetaminophen 2000mg, pseudoephedrine hydrochloride 200mg, anhydrous dextromethorphan hydrobromide 80mg
Get acetaminophen, pseudoephedrine hydrochloride, anhydrous dextromethorphan hydrobromide, press medicine: substrate=1: 1.4, the mixed-matrix of adding soybean oil, soybean lecithin, heating and melting, mixing gets soft capsule content; The preparation of glue: with gelatin: glycerol: water=1: 0.3: 0.7, get gelatin and add an amount of distilled water and make its imbibition, glycerol and remaining water are put be heated to 70～80 ℃ in the glue pot in addition, mix homogeneously adds expansible gelatin and stirs, and makes it to dissolve into uniform glue, in 70 ℃ of insulations 1～2 hour, leave standstill, remove the come-up foam, filter with cloth bag, in encapsulating machine, be pressed into soft capsule, be pressed into soft capsule, put in the drum drying machine and finalize the design, whole ball, drying promptly gets soft capsule.
Embodiments of the invention 4:
Acetaminophen 1000mg, pseudoephedrine hydrochloride 100mg, anhydrous dextromethorphan hydrobromide 20mg
Get acetaminophen, pseudoephedrine hydrochloride, anhydrous dextromethorphan hydrobromide, splash into the ratio that adopts PEG6000 and PEG4000 and be in 4: 3 the mixed-matrix, the water dropper model adopts No. 2 water droppers, and coolant temperature is 18～20 ℃, promptly gets drop pill.
Embodiments of the invention 5:
Acetaminophen 1600mg, pseudoephedrine hydrochloride 150mg, anhydrous dextromethorphan hydrobromide 50mg
By beta-schardinger dextrin-: acetaminophen is that 3: 1 part by weight takes by weighing beta-schardinger dextrin-, beta-schardinger dextrin-is dissolved in 30 ℃ of thermostatted water solution, add corresponding acetaminophen separately, after the 250rmin magnetic agitation 4 hours, drop to room temperature gradually, the clathrate suspension that forms was left standstill in refrigerator 24 hours, sucking filtration, discard filtrate, drain back 50 ℃ of cold drying with distilled water wash, must be to acetyl-amino phenol clathrate; Carrageenan with 0.8% under stirring condition, is put into cold water; make it to disperse, soak 20～30min, make the abundant water absorption and swelling of substrate; stir then, heat, filter, filter the back and under condition of stirring, add acetyl-amino phenol clathrate, pseudoephedrine hydrochloride, anhydrous dextromethorphan hydrobromide; mix homogeneously joins rapidly in the disinfecting container, seals; sterilization is cooled to about 30 ℃ condensation rapidly; drying promptly gets gel.
Embodiments of the invention 6:
Acetaminophen 1600mg, pseudoephedrine hydrochloride 150mg, anhydrous dextromethorphan hydrobromide 50mg
By beta-schardinger dextrin-: acetaminophen is that 3: 1 part by weight takes by weighing beta-schardinger dextrin-, beta-schardinger dextrin-is dissolved in 30 ℃ of thermostatted water solution, add corresponding acetaminophen separately, after the 250rmin magnetic agitation 4 hours, drop to room temperature gradually, the clathrate suspension that forms was left standstill in refrigerator 24 hours, sucking filtration, discard filtrate, drain back 50 ℃ of cold drying with distilled water wash, must be to acetyl-amino phenol clathrate; Agar with 0.7% under stirring condition, is put into cold water; make it to disperse, soak 20～30min, make the abundant water absorption and swelling of substrate; stir then, heat, filter, filter the back and under condition of stirring, add acetyl-amino phenol clathrate, pseudoephedrine hydrochloride, anhydrous dextromethorphan hydrobromide; mix homogeneously joins rapidly in the disinfecting container, seals; sterilization is cooled to about 30 ℃ condensation rapidly; drying promptly gets gel.
Embodiments of the invention 7:
Acetaminophen 1600mg, pseudoephedrine hydrochloride 150mg, anhydrous dextromethorphan hydrobromide 50mg are by beta-schardinger dextrin-: acetaminophen is that 3: 1 part by weight takes by weighing beta-schardinger dextrin-, beta-schardinger dextrin-is dissolved in 30 ℃ of thermostatted water solution, add corresponding acetaminophen separately, after the 250rmin magnetic agitation 4 hours, drop to room temperature gradually, the clathrate suspension that forms was left standstill in refrigerator 24 hours, sucking filtration, discard filtrate, drain back 50 ℃ of cold drying with distilled water wash, must be to acetyl-amino phenol clathrate; Gelatin with 0.8% under stirring condition, is put into cold water; make it to disperse, soak 20～30min, make the abundant water absorption and swelling of substrate; stir then, heat, filter, filter the back and under condition of stirring, add acetyl-amino phenol clathrate, pseudoephedrine hydrochloride, anhydrous dextromethorphan hydrobromide; mix homogeneously joins rapidly in the disinfecting container, seals; sterilization is cooled to about 30 ℃ condensation rapidly; drying promptly gets gel.
Embodiments of the invention 8:
Acetaminophen 1600mg, pseudoephedrine hydrochloride 150mg, anhydrous dextromethorphan hydrobromide 50mg
By beta-schardinger dextrin-: acetaminophen is that 3: 1 part by weight takes by weighing beta-schardinger dextrin-, beta-schardinger dextrin-is dissolved in 30 ℃ of thermostatted water solution, add corresponding acetaminophen separately, after the 250rmin magnetic agitation 4 hours, drop to room temperature gradually, the clathrate suspension that forms was left standstill in refrigerator 24 hours, sucking filtration, discard filtrate, drain back 50 ℃ of cold drying with distilled water wash, must be to acetyl-amino phenol clathrate; Konjac glucomannan with 1.2% under stirring condition, is put into cold water; make it to disperse, soak 20～30min, make the abundant water absorption and swelling of substrate; stir then, heat, filter, filter the back and under condition of stirring, add acetyl-amino phenol clathrate, pseudoephedrine hydrochloride, anhydrous dextromethorphan hydrobromide; mix homogeneously joins rapidly in the disinfecting container, seals; sterilization is cooled to about 30 ℃ condensation rapidly; drying promptly gets gel.
Embodiments of the invention 9:
Acetaminophen 1600mg, pseudoephedrine hydrochloride 150mg, anhydrous dextromethorphan hydrobromide 50mg
By beta-schardinger dextrin-: acetaminophen is that 3: 1 part by weight takes by weighing beta-schardinger dextrin-, beta-schardinger dextrin-is dissolved in 30 ℃ of thermostatted water solution, add corresponding acetaminophen separately, after the 250rmin magnetic agitation 4 hours, drop to room temperature gradually, the clathrate suspension that forms was left standstill in refrigerator 24 hours, sucking filtration, discard filtrate, drain back 50 ℃ of cold drying with distilled water wash, must be to acetyl-amino phenol clathrate; Sodium carboxymethyl cellulose with 1.3% under the stirring condition, is put into cold water; make it to disperse, soak 20～30min, make the abundant water absorption and swelling of substrate; stir then, heat, filter, filter the back and under condition of stirring, add acetyl-amino phenol clathrate, pseudoephedrine hydrochloride, anhydrous dextromethorphan hydrobromide; mix homogeneously joins rapidly in the disinfecting container, seals; sterilization is cooled to about 30 ℃ condensation rapidly; drying promptly gets gel.
Embodiments of the invention 10:
Acetaminophen 1600mg, pseudoephedrine hydrochloride 150mg, anhydrous dextromethorphan hydrobromide 50mg
By beta-schardinger dextrin-: acetaminophen is that 3: 1 part by weight takes by weighing beta-schardinger dextrin-, beta-schardinger dextrin-is dissolved in 30 ℃ of thermostatted water solution, add corresponding acetaminophen separately, after the 250rmin magnetic agitation 4 hours, drop to room temperature gradually, the clathrate suspension that forms was left standstill in refrigerator 24 hours, sucking filtration, discard filtrate, drain back 50 ℃ of cold drying with distilled water wash, must be to acetyl-amino phenol clathrate; Arabic gum with 1.1% under stirring condition, is put into cold water; make it to disperse, soak 20～30min, make the abundant water absorption and swelling of substrate; stir then, heat, filter, filter the back and under condition of stirring, add acetyl-amino phenol clathrate, pseudoephedrine hydrochloride, anhydrous dextromethorphan hydrobromide; mix homogeneously joins rapidly in the disinfecting container, seals; sterilization is cooled to about 30 ℃ condensation rapidly; drying promptly gets gel.
Claims (7)
1, the pseudo-anaesthetic thing of a kind of bis-phenol preparation, it is characterized in that: calculate according to weight, it is to be made into gel, injection by acetaminophen 1000～2000mg, pseudoephedrine hydrochloride 100～200mg and anhydrous dextromethorphan hydrobromide 20～80mg and appropriate amount of auxiliary materials, comprising: injection, powder pin, freeze-dried powder, dispersible tablet, soft capsule, drop pill, slow releasing preparation.
2, according to the pseudo-anaesthetic thing of the described bis-phenol of claim 1 preparation, it is characterized in that: calculate according to weight, it is prepared into gel fruit jelly or soft sweet type gel oral formulations by acetaminophen 1000～2000mg, pseudoephedrine hydrochloride 100～200mg and anhydrous dextromethorphan hydrobromide 20～80mg and an amount of substrate, and wherein: substrate is one or more compositions of carrageenan, agar, carbomer, gelatin, sodium carboxymethyl cellulose or arabic gum.
3, according to claim 1 or the pseudo-anaesthetic thing of 2 described bis-phenols preparation, it is characterized in that: the gel preparation that the substrate that it is mixed to obtain by 1: 2 part by weight by acetaminophen 1600mg, pseudoephedrine hydrochloride 150mg and anhydrous dextromethorphan hydrobromide 50mg and Konjac glucomannan, carrageenan is prepared into is semifluid or solid gel shape.
4, according to claim 1 or the pseudo-anaesthetic thing of 2 described bis-phenols preparation, it is characterized in that: it is by acetaminophen 1600mg, pseudoephedrine hydrochloride 150mg and anhydrous dextromethorphan hydrobromide 50mg and carrageenan: agar: Konjac glucomannan: gelatin: sodium carboxymethyl cellulose: arabic gum=1: 1: 0.5: 1: 3: 1 part by weight mixes the substrate that obtains and is prepared from, the gel preparation that obtains, its shape that is translucent.
5, as the preparation method of the pseudo-anaesthetic thing of bis-phenol as described in the claim 1～4 any preparation, it is characterized in that: will be to acetyl-amino phenol, pseudoephedrine hydrochloride and anhydrous hydrobromic acid right U.S. husky and substrate mix homogeneously, after the sterilization promptly.
6, preparation method according to the pseudo-anaesthetic thing of the described bis-phenol of claim 5 preparation, it is characterized in that: the gel in the described preparation prepares like this: by beta-schardinger dextrin-: acetaminophen is that 3: 1 part by weight takes by weighing beta-schardinger dextrin-, beta-schardinger dextrin-is dissolved in 30 ℃ of thermostatted water solution, add corresponding acetaminophen separately, after the 250rmin magnetic agitation 4 hours, drop to room temperature gradually, the clathrate suspension that forms was left standstill in refrigerator 24 hours, sucking filtration, discard filtrate, drain back 50 ℃ of cold drying with distilled water wash, must be to acetyl-amino phenol clathrate; Konjac glucomannan, carrageenan are pressed 1: 2 part by weight mix homogeneously; under stirring condition; 0.8% mixed-matrix is put into cold water; make it to disperse; soak 20～30min, make the abundant water absorption and swelling of substrate, stir then, heat; filter; filter the back and add under condition of stirring acetyl-amino phenol clathrate, pseudoephedrine hydrochloride, anhydrous dextromethorphan hydrobromide, mix homogeneously joins rapidly in the disinfecting container; seal; sterilization is cooled to about 30 ℃ condensation rapidly; drying, promptly.
7, preparation method according to the pseudo-anaesthetic thing of the described bis-phenol of claim 5 preparation, it is characterized in that: the gel in the described preparation prepares like this: by beta-schardinger dextrin-: acetaminophen is that 3: 1 part by weight takes by weighing beta-schardinger dextrin-, beta-schardinger dextrin-is dissolved in 30 ℃ of thermostatted water solution, add corresponding acetaminophen separately, after the 250rmin magnetic agitation 4 hours, drop to room temperature gradually, the clathrate suspension that forms was left standstill in refrigerator 24 hours, sucking filtration, discard filtrate, drain back 50 ℃ of cold drying with distilled water wash, must be to acetyl-amino phenol clathrate; With carrageenan: agar: Konjac glucomannan: gelatin: sodium carboxymethyl cellulose: arabic gum=1: 1: 0.5: 1: 3: 1 part by weight mix homogeneously; under stirring condition; 0.8% mixed-matrix is put into cold water;, make it to disperse, soak 20～30min; make the abundant water absorption and swelling of substrate; stir then; heating is filtered, and filters the back and adds under condition of stirring acetyl-amino phenol clathrate; pseudoephedrine hydrochloride; anhydrous dextromethorphan hydrobromide; mix homogeneously; join rapidly in the disinfecting container, seal, sterilization; be cooled to rapidly about 30 ℃; condensation, drying, promptly.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410040852 CN1634061A (en) | 2004-10-11 | 2004-10-11 | Pharmaceutical formulation of pseudoephenrine hydrochloride and its preparing process |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410040852 CN1634061A (en) | 2004-10-11 | 2004-10-11 | Pharmaceutical formulation of pseudoephenrine hydrochloride and its preparing process |
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| Publication Number | Publication Date |
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| CN1634061A true CN1634061A (en) | 2005-07-06 |
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| CN 200410040852 Pending CN1634061A (en) | 2004-10-11 | 2004-10-11 | Pharmaceutical formulation of pseudoephenrine hydrochloride and its preparing process |
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Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100448431C (en) * | 2005-10-17 | 2009-01-07 | 重庆医药工业研究院有限责任公司 | Oral disintegrated Anfenmame tablet for treating children's cold and its prepn |
| CN101596158B (en) * | 2008-06-04 | 2011-03-30 | 北京科信必成医药科技发展有限公司 | Compound slow release preparation of acetyl aminophenol, pseudoephedrine and dextromethorphan |
| CN102225065A (en) * | 2011-04-28 | 2011-10-26 | 海南新中正制药有限公司 | Parcetamol pseudoephedrine hydrochloride and dextromethorphan hydrochloride capsule and preparation method thereof |
| CN103110629A (en) * | 2013-02-19 | 2013-05-22 | 青岛正大海尔制药有限公司 | Compound phenol caplets dropping pills and preparation method thereof |
| CN103536539A (en) * | 2013-09-16 | 2014-01-29 | 南通丝乡丝绸有限公司 | Dextromethorphan hydrobromide lyophilized powder and preparation method thereof |
| CN103536527A (en) * | 2013-09-16 | 2014-01-29 | 南通丝乡丝绸有限公司 | Dextromethorphan hydrobromide injection and preparation method thereof |
| CN110025568A (en) * | 2019-03-06 | 2019-07-19 | 广州中天康顺生物医药有限公司 | A kind of thixotroping pharmaceutical hydrogel matrix and its shaddock ped glycosides formulation and preparation method |
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2004
- 2004-10-11 CN CN 200410040852 patent/CN1634061A/en active Pending
Cited By (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100448431C (en) * | 2005-10-17 | 2009-01-07 | 重庆医药工业研究院有限责任公司 | Oral disintegrated Anfenmame tablet for treating children's cold and its prepn |
| CN101596158B (en) * | 2008-06-04 | 2011-03-30 | 北京科信必成医药科技发展有限公司 | Compound slow release preparation of acetyl aminophenol, pseudoephedrine and dextromethorphan |
| CN102225065A (en) * | 2011-04-28 | 2011-10-26 | 海南新中正制药有限公司 | Parcetamol pseudoephedrine hydrochloride and dextromethorphan hydrochloride capsule and preparation method thereof |
| CN102225065B (en) * | 2011-04-28 | 2013-05-15 | 海南新中正制药有限公司 | Parcetamol pseudoephedrine hydrochloride and dextromethorphan hydrochloride capsule and preparation method thereof |
| CN103110629A (en) * | 2013-02-19 | 2013-05-22 | 青岛正大海尔制药有限公司 | Compound phenol caplets dropping pills and preparation method thereof |
| CN103536539A (en) * | 2013-09-16 | 2014-01-29 | 南通丝乡丝绸有限公司 | Dextromethorphan hydrobromide lyophilized powder and preparation method thereof |
| CN103536527A (en) * | 2013-09-16 | 2014-01-29 | 南通丝乡丝绸有限公司 | Dextromethorphan hydrobromide injection and preparation method thereof |
| CN103536539B (en) * | 2013-09-16 | 2015-03-25 | 南通丝乡丝绸有限公司 | Dextromethorphan hydrobromide lyophilized powder and preparation method thereof |
| CN110025568A (en) * | 2019-03-06 | 2019-07-19 | 广州中天康顺生物医药有限公司 | A kind of thixotroping pharmaceutical hydrogel matrix and its shaddock ped glycosides formulation and preparation method |
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