RU2313337C1 - Medicinal agent for treatment of chronic hepatitis b - Google Patents

Abstract

FIELD: medicine, hepatology.

SUBSTANCE: invention proposes a drug for treatment of chronic hepatitis B in the exacerbation stage based on using fumaric acid (tris-2-oxyethylammionium fumarate) triethylamine salt. This salt possesses antioxidant and immunomodulating properties, allows decreasing the level of autoimmune damage of liver cells. Effect of this drug has been studied by indices of intoxication syndrome in patients, decreasing bilirubin content and cytolysis enzymes.

EFFECT: valuable medicinal properties of drug.

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Description

The invention relates to the fields of organic chemistry, medicine, namely to pharmacology, a drug that can be used to treat chronic hepatitis B.

The use of tris-2-hydroxyethylammonium fumarate (triethanolamine salt of fumaric acid) in medicine in the treatment of iron deficiency anemia is known (1).

The use of triethanolamine salt of fumaric acid in medicine in the treatment of chronic hepatitis B is unknown.

The objective of the invention is to expand the treatment of chronic hepatitis B through the use of a new drug - triethanolamine salt of fumaric acid.

This task is achieved by the use of triethanolamine salt of fumaric acid as a medicine for the treatment of chronic hepatitis B in the acute stage.

Tris-2-hydroxyethylammonium fumarate, a triethanolamine salt, is a derivative of fumaric acid, which is obtained by reacting fumaric acid with triethanolamine hydrochloride in a neutral medium.

General formula: C ₁₀ H ₁₈ O ₇ N

Structural formula:

Molecular mass: Mm = 264.

The triethanolamine salt of fumaric acid is a white crystalline substance, practically non-hygroscopic, with a melting point of 100 ° C, highly soluble in water, non-toxic.

It is used as a solution in water, powders and tablets.

The effectiveness of the drug triethylamine salt of fumaric acid is shown in the following examples.

Patient K., 26 years old. Diagnosis: chronic hepatitis B, integrative type, with impaired liver function, during the period of exacerbation, she was in the infectious ward from 01/11/2006 to 01/23/2006. Complaints of weakness, loss of appetite, sleep disturbance, nausea, vomiting, pain in the right hypochondrium, ictericity of the skin, sclera, lightening feces, darkening of urine. Blood pressure - 140/85.

Table 1 shows the results of the analysis of patient K.

Table 1. Analysis Upon enrolment At discharge Total bilirubin, mmol / l 30.5 7.6 Direct bilirubin, mmol / l 14.0 No Indirect bilirubin, mmol / l 16.5 7.6 AlST, mmol / l 2,31 0.47 AsAT, mmol / l 0.75 0.29 Thymol test, units 2.0 4.0 Cholesterol, mmol / L 5.3 3,5 B-lipoproteins, g / l 2.9 2,4 Total protein, g / l 85.0 87.0 Blood sugar, mmol / l 5,0 4.2 Blood diastasis 16,0 20,0 Prothrombin index,% 87 112 HB, g / l 116 123 Red blood cells 3,5 × 10 ¹² / l 3.9 × 10 ¹² / L ESR, mm / h thirty 10 White blood cells 8.0 × 10 ⁹ / L 7.6 × 10 ⁹ / L Reticulocytes 7 6 Beats urine weight 1010 1020 protein No No White blood cells, epithelium (in sight) single single

Prescribed treatment: triethalonamine salt of fumaric acid 0.1 grams three times a day - five days, then 0.3 grams three times a day - five days. Additionally, antiviral, restorative, detoxification drugs, and a protective regimen were prescribed.

While taking this therapy, the patient has a significant decrease in intoxication syndrome, normalization of blood bilirubin level on the 4-7th day of treatment, decrease in cytolysis enzymes, normalization of organoleptic properties of urine and feces, normalization of skin color. All these symptoms of exacerbation of chronic hepatitis B stopped much faster than without taking the drug triethalonamine salt of fumaric acid.

For comparison, we present the results of treatment of a patient without the use of triethanolamine salt of fumaric acid, carried out according to the standard treatment regimen.

Patient P., 36 years old. Diagnosis: chronic hepatitis B, integrative type, with impaired liver function, was in the infectious ward during the period of exacerbation from 01/05/2006 to 01/16/2006. Complaints of weakness, loss of appetite, sleep disturbance, nausea, vomiting, right pain hypochondrium, ictericity of the skin, sclera, lightening feces, darkening of urine. Blood pressure - 130/75.

Table 2 shows the results of analyzes of patient P.

Table 2. Analysis Upon enrolment At discharge Total bilirubin, mmol / l 30.5 24.9 Direct bilirubin, mmol / l 10.0 4.1 Indirect bilirubin, mmol / l 25.0 20.5 AlST, mmol / l 1.85 1.31 AsAT, mmol / l 0.75 0.51 Thymol test, units 4,5 4.0 Cholesterol, mmol / L 4.3 3.0 B-lipoproteins, g / l 2.9 3.4 Total protein, g / l 65.0 70.0 Blood sugar, mmol / l 4.0 4.2 Blood diastasis 20,0 19.0 Prothrombin index,% 80 105 HB, g / l 136 134 Red blood cells 3.4 × 10 ¹² / L 4.0 × 10 ¹² / L ESR 5 four White blood cells 5.1 × 10 ⁹ / L 4.6 × 10 ⁹ / L Reticulocytes 9 6 Beats urine weight 1010 1020 Protein No No White blood cells, epithelium (in sight) single single

Thus, incomplete remission of this symptom is noted, in particular, a decrease in total bilirubin by less than 20%, preservation of the level of indirect bilirubin, symptoms of intoxication, ictericity of the skin and sclera, and the level of hepatocyte cytolysis enzymes.

An exacerbation of the chronic inflammatory process in the liver depends on the general condition of the body, a decrease in its immunobiological reactivity, and the level of autoimmune damage to the liver.

The new drug, the triethanolamine salt of fumaric acid, which has antioxidant and immunomodulating properties, can reduce the level of autoimmune damage to liver cells and significantly reduce hospitalization time and financial costs of treatment.

The action of the drug - triethanolamine salt of fumaric acid - was studied in 30 patients with a diagnosis of exacerbation of chronic hepatitis B. In all cases, all symptoms of chronic hepatitis B stopped much faster than without taking the proposed drug - triethanolamine salt of fumaric acid.

Information sources

1. RF patent No. 2197962, A61K 31/205 "Drug for the treatment of iron deficiency anemia", 02/10/2003, BI No. 4, 2003 - prototype.

Claims (1)

The use of triethanolamine salt of fumaric acid as a medicine for the treatment of chronic hepatitis B in the acute stage.