CN1732908A - Borneol contained spray - Google Patents
Borneol contained spray Download PDFInfo
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- CN1732908A CN1732908A CN 200410070542 CN200410070542A CN1732908A CN 1732908 A CN1732908 A CN 1732908A CN 200410070542 CN200410070542 CN 200410070542 CN 200410070542 A CN200410070542 A CN 200410070542A CN 1732908 A CN1732908 A CN 1732908A
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Abstract
The invention provides a borneol contained spray wherein the medicinal solution contains 0.01-20 wt% of borneo camphor, 5-40 wt% of ethanol, natural or synthesized neutral fatty oil, asarum oil, sandalwood oil, galange oil, long pepper oil and other pharmacological active components.
Description
Technical field:
The invention belongs to medical technical field, relate to a kind of spray, particularly relate to the spray that contains Borneolum Syntheticum.
Background technology:
Borneolum Syntheticum is a kind of water white transparency or the crisp crystallization of white translucent lamellar, and faint scent is arranged, acrid in the mouth, cold, and have volatility.The Pharmacopoeia of the People's Republic of China (hereinafter to be referred as " Chinese pharmacopoeia) existing many editions recorded this product.Have suffering, hardship, be slightly cold and the characteristics of GUIXIN, spleen, lung meridian.And have a refreshment of having one's ideas straightened out, the function of clearing away heat to alleviate pain.Be used for the calentura coma, convulsion is fainted, apoplexy syncope due to accumulation of phlegm, stagnation of QI sudden syncope, attacked by pestiferous factors stupor, conjunctival congestion, aphtha, laryngopharynx swelling and pain, auditory meatus disease such as suppurate.
There are many Chinese patent medicines to add Borneolum Syntheticum at present as pharmacological active substance, Borneolum Syntheticum nasal drop (chief editor such as Ke Mingqing, hospital preparation, Hunan science tech publishing house are more typically arranged, Changsha, 1980:95), the chest stuffiness relieving aerosol (national drug standards WS3-B-2417-97).
Because Borneolum Syntheticum is almost insoluble in water, will use some special methods when preparing preparation, as using dissolve with ethanol, adopting PEG solid dispersions technique etc.In most cases, in order to prepare the homodisperse preparation that contains Borneolum Syntheticum, dissolving with an organic solvent often; Its another characteristics are, be used for the rapid onset of medicine needs when the state of an illness is urgent of some specified disease (as coronary heart disease, angina pectoris etc.), perhaps need the state of an illness of local onset (as oral ulcer, skin ulcer, rhinitis etc.), this has just required drug formulation easily.
Above-mentioned Borneolum Syntheticum nasal drop uses liquid paraffin to be solvent, because the toxicity of liquid paraffin is bigger, and can not biodegradation, the health hazard to human body after the prolonged application is bigger, and this product is rare on market.
Contain Borneolum Syntheticum Chinese patent medicine some be to occur with the form of tablet.Because the using dosage of Borneolum Syntheticum is less, sees on the microcosmic that tablet is a kind of heterogeneous dispersion, the uniformity of dosage units of preparation usually has problems; In addition, the volatility of Borneolum Syntheticum also can influence the chemical stability of medicament, although solve this problem by tablet coating sometimes, clearly, this has increased the production cycle and the cost of product.
Contain Borneolum Syntheticum Chinese patent medicine some be to occur with the form of pill.The interchangeable manufacturing production degree of pill is low, and the sanitary condition of product is relatively poor, and is far apart with the modernization of Chinese medicine target of current China.
Contain Borneolum Syntheticum Chinese patent medicine some be to occur with the form of drop pill.Drop pill is a kind of new form of administration, and applying solid dispersion formulations technology makes medicine have the characteristics of rapid onset.Regrettably, the granularity of drop pill is little, and body surface area is big, particularly when Borneolum Syntheticum concentration is higher, is easy to volatilize from drop pill, thereby influences stability of drug.Another unsurmountable shortcoming of drop pill is preparation technology's long flow path, and the production cycle is longer, and needs special production equipment, and this is that the pharmaceutical engineering technical staff is known.In addition, the above-mentioned Chinese patent medicine drop pill that contains Borneolum Syntheticum all needs to take several in use usually, even grain surplus in the of ten, because the particle diameter of drop pill is less, patient is divided dose and inconvenient, particularly all the more so for some gerontal patients in use.
There is the Chinese patent medicine that much contains Borneolum Syntheticum to be developed to aerosol in recent years and puts goods on the market, as the chest stuffiness relieving aerosol etc.The chest stuffiness relieving aerosol goes on the market for many years in China, and loaded China national drug standards (standard No. WS3-B-2417-97).Its prescription consists of Oleum Asari 23ml, Oleum Santali albi 70ml, Rhizoma Alpiniae Officinarum oil 32ml, Fructus Piperis Longi oil 15ml, Borneolum Syntheticum 22.5g.Its preparation method is with four kinds of volatile oil mixings, is heated to 40 ℃, adds the Borneolum Syntheticum of porphyrize, slight fever makes dissolving, adjusts total amount to 625ml with dehydrated alcohol, mixing, every bottle by containing volatile oil 2ml embedding in withstand voltage aerosol bottle, is pressed into propellant (dichlorodifluoromethane) 12g, promptly.It is reported that the chest stuffiness relieving aerosol is and the pure Chinese medicinal preparations that are used for allevating angina pectoris equally celebrated for their achievements such as SUXIAO JIUXIN WAN, FUFANG DANSHEN DIWAN.The characteristics of this class medicament are in the withstand voltage aerosol bottle of medicinal liquid is housed, to be pressed into propellant (as dichlorodifluoromethane).Self-evident, this class preparation usually except the ethanol that contains higher concentration (as in the chest stuffiness relieving aerosol except that propellant, ethanol content is up to about 77%, v/v) thus as outside the active constituents of medicine such as solvent dissolving Borneolum Syntheticum, owing to have the existence of propellant fluorochloroparaffins, this preparation is inevitably to the infringement of environment, says nothing of it to health effects.Another problem of aerosol is, owing to used high-pressure bottle, not only increased the cost of drug packing material, and the safety of aerosol high-pressure bottle also is very important problem.
Like this, the preparation that this class is contained Borneolum Syntheticum is made and is not contained propellant, has the ethanol of low concentration, the lower viscosity that is suitable for spraying, medication is convenient, and divided dose is accurate, have good stability, safe spray is very significant when producing, storing and transporting and using.That is to say, the Chinese patent medicine that this class is contained Borneolum Syntheticum is mixed with solution, pass through the effect of mechanical pump (as aerosol apparatus or nebulizer) power again, preparation with the medicinal liquid atomisation, such as the spray that contains Borneolum Syntheticum of making no fluorochloroparaffins propellant, contain the chest stuffiness relieving spray of pharmacological component Borneolum Syntheticum etc., just become this area scientific worker's goal in research.
In order to realize this goal, the inventor once attempted to prepare the spray that contains Borneolum Syntheticum, as using excipient such as ethanol, tween 80, water, though can make the solution that contains the higher concentration Borneolum Syntheticum, but, this solution stable unsatisfactory, volatilization loss is bigger in the storage process, and the first discharge rate difference is also bigger.Therefore thisly be the spray that contains Borneolum Syntheticum of solvent and be not suitable for pharmaceuticals industryization with water-pure system.
Prepare the spray that contains Borneolum Syntheticum and need consider two aspects: on the one hand, should use and can dissolve Borneolum Syntheticum, the solvent that can dissolve other active medicines (as volatile oil, plant extract, Chinese crude drug or chemical medicine) again is the excipient of spray; On the other hand, the viscosity of the solution of the spray of making should be lower, so that can successfully change into the medicinal liquid spray vaporific uniformly.Meet this two conditions, can adopt method, select for use short chain (as C as patent US5047230
2～C
4) alcohol, Polyethylene Glycol, C
2～C
8Polyhydroxy-alcohol, and short chain alcohol large usage quantity (even may reach 50～95%) can be by the spray spray that contains Borneolum Syntheticum of medication of pump thereby make.
But thing followed problem is Polyethylene Glycol or C
2～C
8The safety of polyhydroxy-alcohol and viscosity and unsatisfactory, and with the spray of the short chain alcohol with higher concentration (as ethanol) preparation, be stored in the medicinal liquid in the measuring room of holdable pump spray apparatus, it is reported, 30% volatilization can promptly be arranged in short period of storage, can carry away simultaneously and have volatile medicinal liquid, like this, after depositing a period of time, the dosage of first spray has only 70% approximately, this obviously is unsuitable for medicinal for the medicine that is used for the rapid onset of needs.
In addition, because alcoholic acid volatilization, cause that medicine concentrates even separates out, and may cause the valve of atomizing pump to block, thereby make the atomizing functions forfeiture of atomizing pump.
In addition, under the situation that oral cavity (particularly tongue) uses, higher concentration alcohol, particularly alcoholic acid use, also have a shortcoming, promptly the tongue mucosa is caused strong impulse, vasodilation, drug level in the blood is raise rapidly, and this might cause the untoward reaction of medicine source property at short notice.In addition, the pharmaceutical preparation that contains high concentration alcohol is to some patient and be not suitable for, as anemia of pregnant woman, alcohol dependence patient, liver or injury of kidney patient etc.And clearly, the safety in production, storage, transportation and use also has a significant impact to medicine to contain the preparation of high concentration alcohol.
Certainly, containing the alcohol of debita spissitudo, also is useful such as the ethanol that contains 5%～40% (v/v) to the hygiology stability of product, promptly can suppress growth of microorganism effectively.
For this reason, the purpose of this invention is to provide a kind of spray that contains Borneolum Syntheticum, its medicinal liquid has a kind of like this character, be that drug use is convenient, divided dose is accurate, be used for emergency case or need under the situation of the rapid onset of medicine at needs, even if medicine after storage after a while, the first spray amount of medicine still can reach the active medicine of required dosage (or design dosage).
The present invention also aims to provide a kind of spray that contains Borneolum Syntheticum, unlikely because its pure content is lower to agents area generation strong impulse, thus can not cause first spray that a large amount of drug absorption is just arranged, too high blood drug level of moment appears.
The present invention also aims to provide a kind of spray that contains Borneolum Syntheticum, this alcohol that contains that contains the spray of Borneolum Syntheticum is measured low, thereby be applicable to the patient that should not use alcohol formulations above-mentioned, and the safety of preparation in production, storage, transportation and use is better.
The present invention also aims to provide a kind of spray that contains Borneolum Syntheticum, its medicinal liquid is little to the zest of agents areas such as mucosa, and toxicity is low.
The present invention also aims to provide a kind of spray that contains Borneolum Syntheticum, the viscosity of its medicinal liquid is low, can be sprayed into vaporificly uniformly smoothly, and divided dose is accurate.
The present invention also aims to provide a kind of spray that contains Borneolum Syntheticum, can also be added with other active substances (as volatile oil, plant extract, Chinese crude drug or chemical medicine) in this spray, as the volatile oil in the above-mentioned the chest stuffiness relieving aerosol.
The inventor finds pleasantly surprisedly, uses that more a spot of ethanol and low viscous synthetic or natural fat are oily to contain the spray of Borneolum Syntheticum as the solvent preparation, can successfully realize the present invention, and the product that makes has good stable and sprayable performance.This is that prior art can not be led and teaches.
Summary of the invention:
The present invention is the spray that contains Borneolum Syntheticum, wherein can also add other pharmacological components, as Oleum Asari, Oleum Santali albi, Rhizoma Alpiniae Officinarum oil, Fructus Piperis Longi wet goods.
The Borneolum Syntheticum of indication of the present invention, can be synthetic borneol or natural Broneolum Syntheticum, common but do not have exhaustive different name to have: borneol, borneol, Blumeae preparatum Tabellae, BORNEOLUM SYNTHETICUM etc., and " " Borneolum Syntheticum " that Chinese pharmacopoeia version in 2000 is an one the 113rd page, all can be used as a part of the present invention, be referred to as Borneolum Syntheticum among the present invention.Because one of technical scheme of the present invention is Borneolum Syntheticum is made the described spray of goal of the invention, those skilled in the art are understood that easily, in some cases, Borneolum Syntheticum is to be present in the preparation as pharmaceutical necessities, so this class situation has been contained in the present invention simultaneously.
The Oleum Asari of indication of the present invention, Oleum Santali albi, Rhizoma Alpiniae Officinarum oil, four kinds of volatile oil of Fructus Piperis Longi oil can be directly to buy from the market.Four kinds of volatile oil and amount thereof also can be crude drug and the respective amount thereof that is equivalent to extract respective amount volatile oil.Oleum Asari, Oleum Santali albi, Rhizoma Alpiniae Officinarum oil, Fructus Piperis Longi oil are to get Herba Asari (" Chinese pharmacopoeia 2000 version one one the 185th page), Lignum Santali Albi (" Chinese pharmacopoeia 2000 version one one the 314th page), Rhizoma Alpiniae Officinarum (" Chinese pharmacopoeia 2000 version one one the 236th page), Fructus Piperis Longi (" Chinese pharmacopoeia 2000 version one one the 188th page), extract volatile oil respectively, and get through dehydration.The extracting method of various volatile oil does not limit, such as giving an example out but needn't be exhaustive the preparation of steam distillation, supercritical extraction arranged.Therefore as a part of the present invention, four kinds of volatile oil of indication of the present invention can also be to extract the medical material that is equivalent to respective amount volatile oil that obtains through certain method.
Because the technological difficulties that the present invention at first will solve are preparation Borneolum Syntheticum sprays.On this basis, can also in this spray that contains Borneolum Syntheticum, add one or more other pharmacological components, such as above-mentioned volatile oil.
According to the network document
Http:// jsinfo.39.net.cn/Professional/Drug/Herb/200004/ 701920000425.htm(999.com.cn) report, the proved recipe of being made up of Fructus Piperis Longi, Rhizoma Alpiniae Officinarum, Herba Asari, Borneolum Syntheticum four Chinese medicine can be used for the treatment toothache, and for this reason, it also is significant making spray with this four Chinese medicine.
The present invention is the spray that contains Borneolum Syntheticum, and this spray contains the medicinal liquid of pharmacological component by (1) and sprayer unit two parts that (2) are made up of hand spray pump and bottle are formed.Those skilled in the art are well known that, sprayer unit wherein is requisite as spray.Therefore technical characterictic of the present invention is medicinal liquid, with what doubt is not, this technical characterictic prolongs and sprayer unit, and term promptly of the present invention " spray " both can refer to the spraying system that medicinal liquid and sprayer unit are formed, and also can singly refer to medicinal liquid.
Should be noted that, because the present invention is an excipient with ethanol, neutral fat wet goods, therefore the material of sprayer unit of the present invention can be selected from one or more the combination in high density polyethylene (HDPE), polypropylene, metal (as aluminum), the glass etc., thereby can make medicament obtain better stability.
In addition, each spray amount of spray is generally 20～500mg, preferred 50～250mg, and these can be according to the medication needs, select to buy the manual pump (or claiming valve system) of suitable specification from the market and realize, as the quantitative atomizing pump of German Fei Fu company (Pfeiffer).
Like this, the present invention is a kind of spray that contains Borneolum Syntheticum, by weight percentage, contains 0.01～20% Borneolum Syntheticum in its medicinal liquid, 5～40% ethanol, synthetic or natural neutral fat oil.
Further, the present invention is the spray that contains Borneolum Syntheticum, by weight percentage, contain 0.05～20% Borneolum Syntheticum in its medicinal liquid, 0～5% the additives that are selected from correctives class, antioxidant class and viscosifier class, 5～40% ethanol and synthetic or natural neutral fat oil.
Preferably, the present invention is the spray that contains Borneolum Syntheticum, by weight percentage, contain 0.2～20% Borneolum Syntheticum in its medicinal liquid, 0～3% the additives that are selected from correctives class, antioxidant class and viscosifier class, the synthetic or natural fat of 10～30% ethanol and surplus is oily.
Perhaps further, the present invention is the spray that contains Borneolum Syntheticum, by weight percentage, contain 0.48～8% Borneolum Syntheticum in its medicinal liquid, 0.5～8.3% Oleum Asari, 0.7～11.5% Rhizoma Alpiniae Officinarum oil, 0.32～5.3% Fructus Piperis Longi oil, 0～5% the additives that are selected from correctives class, antioxidant class and viscosifier class, 10～30% ethanol, the synthetic or natural fat of surplus is oily.
Preferably, the present invention is the spray that contains Borneolum Syntheticum, by weight percentage, contain 0.96～4.8% Borneolum Syntheticum in its medicinal liquid, 1～5% Oleum Asari, 1.4～7% Rhizoma Alpiniae Officinarum oil, 0.63～3.2% Fructus Piperis Longi oil, 0～3% the additives that are selected from correctives class, antioxidant class and viscosifier class, 10～30% ethanol, the fatty oil of surplus.
Perhaps further, the present invention is the spray that contains Borneolum Syntheticum, by weight percentage, contain 0.48～8% Borneolum Syntheticum in its medicinal liquid, 0.5～8.3% Oleum Asari, 1.5～25% Oleum Santali albi, 0.7～11.5% Rhizoma Alpiniae Officinarum oil, 0.32～5.3% Fructus Piperis Longi oil, 0～5% the additives that are selected from correctives class, antioxidant class and viscosifier class, 10～30% ethanol, the fatty oil of surplus.
Preferably, the present invention is the spray that contains Borneolum Syntheticum, by weight percentage, contain 0.96～4.8% Borneolum Syntheticum in its medicinal liquid, 1～5% Oleum Asari, 3～15% Oleum Santali albi, 1.4～7% Rhizoma Alpiniae Officinarum oil, 0.63～3.2% Fructus Piperis Longi oil, 0～3% the additives that are selected from correctives class, antioxidant class and viscosifier class, 10～30% ethanol, the fatty oil of surplus.
In order to prepare the spray solution of homogeneous, realize that the used ethanol of the present invention should control water content, i.e. the used concentration of alcohol of the present invention should be greater than 95%, and preferably, the used ethanol of the present invention is dehydrated alcohol.
Realize that the used fatty oil of the present invention can be selected from natural or synthetic neutral fat oil.As select for use with medium chain C
8～C
12The fatty glyceride of satisfied fatty acid preparation is (as medium chain acid glycerol one ester, medium chain acid triglyceride, medium chain triglyceride, wherein the former two is referred to as medium chain acid glycerol part ester, English Medium Chain Partial Glycerides by name), more preferably available medium chain triglyceride (is called for short MCT, GTCC; European Pharmacopoeia name medium Chain Triglycerides; Japanese Pharmacopoeia name Caprylic/Capric Triglyceride).
Medium chain acid glycerol part ester can be selected the product I MWITORu of German SASOL company for use
742.
Medium chain triglyceride can be used the product MIGLYOL available from German CONDEA chemical company (CONDEA ChemieGmbH)
812 or MIGLYOL
810; Or available from the product LABRAFAC CC of French GATTEFOSSE company; Or available from the product A LDO of U.S. LONZA company
MCT.The product of these different brands is at sad (C
8) and capric acid (C
10) the ratio aspect difference is arranged slightly, as MIGLYOL
812 contain sad 50～65%, capric acid 30～45%MIGLYOL
810 contain sad 65～80%, capric acid 20～35%; LABRAFAC CC contains sad 50～80%, capric acid 20～50%; ALDO
MCT contains sad 65～80%, capric acid 20～35%.But they are basic identical aspect physicochemical properties such as acid number, saponification number, iodine number, hydroxyl value, viscosity, freezing point, moisture, and the difference of two kinds of fatty acid proportions can not produce significantly influence to preparation nature.
Realize that the used fatty oil of the present invention also can be selected from the natural fatty oil that contains a small amount of unsaturated fatty acid, as rapeseed oil, also can make with the fatty oil hydrogenation that contains a large amount of unsaturated fatty acids.
The present invention contains the medicament additives that also can add small quantities of usual in the spray of Borneolum Syntheticum.As the correctives class, thereby improve the product taste, as menthol, Oleum menthae, milk chocolate essence (as the BFL1227 type, International Flavors ﹠amp; Fragrances company product), sorbitol etc.; Perhaps antioxidant class, thus the product chemical stability improved, as to hydroxyl tert-butyl group methoxybenzene (BHA), toluene di-tert-butyl phenol (BHT) etc.; Perhaps viscosifier class, thus the viscosity of regulating medicinal liquid (is used) medicinal liquid in some cases and is obtained better result of use, as polyvinylpyrrolidone (PVP), hypromellose (HPMC) etc. to desired extent as local skin.
Preparation the present invention contains the spray of Borneolum Syntheticum, compositions such as Borneolum Syntheticum can be dissolved in the ethanol, add fatty oil, additives etc., make medicinal liquid dissolving evenly after, medicinal liquid filters with filter (as sintered glass filter, microporous filter membrane) in case of necessity, again with liquid medicine filling in the high density polyethylene (HDPE) spray bottle, screw hand spray pump (standard atomizing pump, 0.1ml, screw thread 18/415, Germany Pfeiffer company China portion), promptly.
Above preparation method is not limited by the preparation process.After being dissolved in Borneolum Syntheticum in the ethanol, other oiliness pharmacological active substancies and fatty oil dissolving are mixed the two again.Dosing temperature for another example is feasible in 10～60 ℃ scope, is more preferably at 20～30 ℃.In addition, can also select the hand spray pump and the spray bottle of suitable specification, thereby reach the medication effect of most convenient according to the using dosage of medicine, drug level, medicinal liquid viscosity, every discharge rate etc. in the medicinal liquid.These adjustment are that those of ordinary skills are readily appreciated that.
The product of the spray that contains Borneolum Syntheticum of the present invention's preparation, can investigate its pharmaceutics character by the following method:
1. spraying uniformity: the horizontal direction spraying, observe spray discharge pattern and uniformity thereof.
2. medicinal liquid volatile quantity: spray bottle and atomizing pump that the spray of medicinal liquid will be housed screw, and keep sealing state, place 3 months in 40 ℃ calorstat, take by weighing the weight of spray before and after placing, and are calculated as follows the medicinal liquid volatile quantity.10 bottles of replications are asked the calculation meansigma methods.
In the formula
*Bottle heavily be the average weight (n=10) of the sprayer unit formed by spray bottle and atomizing pump.
3. the 1st discharge rate difference: get the spray that contains Borneolum Syntheticum, spray after 10 times, place the room temperature place to place 7 days, measured in the 7th day.Precision takes by weighing the 1st spray weight, sprays 10 times again, and precision takes by weighing 10 times gross weight, calculates every spray average weight; Be calculated as follows the 1st discharge rate diversity factor.10 bottles of replications are asked the calculation meansigma methods.
4. maximum discharge rate difference: get the spray that contains Borneolum Syntheticum, spray 10 times, remove, spray 10 times, precision takes by weighing the gross weight of each weight and 10 times, calculates every spray average weight again, be calculated as follows the discharge rate difference of single, thereby try to achieve the maximum discharge rate difference in the spraying 10 times.
5. Borneolum Syntheticum relative concentration: spray bottle and atomizing pump that the spray of medicinal liquid will be housed screw, keep sealing state, in 40 ℃ calorstat, placed 3 months, by " the method under [assay] in the Chinese pharmacopoeia version in 2000 one the 113rd page " Borneolum Syntheticum ", 0 month and the Borneolum Syntheticum concentration in March in the medicinal liquid of mensuration spray, with 0 month concentration was 100%, and the relative percent of Borneolum Syntheticum concentration in the medicinal liquid is the Borneolum Syntheticum relative concentration of setting-out during March when calculating March.Promptly as shown in the formula calculating:
Because the present invention contains fatty oil in the spray of Borneolum Syntheticum to skin and mucosa nonirritant, even eye also has good tolerability to this fatty oil, and the pure content in the product is low, so the toxicity of product is low, safety good.
By spray of the present invention, its viscosity is low, and volatility is low, and spraying is even, and divided dose is accurate, has good stability.The first spray amount of medicine can reach the active medicine of design dosage more than 90%.It is low to contain the alcohol amount, is applicable to the patient that some should not use alcohol formulations, and the safety of preparation in production and storage is good.Thereby realized the present invention.
The specific embodiment:
The invention provides a kind of spray that contains Borneolum Syntheticum, wherein can also contain other pharmaceutically-active ingredients of Rhizoma Alpiniae Officinarum wet goods.Below be described in further detail the present invention by specific embodiment, but and unrestricted the present invention.
Embodiment 1
Prescription:
Borneolum Syntheticum 20g
Dehydrated alcohol 20g
LABRAFAC CC 59g
Oleum menthae 1g
Preparation method: get Borneolum Syntheticum, use anhydrous alcohol solution, add LABRAFAC CC and Oleum menthae, stir, filter, divide to install in the aerosol container, screw atomizing pump, promptly with exsiccant G6 sintered glass filter.
Embodiment 2
Prescription:
Borneolum Syntheticum 10g
Dehydrated alcohol 40g
LABRAFAC CC 40g
IMWITOR 742 8g
Oleum menthae 1g
Milk chocolate essence 1g
Preparation method: at room temperature, get Borneolum Syntheticum, use anhydrous alcohol solution, add LABRAFAC CC, IMWITOR 742, Oleum menthae and milk chocolate essence, stirring and dissolving divides to install in the aerosol container, screws the hand spray pump, promptly.
Embodiment 3
Prescription:
Borneolum Syntheticum 0.01g
95% ethanol 5g
LABRAFAC CC 94g
Menthol 0.5g
PVP(K30) 0.5g
Preparation method: get PVP and be dissolved in 95% ethanol, add Borneolum Syntheticum and menthol, make dissolving, add LABRAFAC CC, stirring and dissolving divides to install in the aerosol container, screws the hand spray pump, promptly.
Embodiment 4
Prescription:
Borneolum Syntheticum 8g
Oleum Asari 8.3g
Rhizoma Alpiniae Officinarum oil 11.5g
Fructus Piperis Longi oil 5.3g
Dehydrated alcohol 10g
LABRAFAC CC 56g
Oleum menthae 0.88g
Toluene di-tert-butyl phenol 0.02g
Preparation method: get Borneolum Syntheticum, use anhydrous alcohol solution, add LABRAFAC CC, mix homogeneously adds other compositions in the prescription, stirring and dissolving, and with the microporous filter membrane vacuumizing filtration of 0.45 μ m, install in the aerosol container filtrate branch, screws the hand spray pump, promptly.
Embodiment 5
Prescription:
Borneolum Syntheticum 0.48g
Oleum Asari 0.5g
Rhizoma Alpiniae Officinarum oil 0.7g
Fructus Piperis Longi oil 0.32g
95% ethanol 30g
Sorbitol 5g
LABRAFAC CC 63g
Preparation method: get Borneolum Syntheticum and sorbitol, use dissolve with ethanol, add LABRAFAC CC, mix homogeneously adds other compositions in the prescription, and stirring and dissolving divides to install in the aerosol container, screws the hand spray pump, promptly.
Embodiment 6
Prescription:
Borneolum Syntheticum 1.6g
Oleum Asari 1.65g
Rhizoma Alpiniae Officinarum oil 2.3g
Fructus Piperis Longi oil 1.05g
98% ethanol 20g
LABRAFAC CC 71g
Oleum menthae 1g
Milk chocolate essence 1.4g
Preparation method: get Borneolum Syntheticum, use 98% dissolve with ethanol, add LABRAFAC CC, mix homogeneously adds other compositions in the prescription, and stirring and dissolving divides to install in the aerosol container, screws the hand spray pump, promptly.
Embodiment 7
Prescription:
Borneolum Syntheticum 8g
Oleum Asari 8.3g
Oleum Santali albi 25g
Rhizoma Alpiniae Officinarum oil 11.5g
Fructus Piperis Longi oil 5.3g
Dehydrated alcohol 10g
LABRAFAC CC 31g
Oleum menthae 0.8g
Toluene di-tert-butyl phenol 0.1g
Preparation method: get Borneolum Syntheticum, use anhydrous alcohol solution, add LABRAFAC CC, mix homogeneously adds other compositions in the prescription, and stirring and dissolving is filtered with exsiccant G6 sintered glass filter, and install in the aerosol container filtrate branch, screws atomizing pump, promptly.
Embodiment 8
Prescription:
Borneolum Syntheticum 0.48g
Oleum Asari 0.5g
Oleum Santali albi 1.5g
Rhizoma Alpiniae Officinarum oil 0.7g
Fructus Piperis Longi oil 0.32g
Dehydrated alcohol 30g
Rapeseed oil 40g
IMWITOR 742 25.5g
Oleum menthae 1g
Toluene di-tert-butyl phenol 0.02g
Preparation method: get Borneolum Syntheticum, use anhydrous alcohol solution, add rapeseed oil and IMWITOR 742, mix homogeneously adds other compositions in the prescription, and stirring and dissolving divides to install in the aerosol container, screws the hand spray pump, promptly.
Embodiment 9
Prescription:
Borneolum Syntheticum 1.6g
Oleum Asari 1.65g
Oleum Santali albi 5g
Rhizoma Alpiniae Officinarum oil 2.3g
Fructus Piperis Longi oil 1.05g
Dehydrated alcohol 20g
LABRAFAC CC 67g
Oleum menthae 0.8g
Milk chocolate essence 0.6g
Preparation method: get Borneolum Syntheticum, use anhydrous alcohol solution, add LABRAFAC CC, mix homogeneously adds other compositions in the prescription, and stirring and dissolving divides to install in the aerosol container, screws the hand spray pump, promptly.
Comparative examples 1 is homemade to be the spray that contains Borneolum Syntheticum of carrier with alcohol-water system.
Prescription:
Borneolum Syntheticum 10g
98% ethanol 26g
Tween 80 4g
1,2-propylene glycol 40g
Water 20g
Preparation method: get Borneolum Syntheticum, use 98% dissolve with ethanol, add tween 80 and 1, the 2-propylene glycol, mix homogeneously slowly adds the water of recipe quantity under the stirring, left standstill 2 hours, filters, and the medicinal liquid branch is installed in the aerosol container, screws the hand spray pump, promptly.
The preparation of comparative examples 2 referenced patent US5047230 methods contains the spray of Borneolum Syntheticum.
Prescription:
Borneolum Syntheticum 10g
98% ethanol 75g
Propylene glycol 15g
Preparation method: get Borneolum Syntheticum, use 98% dissolve with ethanol, add propylene glycol, mix homogeneously filters, and the medicinal liquid branch is installed in the aerosol container, screws the hand spray pump, promptly.
Experimental example 1
Investigate spraying uniformity, medicinal liquid volatile quantity, the 1st discharge rate difference, maximum discharge rate difference, the Borneolum Syntheticum relative concentration of 9 embodiment samples and 2 comparative examples samples according to preceding method.The results are shown in Table 1.
Table 1 sample is investigated the result
| Sample | The spraying uniformity | The medicinal liquid volatile quantity | The 1st discharge rate difference | Maximum discharge rate difference | The Borneolum Syntheticum relative concentration |
| Embodiment 1 | Spraying is even, and droplet is tiny | -0.86％ | 94.1％ | 4.1％ | - |
| Embodiment 2 | Spraying is even, and droplet is tiny | 1.03％ | 93.3％ | 3.5％ | 99.1％ |
| Embodiment 3 | Spraying is even, and droplet is tiny | 0.77％ | 95.7％ | 3.2％ | - |
| Embodiment 4 | Spraying is even, and droplet is tiny | 0.94％ | 95.1％ | 5.4％ | - |
| Embodiment 5 | Spraying is even, and droplet is tiny | 1.17％ | 94.3％ | 5.0％ | - |
| Embodiment 6 | Spraying is even, and droplet is tiny | -1.16％ | 95.0％ | 2.7％ | - |
| Embodiment 7 | Spraying is even, and droplet is tiny | -0.61％ | 97.1％ | 5.5％ | - |
| Embodiment 8 | Spraying is even, and droplet is tiny | 0.84％ | 93.5％ | 4.8％ | - |
| Embodiment 9 | Spraying is even, and droplet is tiny | 0.35％ | 96.4％ | 4.6％ | - |
| Comparative examples 1 | Spraying is even, and droplet is tiny | 4.36％ | 88.1％ | 5.8％ | 95.4％ |
| Comparative examples 2 | Spraying is even, and droplet is tiny | 5.15％ | 76.3％ | 4.5％ | 96.1％ |
From the measurement result of embodiment as seen, aerosol spray of the present invention is even, droplet is tiny, at polyethylene is to preserve in the sprayer unit formed of the spray bottle of material and atomizing pump, it is good to place after 3 months product stability in 40 ℃ the calorstat, first discharge rate and every spray average magnitude are approaching, and maximum discharge rate difference is little, and divided dose is accurate.But the sample that with alcohol-water system is the spray of carrier and the preparation of referenced patent US5047230 method is all can not be satisfactory aspect the stability and the first discharge rate difference.
Experimental example 2
The medicinal liquid of embodiment 1 is packed in the spray bottle, and every bottle of 25ml (30ml spray bottle) sprays with the atomizing pump of 0.05ml, 0.1ml, 0.15ml, 0.2ml respectively, the uniformity of relatively spraying and maximum discharge rate difference.The results are shown in Table 2.
The investigation result of table 2 different size atomizing pump
| Sample | The spraying uniformity | Maximum discharge rate difference |
| 0.05ml pump | Spraying is solid cone shaped, and droplet is evenly distributed, and drop is tiny | 5.8％ |
| 0.10ml pump | Spraying is solid cone shaped, and droplet is evenly distributed, and drop is tiny | 3.3％ |
| 0.15ml pump | Spraying is solid cone shaped, and droplet is evenly distributed, and drop is tiny | 3.7％ |
| 0.20ml pump | Spraying is solid cone shaped, and droplet is evenly distributed, and drop is tiny | 4.1％ |
By contrast, the viscosity of the medicinal liquid of embodiment 1 is higher, but from the investigation result of last table as seen, spray of the present invention all can obtain uniform spray effect with the atomizing pump spraying of different size, and maximum discharge rate difference is basically identical also, divided dose is accurate, thereby has realized the present invention.
Although the present invention has carried out description to a certain degree, significantly, under the condition that does not break away from the spirit and scope of the present invention, can carry out the variation of component condition etc.Be appreciated that to the invention is not restricted to described embodiment, and belong to the scope of claim, it comprises the replacement that is equal to of described each factor.
Claims (10)
1. a spray is characterized in that, by weight percentage, contains 0.01～20% Borneolum Syntheticum in its medicinal liquid, 5～40% ethanol, synthetic or natural neutral fatty oil.
2. by the spray of claim 1, it is characterized in that, by weight percentage, contain 0.05～20% Borneolum Syntheticum in its medicinal liquid, 5～40% ethanol, 0～5% the additives that are selected from correctives class, antioxidant class and viscosifier class, fatty oil.
3. by the spray of claim 2, it is characterized in that, by weight percentage, contain 0.2～20% Borneolum Syntheticum in its medicinal liquid, 10～30% ethanol, 0～3% the additives that are selected from correctives class, antioxidant class and viscosifier class, the fatty oil of surplus.
4. press the spray of claim 1, it is characterized in that, by weight percentage, contain 0.48～8% Borneolum Syntheticum, 0.5～8.3% Oleum Asari in its medicinal liquid, 0.7～11.5% Rhizoma Alpiniae Officinarum oil, 0.32～5.3% Fructus Piperis Longi oil, 0～5% the additives that are selected from correctives class, antioxidant class and viscosifier class, 10～30% ethanol, the fatty oil of surplus.
5. press the spray of claim 4, it is characterized in that, by weight percentage, contain 0.96～4.8% Borneolum Syntheticum in its medicinal liquid, 1～5% Oleum Asari, 1.4～7% Rhizoma Alpiniae Officinarum oil, 0.63～3.2% Fructus Piperis Longi oil, 0～3% the additives that are selected from correctives class, antioxidant class and viscosifier class, 10～30% ethanol, the fatty oil of surplus.
6. press the spray of claim 1, it is characterized in that, by weight percentage, contain 0.48～8% Borneolum Syntheticum in its medicinal liquid, 0.5～8.3% Oleum Asari, 1.5～25% Oleum Santali albi, 0.7～11.5% Rhizoma Alpiniae Officinarum oil, 0.32～5.3% Fructus Piperis Longi oil, 0～5% the additives that are selected from correctives class, antioxidant class and viscosifier class, 10～30% ethanol, the fatty oil of surplus.
7. press the spray of claim 6, it is characterized in that, by weight percentage, contain 0.96～4.8% Borneolum Syntheticum in its medicinal liquid, 1～5% Oleum Asari, 3～15% Oleum Santali albi, 1.4～7% Rhizoma Alpiniae Officinarum oil, 0.63～3.2% Fructus Piperis Longi oil, 0～3% the additives that are selected from correctives class, antioxidant class and viscosifier class, 10～30% ethanol, the fatty oil of surplus.
8. by any one spray in the claim 1～7, wherein said fatty oil is selected from saturated natural fat oil and C
8～C
12The mixture of one or more in the fatty glyceride.
9. by the spray in the claim 8, wherein said saturated natural fat oil is rapeseed oil.
10. by the spray in the claim 8, wherein said C
8～C
12Fatty glyceride is C
8～C
12MCT Oil.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410070542 CN1732908A (en) | 2004-08-09 | 2004-08-09 | Borneol contained spray |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410070542 CN1732908A (en) | 2004-08-09 | 2004-08-09 | Borneol contained spray |
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| Publication Number | Publication Date |
|---|---|
| CN1732908A true CN1732908A (en) | 2006-02-15 |
Family
ID=36075664
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200410070542 Pending CN1732908A (en) | 2004-08-09 | 2004-08-09 | Borneol contained spray |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103518715A (en) * | 2013-11-05 | 2014-01-22 | 华中农业大学 | Brown scatopsidae trapping agent |
| CN104323992A (en) * | 2014-11-09 | 2015-02-04 | 常州迪力卫生材料有限公司 | Sodium alginate spray and production process thereof |
| CN106361785A (en) * | 2016-08-30 | 2017-02-01 | 杭州苏泊尔南洋药业有限公司 | Sandalwood oil extract and application thereof |
| CN110075239A (en) * | 2019-05-28 | 2019-08-02 | 沈阳药科大学 | Nanoemulsions and its preparation method and application |
-
2004
- 2004-08-09 CN CN 200410070542 patent/CN1732908A/en active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103518715A (en) * | 2013-11-05 | 2014-01-22 | 华中农业大学 | Brown scatopsidae trapping agent |
| CN103518715B (en) * | 2013-11-05 | 2015-07-08 | 华中农业大学 | Brown scatopsidae trapping agent |
| CN104323992A (en) * | 2014-11-09 | 2015-02-04 | 常州迪力卫生材料有限公司 | Sodium alginate spray and production process thereof |
| CN106361785A (en) * | 2016-08-30 | 2017-02-01 | 杭州苏泊尔南洋药业有限公司 | Sandalwood oil extract and application thereof |
| CN110075239A (en) * | 2019-05-28 | 2019-08-02 | 沈阳药科大学 | Nanoemulsions and its preparation method and application |
| CN110075239B (en) * | 2019-05-28 | 2021-09-03 | 沈阳药科大学 | Nano emulsion and preparation method and application thereof |
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