CN-121987582-A - Tiopronin composition and preparation method thereof

Abstract

The invention belongs to the technical field of medicines, and particularly relates to a tiopronin composition and a preparation method thereof. The composition is an enteric-coated tablet, and consists of a tablet core and an enteric-coated layer, wherein the tablet core contains tiopronin, porous starch, chitosan, vitamin C and other pharmaceutically acceptable fillers, binders, disintegrants and lubricants. The tablet prescription can reduce the impurity content of a preparation product, improve the stability, improve the dissolution rate of tiopronin, has uniform content, effectively covers bad smell, is beneficial to improving the compliance of patients and the like, and the preparation method of the composition is simple and is suitable for industrial production.

Inventors

• CHEN JISONG
• LI XIAOFENG
• CHEN XINGYU
• XU JUNLAN

Assignees

• 泰州市第四人民医院

Dates

Publication Date

20260508

Application Date

20260403

Claims (9)

1. 1. An enteric-coated tiopronin tablet is characterized in that the enteric-coated tablet consists of a tablet core and an enteric coating layer, wherein the tablet core contains tiopronin, porous starch, chitosan, vitamin C and other pharmaceutically acceptable fillers, binders, disintegrants and lubricants.
2. 2. The enteric coated tablet according to claim 1, wherein the tablet core contains tiopronin, porous starch, chitosan, vitamin C, filler, adhesive, disintegrating agent and lubricant in a mass ratio of 1 (1-5): (1.2-1.4): (0.2-0.4): (0.1-0.2): (0.03-0.1): (0.05-0.1): (0.02-0.05).
3. 3. Enteric coated tablet according to claim 1, wherein the porous starch has a particle size of 10-20 mm and a pore size of 1-2 mm.
4. 4. The enteric coated tablet of claim 1, wherein the filler is selected from one or more of lactose, microcrystalline cellulose, pregelatinized starch, dextrin, sorbitol, sucrose.
5. 5. Enteric coated tablet according to claim 1, wherein the binder is selected from one or more of hypromellose, hydroxypropyl cellulose, povidone K30 and pre-cross-linked starch, preferably povidone K30.
6. 6. Enteric coated tablet according to claim 1, wherein the disintegrant is selected from one or more of croscarmellose sodium, low substituted hydroxypropylcellulose, crospovidone, calcium carboxymethylcellulose and starch, preferably croscarmellose sodium.
7. 7. The enteric coated tablet of claim 1, wherein the lubricant is one or more of magnesium stearate, calcium stearate, talc, sodium stearyl fumarate, preferably magnesium stearate.
8. 8. The enteric coated tablet according to claim 1, wherein the enteric coated layer is prepared by weighing the Ophioglossow enteric coated powder PVAP (with pH of not less than 5) and adding into 90% ethanol water solution, stirring, and sieving with 40 mesh sieve to obtain coating solution (solid content of 15%).
9. 9. The enteric-coated tablet according to any one of claims 18, wherein the enteric-coated tablet is prepared by the steps of (1) dissolving tiopronin with a prescription amount in an appropriate amount of ethanol solution, then adding porous starch with a particle size of 10-20 μm and a pore diameter of 1-2 mm, fully stirring and adsorbing, volatilizing ethanol at 40-50 ℃ to obtain precipitate, adding the precipitate into an aqueous solution of chitosan and vitamin C with a prescription amount, stirring uniformly, and then drying at 40-50 ℃ to obtain the precipitate, namely the coated tiopronin; (2) Crushing the precipitate obtained in the step (1), granulating, adding a filler and a disintegrating agent, uniformly mixing, adding an adhesive aqueous solution into a wet granulator under high-speed stirring and shearing to prepare a soft material, granulating, drying and granulating; (3) Uniformly mixing the granulated particles with a lubricant, and tabletting; (4) And coating the obtained tablet with enteric coating to obtain the tiopronin enteric coated tablet.

Description

Tiopronin composition and preparation method thereof Technical Field The invention belongs to the technical field of medicines, and particularly relates to a tiopronin composition and a preparation method thereof. Background Tiopronin (Tiopronin) is a mercapto glycine derivative, and is known as N- (2-mercaptopropionyl) -glycine. Tiopronin is a compound developed by japan asian pharmaceutical co. The effect and effect of increasing mercury excretion in early senile cataract and mercury poisoning were added in 1979, and the re-evaluation in 1995 was completed, which was the earliest in 1964 on Japanese market under the trade name Thiola. Tiopronin tablet with the trade name Thiola cubic standard of 100mg and the certification carrier Mylan Pharmaceutical co, ltd,2023, 7 months, the certification carrier is transferred from the company of michelia pharmaceutical limited to the company of veratric pharmaceutical (VIATRIS) for production and sale. Because the tiopronin raw material has specific odor and strong acidity, most of the oral medicines on the market are enteric-coated tablets at present so as to relieve the acidic stimulation to the stomach. Because the specific odor is strong, most of the products sold on the market at present can not effectively cover the odor, so that patients can generate contradiction to taking the medicine, and the medicine is not beneficial to the patients. The mode of increasing the thickness of the enteric coating has a certain effect on masking specific odor, but is not obvious, and meanwhile, the enteric coating tablet is slowly dissolved out, so that the quality of the medicine cannot be ensured. CN200810113707.8 provides a preparation method of tiopronin enteric-coated tablet. The method comprises the steps of preparing tiopronin tablets, plain tablet coating isolation coating, enteric coating and the like. The starch slurry has a lighter taste than granules prepared by using other binders, ethanol and other granulating processes, and meanwhile, the film coating material is used as an isolating layer, so that the smell of raw materials can be effectively covered. CN201110420627.9 provides a tiopronin enteric capsule prescription and a preparation process thereof, so as to be more suitable for clinical needs and convenient for patients to take. The invention also provides a preparation process of the tiopronin enteric capsule. The tiopronin enteric capsule prepared by the process of the invention is insoluble in gastric juice, and is released in the intestinal tract in a positioning way, so that the gastrointestinal reaction of the tiopronin can be lightened, and the damage of the tiopronin in gastric juice can be reduced. CN201210209115.2 discloses a tiopronin enteric coated tablet and a preparation method, and is characterized in that the tiopronin enteric coated tablet (per 1000 tablets) comprises 96.5-108.0 g of tiopronin, 58.0-64.5 g of microcrystalline cellulose, 32.0-38.5 g of lactose, 6.8-7.6 g of crospovidone, a proper amount of povidone k30 (9% -11% ethanol solution), 2.7-3.3 g of magnesium stearate, 1.8-2.2 g of silicon dioxide, 11.6-14.0 g of coating powder and 140.0-158.5 g of 75% -85% ethanol (w/w). According to the preparation method of the tiopronin tablet provided by CN201410017138.2, the auxiliary materials, namely the diluent and the disintegrating agent, are granulated by using the adhesive and then dried, and then the tiopronin raw materials and the additional auxiliary materials are added for mixing and tabletting, so that the active ingredients in the tiopronin can be prevented from being damaged by damp and heat in the traditional wet granulation process, the good stability of the medicine is maintained, the problem that the traditional wet granulation process is not suitable for producing the tiopronin tablet is solved, and the preparation method of the tiopronin tablet is low in production cost and simple to operate. CN202310720675.2 provides a pharmaceutical composition containing tiopronin with excellent stability and a preparation process thereof, wherein the pharmaceutical composition with excellent stability is a tablet, and comprises cysteine hydrochloride or cysteine serving as an antioxidant, and corn starch with water content not higher than 5.0% accounting for not lower than 0.1% of the prescription weight. In addition, the preparation process of the medicinal composition is also disclosed. The technical scheme of the invention effectively solves the problem of rapid growth of dithio impurities. Compared with the existing tiopronin enteric-coated tablet, the provided tiopronin enteric-coated tablet has the advantages of common tablets and pellets, is accurate in dosage, is beneficial to swallowing, can improve patient compliance, and has good application prospect. CN202510753572.5 relates to a composition containing sulfur and protamine, its preparation method and application. According to the invention, the tablet core with extremely lo