CN100367954C - Andrographolide soft capsule formulation and preparation method - Google Patents

Abstract

The present invention relates to a green chiretta lactone soft capsule preparation and a preparation method thereof. In the present invention, capsule medicine liquid comprises green chiretta lactone in enough dosage as an effective component; the green chiretta lactone is matched with medicinal auxiliary materials in a proper proportion; the medicinal auxiliary materials comprise a diluting agent, a suspending agent, an antioxidant, a preservative, etc.; a capsule shell is mainly composed of gelatin, glycerin and water. The soft capsule prepared by the present invention has the advantages of stable quality, convenient taking, fast dissolution of effective components and timely effect.

Description

Andrographolide soft capsule formulation and preparation method thereof

Technical field

The invention belongs to medical technical field, be specifically related to a kind of pharmaceutical preparation of andrographolide,, the invention still further relates to the preparation method of said preparation simultaneously more specifically to a kind of andrographolide soft capsule.

Background technology

Andrographolide has the effect of heat-clearing and toxic substances removing, anti-inflammation, is used for upper respiratory tract infection, bacillary dysentery clinically.

The preparation of andrographolide has injection and tablet etc. clinically at present, and injection exists the shortcoming of patient's medication inconvenience when curative effect can be affirmed.Tablet is because the dissolubility of andrographolide is bad, and the effective ingredient stripping is slow, and onset is slower.Simultaneously, the andrographolide bitter in the mouth, patient's doctor is relatively poor from property.Andrographolide soft capsule can overcome the above-mentioned shortcoming of injection and tablet.

Summary of the invention

The object of the present invention is to provide a kind of andrographolide soft capsule and production method thereof, product is an oral administered dosage form, its steady quality, and easy to use, disintegrate is fast, and onset is timely.

The andrographolide soft capsule that the present invention proposes is made of medicinal liquid and softgel shell two parts.Wherein, medicinal liquid contains the andrographolide of certain effective dose as effective ingredient, and is equipped with pharmaceutic adjuvant, and pharmaceutic adjuvant comprises diluent, antioxidant, antiseptic, suspending agent etc.; Softgel shell mainly is made up of gelatin, water and glycerol, and the weight proportion of gelatin and glycerol is 10: 3.15～10: 3.35.

The structural formula of Main Ingredients and Appearance andrographolide of the present invention is:

Diluent of the present invention can be one or more in Polyethylene Glycol, propylene glycol, vegetable oil, the mineral oil; Antioxidant can be one or more in ethylenediaminetetraacetic acid, disodium EDTA, dibenzylatiooluene, glycine, inositol, ascorbic acid, sodium ascorbate, lecithin, malic acid, hydroquinone, citric acid, succinic acid, the sodium pyrosulfite; Suspending agent is one or more in Cera Flava, ethylhydroxyethylcellulose, chitin, chitose, methylcellulose, carboxymethyl cellulose, agar, hydroxypropyl emthylcellulose, the xanthan gum etc.; Antiseptic is one or more in sorbic acid, sorbic acid methyl ester, methyl parahydroxybenzoate, ethylparaben, propyl p-hydroxybenzoate, butyl p-hydroxybenzoate, benzyl p-hydroxybenzoate, Sodium Methyl Hydroxybenzoate, benzoic acid, the benzyl alcohol; Can also add coloring agent, opacifier in the softgel shell, specifically can be in white carbon black, iron oxide black, cologne earth, iron oxide red, the titanium dioxide one or more.

Among the present invention, the medicinal liquid of andrographolide soft capsule, reasonable component weight proportion is as follows:

Andrographolide 1

Diluent 1.4～20

Suspending agent 0.04～1

Antioxidant 0.008～0.1

Antiseptic 0.008～0.1

In the process of research andrographolide soft capsule, solved following problem:

1, softgel shell prescription (being applicable to the oil-soluble medicinal liquid)

Gelatin, glycerol proportioning are difficult to grasp in the prescription of softgel shell.The amount of glycerol is too many, and softgel shell is softer, than being easier to extrusion; The amount of glycerol very little, softgel shell is harder, crisp, influences the quality stability and the disintegration time of soft capsule.Gelatin, glycerol proportioning to softgel shell have been carried out detailed experimental study, have obtained a proportioning preferably at last.

An amount of gelatin is added in the rustless steel glue pot, add suitable quantity of water again, airtight, 70 degree insulation 3hr, add glycerol, the coloring agent of test consumption more respectively, stir vacuumize degassing 2hr, put into gelatin heat-preserving container 70 degree insulation standing over night, second day moulding ball, drying at room temperature keeps sample and investigates 3 months, examination softgel shell outward appearance and physical property, found that gelatin and glycerol proportioning be 10: 3.15～10: 3.35 o'clock the most suitable.The softgel shell prescription that is filtered out is applicable to common preservation environment.

2, medicinal liquid prescription

The softgel shell of soft capsule has determined that the used diluent of medicinal liquid can not be water, ethanol and the bigger organic solvent of some toxicity, and ideal is oil substances.But because andrographolide is insoluble in vegetable oil, so the medicinal liquid prescription has adopted the oil suspension system.Simultaneously by a large amount of experiments, selected for use toxicity less, can well andrographolide be suspended in the suspending agent in the vegetable oil.

An amount of suspending agent is melted in an amount of vegetable oil, again andrographolide is added wherein, add suitable antioxidant afterwards and in storage process, take place rotten to prevent the medicinal liquid in the soft capsule.Every of soft gelatin capsule contains the amount of principal agent andrographolide to be determined, is generally 0.01-0.10g.

3, preparation technology

The preparation technology of andrographolide soft capsule may further comprise the steps:

Gelatin adds suitable quantity of water under stirring, treat that gelatin dissolves fully after, add glycerol, amount of colorant, stir, be incubated set aside for use after the vacuumize degassing.

Suspending agent is added in the vegetable oil, and mixing mixes andrographolide again with vegetable oil, treat complete mixing after, add antioxidant, antiseptic again, stir, room temperature leaves standstill.

The medicinal liquid for preparing is poured in the medicinal liquid bucket, suppressed soft capsule with mould.

Compare with existing other dosage forms of andrographolide, the advantage of andrographolide soft capsule is a steady quality, carries, convenient drug administration, and the effective ingredient stripping is fast, and onset speed is fast, and the shortcoming of bitter in the mouth is overcome.

The specific embodiment

Embodiments of the invention are as follows:

Embodiment 1;

Component amount (g/ grain)

Andrographolide 0.025

Polyethylene Glycol 0.225

Gelatin 0.16

Glycerol 0.09

Hydroxyethyl-cellulose 0.007

Citric acid 0.008

Sorbic acid methyl ester 0.001

Cera Flava 0.01

Water 0.25

Embodiment 2:

Component amount (g/ grain)

Andrographolide 0.05

Oleum Arachidis hypogaeae semen 0.39

Gelatin 0.12

Glycerol 0.05

Ethyl cellulose 0.008

Ethylenediaminetetraacetic acid 0.001

Benzoic acid 0.002

Cera Flava 0.02

Water 0.25

Embodiment 3:

Component amount (g/ grain)

Andrographolide 0.01

Oleum Glycines 0.08

Gelatin 0.18

Glycerol 0.08

Chitose 0.006

Ascorbic acid 0.007

Propyl p-hydroxybenzoate 0.002

Cera Flava 0.006

Water 0.25

The preparation technology of above embodiment andrographolide soft capsule is:

Take by weighing gelatin and add 100L gelatin retort, under stirring, add suitable quantity of water, airtight, treat that gelatin dissolves fully after, add glycerol, amount of colorant again, stir, vacuumize degassing 2 hours is put into the gelatin heat-preserving container, the insulation standing over night is stand-by.

Suspending agent is added in the diluent, and mixing takes by weighing andrographolide, pulverizes, and sieves, and with andrographolide and mixing diluents, treats to add antioxidant, antiseptic behind the complete mixing, stirs, and room temperature leaves standstill.

The gelatin heat-preserving container is suspended from certain altitude, the medicinal liquid for preparing is poured in the drug bucket, change mould and begin to press soft capsule, adjust the soft capsule device to scope of design, dry 24 hours, reject the soft gelatin capsule of presentation quality difference, with the soft gelatin capsule washing, dry 24 hours again, get the andrographolide soft capsule semi-finished product, the qualified back packing of quality inspection, labeling, packing promptly get the andrographolide soft capsule finished product.These capsule finished product quality are all very stable, and result of use is good.

Claims (7)

1. an andrographolide soft capsule is made of medicinal liquid and softgel shell two parts, it is characterized in that andrographolide that medicinal liquid contains effective dose as effective ingredient, and is equipped with pharmaceutic adjuvant, and pharmaceutic adjuvant comprises diluent, antioxidant, suspending agent, antiseptic; The weight proportion of medicinal liquid is: andrographolide is 1, and diluent is 1.4～20, and suspending agent is 0.04～1, and antioxidant is 0.008～0.1, and antiseptic is 0.008～0.1; Softgel shell mainly is made up of gelatin, water and glycerol, and the weight proportion of gelatin and glycerol is 10: 3.15～10: 3.35.

2. andrographolide soft capsule according to claim 1 is characterized in that diluent is one or more in Polyethylene Glycol, propylene glycol, vegetable oil, the mineral oil.

3. andrographolide soft capsule according to claim 1 is characterized in that antioxidant is one or more in ethylenediaminetetraacetic acid, disodium EDTA, dibenzylatiooluene, glycine, inositol, ascorbic acid, sodium ascorbate, lecithin, malic acid, hydroquinone, citric acid, succinic acid, the sodium pyrosulfite.

4. andrographolide soft capsule according to claim 1 is characterized in that suspending agent is one or more in Cera Flava, ethylhydroxyethylcellulose, chitin, chitose, methylcellulose, carboxymethyl cellulose, agar, hydroxypropyl emthylcellulose, the xanthan gum etc.

5. andrographolide soft capsule according to claim 1 is characterized in that antiseptic is one or more in sorbic acid, sorbic acid methyl ester, methyl parahydroxybenzoate, ethylparaben, propyl p-hydroxybenzoate, butyl p-hydroxybenzoate, benzyl p-hydroxybenzoate, Sodium Methyl Hydroxybenzoate, benzoic acid, the benzyl alcohol.

6. andrographolide soft capsule according to claim 1 is characterized in that also being added with coloring agent, opacifier in the softgel shell, is specially in white carbon black, iron oxide black, cologne earth, iron oxide red, the titanium dioxide one or more.

7. preparation method as the described andrographolide soft capsule of claim 1-6 is characterized in that may further comprise the steps:

Gelatin adds suitable quantity of water under stirring, treat that gelatin dissolves fully after, add glycerol, coloring agent, stir, be incubated set aside for use after the vacuumize degassing;

Suspending agent is added in the diluent, and mixing adds andrographolide again, treat complete mixing after, add antioxidant, antiseptic, stir, the quiet reason of room temperature is stand-by;

The medicinal liquid for preparing is poured in the medicinal liquid bucket, suppressed soft capsule with mould.