CN1331476C - Method for preparing coenzyme-A sublingual lozenge - Google Patents

Abstract

The present invention discloses a preparation method for a sublingual buccal tablet containing coenzyme A, which is prepared from coenzyme A, an antioxidant and medicinal auxiliary materials. Blank granules and the coenzyme A are uniformly mixed and compressed into tablets. The preparation method solves the problems that coenzyme A for injection is not convenient for use for a long period of time and the activity of oral coenzyme A is easy to damage when the oral coenzyme A passes through gastrointestinal tracts; thus, the coenzyme A can be conveniently used for preventing and treating various metabolic disorder diseases, (such as hyperlipemia, adiposis, fatty liver, and the like.), cardiovascular disease and alcoholism which are caused by the shortage of the coenzyme A. The sublingual buccal tablet containing coenzyme A has very good development and application prospects.

Description

A kind of coenzyme-A sublingual lozenge and preparation method thereof

Technical field

The invention belongs to medicine, health product, new resource food technical field, be specially a kind of manufacture method and application of coenzyme-A sublingual lozenge.

Technical background

Coenzyme A is a kind of natural biochemical substances that extensively is present in animal, plant, microorganism cultures and cell, has no side effect.Its molecule by pantothenic acid, Mercamine Cysteamine and 3 ', 5 '-adenosine diphosphate (ADP) forms, and is soluble in water, is insoluble to ethanol, acetone and other organic solvent, more stable, but in the presence of alkalescence, high temperature, oxidant easy inactivation.Coenzyme A is the coenzyme of acetylization reaction in the organism; sugar, lipid and proteinic metabolism in the body are played an important role; as synthetic, the reduction of cholesterol of the accumulating of tricarboxylic acid cycle, hepatic glycogen, acetylcholine and the adjusting of blood plasma lipide content, synthetic (aldosterone, hydrocortisone and the gonadal hormone) of steroid hormone etc.; also but activating immune system does not have internal metabolism to detoxifcation, the formation of promotion connective tissue and the reparation etc. of harmful substance without coenzyme A.Coenzyme A lacks in the body, all kinds of diseases that will cause Developmental and Metabolic Disorder to cause.Clinical hyperlipemia, fatty liver, obesity, arteriosclerosis, myocardial infarction, thrombocytopenic purpura, leukopenia, the nephrotic syndrome, diabetes acidosis, the alcoholism of being used for, also can treat acne, the speckle etc. that discolors is a kind of important biochemical drug, health product.Because the easy oxidation inactivation of coenzyme A and in intestinal destructible, coenzyme A can only be by injection administration so far, and when preventing, treating metabolic imbalance class disease, the course of treatment is long, drug administration by injection is very inconvenient, has limited the extensive use of coenzyme A.

Summary of the invention

The present invention enriches medicine according to hypoglossis mucous membrane and absorbs easily and the little characteristics of coenzyme A dosage, adopt suitable antioxidant, correctives and adjuvant that coenzyme A is made and be easy to the sublingual lozenge that absorbs and utilize, overcome the difficult problem of coenzyme A drug administration by injection inconvenience and oral destructible, but make coenzyme A long-term prescription, extensive use, have a extensive future.

The invention provides a kind of coenzyme-A sublingual lozenge preparation method.

Coenzyme-A sublingual lozenge of the present invention is made up of active component coenzyme A and adjuvant antioxidant, diluent, adhesive, lubricant, fluidizer.

The used coenzyme A of coenzyme-A sublingual lozenge of the present invention can be derive from that animal livers, heart extract, yeast extracts or microbial fermentation.Antioxidant can be a kind of of vitamin C, cysteine, glutathion or it is several compound, diluent can be a kind of of sucrose, glucose, lactose, mannitol or it is several compound, adhesive is a 30 POVIDONE K 30 BP/USP 30, and lubricant is a polyethylene glycol 6000, and fluidizer is micropowder silica gel.

The antioxidant vitamin C has another name called ascorbic acid in the above-mentioned adjuvant, is that human life institute is essential, can make medicine and can make health food again, mainly makes antioxidant in this coenzyme-A sublingual lozenge, can make acidulant, correctives again.Cysteine, glutathion are the amino acids nutrient substance, all contain sulfydryl, can make antioxidant and nutrient substance.Diluent sucrose, glucose, the easy compression molding of lactose easily dissolve in the Sublingual, and pleasantly sweet, mouthfeel is good, also can make correctives.Polyvidone not only is easy to granulate, and also is easy to buccal tablet and is bonding on the Sublingual.Polyethylene Glycol, micropowder silica gel are easy to tabletting as lubricant and fluidizer, and mouthfeel is good.

Every of above-mentioned coenzyme-A sublingual lozenge contains coenzyme A 10-10000U, and the adjuvant ratio of components is: antioxidant 10%-50%, diluent 50%-80%, 30 POVIDONE K 30 BP/USP 30 0.1%-1.5%, polyethylene glycol 6000 1%-5%, micropowder silica gel 0.1%-15%.

Above-mentioned coenzyme-A sublingual lozenge adopts blank pelletizing press sheet technology, contains following operation successively:

1) coenzyme A is passed with antioxidant doubly diluted 10-20 doubly, standby;

2) diluent was pulverized 100 mesh sieves, standby;

3) it is an amount of that inventory 30 POVIDONE K 30 BP/USP 30 adds 70% ethanol, and stirring and dissolving is standby;

4) diluent, antioxidant were mixed in mixer 20 minutes by the prescription proportioning according to inventory, stir slow down solvent 30 POVIDONE K 30 BP/USP 30 solution that add, mix the system soft material;

5) soft material is granulated with 18 mesh sieves, and particle requirement is evenly loose, sabot;

6) wet grain is put drying in the 50-60 ℃ of baking oven, notes turning over, and makes oven dry evenly, and moisture Control is at 5 5%-7%;

7) dry granular takes out the back and crosses 20 mesh sieve granulate, makes blank granule;

8) will dilute good coenzyme A and polyethylene glycol 6000, micropowder silica gel adds in the blank granule mix homogeneously, sample examination, tabletting by proportioning according to inventory;

9) pick test, qualified back packing.

Use a kind of coenzyme-A sublingual lozenge of the present invention's preparation, every contains coenzyme A 200 units, as follows to treatment hyperlipidemia (triglyceride TG, cholesterol TC) and fatty liver result of the test.

1. treatment hyperlipidemia

Object: select hyperlipemic patients for use, i.e. triglyceride TG 〉=2.1mmol/l or serum cholesterol TC 〉=5.2mmol/l person's 46 examples, male's 28 examples wherein, women's 18 examples, age 30-73 year.

Method: 1 of everyone each sublingual administration, sooner or later respectively once, 12 weeks of the course of treatment.

Lipid determination: before using coenzyme-A sublingual lozenge, reached for the 4th, 8,12 weekends, 12-14 hour on an empty stomach, venous blood samples, in time separation of serum is measured serum cholesterol and content of triglyceride, and measuring blood pressure, liver function and blood glucose.

The result: use coenzyme-A sublingual lozenge after the 4th, 8,12 weeks, triglyceride TG has on average descended 9.1%, 12.2%, 13.9% than with preceding difference, and serum cholesterol TC has on average descended 7.5%, 17.1%, 21.3% than with preceding difference, the effect highly significant.After 46 examples used for 12 weeks, triglyceride TG descended and surpasses 1.0mmol/l person's 35 examples, and effective percentage reaches 76%, and serum cholesterol descends and surpasses 2.0mmol/l person's 30 examples, and effective percentage reaches 65%.Data see Table 1.

Table 1: coenzyme-A sublingual lozenge is to the influence of hyperlipemic patients

Blood lipids index	Case	Meansigma methods before the treatment	The 4th weekend meansigma methods	Reduce %	The 8th weekend meansigma methods	Reduce %	The 8th weekend meansigma methods	Reduce %
									TG (mmol/l)	46	3.020	2.745	9.1	2.651	12.2	2.598	13.9
TC (mmol/l)	46	7.705	7.127	7.5	6.39	17.1	6.108	21.3

2. treatment fatty liver

Patients with Fatty Liver 16 examples, 1 of everyone each sublingual administration, each once adopts the abdominal CT inspection 6 months courses of treatment sooner or later, and 9 routine fatty livers disappear, and other case all significantly improves.

The specific embodiment

Example 1: coenzyme A 1,000,000 U

Vitamin C 200g

Sucrose 500g

Lactose 300g

Polyethylene glycol 6000 10g

Micropowder silica gel 5g

30 POVIDONE K 30 BP/USP 30 4.5g

Make 10000

Example 2: coenzyme A 2,000,000 U

Vitamin C 200g

Sucrose 500g

Lactose 200g

Polyethylene glycol 6000 10g

Micropowder silica gel 5g

30 POVIDONE K 30 BP/USP 30 4.5g

Make 10000

Example 3: coenzyme A 2,000,000 U

Glutathion 100g

Sucrose 600g

Lactose 200g

Polyethylene glycol 6000 20g

Micropowder silica gel 6g

30 POVIDONE K 30 BP/USP 30 5g

Make 10000

Example 4: coenzyme A 2,500,000 U

Glutathion 100g

Vitamin C 200g

Sucrose 500g

Lactose 200g

Polyethylene glycol 6000 20g

Micropowder silica gel 6g

30 POVIDONE K 30 BP/USP 30 6g

Make 10000

Example 5: coenzyme A 3,000,000 U

Glutathion 100g

Vitamin C 200g

Lactose 400g

Glucose 300g

Polyethylene glycol 6000 20g

Micropowder silica gel 6g

30 POVIDONE K 30 BP/USP 30 6g

Make 10000

Example 6: coenzyme A 3,000,000 U

Cysteine 100g

Vitamin C 200g

Lactose 800g

Glucose 300g

Polyethylene glycol 6000 20g

Micropowder silica gel 8g

30 POVIDONE K 30 BP/USP 30 8g

Make 10000

Claims (3)

1. a coenzyme-A sublingual lozenge is characterized by described coenzyme-A sublingual lozenge, and every contains coenzyme A 10-10000U, the adjuvant ratio of components is: antioxidant 10%-50%, diluent 50%-80%, 30 POVIDONE K 30 BP/USP 30 0.1%-1.5%, polyethylene glycol 6000 1%-5%, micropowder silica gel 0.1%-1.5%.

2. coenzyme A Sublingual tablet according to claim 1 is characterized by: antioxidant is one or more in the plain C of dimension dirt, cysteine, the glutathion; Diluent is one or more in sucrose, glucose, lactose, the mannitol.

3. the preparation method of the coenzyme A Sublingual tablet of a claim 1 comprises the steps:

1) coenzyme A is passed with antioxidant doubly diluted 10-20 doubly, standby;

2) prepare blank granule

A, diluent was pulverized 100 mesh sieves, standby;

It is an amount of that B, 30 POVIDONE K 30 BP/USP 30 adds 70% ethanol, and stirring and dissolving is standby;

C, diluent, antioxidant were mixed in mixer 20 minutes, stir and slowly add solvent 30 POVIDONE K 30 BP/USP 30 solution down, mix the system soft material;

D, soft material are granulated with 18 mesh sieves, and particle requirement is evenly loose, sabot;

E, wet grain are put in the 50-60 ℃ of baking oven dry, note turning over, and make oven dry evenly, and moisture Control is at 5%-7%;

F, dry granular take out the back and cross 20 mesh sieve granulate, make blank granule;

3) will dilute good coenzyme A and polyethylene glycol 6000, micropowder silica gel adds in the blank granule mix homogeneously, sample examination, tabletting by proportioning according to inventory;

4) pick test, qualified back packing.