CN102512430B

CN102512430B - Medicinal composition for intestinal tract cleaning

Info

Publication number: CN102512430B
Application number: CN201110444334.4A
Authority: CN
Inventors: 唐一林; 郗遵波; 高绍丰
Original assignee: Jinan Shengquan Group Share Holding Co Ltd
Current assignee: Jinan Shengquan Group Share Holding Co Ltd
Priority date: 2011-12-27
Filing date: 2011-12-27
Publication date: 2015-04-22
Anticipated expiration: 2031-12-27
Also published as: CN102512430A

Abstract

The invention discloses a medicine for colonoscopy and intestine tract preparation before colonic and rectal surgeries. The medicine is a medicinal combination containing L-glucose and L-mannose. The L-glucose and the L-mannose are not required to be separated, so the production cost is reduced; and the method has high industrial value. The medicinal combination of the L-glucose and the L-mannose has the characteristics of safety, reliability, convenience for use, good patient compliance and the like.

Description

A kind of pharmaceutical composition for intestinal tract cleaning

Technical field

The present invention relates to a kind of pharmaceutical composition for intestinal tract cleaning, specifically a kind of Pharmaceutical composition containing L-glucose and L-mannose.

Background technology

First intestinal tract cleaning need be carried out during INTESTINAL CLEANSING before colonoscopy, colonic operation, before operation on rectum.Intestinal tract cleaning and nosocomial infection control, the generation of clinical medical and nursing quality, complication is closely related, and the clean-up performance of INTESTINAL CLEANSING even directly affects operation, the carrying out of check result and every treatment work.

The restricted diet of INTESTINAL CLEANSING method, clysmata, oral drugs method etc.Keep on a diet separately and can not reach the object of INTESTINAL CLEANSING, just various inspection and the basic householder method generally applied of performing the operation.Light slag low fat diet, last late liquid diet, fasting in morning on the same day less in conventional 1 ~ 2 day.Clysmata, complex operation, has certain damage to direct intestinal, general and oral medicine method coupling.Oral drugs method, taking convenience, is easy to accept.Oral hyperosmotic dehydrant 20% mannitol, its zymolysis in enteric cavity can produce a large amount of gas, and GI irritation is obvious.The shortcomings such as polyethylene glycol electrolyte liquid main component is the isotonic Polyethylene Glycol of nonabsorbable, is at present relatively more conventional INTESTINAL CLEANSING medicine, but also there is effective dose large (each 4L), and taste bad will, side effect are many, add the misery of patient's INTESTINAL CLEANSING.

L-glucose is as intestinal tract cleaning medicine (GASTROINTESTINAL ENDOSCOPY VOLUME 58, NO.1,2003), and intestinal tract cleaning is respond well and be 80% above, close with the intestinal cleaning agents 82.3% ten point of current extensive use.L-glucose is pleasantly sweet, and using dosage little (each 240ml), is conducive to patient and takes.It is raw material with L-arabinose that american documentation literature US4581447 discloses a kind of, pass through and Blausure (German) addition, obtain the mixture of 1-cyano group-L glucitol and 1-cyano group-L mannitol, then through hydrogenation, obtain the mixture of L-glucose and L-mannose, best ratio is 1:1.The method is considered to the method for the acquisition L-glucose having industrial value most.However, because the difficulty isolating L-glucose in the mixture from L-glucose and L-mannose is large, yield is low, causes L-glucose expensive.According to L-glucose market price 10000 yuan of/kilogram of calculating, each use amount 24g of each patient, only the cost of raw material that is 240 yuan, exceeds existing product market price greatly, the serious application constraining L-glucose.Similarly, preparation L-mannose cost is high separately, is not therefore applied to intestinal tract cleaning.

Summary of the invention

For this reason, technical problem to be solved by this invention overcomes that L-glucose difficulty for intestinal tract cleaning in prior art is separated, yield is low and cause the expensive problem of L-glucose, thus provide a kind of low cost, features good taste, safely and effectively for the pharmaceutical composition of intestinal tract cleaning.

For achieving the above object, the invention provides a kind of pharmaceutical composition for intestinal tract cleaning.

Described compositions is made up of L-glucose and L-mannose.

The content of described L-glucose is 0.1wt% ~ 99.9wt%, and the content of described L-mannose is 0.1wt% ~ 99.9wt%.

Preferably, the content of described L-glucose is 10wt% ~ 90wt%, and the content of described L-mannose is 10wt% ~ 90wt%.

More preferably, the content of described L-glucose is 45wt% ~ 55wt%, and the content of described L-mannose is 45wt% ~ 55wt%.

For an oral formulations for intestinal tract cleaning, comprise following component: the pharmaceutical composition for intestinal tract cleaning: 0.1wt% ~ 99.9wt%; Water: 0.1wt% ~ 99.9wt%.

For a medicament for intestinal tract cleaning, comprise following component: L-glucose: 0.1wt% ~ 99.9wt%, L-mannose: 0.1wt% ~ 99.9wt%.

The application of described pharmaceutical composition in the medicine preparing intestinal tract cleaning.

Technique scheme of the present invention compared with prior art has the following advantages:

1. the invention provides a kind of pharmaceutical composition for intestinal tract cleaning, described compositions is made up of L-glucose and L-mannose.L-glucose and L-mannose, pleasantly sweet, using dosage is little, improves the compliance of patient, meanwhile, with both the mixture medicine as intestinal tract cleaning, avoids and the two is separated the difficulty brought, significantly reduce use cost.

2.L-mannose can as the medicine of intestinal tract cleaning.L-mannose is similar to L-glucose: not by intestinal absorption, can form hyperosmosis at intestinal, reaches the object of intestinal tract cleaning.L-mannose, not by enteric microorganism metabolism, therefore can not form intestinal tract flatulence.L-mannose is pleasantly sweet, improves the compliance of patient.

3. the content of L-glucose is the content of 0.1wt% ~ 99.9wt%, L-mannose is 0.1wt% ~ 99.9wt%.Obtained in the process of L-glucose and L-mannose by L-arabinose, regulate the consumption of catalyst, obtain L-glucose different with the mixed proportion of mannose, this combination can mix with arbitrary proportion, reducing workload, providing convenient for realizing industrialization large-scale production.

4. the pharmaceutical composition of L-glucose and L-mannose is as the oral formulations of intestinal tract cleaning or medicament, can be solid mixture or liquid mixture two kinds of forms, makes medicament forms multiformity provide washability to suffering from patient.

5. pharmaceutical composition is peroral dosage form, and taking convenience is quick, is easily accepted.

Detailed description of the invention

Below will the invention will be further described by specific embodiment.

The patient that 239 examples accept the patient of outpatient service colonoscopy, 247 examples accept colonic operation, 200 examples accept operation on rectum patient (get rid of the age be less than 18 and be greater than 75 and have pulmonary, heart, kidney, dysautonomia and endocrine regulation person to use the patient of anesthetis, fiber supplement, anticholinergic agent and light purgative prescription clinical observation exception) be divided into respectively 2 groups (A group, B groups).

A group carries out intestinal tract cleaning: the normal breakfast in morning of inspection or one day before surgery, noon a small amount of lunch, food, sugar and caffeine is avoided, the ratio (containing dry 25g) of the pharmaceutical composition of L-glucose and L-mannose in 5-6pm in evening 10 minutes lower embodiment 1-embodiments 11 for oral administration after 2 pm; Drink 250ml water again after defecation for the first time, check and terminate front fasting.To before clean, clean after, check after or Post operation carry out serum and urine test.

B group carries out intestinal tract cleaning: the normal breakfast in morning of inspection or one day before surgery, noon a small amount of lunch, avoid food, sugar and caffeine after 2 pm, evening 5-6pm take first Polyethylene Glycol-electrolyte Powder (1 box of getting and feel well, bag medicated powder each in box is poured in the lump band graduated cup in, warm water is to 1000ml, stirring makes to dissolve completely), take 600-1000ml first, take 1 time every 10-15 minute later, be no less than 250ml at every turn, until take or until discharge water sample do as you wish.

Embodiment 1:

By the aqueous solution 2500ml (pH is 11.53) containing 639.7g Cyanogran., after adding nitrogen displacement container 10min, solution is cooled to 7 DEG C, slowly adds dense vinegar acid for adjusting pH to 7.94, temperature 16 DEG C.Then add the 60wt% L-arabinose aqueous solution of 1666g, again adding dense acetic acid adjust ph is 8.1, and reaction is carried out at 23 DEG C.Add 385ml concentrated sulphuric acid after cooling 1.25h and regulate pH to 2.05.Product analysis shows that L-arabinose conversion ratio is 99.4%.

Cyaniding product is added in the hydrogenation still of nitrogen protection, separately adds the palladium barium sulphate catalyst of 500g 5wt%.Adding sulphuric acid makes hydrogenation reaction pH value control 2.0.After reaction does not absorb hydrogen, Filtration of catalyst, ion-exchange process removing dissolving salt, obtains the mixture of L-glucose and L-mannose.The content of described L-glucose is 52%, and the content of described L-mannose is 48%.Product analysis shows that intermediate cyanalcohol 100% transforms, glucose and mannose yield 75%.This mixture L-glucose and L-mannose are used for intestinal tract cleaning.This pharmaceutical composition is solid form.

By regulating catalyst amount, obtain the L-glucose of different proportion and the mixture of L-mannose.

A, B group intestinal tract cleaning Contrast on effect of table 1 embodiment 1

Embodiment 2 ~ embodiment 11

Be formulated as follows L-glucose and the L-mannose mixture of (see table 2) ratio, the intestinal tract cleaning effect obtained is in table 3:

The ratio of table 2 embodiment 2 ~ embodiment 11 Chinese medicine compositions

Described in embodiment 2 for intestinal tract cleaning oral formulations, pharmaceutical composition proportion is 68wt%; Water accounting example is 32wt%, and wherein L-glucose accounts for the ratio of pharmaceutical composition is 21.4wt%; The ratio that L-mannose accounts for pharmaceutical composition is 78.6wt%.Similarly, each component ratio of embodiment 3 ~ embodiment 11 is in table 2.

A, B group intestinal tract cleaning Contrast on effect of table 3 embodiment 2 ~ embodiment 11

Show from the above results display, the combination colon of L-glucose and L-mannose cleans respond well, is better than Polyethylene Glycol-electrolyte Powder (with refreshing).The combination of L-glucose and L-mannose is a kind of desirable intestinal tract cleaning medicine of safe, effective, good patient dependence.

Obviously, above-described embodiment is only for clearly example being described, and the restriction not to embodiment.For those of ordinary skill in the field, can also make other changes in different forms on the basis of the above description.Here exhaustive without the need to also giving all embodiments.And thus the apparent change of extending out or variation be still among the protection domain of the invention.

Claims

1. the compositions be made up of L-glucose and L-mannose, preparing the application that has in the pharmaceutically-active medicine of intestinal tract cleaning, is characterized in that, content be 52% L-glucose and content be that the compositions of the L-mannose composition of 48% obtains by the following method:

By the aqueous solution 2500ml containing 639.7g Cyanogran., pH is 11.53, after adding nitrogen displacement container 10min, solution is cooled to 7 DEG C, slowly adds dense vinegar acid for adjusting pH to 7.94, temperature 16 DEG C, then the 60wt%L-arabinose aqueous solution of 1666g is added, again adding dense acetic acid adjust ph is 8.1, and reaction is carried out at 23 DEG C, adds 385ml concentrated sulphuric acid and regulate pH to 2.05 after cooling 1.25h; Cyaniding product is added in the hydrogenation still of nitrogen protection; separately add the palladium barium sulphate catalyst of 500g5wt%; adding sulphuric acid makes hydrogenation reaction pH value control 2.0; after reaction does not absorb hydrogen; Filtration of catalyst; ion-exchange process removing dissolving salt, obtains the mixture of L-glucose and L-mannose.

2., according to the arbitrary described application of claim 1, it is characterized in that, described intestinal tract cleaning medicine is oral formulations.

3. application according to claim 2, is characterized in that, described intestinal tract cleaning medicine comprises the compositions 0.1wt% ~ 99.9wt% be made up of L-glucose and L-mannose, and water 0.1wt% ~ 99.9wt%.