CN100471489C - Soft capsule containing common lamiophlomis root extract - Google Patents

Abstract

The present invention provides soft capsule of common lamiophlomis root extract as one new type of common lamiophlomis preparation form. The common lamiophlomis root soft capsule has inclusion containing common lamiophlomis root extract in 20-70 wt% as well as matrix, liquid paraffin and suspending agent in the weight ratio between matrix and liquid paraffin of 1 to 0.05-5. Compared with marketable similar products, the present invention has higher stability and treating effect.

Description

The soft capsule that contains Radix Lamiophlomidis Rotatae extract

Technical field

The present invention relates to a kind of medicinal soft capsule preparation that contains Radix Lamiophlomidis Rotatae extract, it can significantly strengthen the beneficial effect of Radix Lamiophlomidis Rotatae.

Background technology

Radix Lamiophlomidis Rotatae Lamiophlomis rotata (Benth.) Kudo is a Labiatae Radix Lamiophlomidis Rotatae platymiscium, its medical material is withered, gas is stench, be Tibetan, illiteracy, Naxi's medical herbs commonly used among the people, clinically be mainly used in diseases such as edge of a knife pain behind the surgical operation, hemorrhage, exogenous injury, muscles and bones are sprained, rheumatic arthralgia.

The Radix Lamiophlomidis Rotatae dosage form of clinical practice at present mainly is used as medicine with the direct pulverizing of medical material or the extract drying and crushing provides medicinal with capsule, tablet or particulate form, for example Radix Lamiophlomidis Rotatae capsule and Radix Lamiophlomidis Rotatae sheet.But for many years production and clinical practice prove that existing Radix Lamiophlomidis Rotatae hard capsule and Radix Lamiophlomidis Rotatae sheet exist certain defective.For example, bioavailability is low; The useful life is short, phenomenons such as the content deliquescence easily takes place long-term storage, the in bulk that hardens; And affected by environment in actual use big, often promptly inefficacy or character are defective before the deadline; The smell is awful for tablet, compliance difference of pain patients or the like.

Among numerous peroral dosage forms, soft capsule have bioavailability height, good airproof performance, content accurately, good looking appearance, cover characteristics such as bad smell.As everyone knows, the physicochemical property of Radix Lamiophlomidis Rotatae extract makes it to be not easy to make very much soft capsule, though have relevant instruction is arranged in the relevant patented technology.But the inventor finds through the research back, Radix Lamiophlomidis Rotatae is made soft capsule, though dosage form has improved, but need overcome a lot of difficulties, for example disintegrate becomes and material migration, effective ingredient generation sedimentation and content composition seepage equistability problem takes place in defective, the capsule in soft capsule storage period of prior art.To those skilled in the art, these problems are difficult to expect.Up to now, in view of the problem that occurs in the complexity of Radix Lamiophlomidis Rotatae physicochemical property and the clinical practice thereof, also have no talent and the beneficial effect of the soft capsule that comprises Radix Lamiophlomidis Rotatae is provided the prediction of science.

Therefore, this area presses for the Radix Lamiophlomidis Rotatae oral Pharmaceutical dosage forms that exploitation makes new advances, and said preparation should be reduced to bottom line with its negative effect when effectively improving product stability.This pharmaceutical dosage form can improve patient's treatment compliance, and must be safe.

Summary of the invention

The invention provides the soft capsule of Radix Lamiophlomidis Rotatae, it can significantly strengthen the beneficial effect of Radix Lamiophlomidis Rotatae, than present commercially available prod remarkable stability and treatment advantage is arranged.Simultaneously, the invention provides a kind of selection, it provides a kind of new safety product as the substituting of prior art, and this dosage form will be the approval that the doctor recommends to use and obtain doctor and patient.

The object of the present invention is to provide a kind of Duyiwei soft capsule pharmaceutical preparation, the soft capsule preparation that particularly contains Radix Lamiophlomidis Rotatae, it has overcome the defective of existing Radix Lamiophlomidis Rotatae oral formulations, and overcome defective, the interior problem that material migration, effective ingredient sedimentation and content composition seepage equistability difference take place of capsule of disintegrate that soft capsule usually occurs, and strengthened the beneficial effect of Radix Lamiophlomidis Rotatae.

The invention provides Duyiwei soft capsule, it is characterized in that this soft capsule is made up of content and capsule material, wherein the content of this soft capsule contains 20～70% Radix Lamiophlomidis Rotatae extract at least, substrate, liquid Paraffin and suspending agent, the weight ratio of described substrate and liquid Paraffin is 1:0.05～5, is preferably 1:0.05～1.

The content of above-mentioned Duyiwei soft capsule preferably contains Radix Lamiophlomidis Rotatae extract 30%～55%, substrate 15%～65%, the suspending agent of liquid Paraffin 1%～40% and surplus.(more preferably containing Radix Lamiophlomidis Rotatae extract 35%～50%, substrate 20%～55%, liquid Paraffin 2%～25%, suspending agent 5～15%)

Above percentage ratio is weight percentage.

The substrate of above-mentioned Duyiwei soft capsule generally can be vegetable oil (comprising its derivant) and/or refined oil, preferably vegetable oil; Described vegetable oil is one or more mixture in Oleum Sesami, Oleum Arachidis hypogaeae semen, Semen Maydis oil, olive oil, Oleum Helianthi, soybean oil, salad oil, Oleum Gossypii semen, the Oleum Brassicae campestris, is preferably one or more mixture in soybean oil, Semen Maydis oil, Oleum Sesami or the salad oil.

Described suspending agent is selected from various waxes, its derivant of hydrogenated vegetable oil, stearic acid or its salt, various tristerins, fatty acid or its salt or its ester, the cocos nucifera oil ester, various fatty glycerides, the cocoa ester, and/or phospholipid, for example: Cera Flava, Cera Flava, white beeswax, insect wax, paraffin (also being hard paraffin), ceresine, hydrogenated palm oil, hydrogenation silk floss oil, cocoa ester, Myrij, aluminium stearate, glyceryl monostearate, fatty acid ester, the cocos nucifera oil ester, semi-synthetic cocos nucifera oil ester, fatty glyceride, semi-synthetic fatty acid glyceride, mixed fatty glycerides, fabaceous lecithin, lecithin, cephalin; Arbitrary or its combination in preferred Cera Flava, Cera Flava, hydrogenated palm oil, hydrogenation silk floss oil, tristerin, glyceryl monostearate, fatty glyceride, mixed fatty glycerides and soybean phospholipid, the lecithin; More preferably arbitrary or its combination in Cera Flava, hydrogenated palm oil, glyceryl monostearate and the soybean phospholipid.

In Duyiwei soft capsule content of the present invention, liquid paraffin accounts for 5～85% of substrate weight can reach beneficial effect of the present invention and purpose.

In a preferred embodiment of the invention, described Duyiwei soft capsule, its content preferably contains Radix Lamiophlomidis Rotatae extract 0.25g, vegetable oil substrate 0.22g, liquid Paraffin 0.03g, suspending agent 0.05g.

Described Radix Lamiophlomidis Rotatae extract can be prepared according to the step method under the Radix Lamiophlomidis Rotatae medicinal material extract item in the Radix Lamiophlomidis Rotatae capsule in the version pharmacopeia in 2000, is for example made by following method: get the Radix Lamiophlomidis Rotatae medical material, pulverize, decoct with water, decocting liquid filters, and filtrate concentrates after drying, pulverize, promptly.Method for optimizing is: get the Radix Lamiophlomidis Rotatae medical material, pulverize, decoct with water 3 times, each 1 hour, collecting decoction filtered, and it is 1.30 clear paste that filtrate is condensed into relative density, and drying is pulverized and promptly got Radix Lamiophlomidis Rotatae extract.

The present invention also provides a kind of method for preparing above-mentioned Duyiwei soft capsule, comprising:

(1). get Radix Lamiophlomidis Rotatae extract, pulverizing becomes 80 order fine powders at least.

(2). get vegetable oil and liquid paraffin, add suspending agent, heating makes the suspending agent fusion, stirs, and adds above-mentioned Radix Lamiophlomidis Rotatae extract, cools to about 40 (30～50 degrees centigrade), stirs once more, crosses colloid mill, is pressed into soft capsule.

Test is found, different types of suspending agent fusing point difference when using multiple suspending agent at the same time, could guarantee that whole solution is in complete molten condition in the time of temperature must being increased to the highest suspending agent of fusing point; And some suspending agent is to the high temperature instability, for example: phospholipid; So we have more optimized preparation technology on the basis of above-mentioned test, promptly guarantee the uniformity of whole solution, increased the stability of phospholipid in the solution again.

Optimize following technology:

1) get Radix Lamiophlomidis Rotatae extract, pulverizing becomes 80 order fine powders at least.

2) get vegetable oil and liquid paraffin, add the part suspending agent, this part suspending agent is Cera Flava and/or hydrogenated palm oil and/or glyceryl monostearate, and heating makes its fusion, adds above-mentioned Radix Lamiophlomidis Rotatae extract, stir, cool to 40 degree (30～50 degree), add remaining suspending agent again, this remaining suspending agent is soybean phospholipid and/or lecithin, cross colloid mill after stirring once more, be pressed into soft capsule.

Wherein above-mentioned Radix Lamiophlomidis Rotatae extract is the water extract of Radix Lamiophlomidis Rotatae medical material, preferably through water carry, make with extra care, dried Powdered solids.

It can be single-matrixes such as vegetable oil, Polyethylene Glycol that prior art is instructed the substrate of our soft capsule, adds the content that suspending agent or lubricant etc. are formed soft capsule in addition.With regard to simple vegetable oil substrate, the character of therapeutic component is most important to the quality influence of soft capsule finished product in the content, mainly has following problem:

1. prolonged disintegration, often disintegrate before the deadline defective (above 60 minutes);

2. leakage of oil;

3. content layering

The problems referred to above, people such as Peng Zhicong just once reported in 2004, but also how we overcome the existing above-mentioned all problems of Duyiwei soft capsule preparation without any teach literature up to now.The Li Tongtong of Tianjin Central Pharmaceutical Co., Ltd once discussed " the soft capsule oil impregnate problem that improvement contains Chinese medicine extract " as far back as 1999; The people such as Ma Xu of China Medicine University's pharmaceutical preparation institute studied soft capsule prolonged disintegration phenomenon influence factor in 2003; The inventor tests according to wherein cited measure, though a large amount of oil leakage phenomenon makes moderate progress, still has to occur leakage of oil on a small quantity, and along with the prolongation meeting of standing time is constantly found; Especially the phenomenon of prolonged disintegration is not obviously improved, and the existence of this phenomenon has caused this advantage dosage form of soft capsule can't increase the purpose that the medicine stripping reaches the raising drug effect.This is relevant with Radix Lamiophlomidis Rotatae extract its own particularity matter.

Through a large amount of creationary exploratory experiments, the inventor finds, adds an amount of liquid Paraffin in the soft capsule, can specifically, unexpectedly solve the existing problem of Duyiwei soft capsule.Therefore, the soft capsule that contains liquid Paraffin has constituted pith of the present invention.

The medicine that liquid Paraffin records as 2005 editions pharmacopeia, be described to a kind ofly can cause the diarrheal active component, and be applied in clinically in a large number widely as national medical care insurance kind, its usage and dosage must reach each 10～30 milliliters, just can bring into play the effect that becomes cathartic.As everyone knows, the extensive application of liquid Paraffin can cause diarrhoea.The inventor is fully realizing under this prerequisite, has carried out a series of consumption test, guarantees the safety of Duyiwei soft capsule of the present invention.

As the improvement of dosage form, the present invention finds through overtesting, selects suitable substrate and suitable proportioning, makes up with effective ingredient then, can obtain the remarkable enhanced soft capsule of stability.For choice of base, the present invention has done a large amount of screening experiment.

At first, if the consumption of vegetable oil in the sample is decided to be 10, as follows to the consumption screening of liquid Paraffin:

Prescription one: vegetable oil 10 (that is, the Duyiwei soft capsule that prior art makes, its liquid Paraffin are 0%);

Prescription two: vegetable oil: liquid Paraffin=9:1 (liquid Paraffin account for substrate total amount 10%);

Prescription three: vegetable oil: liquid Paraffin=7:3 (liquid Paraffin account for substrate total amount 30%);

Prescription four: vegetable oil: liquid Paraffin=5:5 (liquid Paraffin account for substrate total amount 50%);

Prescription five: vegetable oil: liquid Paraffin=2:8 (liquid Paraffin account for substrate total amount 80%);

Prescription six: liquid Paraffin=10 (liquid Paraffin account for substrate total amount 100%)

Product is taken 3 times every day, each 3.Each dose (relative density of liquid Paraffin is calculated according to 0.85) is calculated in the conversion back:

Write out a prescription one: 0 milliliter;

Prescription two: each 0.25*10%*3/0.85=0.09 milliliter, every day, consumption was 0.27 milliliter;

Prescription three: each 0.25*30%*3/0.85=0.26 milliliter, every day, consumption was 0.79 milliliter;

Prescription four: each 0.25*50%*3/0.85=0.44 milliliter, every day, consumption was 1.33 milliliters;

Prescription five: each 0.25*80%*3/0.85=0.71 milliliter, every day, consumption was 2.12 milliliters;

Prescription six: each 0.25*100%*3/0.85=0.89 milliliter, every day, consumption was 2.65 milliliters;

Safety testing:

Give the content of the above-mentioned prescription of mouse stomach, dosage gives 0.3g (being equivalent to more than 10 times of ordinary people's single oral dose) according to per kilogram of body weight, observes the defecation situation of mice.Wherein have only prescription six the rare partially phenomenon of slight stool to occur, all the other 5 prescription mice defecations are all normal.Above-mentioned test fully proves the security reliability of the first five prescription clinical practice of this product.

Slaking test: assay method is stipulated down referring to 2005 editions two relevant appendix items of Chinese Pharmacopoeia.

1, accelerated test:

Experimental condition: with packaged sample, be placed on 37 ℃ of temperature, in the climatic chamber of relative humidity 70%,, measure disintegration time in different time period samplings.See Table 1.

Table 1

	0 day	Quickened 1 month	Quickened 2 months	Quickened 3 months	Quickened 6 months
						Prescription one (aqueous stone accounts for 0%)	11 minutes	15 minutes	29 minutes	98 minutes	The capsule shell infinite swelling did not have any disintegrate sign in 120 minutes
Prescription two (liquid Paraffin 10%)	12 minutes	14 minutes	18 minutes	52 minutes	78 minutes
						Prescription three (liquid Paraffin 30%)	10 minutes	11 minutes	16 minutes	48 minutes	72 minutes
Prescription four (liquid Paraffin 50%)	11 minutes	16 minutes	18 minutes	36 minutes	66 minutes
						Prescription five (liquid Paraffin 80%)	9 minutes	12 minutes	15 minutes	31 minutes	52 minutes

2, room temperature test:

Experimental condition: with packaged sample, be placed on indoorly, temperature and relative humidity are with extraneous consistent, in different time period samplings, mensuration disintegration time.See Table 2, table 3.

Table 2

	0 day	April, (1 month) mean temperature was 15.3 ℃	May (2 months), 18.6 ℃ of mean temperatures	June (3 months), 23.7 ℃ of mean temperatures	July (4 months), 27.8 ℃ of mean temperatures	August (5 months), 27.1 ℃ of mean temperatures
							Prescription one	11 minutes	14 minutes	16 minutes	31 minutes	69 minutes	104 minutes
Prescription two	12 minutes	11 minutes	14 minutes	20 minutes	27 minutes	44 minutes
							Prescription three	10 minutes	12 minutes	10 minutes	11 minutes	14 minutes	21 minutes
Prescription four	11 minutes	10 minutes	13 minutes	16 minutes	13 minutes	18 minutes

Prescription five

9 minutes

11 minutes

12 minutes

10 minutes

12 minutes

17 minutes

Table 3

	JIUYUE (6 months), 24.2 ℃ of mean temperatures	October (7 months), 18.8 ℃ of mean temperatures	November (8 months), 11.3 ℃ of mean temperatures	December (9 months), 7.1 ℃ of mean temperatures	January (10 months), 6.4 ℃ of mean temperatures	February (11 months), 8.3 ℃ of mean temperatures
							Prescription one	There was not any disintegrate sign in 120 minutes	There was not any disintegrate sign in 120 minutes	There was not any disintegrate sign in 120 minutes	There was not any disintegrate sign in 120 minutes	There was not any disintegrate sign in 120 minutes	There was not any disintegrate sign in 120 minutes
Prescription two	56 minutes	62 minutes	69 minutes	71 minutes	77 minutes	74 minutes
							Prescription three	35 minutes	47 minutes	55 minutes	60 minutes	67 minutes	65 minutes
Prescription four	23 minutes	35 minutes	34 minutes	38 minutes	44 minutes	48 minutes
							Prescription five	25 minutes	30 minutes	33 minutes	31 minutes	40 minutes	44 minutes

3, low-temperature test:

Experimental condition: with packaged sample, be placed in the low temperature chamber, temperature is lower than 20 ℃ throughout the year, in different time period samplings, measures disintegration time.See Table 4 and table 5.

Table 4

	0 day	1 month	3 months	6 months	9 months	10 months	11 months	12 months
									Prescription one	11 minutes	13 minutes	14 minutes	16 minutes	14 minutes	17 minutes	27 minutes	35 minutes
Prescription two	12 minutes	11 minutes	13 minutes	12 minutes	17 minutes	15 minutes	16 minutes	18 minutes
									Prescription three	10 minutes	13 minutes	14 minutes	15 minutes	13 minutes	16 minutes	13 minutes	21 minutes
Prescription four	11 minutes	11 minutes	13 minutes	15 minutes	15 minutes	16 minutes	18 minutes	20 minutes
									Prescription five	9 minutes	10 minutes	15 minutes	16 minutes	15 minutes	16 minutes	17 minutes	18 minutes

Table 5

	12 months	13 months	14 months	15 months	16 months	17 months	18 months
								Prescription one	42 minutes	49 minutes	58 minutes	66 minutes	78 minutes	95 minutes	114 minutes

Prescription two	20 minutes	19 minutes	19 minutes	20 minutes	27 minutes	36 minutes	43 minutes
								Prescription three	19 minutes	22 minutes	18 minutes	20 minutes	25 minutes	29 minutes	36 minutes
Prescription four	21 minutes	18 minutes	16 minutes	18 minutes	22 minutes	25 minutes	33 minutes
								Prescription five	19 minutes	20 minutes	17 minutes	16 minutes	19 minutes	23 minutes	27 minutes

At above-mentioned every result of the test, can obtain as drawing a conclusion:

1, according to the product that scheme obtained of prior art instruction, the disintegrate in 3 months of 37 ℃ of accelerated tests is just defective, and the effect duration of prompting product is very short, substantially in 1 year; And room temperature test (having experienced hot summer) disintegrate in 4 months is defective, shows the necessary cryopreservation of this product, even but low temperature placement down, test has been carried out 15 months, and the result shows that disintegrate is still defective.

As everyone knows, producing medicine from the pharmaceutical factory generally will experience to the process that consumer uses: production, warehouse-in, pharmaceutical factory storage, transportation, distributor's storage, pharmacy or hospital put on the shelf after picking up goods, consumer buys, consumer uses in expiration date of drug.The said goods is except keeping the cryogenic desirable environment of preserving in storage so, other links all become the unfavorable factor that influences disintegrate, and the product of above-mentioned prior art and existing Duyiwei soft capsule commodity can't overcome above unfavorable factor, this just inevitably brings product disintegrate before the deadline defective, influence pharmaceutical effectiveness and can't reach therapeutic purposes, product and existing Duyiwei soft capsule product that the scheme of prior art instruction obtains are described, its ubiquity effect duration is short, disintegrate is defective, necessary cryopreservation (still lack under the low temperature by effect duration, disintegrate is defective), producing, inevitable defective on transportation and the sales section.

2, according to the product of the method preparation of the present invention instruction, can guarantee cryogenic preservation condition in following effect duration disintegrate qualified fully, even acceleration and room temperature test guarantee that simultaneously product is still qualified in the quite a while disintegrate of leaving cryogenic preservation condition, this provides guarantee for product in intermediate links, has guaranteed product quality.

The present invention selects quantitative liquid wax (liquid Paraffin also claims liquid paraffin), and the effect that obtains is: constant product quality, and clinical efficacy obviously improves, and convenient the storage transported and patient's use; Solved problems such as prolonged disintegration that Duyiwei soft capsule for a long time fails to solve, leakage of oil, content layering, and clinical safety is good.

The inventor is in a large amount of groping in the experiment of the present invention, analyzing the mechanism of selecting quantitative liquid wax obviously to improve the quality of Duyiwei soft capsule is: Radix Lamiophlomidis Rotatae extract contains a large amount of flavones ingredients, for the oleaginous base of soft capsule field routine, these compositions show as more hydrophilic (being that water solublity is better), and contain at least 10% moisture in the soft capsule skin, the existence of these moisture can guide Flavonoid substances slowly to be transferred to the soft capsule Intradermal, thus the disintegrate that prolongs soft capsule with cross linking of gelatin; The adding of liquid Paraffin has changed the character of content, content and capsule shell intermediate formation layer protecting film, stop or delayed the transfer of flavones ingredient to capsule shell, thus the disintegrate of having protected the intrinsic property of gelatin self to prolong soft capsule.

The present invention selects Cera Flava to be because its suspending effect is best, but mellisic fusing point is more than 70 ℃, though only add the problem that Cera Flava can solve suspendible, in preparation process, often do not reach the requirement of fill, because the temperature of moulding is between 35-37 ℃, that is to say to have little time fill, the substrate that contains medicinal liquid will be solidified, and has only and selects extra add another kind of have the suspending effect and low-melting suspending agent; Through screening, add an amount of hydrogenated palm oil of fusing point about 37 ℃, the problem of content flowability when having solved fill; We find that in experiment even solved fill, unsettled phenomenons such as layering also can appear in soft capsule content very soon, and suspendible is still unresolved.And because Radix Lamiophlomidis Rotatae extract is water miscible composition, after having added conventional substrate, disintegrate very easily takes place become defective, the material migration takes place in the capsule, phenomenons such as effective ingredient generation sedimentation and oiliness composition seepage, only in the soft capsule prescription design of this kind, grope comprehensively, look for out the substrate and the usage ratio thereof that are fit to Radix Lamiophlomidis Rotatae extract, the stability of this soft capsule dosage form could take place significantly to change, final the present invention selects a certain proportion of Cera Flava, glyceryl monostearate, hydrogenated palm oil and/or soybean phospholipid, and vegetable oil (preferably corn oil, soybean oil), because (Semen Maydis oil and soybean oil contain a large amount of unsaturated fatty acids and linoleic acid to vegetable oil, and the human absorptivity is very high; Contain abundant vitamin, can cholesterol reducing, cardiovascular health is had great help) when successfully having solved suspendible and fill, also solved the problem that material migration and sedimentation etc. take place in the capsule.

Its specification of Duyiwei soft capsule of the present invention generally can be divided into 0.4～0.8g/ grain, and clinical recommendation consumption is 3～8g/ day.

Active component among the present invention---Radix Lamiophlomidis Rotatae extract is the Radix Lamiophlomidis Rotatae extract that meets 2005 editions standards of pharmacopoeia, and described Radix Lamiophlomidis Rotatae extract can prepare voluntarily, also can sell by the merchant and buy.

Select as another kind, Radix Lamiophlomidis Rotatae extract dry powder also can keep smaller particle size to satisfy the dissolution requirement as far as possible in the soft capsule of the present invention, for example reaches the purpose of quick stripping by superfine powder.

The present invention has following characteristic: good storing stability, and the deliquescence and the deterioration of preparation are suppressed, and active component preparation characteristics such as speed of stripping from preparation do not change, and overcome a series of defectives of existing product.More advantageously be, preparation of the present invention has been covered the bad stench flavor of Radix Lamiophlomidis Rotatae fully, can also improve the taste of Chinese medicine preparation, and quantitatively accurately, even also can be easily under anhydrous situation,, have significantly improved the compliance of patient to treatment without any the administration of uncomfortable ground.To further make non restrictive description below to the present invention.

Active component:

In context, the Radix Lamiophlomidis Rotatae extract among the present invention promptly is active component (effective site), and this active component mainly is meant total flavonoid composition wherein, especially contains rutin, luteolin (C ₁₅H ₁₀O ₆), the total flavones active component of Quercetin and apigenin.

Soft capsule content:

Described inclusions is meant the active component in the soft capsule (or claim soft gelatin capsule) and/or is carried on active component in the excipient, and wherein content can following arbitrary state and exist.In view of the special requirement of pain therapy, the present invention especially preferably provides the content of suspension or common aqueous type to prepare soft capsule dosage form.This is because the Radix Lamiophlomidis Rotatae active component that is carried in substrate and/or the excipient has dispersibility highly, has effectively improved its bioavailability.

Because the content of above-mentioned form is liquid state/hybrid state differential prose style free from parallelism system, when inserting in soft capsule as content it, to guarantee on the one hand the stability of content, should guarantee that on the other hand adjuvant wherein has no adverse effects to the stability (the especially migration of the material in the soft capsule) of soft capsule.With ethanol and other volatility cosolvents is example, and it can see through the cyst wall volatilization at normal temperatures, cause the capsule material softening, and this not only makes formulation content inaccurate but also influence the bioavailability of Radix Lamiophlomidis Rotatae active component.Through further investigation, we find, add stabilizing agent (as phospholipid) when this soft capsule of preparation in content, can further improve stability and flowability, not only play the effect of suspendible, but also can reduce the osmosis of water soluble ingredient to capsule wall.

Pharmaceutical composition provided by the invention, it contains the Radix Lamiophlomidis Rotatae extract and the conventional medicine adjuvant of clinical treatment effective dose.

The preparation of soft capsule method:

The present invention does not make specific limited to the preparation method of Duyiwei soft capsule, can adopt this area conventional method, for example pressing or dropping preparation method (drop pill method).

The specific embodiment

Embodiment 1:

The content prescription of Duyiwei soft capsule:

Radix Lamiophlomidis Rotatae extract: 0.25g

Soybean oil: 0.22g

Liquid Paraffin: 0.03g

Cera Flava: 0.02g

Hydrogenated palm oil: 0.015g

Soybean phospholipid: 0.015g

Make 1 (0.55g)

Preparation technology

Get the Radix Lamiophlomidis Rotatae medical material, pulverize, decoct with water 3 times, each 1 hour, collecting decoction filtered, and it is 1.30 clear paste that filtrate is condensed into relative density, dry below 80 ℃, pulverizes 100 mesh sieves, Radix Lamiophlomidis Rotatae extract, standby.

Get the soybean oil and the liquid paraffin of recipe quantity, add Cera Flava and hydrogenated palm oil, heating makes the suspending agent fusion, adds the fine powder of above-mentioned Radix Lamiophlomidis Rotatae extract, stirs, cool to 40 the degree about, add soybean phospholipid and stir once more, cross several all over colloid mill, if bubble is arranged, behind an amount of adding defoamer, be pressed into soft capsule.

Embodiment 2:

Radix Lamiophlomidis Rotatae extract: 0.25g

Semen Maydis oil: 0.16g

Liquid Paraffin: 0.06g

Cera Flava: 0.03g

Make 1 (0.5g)

Preparation technology

Get the Radix Lamiophlomidis Rotatae medical material, pulverize, decoct with water 3 times, each 2 hours, collecting decoction filtered, and it is 1.20 clear paste that filtrate is condensed into relative density, and drying was pulverized 80 mesh sieves, Radix Lamiophlomidis Rotatae extract, standby.

Get the Semen Maydis oil and the liquid paraffin of recipe quantity, add Cera Flava, heating makes the suspending agent fusion, adds the fine powder of above-mentioned Radix Lamiophlomidis Rotatae extract, stir, cool to 40 degree, stir, cross several all over colloid mills, if bubble is arranged, add defoamer in right amount after, be pressed into soft capsule.

Embodiment 3:

Extract: 0.20g

Salad oil: 0.20g

Liquid Paraffin: 0.25g

Glyceryl monostearate: 0.03g

Soybean phospholipid: 0.02g

Make 1 (0.7g)

Preparation technology

Get the Radix Lamiophlomidis Rotatae medical material, pulverize, decoct with water 2 times, each 2 hours, collecting decoction filtered, and it is 1.40 clear paste that filtrate is condensed into relative density, and spray drying was pulverized 200 mesh sieves, Radix Lamiophlomidis Rotatae extract, standby.

Get the salad oil and the liquid paraffin of recipe quantity, add glyceryl monostearate, heating makes the suspending agent fusion, adds the fine powder of above-mentioned Radix Lamiophlomidis Rotatae extract, stirs, cool to 40 the degree about, stir once more after adding soybean phospholipid, cross several all over colloid mill, if bubble is arranged, behind an amount of adding defoamer, be pressed into soft capsule.

Embodiment 4

Extract: 0.22g

Oleum Sesami: 0.20g

Liquid Paraffin: 0.08g

Glyceryl monostearate: 0.01g

Hydrogenated palm oil: 0.03g

Make 1 (0.54g)

Preparation technology

Get the Radix Lamiophlomidis Rotatae medical material, pulverize, decoct with water 3 times, each 1.5 hours, collecting decoction filtered, and it is 1.30 clear paste that filtrate is condensed into relative density, and vacuum drying was pulverized 150 mesh sieves, Radix Lamiophlomidis Rotatae extract, standby.

Get the Oleum Sesami and the liquid paraffin of recipe quantity, add glyceryl monostearate and hydrogenated palm oil, heating makes the suspending agent fusion, adds the fine powder of above-mentioned Radix Lamiophlomidis Rotatae extract, stir, cool to 40 degree, cross several all over colloid mills, if bubble is arranged, add defoamer in right amount after, be pressed into soft capsule.

Embodiment 5

Extract: 0.18g

Soybean oil: 0.23g

Liquid Paraffin: 0.02g

Cera Flava: 0.03g

Hydrogenated palm oil: 0.04g

Make 1 (0.5g)

Preparation technology

Get the Radix Lamiophlomidis Rotatae medical material, pulverize, decoct with water 3 times, each 1 hour, collecting decoction filtered, and it is 1.30 clear paste that filtrate is condensed into relative density, dry below 80 ℃, pulverizes 100 mesh sieves, Radix Lamiophlomidis Rotatae extract, standby.

Get the soybean oil and the liquid paraffin of recipe quantity, add Cera Flava and hydrogenated palm oil, heating makes the suspending agent fusion, adds the fine powder of above-mentioned Radix Lamiophlomidis Rotatae extract, stirs, cool to 40 the degree about, stir once more, cross several all over colloid mill, if bubble is arranged, behind an amount of adding defoamer, be pressed into soft capsule.

Embodiment 6

Extract: 0.15g

Semen Maydis oil: 0.158g

Liquid Paraffin: 0.07g

Cera Flava: 0.012g

Hydrogenated palm oil: 0.01g

Make 1 (0.4g)

Preparation technology

Get the Radix Lamiophlomidis Rotatae medical material, pulverize, decoct with water 3 times, each 1 hour, collecting decoction filtered, and it is 1.30 clear paste that filtrate is condensed into relative density, and drying was pulverized 80 mesh sieves, Radix Lamiophlomidis Rotatae extract, standby.

Get the Semen Maydis oil and the liquid paraffin of recipe quantity, add Cera Flava and hydrogenated palm oil, heating makes the suspending agent fusion, adds the fine powder of above-mentioned Radix Lamiophlomidis Rotatae extract, stirs, cool to 40 the degree about, stir once more, cross several all over colloid mill, if bubble is arranged, behind an amount of adding defoamer, be pressed into soft capsule.

More than described the preferred embodiment for the present invention, so it is not in order to limit the present invention.Those skilled in the art can not depart from the improvement and the variation of category of the present invention and spirit to embodiment disclosed herein.

Claims (10)

1. it is 20～70% Radix Lamiophlomidis Rotatae extract that Duyiwei soft capsule, the content that it is characterized in that this soft capsule contain percentage by weight, substrate, liquid Paraffin and suspending agent, and the weight ratio of described substrate and liquid Paraffin is 1:0.05～5.

2. Duyiwei soft capsule as claimed in claim 1 wherein contains the Radix Lamiophlomidis Rotatae extract 30%～55% of following percentage by weight in the content, substrate 15%～65%, liquid Paraffin 1%～40% and 5～15% suspending agent.

3, the described Duyiwei soft capsule of claim 2, its mesostroma is vegetable oil and/or refined oil.

4, each described Duyiwei soft capsule of claim 1～3, wherein the content of this soft capsule contains the Radix Lamiophlomidis Rotatae extract 35%～50% of following percentage by weight, vegetable oil 20%～55%, liquid Paraffin 2%～25%, suspending agent 5～15%.

5, the described Duyiwei soft capsule of claim 1, wherein said Radix Lamiophlomidis Rotatae extract is made by following method:

Get the Radix Lamiophlomidis Rotatae medical material, pulverize, decoct with water, decocting liquid filters, and filtrate concentrates after drying, pulverizes, promptly.

6. the described Duyiwei soft capsule of claim 3, wherein said vegetable oil is one or more mixture in Oleum Sesami, Oleum Arachidis hypogaeae semen, Semen Maydis oil, olive oil, Oleum Helianthi, soybean oil, salad oil, Oleum Gossypii semen, the Oleum Brassicae campestris.

7. the described Duyiwei soft capsule of claim 6, wherein said vegetable oil is one or more mixture in soybean oil, Semen Maydis oil, Oleum Sesami or the salad oil.

8, the method for preparing the described Duyiwei soft capsule of claim 1, comprising:

1) get Radix Lamiophlomidis Rotatae extract, pulverizing becomes 80 order fine powders at least.

2) get vegetable oil and liquid paraffin, add suspending agent, heating makes the suspending agent fusion, stirs, and adds above-mentioned Radix Lamiophlomidis Rotatae extract, cools to 30～50 degree, stirs once more, crosses colloid mill, is pressed into soft capsule.

9, the method for preparing Duyiwei soft capsule as claimed in claim 8, wherein said suspending agent are selected from arbitrary or its combination in Cera Flava, Cera Flava, hydrogenated palm oil, hydrogenation silk floss oil, tristerin, glyceryl monostearate, fatty glyceride, mixed fatty glycerides and soybean phospholipid, the lecithin.

10, as claim 8 or 9 each described methods that prepare Duyiwei soft capsule, comprising:

1) get Radix Lamiophlomidis Rotatae extract, pulverizing becomes 80 order fine powders at least.

2) get vegetable oil and liquid paraffin, add the part suspending agent, this part suspending agent is Cera Flava and/or hydrogenated palm oil and/or glyceryl monostearate, and heating makes its fusion, adds above-mentioned Radix Lamiophlomidis Rotatae extract, stir, cool to 30～50 degree, add remaining suspending agent again, this remaining suspending agent is soybean phospholipid and/or lecithin, cross colloid mill after stirring once more, be pressed into soft capsule.