Preclinical study of pharmacological activity of enterosorbente on the basis of montmorillonite

At present, enterosorbents based on mineral raw materials are in high demand among the population. However, there are no enterosorbents on the Russian pharmaceutical market on the basis of domestic mineral raw materials, to study the pharmacological activity of enterosorbent based on montmorillonite of Russian origin under experimental conditions. The methodological approach was based on the implementation of a complex of theoretical, pharmacological, toxicological, histological, biochemical, statistical methods. Models of experimental diarrhea, acute and toxic liver damage, acute experimental pancreatitis were selecte

Moxonidine-based combination antihypertensive therapy in patients with metabolic syndrome

Aim. To assess the effects of moxonidine-based combination therapy on clinical status, laboratory parameters, and target organs in patients with metabolic syndrome (MS). Material and methods. In total, 60 MS patients with Stage 1-2 arterial hypertension (AH) were randomised into 3 groups. Group I was administered moxonidine (0,2-0,4 mg/d) and amlodipine (5-10 mg/d); Group II received moxonidine (0,2-0,4 mg/d) and hydrochlorothiazide (12,5 mg/d); Group III was treated with moxonidine (0,2-0,4 mg/d) and enalapril (10-20 mg/d). At baseline and after 24 weeks of treatment, the following characteristics were assessed: waist circumference (WC), body mass index (BMI), 24-hour blood pressure monitoring (BMP) parameters, left ventricular myocardial mass index (LVMMI), E/A ratio, isovolumetric relaxation time (IVRT), deceleration time (DT) of early diastolic velocity, peak Em velocity at interventricular septum and lateral wall levels, E/Em ratio (myocardial tissue Doppler echocardiography), pulse wave velocity (PWV) between descending aorta and aortic bifurcation levels (ultrasound method), and stiffness index β of ascending aorta. In addition, lipid, carbohydrate, and purine metabolism parameters were assessed; glomerular filtration rate (GFR) was calculated (MDRD method); and urine albumin levels were measured. Results. In Group I (moxonidine + amlodipine), target blood pressure (BP) levels were achieved in 70% of the patients. Systolic BP (SBP) levels, LVMMI, and DT decreased by 19,3±11,4 mm Hg, 4,4 g/m2 (p=0,09), and 10,6 ms (p<0,05), respectively. The increase in E/A ratio and Em annular velocity (Em av) reached 0,4 (p<0,05) and 1,4 cm/s (p<0,05), respectively, while E/Em av ratio decreased by 0,8 (p<0,05), and PWV decreased by 1,6 ms (p<0,05). The BMI decrease reached 0,7 kg/m2 (p<0,05). In Group II (moxonidine + hydrochlorothiazide), target BP levels were achieved in 40% of the participants, with a decrease in SBP levels by 14,7 mm Hg (p<0,05). DT was reduced by 9,4 ms (p<0,05), E/A ratio increased by 0,1 (p<0,05), while PWV, BMI, and GFR decreased by 1,3 m/s (p<0,05), 0,8 kg/m2 (p<0,05), and 5,6 ml/min/1,73 m2 (p<0,05), respectively. In Group III (moxonidine + enalapril), 60% of the patients achieved target BP levels, and SBP levels were reduced by 21,1 mm Hg (p<0,05). LVMMI decreased by 5,1 g/m2 (p<0,05), Em av increased by 0,3 cm/s (p<0,05), while the respective reduction in PWV, WC, and BMI reached 1,1 m/s (p<0,05), 1,8 cm (p<0,05), and 0,5 kg/m2 (p<0,05). All three groups demonstrated a significant reduction in urine albumin levels. Conclusion. The moxonidine-based combination therapy effectively reduced the levels of BP and urine albumin. The combination of moxonidine with amlodipine or enalapril improved cardiac structure and function, as well as renal excretory function. The combination of moxonidine and hydrochlorothiazide, however, negatively affected renal excretion. All three variants of combination therapy were metabolically neutral and demonstrated beneficial effects on visceral obesity

Direct renin inhibitor aliskiren in women with menopausal metabolic syndrome and arterial hypertension

Aim. To study the effectiveness of a direct renin inhibitor, aliskiren, in patients with menopausal metabolic syndrome (MMS), and to assess aliskiren effects on blood pressure (BP), carbohydrate and lipid metabolism parameters, microalbuminuria, and arterial stiffness. Material and methods. The study included 23 women with MMS, to whom aliskiren monotherapy (150-300 mg/d) was administered. At baseline and in the end of the study, anthropometry, carbohydrate and lipid metabolism parameters assessment, 24-hour BP monitoring, and arterial stiffness assessment by volume sphygmography were performed. Results. By the end of the study, most parameters of circadian BP profile significantly decreased. Target levels of systolic and diastolic BP were achieved in 80 % of the patients. There was a significant reduction in postprandial glucose levels. According to the volume sphygmography results, a decrease in arterial stiffness was accompanied by a significant reduction in pulse wave velocity and augmentation index, with normalization of the former parameter. Conclusion. Aliskiren therapy demonstrated not only high antihypertensive effectiveness in MMS patients, but also a reduction in postprandial glucose levels and arterial stiffness

Physico-chemical properties of montmorillonite clays and their application in clinical practice (review)

The review is devoted to the medical application of montmorillonite clay minerals. Properties and mechanisms of action of enterosorbents. The properties of the enterosorbents include an absorption capacity and active surface. The mechanisms of action include the sorption of toxins in the gastrointestinal tract, the contact effect on the mucosa, enhancing the release of toxins in the gastrointestinal tract, increasing the metabolism and excretion of toxin

Perspectives of impaired glucose tolerance management in patients with metabolic syndrome

Aim. To assess the effectiveness of vildagliptin, its effects on visceral obesity (VO), carbohydrate and lipid metabolism parameters, and circadian profile (CP) of blood pressure (BP) in patients with metabolic syndrome (MS), Stage I arterial hypertension (AH), and impaired glucose tolerance (IGT). Material and methods. The study included 30 patients, aged 18-60 years (16 men and 14 women). All patients had IGT, VO, and Stage I AH. Previously prescribed antihypertensive therapy (AHT) was not modified after the start of the study. In all participants, carbohydrate and lipid metabolism parameters, BP CP, and body weight were measured at baseline and after 24 weeks of vildagliptin treatment. Results. Vildagliptin therapy was associated with a significant reduction in body weight, waist circumference, postprandial and fasting glucose levels, the levels of total cholesterol and low-density lipoprotein cholesterol, as well as with a sustained reduction in systolic and diastolic BP levels. Conclusion. Vildagliptin therapy resulted in weight reduction, improved carbohydrate and lipid profiles, and target BP achievement, without inducing hypoglycemia episodes

Preclinical study of pharmacological activity of enterosorbente on the basis of montmorillonite

At present, enterosorbents based on mineral raw materials are in high demand among the population. However, there are no enterosorbents on the Russian pharmaceutical market on the basis of domestic mineral raw materials, to study the pharmacological activity of enterosorbent based on montmorillonite of Russian origin under experimental conditions. The methodological approach was based on the implementation of a complex of theoretical, pharmacological, toxicological, histological, biochemical, statistical methods. Models of experimental diarrhea, acute and toxic liver damage, acute experimental pancreatitis were selecte

STUDY OF THE SORPTION ACTIVITY OF ENTEROSORBENT ON THE BASIS OF MONTMORILLONITEAGAINST THE E.coli ENTEROTHOXIN ON THE MODEL OF ISOLATED LOOPES OF THE INTESTINE

Aim. To study the sorption activity of enterosorbent based on montmorillonite under the laboratory cipher of Crim_04 against E.coli enterotoxin in vivo.Material and Methods. Isolated loops of the small intestine were formed in laboratory rats under anesthesia, and E. coli toxin was injected into the control loops at a dose of 2 μg/loop. The enterosorbent under the code Crim_04 in the form of water suspensions with concentrations of 50 mg/ml, 100 mg/ml and 200 mg/ml was injected into the lumen of the loops with toxin. After 4 hours, the expression of the fluid in the lumen of the intestine and its inhibition by the enterosorbent were evaluated. Comparison was Smekta.Results. The introduction of toxin into the lumen of the gut caused an increased fluid yield, the dilatation index for the control loops was 112,7±1,2 mg/cm versus 27,4±0,4 mg / cm in intact loops. The enterosorbent under the Crim_04 cipher exhibited a dose-dependent inhibitory effect on the fluid outlet into the lumen of the gut, at a concentration of 200 mg/ml, the dilation index was 31,6±0,8 mg / cm, inhibiting the fluid yield by 95,1%. This effect is confirmed morphologically, the morphometric parameters when using enterosorbent under the Crim_04 cipher are close to the level of intact loops.Conclusion. The montmorillonite-based enterosorbent under the laboratory cipher Crim_04 has a high sorption activity against the thermolabile cholera-like E. coli enterotoxin on the isolated bowel loop model