CN102526750A - Plant colonic-coated hollow capsule - Google Patents

Abstract

The invention discloses a plant colonic-coated hollow capsule, which is prepared by treating 80-95 percent of zein powder and 5-20 percent of a plasticizer serving as raw materials in a more than or equal to 80 percent ethanol solution or a more than or equal to 70 percent acetone solution with a known process and equipment. The quality of the capsule is accordant with the specifications in the colonic-coated hollow capsule standard of the Chinese Pharmacopoeia of the version 2010, the capsule is not disintegrated in an enteric process, is disintegrated on a colonic part within one hour, and has three years of shelf life.

Description

One kind of plant colon dissolves Capsules

One, technical field

The present invention relates to a kind of pharmaceutic adjuvant Capsules; Be particularly related to a kind of plant hollow capsule; Exactly be a kind ofly not allow disintegrate, also do not dissolve or disintegrate at the human small intestine position the human stomach, and only rapid dissolved targeting property, vegetalitas, colon dissolubility Capsules at the colon position of human body.

Two, technical background

Capsules (softgel shell) is the main adjuvant of processing capsule; " Chinese pharmacopoeia version regulation in 2010 colon dissolves Capsules and is meant softgel shell not disintegrate in 2 hours in gastric juice; Then can not dissolve or disintegrate disintegrate or dissolve and discharge medicine in the capsule in colonic fluid in 3 hours at the human small intestine position.The colon that uses at present dissolve Capsules by gelatin machine-shaping after the anti-gastric acid of outsourcing and dissolve coating material at the colon of pH value 6.8 not disintegrates.Production technology is that gelatin is earlier with glue after purified water immersion, the swelling; After send the capsule manufacture line through dipping in gum forming, dry solidification, obtaining gelatin Capsules capsule material; Carry out forming colon after colon dissolves Cotton seeds in gelatin Capsules capsule material surface again and dissolve Capsules capsule material, operations such as dry solidification cooling again, cutting, fit obtain colon and dissolve Capsules (softgel shell).Described glue stirs dropping into to heat up in the mixing kettle with water surface activating agent etc. after the gelatin swelling exactly, after filtering, remove bubble, accent proportion, obtains sizing material.

Present colon dissolves the Capsules main component to be formed by anti-gastric acid and at molten coating material of not disintegrate of small intestinal colon and gelatin.Anti-gastric acid also dissolves coating material at the colon of not disintegrate of small intestinal and is mostly acrylic resin III.

The water soluble protein that gelatin is obtained through hydrolysis by the collagen protein in the connective tissues such as the skin of animal, bone, tendon, ligament.Protein is subject to the influence of acid, alkali, and medicated powder acidity or alkalescence that Ruo Qinei fills are stronger, can cause hydrolysis of gelatin Capsules or sclerosis.Also have because of the religions belief reason, take like taboos such as Islam, kosher; Epidemic situations such as " bovine spongiform encephalopathy " that occurs in recent years, " foot and mouth disease " again serious impact the Capsules agent market of gelatin class.Other feedstock production capsules that exploitation substitutes gelatin have realistic meaning.So someone just prepares plant hollow capsule with hydroxypropyl emthylcellulose (HPMC) and polysaccharide.The applicant has developed CMC plant hollow capsule (ZL200910116242.6) and pectin plant enteric hollow capsule (ZL200910185990.X), but this type capsule can only the stomach of human body or at the human small intestine position dissolved vegetalitas Capsules.

Three, summary of the invention

The object of the present invention is to provide a kind of each item physicochemical property all to meet " the molten Capsules of vegetalitas colon of Chinese pharmacopoeia version regulation in 2010; Technical problem to be solved is softgel shell not disintegrate in 2 hours in gastric juice; Then can not dissolve or disintegrate in 3 hours at the human small intestine position, can only be in the human colon position disintegrate or dissolve and discharge medicine in the capsule.

The applicant is through years of researches and exploration, and selecting with the zein powder is primary raw material, is aided with plasticizer and directly is processed into the molten Capsules of plant colon, and each component has following percentage by weight:

Zein powder 80～95%,

Plasticizer 5～20%.

Contain 8～14% the protein of having an appointment in the corn, these protein have 20% in plumule, and 75% in endosperm.The embryo protein of milk mainly is alcohol soluble protein and glutelin, is not the protein resource of ideals of human being from nutrition angle zein.Alcohol soluble protein separates in processing corn starch process and obtains.Flow process is following: corn is at first washed embryo after soaking, roughly grinding; Isolate plumule and be used to process Semen Maydis oil; Coarse grain behind the separated plumule is isolated protein with the cyclonic separation method and is used to process the forage protein powder after correct grinding, screening; Last dehydrate obtains corn starch (" grain oil product processing and storage new technique " Wang Depei etc. writes " publishing house of South China Science & Engineering University ", publication in March calendar year 2001).The zein raw material sources are abundant, and manufacturer is a lot, give birth to section's bio tech ltd etc. like Guangdong Guang Ye Qing Yi Food Technology Co., Ltd, Shanghai.

The zein representative property is water insoluble, but dissolves in the urea liquid of alcoholic solution, high concentration, the alkali liquor of high concentration (pH＞11) or anionic detergent agent solution.This is because its amino acid whose compositing characteristic determines.Zein contains glutamic acid (21-26%), leucine (20%), proline (10%) and alanine (10%); Zein is the mixture that 25000～45000 protein is formed by mean molecule quantity; It receives hydroxyl and the hydrogen bond action of imino group on the peptide main chain, forms the alpha-helix body; Low-surface-energy is arranged, have unique film forming characteristics.In alcohol-water solution; Become random ball of string structure; But become a kind of transparent, glossiness thin film after the solvent evaporation; Have characteristics such as protection against the tide, oxygen barrier, uvioresistant, guarantor's perfume, oil resistance, antistatic, because zein is taken from corn, the Capsules that processes dissolves Capsules so claim the plant colon.

Described plasticizer is selected from the material of organic solvent dissolution, like a kind of or both above mixed plasticizers in Oleum Ricini, triethyl citrate, the glycerol triethyl etc.

Zein, plasticizer are the key components that this plant colon dissolves Capsules.In addition, the gelatin Capsules is the same with processing, and also can add according to actual needs to be dissolved in alcoholic acid food coloring ingot and/or opacifier titanium dioxide, gives the performance of capsule shades of colour and lucifuge.

The preparation that this plant colon dissolves Capsules comprises the preparation of glue and the processing of softgel shell.The aqueous acetone solution of the ethanol water of zein and mass percentage concentration >=80% or mass percentage concentration >=70% mixed to drop in the agitator add plasticizer after the stirring and dissolving; Stir after-filtration, remove bubble, transfer proportion (being zein concentration), send capsule manufacture line processing softgel shell then.Technical process is identical with processing gelatin Capsules with equipment.

This plant colon dissolves the Capsules experiment and shows that quality index can meet " the Chinese pharmacopoeia molten Capsules standard code of version colon in 2010 fully; Following through detecting index: gastric juice 3---4 disintegration hour; Intestinal juice not disintegrate in 4 hours can disintegrate in 1 hour at the colon position." Chinese pharmacopoeia 2010 editions regulation colon dissolves Capsules in gastric juice disintegration＞2 hour, intestinal juice disintegration＞3 hour.In disintegration＜1, colon position hour.

This capsule is compared with the colon colloidal sol capsule of selling in the market, has a lot of advantages, and the one, raw material sources are corns of plant class, the source is wide; Not in short supply, price is low, and content of beary metal is low; Safety is good, is to derive from animal Os Bovis seu Bubali and Corii Sus domestica and do raw material with gelatin, and it is limited to originate; Price is high, and content of beary metal is higher, also has the impact of epidemic situations such as " bovine spongiform encephalopathy ", " foot and mouth disease " etc.; The 2nd, process aspect; The application's capsule technology is simple; Drop into zein and medicinal alcohol and water or acetone in the agitator with mixing of water and to add plasticizer after the stirring and dissolving; Stir after-filtration, remove bubble, transfer proportion (being zein concentration), send capsule manufacture line dry processing to solidify operations such as cooling, cutting, fit then and directly obtain the plant colon and dissolve Capsules (softgel shell).And the molten Capsules of colon is at first used the gelatin glue in the market; Send the capsule manufacture line through dipping in gum forming, dry solidification, obtaining gelatin Capsules capsule material; Carry out forming colon after colon dissolves Cotton seeds in gelatin Capsules capsule material surface again and dissolve Capsules capsule material; Operations such as dry solidification cooling again, cutting, fit obtain colon and dissolve Capsules (softgel shell) and need repeatedly twice, and technology is loaded down with trivial details; The 3rd, the quality aspect, this capsule friability good (promptly being difficult for crisp broken), flexible; And water content, residue are all low, and it is still all qualified that stored through 3 years disintegration, because of zein itself has colon dissolubility matter; And indeformable at the normal temperature storage capsule, never degenerate, and colon dissolves Capsules such as coating has broken or bottom pour ladle in the market, capsule is just defective disintegration; And enteric coating exists moisture content to descend and problem of aging; Therefore capsule is along with the storage time is long more, and capsule is just crisp all the more, and condition of storage is harsh and will lack; The 4th, the cost aspect, colon dissolves Capsules in the market, and cost of material is high, and the feed back that cuts down can not utilize once more, and technology is loaded down with trivial details, and qualification rate is low, and condition of storage is harsh, and the shelf-life, short the grade all can cause the capsule cost to rise, and the market competitiveness weakens.And the new product cost is just much lower, has saved the coating operation, work simplification, and also feed back can recycle, has protected environment, helps raising the efficiency, having reduced cost.

Four, the specific embodiment

Below the present invention is described in further detail, and provide the specific embodiment.

1, zein powder 30kg, 85% alcoholic solution 64-68.5kg, plasticizer Oleum Ricini 1.6kg.

Production equipment is with existing identical with the manufacturing of gelatin Capsules.Together pour zein powder and alcoholic solution, plasticizer into stirring in the agitator, dissolving; Stir more than 6 hours, fully solvent liquid is filtered with 200 purpose filter bags in the dissolving back, is stored in the bucket; See proportion; Regulate gelatin concentration, according to user's demand add various required colors the food coloring ingot or/and a certain amount of opacifier titanium dioxide etc. leave standstill except that bubble; Put into again on the capsule manufacture line through dipping in glue, oven dry, cooling, the demoulding, cutting, fit, check, packing, need lettering lettering etc. behind fit.

2, zein powder 30kg, 75% acetone soln 64-68.5kg, plasticizer triethyl citrate 2kg.Its production method is with embodiment 1.

3, plasticizer Oleum Ricini 2kg, triethyl citrate 2kg, other are with embodiment 1.

4, plasticizer Oleum Ricini 2kg, triethyl citrate 2kg, glycerol triethyl 2kg, other proportionings are with embodiment 2, and operation is with embodiment 1.

Claims (2)

1. a kind of plant colon dissolves Capsules, comprises zein powder and plasticizer, and it is characterized in that: each component has following percentage by weight:

The zein powder: 80～95%,

Plasticizer: 5～20%.

2. capsule according to claim 1 is characterized in that: described plasticizer is selected from a kind of or both above mixed plasticizers in Oleum Ricini, triethyl citrate, the glycerol triethyl.