CN1698688A - Compound defervesce foam for children - Google Patents

Abstract

The invention discloses a compound defervesce foam for children, which is prepared from the raw materials of acetaminopher, artificial ox gallstone, isatic root powder, propylene glycol, polyvidon K3O, stearic acid, lanoline and ethanol through the following steps, mixing homogeneously, stirring homogeneously, split charging, pushing in casting agent, and loading into bottles.

Description

The compound infantile foam of bringing down a fever

Technical field

The present invention relates to a kind of pharmaceutical preparation, particularly a kind of pharmaceutical foam agent for the treatment of pediatric disease.

Background technology

Paracetamol compound suppository is the conventional medicine of infantile fever such as treatment fever of children and upper respiratory tract infection.This medicine is the Chinese medicine and western medicine compound preparation, through clinical verification for many years, and its determined curative effect, without any side effects.But suppository exists one to dissolve dispose procedure at internal rectum, and owing to be local contact, and is little with the mucous membrane of rectum contact area, may the induce drug inflammation; The local concentration height can cause infiltration rate slow, and the performance drug effect is slow, uses inconvenience.

Summary of the invention

The objective of the invention is to, a kind of compound infantile foam of bringing down a fever is provided.This foam dissolves that to discharge medicine fast, and big with the mucous membrane of rectum contact area, infiltration rate is fast, and the performance drug effect is fast and lasting, easy to use, better efficacy.

Technical scheme of the present invention is, the compound infantile foam of bringing down a fever is characterized in that it is to be made by the following weight proportion raw material:

2～3 parts of 60～65 parts of artificial Calculus Boviss of acetaminophen

70～80 parts of 20～22 parts of propylene glycol of Rhizoma Et Radix Baphicacanthis Cusiae extractum powder

8～20 parts of 30 1～5 parts of stearic acid of 30 POVIDONE K 30 BP/USP

200～250 parts of 1～5 part of ethanol of lanoline

90～120 parts of purified water

Preparation method is, gets acetaminophen, Rhizoma Et Radix Baphicacanthis Cusiae extractum powder and 30 POVIDONE K 30 BP/USP 30, adds 2/3rds amount propylene glycol, ethanol and purified water mix homogeneously in 75 ℃ water-bath; Add emulsifying agents such as stearic acid, lanoline again after the propylene glycol mixing dissolving of artificial Calculus Bovis elder generation and remainder and in 77 ℃ water-bath, fully be dissolved into mixed solution, mix homogeneously; The solution of two parts mix homogeneously is mixed in 60 ℃ of water-baths, stir, packing is pressed into propellant, and bottling gets product.

Above-mentioned compound infantile is brought down a fever in the foam, and described materials of weight proportions is reasonable to be:

2 parts of 62.5 parts of artificial Calculus Boviss of acetaminophen

50 parts of 20.8 parts of propylene glycol of Rhizoma Et Radix Baphicacanthis Cusiae extractum powder

12.5 parts of 30 1.7 parts of stearic acid of 30 POVIDONE K 30 BP/USP

225 parts of 1 part of ethanol of lanoline

94.2 parts of purified water

Requirement according to the foam dosage form: should be evenly not stratified, in the lacuna holdup time long, and the efficacy of a drug is comparatively lasting, the ejection total amount should be not less than 85%, in order to reach above-mentioned requirements, we adopt o/w type Emulsion and thickening agent and freon as propellant.By analyzing and screening,, the adjuvant and the consumption that are suitable for have been determined through testing repeatedly, contrast, summing up with the use and the consumption thereof of orthogonal experiment to adjuvant.

The experiment that the present invention did

The quasi-factor design method in the orthogonal test is adopted in this experiment, and according to documents and materials and trial test result, we select 30 POVIDONE K 30 BP/USP 30, propylene glycol, stearic acid, lanoline, freon five factors for use, considers that simultaneously four levels adopt L ₁₆(4 ⁵) arrange orthogonal test to the bring down a fever influence of foam quality of compound infantile, found out the best ratio of each factor.

1, method and result

1.1 preparation technology: with acetaminophen, Rhizoma Et Radix Baphicacanthis Cusiae extractum powder and 30 POVIDONE K 30 BP/USP 30, ethanol, 2/3rds propylene glycol, the purified water mix homogeneously of measuring in 75 ℃ water-bath of recipe quantity; Add emulsifying agents such as stearic acid, lanoline again after the propylene glycol mixing dissolving of artificial Calculus Bovis elder generation and remainder and in 77 ℃ water-bath, fully be dissolved into mixed solution, mix homogeneously; The solution of two parts mix homogeneously is mixed in 60 ℃ of water-baths, stir, packing is pressed into propellant, and bottling gets product.

1.2 preparation process condition preferably sees Table 1 and table 2, table 3.After allotting liquid medicine filling, spray volume of foam (cm ³) and foam duration (min) and the ejection total amount (%) carry out comprehensive grading.Wherein hold speed time (min) medicinal liquid is sprayed into graduated cylinder, put 37 ℃ of observing in water-soluble.Calculate according to tripartite mask body situation.

Table 1 investigation factor and level

Level	Factor
						A (stearic acid dosage %)	B (propylene glycol consumption %)	C (polyvidone consumption %)	D (lanoline consumption %)	E (freon consumption %)
	??1	?1.8	?0	?0.34	?0.15						?25
??2						?2.5	?10	?0.29	?0.3	?30
	??3	?3.6	?15	?0.17	?0.1						?40
??4						?2.0	?20	?0.46	?0.2	?35

Table 2 Orthogonal Experiment and Design table

Table 3 analysis of variance table

Soruces of variation	Sum of deviation square	Degree of freedom	Variance	The F value
					??A	??2082.19	??3	??694.06	??2.62
??B	??2232.69	??3	??744.23	??2.80
					??C	??1630.69	??3	??543.56	??2.05
??D	??716.19	??3	??265.40
					??E	??3498.69	??3	??1166.23	??4.39

Interpretation of result his-and-hers watches 2, table 3 columns carry out intuitive analysis and variance analysis, and the result shows: optimised process is A ₂B ₂C ₁D ₄E ₃, promptly the propylene glycol consumption is 10%, and the polyvidone consumption is 0.34%, and stearic acid dosage is 2.5%, and the lanoline consumption is 0.2%, the freon consumption is that the resultant effect of 40% o'clock product is best.R _E＞R _B＞R _A＞R _C＞R _D，E＞B＞A＞C＞D。

Experiment adopts the comprehensive grading method that bring down a fever foam duration, ejection total amount, the ejection volume of foam of compound infantile carried out comprehensive grading, selects optimised process, experimentizes by optimised process, and made finished product is through observing and check.Stability better, meet quality standard.

Foam aerosol of the present invention has the advantages that activity is high and the holdup time is long, and its usefulness performance is faster than general peroral dosage form, suppository.The present invention and suppository show in pharmacology, toxicity contrast test: the present invention uses more convenient, and dosage is easy to grasp, and is applicable to that more children's uses.Zoopery proves, to noninfectious fever---inject the foreign preteins fever model, and infective fever---inject typhoid fever, paratyphoid fever fever model, significant refrigeration function is all arranged, after medication half an hour, each administration group body temperature all obviously descends, and compares with adstante febre body temperature, have significant difference, P＜below 0.05.Cooling effect can be kept 3 hours.Cooling effect shows certain dose-effect dependency.Analgesic experiment is the result show, the present invention has remarkable analgesic activity, can obviously improve the threshold of pain of mice, compare with suppository, have the difference of highly significant, in the time of 20 minutes 100mg/kg group P＜0.05,200mg/kg organizes P＜0.02, and 400mg/kg organizes P＜0.001, has good dose-effect relationship.The experimental result of writhing method is similar to hot plate method, and the body number of times of turning round of foam group obviously is less than the suppository group, and this explanation foam all has better analgesic activity to the pain due to physical property stimulation and the chemical irritation.After experiment showed, that this pharmaceutically dosage form of the present invention changes, do not influence its analgesic, analgesic activity.This dosage form toxic and side effects is little, is easy to tolerance.

The present invention shows that through clinical trial its effective percentage is better than suppository up to 94.5%.Antipyretic-antalgic there is good effect.

Compare with original suppository, the present invention is a kind of new pharmaceutical dosage form.The holdup time of the present invention in lacuna is long, and its usefulness performance is faster than peroral dosage form, suppository.It is more convenient that the present invention has use, and dosage is easy to grasp, and better efficacy more is applicable to the characteristics that children's uses.

The specific embodiment:

Embodiment 1, gets raw material by following weight proportion:

Acetaminophen 2250g artificial Calculus Bovis 75g

Rhizoma Et Radix Baphicacanthis Cusiae extractum powder 750g propylene glycol 1800g

30 POVIDONE K 30 BP/USP 30 61.2g stearic acid 450g

Lanoline 36g ethanol (95%) 8100g

Purified water 3391g

Preparation method is, gets acetyl aminophenol, Rhizoma Et Radix Baphicacanthis Cusiae extractum powder and 30 POVIDONE K 30 BP/USP 30 and mixes, and adds 1200g propylene glycol, ethanol (95%), purified water mix homogeneously in 75 ℃ water-bath again; Add emulsifying agents such as stearic acid, lanoline again after the propylene glycol mixing dissolving of artificial Calculus Bovis elder generation and remainder and in 77 ℃ water-bath, fully be dissolved into mixed solution, mix homogeneously; The solution of two parts mix homogeneously is mixed in 60 ℃ of water-baths, stir, packing is pressed into propellant, dresses up 1000 bottles, the compound infantile that the gets product foam of bringing down a fever.This product is a rectal application.Using method is: 1～2 time on the one.Use preceding first jolting even, propeller is placed on the valve, the promptly full propeller of pressing valve, foam inserts propeller the about 3cm of anus more gently, and foam is injected anus.Inject two envelope foams for using once amount (children's was 1 time on the one in to three years old, three to six years old 2 times on the one).

Claims (3)

1, the compound infantile foam of bringing down a fever is characterized in that it is to be made by the following weight proportion raw material:

2～3 parts of 60～65 parts of artificial Calculus Boviss of acetaminophen

40～55 parts of 20～22 parts of propylene glycol of Rhizoma Et Radix Baphicacanthis Cusiae extractum powder

8～20 parts of 30 1～5 parts of stearic acid of 30 POVIDONE K 30 BP/USP

200～250 parts of 1～5 part of ethanol of lanoline

90～120 parts of purified water

Preparation method is, gets acetaminophen, Rhizoma Et Radix Baphicacanthis Cusiae extractum powder and 30 POVIDONE K 30 BP/USP 30, adds 2/3rds amount propylene glycol, ethanol and purified water mix homogeneously in 75 ℃ water-bath; Add emulsifying agents such as stearic acid, lanoline again after the propylene glycol mixing dissolving of artificial Calculus Bovis elder generation and remainder and in 77 ℃ water-bath, fully be dissolved into mixed solution, mix homogeneously; The solution of two parts mix homogeneously is mixed in 60 ℃ of water-baths, stir, packing is pressed into propellant, and bottling gets product.

2, the compound infantile according to claim 1 foam of bringing down a fever is characterized in that described materials of weight proportions is:

2 parts of 62.5 parts of artificial Calculus Boviss of acetaminophen

50 parts of 20.8 parts of propylene glycol of Rhizoma Et Radix Baphicacanthis Cusiae extractum powder

12.5 parts of 30 1.7 parts of stearic acid of 30 POVIDONE K 30 BP/USP

225 parts of 1 part of ethanol of lanoline

94.2 parts of purified water

3, the compound infantile according to claim 1 and 2 foam of bringing down a fever is characterized in that described ethanol is the ethanol of concentration 95%.