Mg Of Acarbose Research Articles

The efficacy and tolerability of intermittent prandial acarbose to reduce glucose spikes in healthy individuals

Acarbose is an α-glucosidase inhibitor that slows the digestion of carbohydrates and can prevent sharp increases in blood sugar levels after meals (spikes). Excessive postprandial blood glucose spikes have been associated with chronic conditions, increase all-cause mortality, and may contribute to aging. Therefore, the prevention of glucose spikes may contribute to the preservation of human healthspan. Indeed, acarbose has been associated with increased lifespan in animal models. However, its tolerability profile has limited acarbose use in healthy individuals. We hypothesized that using low-dose acarbose right before the occasional high-carbohydrate meal may prevent glucose spikes in healthy individuals. We performed a prospective clinical study to evaluate the tolerability and efficacy of acarbose in healthy individuals. Participants were randomized into two arms, each performing two control tests and two treatment tests. Continuous glucose monitor (CGM) measurements were collected for 2 h after high carbohydrate meals with or without pre-meal 50 mg acarbose intake. Tolerability was assessed using questionnaires. Twelve patients had evaluable results. Acarbose pretreatment resulted in reductions in CGM glucose measurements, with a significant decrease in glucose levels at the start, after 15 min, and at peak glucose levels. Few participants reported acarbose adverse events, and these included flatulence, bloating, nausea, abdominal pain, and stomach aches. No statistical difference in tolerability was detected between periods with and without acarbose. In conclusion, treatment with 50 mg of acarbose before meals was found to be well tolerated and efficacious in blunting the postprandial glucose spike by over 17% in healthy individuals.

Protein hydrolysates of a probiotic strain of Lactobacillus plantarum as new promising sources of inhibitors for diabetes regulatory enzymes

Diabetes is a chronic metabolic disorder characterized by persistent hyperglycaemia. It has been classified as one of the main pathologies that promotes the most severe and fatal forms of COVID-19. Although there are nowadays synthetic molecules for the regulation of this disease, their disastrous side effects still open up prospects for the search of new and healthy molecules of therapeutic interest. This study aimed at evaluating the inhibitory effect of peptides extracts produced during the cultivation of a Lactobacillus plantarum strain with probiotic properties. The peptides extracts were obtained by thermal hydrolysis of protein extracts at 70°C or 80°C for 10, 20 and 30 min. The potential hypoglycaemic activity was examined by testing their inhibitory effect on amylolytic enzymes. Our results showed that the studied proteins hydrolysates, when used at 0.024 mg (biomass) or 0.156 mg (growth broth), were capable of total inhibition of amylolytic enzymes activity. The biomass peptides showed higher inhibition rate compared to 95% obtained with 0.050 mg of acarbose, a potent and widely used anti-diabetic inhibitory. This study clearly shows that the investigated protein hydrolysates contain interesting inhibitory peptides that deserve further investigations for their real use as bioactive inhibitors of diabetes regulating enzymes.

Pharmacodynamic comparison of acarbose tablets in Chinese healthy volunteers under chewing and swallowing conditions.

Acarbose can efficiently block glucose absorption in the intestine as an alpha-glucosidase inhibitor. It is currently manufactured in several oral dosage forms, with the most common types being tablets and chewable tablets. The acarbose tablet (Glucobay® , 50mg, Bayer) package insert gives instructions for either directly swallowing or chewing then swallowing. This study compared the pharmacodynamic effects of a single formulation of acarbose tablets under these two different administration routes. This randomized, crossover study enrolled 24 healthy subjects who were instructed to chew (C group) or swallow (S group) the acarbose tablet. Glucose levels were monitored in subjects for up to 4h following administration of 75g of sucrose to establish a baseline firstly, after which subjects in the C and S groups were administered 50- or 100-mg of acarbose along with 75g of sucrose. Then, subjects entered a 1-week washout period before being crossed over to the alternate dosing route. Compared with the S group, the C group had a lower maximum concentration of serum glucose (Cmax ) and areas under the concentration-time curve (AUC0-2 , AUC0-1.5 ). In addition, the maximum reduction in serum glucose (ΔCmax ) and the reduction in the AUC (AUEC0-1.5 ) were both increased in the S group. This occurred at both the 50mg and 100mg dosages. These results indicate that fluctuations in blood glucose were lower following chewing of the acarbose tablet. Both administration routes exhibited similar safety and tolerance profiles. In summary, chewing acarbose tablets appears to induce a superior glycaemic-controlling effect compared with swallowing them directly, at least with a single dose. It will be important to inform both clinicians and patients about these differences between the two administrations so that informed clinical decisions can be made, as numerous patients with diabetes are inclined to directly swallow acarbose tablets for convenience.

Antihyperglicemic effectiveness comparison of ethanol extract of soursop leaf (Annona muricata L.) againts acarbose in streptozotocin-induced diabetic white rats

Type 2 diabetes mellitus is major health problem worldwide, including in Indonesia. Acarbose, an alpha glucosidase inhibitor, is one of oral pharmacologic management commonly used in clinical practice with potent side effect in long-term use. Flavonoid-and-tannins containing soursop leaf can stimulate insulin secretion and repair beta pancreatic cell dysfunction. This study was aimed to investigate the comparison on antihyperglycemic effect between ethanol extract of soursop leaf (Annona muricata L.) and acarbose in streptozotocin-induced diabetic white rats. This sudy was experimental research with pre- and post-test control group design enrolling 30 hyperglycemic white male rats. They were divided into 2 control groups (C(+) was given by aquades and C(-) was given by acarbose) and 3 treatment groups (P1 was given 10 mg/200gBW extract, P2 was given 20 mg/200gBW extract, and P3 was given 30 mg/200gBW extract). Data analysis was using paired-T test. This study showed that there is a significant decrease in blood glucose levels in P1, P2, and P3 (95.08 mg/dL, 113.31 mg/dL, and 125.17 mg/dL; p<0.05). Ethanol extract of soursop leaf has antihyperglycemic effect in dose-dependent response. The 30 mg of ethanol extract of soursop leaf is not inferior to 1.8 mg of acarbose in antihyperglycemic effect.

Use of almond shell as food ingredient

Almond shell is a major waste from the almond processing industry. Its feasibility as natural source of health-promoting components was examined. The by-product was fractionated under basic conditions following an easy scale-up process. The chemical composition of the recovered fraction and its antioxidant and antidiabetic properties were evaluated. Novel information regarding the chemical composition of the polysaccharides was also obtained. Almond shell is formed by lignin-carbohydrate complexes possessing antioxidant properties and capacity to inhibit α-glucosidase. According to our knowledge, this is the first time α-glucosidase inhibitory activity of a lignin-carbohydrate complex is reported. Biscuits containing non-caloric sweetener soluble (2.5%) and insoluble (5.6%) dietary fiber, natural antioxidants (1.34 mg of gallic acid equivalents/g) and α-glucosidase inhibitors (1 g of biscuit–1 mg of acarbose) achieved a high sensorial score (7.2 out of 9) when almond shell was incorporated to them. The application of a fraction from almond shell containing lignin-polysaccharides complexes as food ingredient in biscuit formulations for people with particular nutritional requirements is feasible and new.

Effect of Acarbose Therapy Once or Twice a Day on Glycemic Control in Japanese Patients with Type 2 Diabetes

A possible reason for poor adherence to α-glucosidase inhibitor (αGI) therapy is the three times daily dosing regimen. Up to now, no investigations on αGI therapy starting with a once or twice daily dosing in Japanese type 2 diabetic patients have been reported. We assessed the improvement of blood glucose by administration of acarbose once or twice daily. At first, the patients were directed to take 50 mg of acarbose once daily just before meal. After one to three months, drug taking was increased to 50 mg twice daily just before meal. HbA1c and glycoalbumin (GA) levels were measured. Ten out of 14 patients completed 3 months of treatment. After 3 months, HbA1c decreased significantly compared with before treatment and after 1 month of treatment. After 3 months, GA decreased significantly compared with before treatment. Achievement of good glycemic control while maintaining compliance is considered possible by employing the acarbose regimen used in this study.

Acarbose Improves Hypoglycaemia Following Gastric Bypass Surgery Without Increasing Glucagon-Like Peptide 1 Levels

Postprandial hypoglycaemia is a severe complication of Roux-en-Y gastric bypass (RYGBP). Acarbose, an α-glucosidase inhibitor (AGI), is employed in its treatment. Several studies have shown that AGIs increase the postprandial levels of glucagon-like peptide 1 (GLP-1). However, an excessive level of GLP-1 is one of the factors involved in the physiopathology of this condition. We analysed the effect of acarbose oral administration in eight RYBGP patients with clinically significant hypoglycaemia or dumping syndrome. Glucose, insulin and GLP-1 plasma levels in fasting and after ingestion of a standard meal (Ensure Plus®; 13g protein, 50g carbohydrate, 11g fat) were measured. The test was repeated the following week with the oral administration of 100mg of acarbose 15min prior to the meal. Five patients developed asymptomatic hypoglycaemia during the test (glucose level <50mg/dl) with inappropriately high insulin levels and exaggerated GLP-1 response. Acarbose ingestion avoided hypoglycaemia in all of the patients and increased the lowest plasma glucose level (46.4 ± 4.8 vs. 59.0 ± 2.6mg/dl, p < 0.01). Acarbose ingestion decreased the area under the curve for serum insulin and GLP-1 levels at 15min after the meal. Acarbose avoided postprandial hypoglycaemia following RYGBP by decreasing the hyperinsulinemic response. This was associated with a decrease in early GLP-1 secretion, in contrast to that observed in non-surgical subjects. This finding could be explained by the reduction of glucose load in the jejunum produced by the α-glucosidase inhibition, which is the main stimulus for GLP-1 secretion.

Effects of Acarbose Treatment on Markers of Insulin Sensitivity and Systemic Inflammation

This study assessed the effect of postprandial glucose reduction by acarbose on insulin sensitivity and biomarkers of systemic inflammation. This was a single-center, double-blind, randomized, placebo-controlled, crossover study <40 weeks in duration, involving 66 subjects with varying degrees of glucose tolerance. Eligible patients completed a 3-week run-in period and were randomized to receive either 100 mg of acarbose three times daily followed by placebo, or vice versa, lasting 12 weeks each with a 12-week washout between interventions. Liquid meal challenges and hyperinsulinemic-euglycemic glucose clamp were performed at weeks 0, 12, 24, and 36. Fasting proinsulin levels and proinsulin-to-adiponectin ratios but not fasting adiponectin levels were significantly lower during acarbose versus placebo treatment. Clamp-derived insulin sensitivity index and body weight were unchanged by the intervention. Levels of fasting insulin, fasting glucose, monocyte chemoattractant protein-1, interleukin-6, and interleukin-1β were comparable between treatments. In the liquid meal challenge tests, postprandial glucose and insulin responses were significantly lower during acarbose versus placebo treatment. The effects of acarbose on the reduction of fasting proinsulin was most pronounced in subjects with impaired fasting glucose/impaired glucose tolerance (n = 24). Reduction of the glycemic load by acarbose decreased fasting levels of proinsulin but had no effect on adiponectin and whole-body insulin sensitivity as well as biomarkers reflecting inflammation. The preventive effects of acarbose on type 2 diabetes mellitus and cardiovascular risk need further investigation and cannot be explained by changes of insulin resistance and inflammatory biomarkers.

Comparison of Adverse Gastrointestinal Effects of Acarbose and Miglitol in Healthy Men: A Crossover Study

The incidence of the gastrointestinal adverse effects is important to determine as these effects are the reason for lower compliance of alpha-glucosidase inhibitors (alphaGIs). There has been no direct investigation of the adverse effects with acarbose or miglitol, therefore we compared them in healthy subjects. Twenty-two healthy men were administered 75 mg of miglitol or 100 mg of acarbose per every meal for three days. After four drug-free washout days, they were administered 100 mg of acarbose or 75 mg of miglitol per every meal, respectively. They reported the state of their stool, borborygmi, abdominal bloating, flatus, and abdominal pain on the 1st and 3rd day. Stool tended to be soft when miglitol was administered and to be firm when acarbose was administered. The flatus score of acarbose was greater than that of miglitol. The abdominal bloating score of acarbose was greater than that of miglitol on the 1st day. Our results suggest that if diabetic patients have constipation, firm stool, or flatus they may be administered miglitol and if they have diarrhea or soft stool they may be administered acarbose.

Acarbose, an α-Glucosidase Inhibitor, Attenuates Postprandial Hypotension in Autonomic Failure

Postprandial hypotension is an important clinical condition that predisposes to syncope, falls, angina, and cerebrovascular events. The magnitude of the fall in blood pressure after meals depends on enteric glucose availability. We hypothesized that acarbose, an alpha-glucosidase inhibitor that decreases glucose absorption in the small intestine, would attenuate postprandial hypotension. Acarbose or placebo was given 20 minutes before a standardized meal in 13 patients with postprandial hypotension in the setting of autonomic failure (age: 65+/-2.64 years; body mass index: 25+/-1.08 kg/m(2); supine plasma norepinephrine: 110+/-26.6 pg/mL). Four patients were studied in a single-blind protocol and 9 patients in a double-blind, randomized, crossover fashion. Patients were studied supine, and blood pressure, heart rate, and neuroendocrine parameters were obtained at baseline and for 90 minutes after meal intake. After adjusting for potential confounders, acarbose significantly attenuated the postprandial fall in systolic and diastolic blood pressures by 17 mm Hg (95% CI: 7 to 28; P=0.003) and 9 mm Hg (95% CI: 5 to 14; P=0.001), respectively. Furthermore, acarbose effectively reduced plasma levels of insulin, a known vasodilator, by 11 microU/mL (95% CI: 5 to 18; P=0.001) compared with placebo. After adjusting for insulin levels, the attenuation of postprandial hypotension by acarbose remained significant, indicating that additional mechanisms contribute to this effect. In conclusion, 100 mg of acarbose successfully improved postprandial hypotension in patients with severe autonomic failure. This effect is not explained solely by a reduction in insulin levels.

Acarbose improves fibrinolytic activity in patients with impaired glucose tolerance

Acarbose has been shown to ameliorate insulinemia, suggesting that it may exert favorable effects on the impaired fibrinolytic state in prediabetic patients. We therefore conducted a randomized controlled study to examine the effects of acarbose on fibrinolysis in patients with impaired glucose tolerance (IGT). The participants were randomized to receive (n = 20) or not (control, n = 20) 100 mg of acarbose before each meal (300 mg/d) for 3 months. A marked decrease in the plasma levels of plasminogen activator inhibitor 1 (by 42%) and fibrinogen (by 27%) was observed in the acarbose group at the end of the study, whereas no significant changes in the levels of these parameters were observed in the control group. We also conducted postprandial evaluation of insulin-related clinical markers and found ameliorated hyperinsulinemia in the subjects treated with acarbose. These results indicate that acarbose could improve fibrinolysis in patients with IGT, mainly by ameliorating insulinemia. Other favorable effects of acarbose, such as reduction in the plasma levels of oxidized low-density lipoprotein, glucose toxicity, and hyperglycemia, might also contribute, at least in part, to the beneficial effects of the drug on the fibrinolytic state in patients with IGT.

P1152 APPLICATION OF AN ALPHA-GLUCOSIDASE INHIBITOR IN THE TREATMENT OF GLYCOGEN STORAGE DISEASE TYPE 1. A FEASIBILITY STUDY IN HEALTHY SUBJECTS.

Introduction: Uncooked cornstarch (UCCS) is widely used to maintain normoglycemia in patients with glycogen storage disease type 1 (GSD1). However, compliance of the UCCS treatment is suboptimal because of the unpleasant taste of the UCCS. Acarbose, an alpha-glucosidase inhibitor supposed to delay carbohydrate digestion, added to a carbohydrate rich meal, might be an alternative approach in the treatment of GSD1. A cross-over study in healthy subjects was conducted to investigate the feasibility to apply an alpha-glucosidase inhibitor in the treatment of GSD1. This study compared the absorption profile after ingestion of UCCS with that after ingestion of corn pasta with acarbose. Methods: Seven healthy male volunteers (age: 23 ± 1 (mean ± SE) years, BMI 22 ± 1.1 kg/m2) ingested at least one week apart UCCS in 250 ml water or corn pasta with 12.5 mg of acarbose (CPac). Both test meals contained an equivalent of 50 g of glucose and were naturally enriched with 13C. During the 6 hours following consumption of the test meals plasma glucose and insulin were monitored. Using a primed continuous infusion of D-[6,6-2H2]glucose, the systemic appearance of exogenous glucose (RaE) was estimated, which reflects the intestinal carbohydrate absorption. Results: Significant higher total glucose responses were observed between 60 and 150 min after consumption of UCCS compared to CPac (p<0.04). Insulin responses between 60 and 240 min were significantly higher after ingestion of UCCS than those after ingestion of CPac (p<0.03). In the fasting state, before ingestion of the test meals, the endogenous glucose production was 2.24 ± 0.09 mg/kg/min. Between 30–180 min the mean RaE after consumption of UCCS (2.27 ± 0.24 mg/kg/min) was significantly higher than the mean RaE of CPac (1.16 ± 0.14 mg/kg/min)(p<0.02). Six hours after ingestion of UCCS the recovery of glucose was significantly higher than after ingestion of CPac (88 ± 6% and 45 ± 4% of the administered dose respectively, p<0.02). Conclusion: After ingestion of UCCS the mean RaE between 30 and 180 min equals the rate of endogenous glucose production. Addition of 12.5 mg of acarbose to corn pasta does not result in an absorption profile able to provide for the glucose requirements. The low 6 hours recovery of glucose after ingestion of CPac (45%) indicates that the digestion of corn pasta is inhibited to some extent. Acarbose applied in combination with the amount and type of carbohydrate used in this study is not a suitable alternative in the treatment of GSD1.

Short-term effect of acarbose on specific intestinal disaccharidase activities and hyperglycaemia in CBA diabetic mice.

The purpose of this study was to examine the short-term effects of 75, 100 and 150 mg of acarbose mixed in 100 g standard laboratory chow on specific intestinal disaccharidase activities and on hyperglycaemia in diabetic CBA strain mice on standard diet. The small intestine was excised and divided into three segments, from pylorus to duodenum, and two equal lengths of the jejunum and ileum of control and diabetic mice with or without added acarbose. Specific maltase and sucrase activities were determined using maltose and sucrose as substrates respectively. Increased specific activities of maltase and sucrase were detected in the intestines of CBA mice on standard laboratory diet seven days after alloxan-induced diabetes. Feeding for 7 days with 75, 100 or 150 mg acarbose uniformly mixed in 100 g standard laboratory chow, induced a decrease in the specific maltase and sucrase activities, compared with diabetic mice on standard laboratory diet. Feeding with 75 mg acarbose mixed in 100 g standard laboratory chow caused a statistically significant decrease of maltase in the duodenum and of sucrase in duodenum and jejunum, without a antihyperglycaemic effect. Feeding with 100 or 150 mg caused statistically significant decreases in specific maltase and sucrase activities in duodenum, jejunum and ileum. An antihyperglycaemic effect was observed only in the group of diabetic mice fed with 100 mg acarbose. This indicates that the antihyperglycaemic effect of acarbose involves factors other than these, related only to its inhibitory effect on disaccharidase activities.

Dose-response profile of acarbose in older subjects with type 2 diabetes.

To examine the dose-response relationship of acarbose, an alpha-glucosidase inhibitor, in older subjects with type 2 diabetes. Fourteen subjects with type 2 diabetes who were over 65 years old were studied. Five subjects had been treated with diet alone and 9 were receiving a sulfonylurea. The subjects underwent a meal tolerance test in the presence of varying doses of acarbose (0, 25, 50, and 100 mg) on 4 occasions, each 1 week apart. The test meal was chosen to include food items commonly consumed during breakfast in the United States. The 483-kcal meal consisted of 51% of calories in the form of carbohydrates, 14% protein, and 35% fat. The serum glucose, insulin, and triglyceride levels were measured at 0, 1, and 2 hours after the meal. The postprandial hyperglycemic response to the test meal was significantly reduced with 25 mg of acarbose compared with baseline values. Increasing doses of acarbose to 50 or 100 mg had no significant additional ameliorating effects on postprandial hyperglycemia. Postprandial insulin or triglyceride levels were not significantly altered with single dose acarbose treatment. It is concluded that the acute efficacy of acarbose is near maximal at 25 mg when the meal size does not exceed 483 kcal and contains only 61 gm of carbohydrates.

Dose-Response Profile of Acarbose in Older Subjects with Type 2 Diabetes

ABSTRACT Objective To examine the dose-response relationship of acarbose, an a-glucosidase inhibitor, in older subjects with type 2 diabetes. Research Oesign Fourteen subjects with type 2 diabetes who were over 65 years old were studied. Five subjects had been treated with diet alone and 9 were receiving a sulfonylurea. The subjects underwent a meal tolerance test in the presence of varying doses of acarbose (0, 25, 50, and 100 mg) on 4 occasions, each 1 week apart. The test meal was chosen to include food items commonly consumed during breakfast in the United States. The 483-kcal meal consisted of 51 % of calories in the form of carbohydrates, 14% protein, and 35% fat. The serum glucose, insulin, and triglyceride levels were measured at 0, 1, and 2 hours after the meal. Results The postprandial hyperglycemic response to the test meal was significantly reduced with 25 mg of acarbose compared with baseline values. Increasing doses of acarbose to 50 or 100 mg had no significant additional ameliorating effects on postprandial hyperglycemia. Postprandial insulin or triglyceride levels were not significantly altered with single dose acarbose treatment. Conclusions It is concluded that the acute efficacy of acarbose is near maximal at 25 mg when the meal size does not exceed 483 kcal and contains only 61 gm of carbohydrates.

アカルボースとボクリボースの臨床的効果の比較 アカルボースからボクリボースに処方変更された症例での調査

Several years have passed since α-glycosidase inhibitors entered the market as antidiabetics. At present, acarbose and voglibose are the only drugs in this category that are available in Japan. Although several studies have been perfomed on the efficacy and side effects of these drugs, the results are still not uniform. In this study, changes in the laboratory data were investigated in patients treated at our department in whom their medication was changed from acarbose to voglibose. The subjects consisted of 11 outpatients with non-insulin-dependent diabetes mellitus (NIDDM) in whom their medication was changed from 300 mg of acarbose to 0.6 mg of voglibose without any alterations in concomitant drugs.No significant changes were noted in the HbAic, TG, TC, or HDL-C levels at 16 weeks after the change in medication. In addition, no abnormal data were observed in the GOT, GPT, γ-GTP, ALP, or K levels in patients before or after the change in medication. An interview study showed no remarkable changes in the symptoms except for a decreased frequency of flatus after the change in medication from acarbose to voglibose. The above results suggested that 0.6 mg of voglibose was superior in terms of QOL to 300 mg of acarbose because of a lower incidence of gastrointestinal symptoms, although the hypoglycemic effect was comparable between the 2 drugs.Additional studies should be performed in a larger number of patients to obtain more reliable results.

Effects of the α-glucosidase inhibitor acarbose on postprandial serum glucose and insulin concentrations in healthy dogs

Abstract Objective To determine effects of acarbose on baseline and postprandial serum glucose and insulin concentrations in healthy dogs, if effects of acarbose were dosage related, and if acarbose caused any short-term adverse effects. Animals 5 healthy dogs fed a high-fiber diet. Procedure A Latin-square design was used. During each 1-week treatment period, dogs were given a placebo or 25, 50, 100, or 200 mg of acarbose, PO, twice daily immediately prior to feeding. There was a 1-week interval between periods. At the end of each treatment period, serum glucose and insulin concentrations were measured prior to feeding and at 30- to 60-minute intervals for 6 hours after feeding. Results Baseline serum glucose and insulin concentrations, insulin peak response, and total glucose absorption were not significantly different following treatment with placebo and treatment with acarbose; however, total insulin secretion was significantly decreased when dogs were treated with 100 or 200 mg of acarbose. Four dogs developed soft to watery stools when treated with 200 mg of acarbose, and 2 dogs lost weight during the study. Results of CBC and serum biochemical analyses were within reference ranges throughout the study. Conclusions Acarbose did not induce any serious adverse effects and was effective in healthy dogs in reducing total postprandial insulin secretion when administered immediately prior to meals. Clinical Relevance Results suggest that acarbose may help control hyperglycemia in dogs with insulin-dependent diabetes mellitus. Additional studies designed to evaluate the effect of acarbose on postprandial blood glucose concentrations in dogs with diabetes mellitus are indicated. (Am J Vet Res 1999;60:541–545)

Effect of Acarbose Taken Just before and after a Meal on Plasma Glucose Level in Japanese Healthy Subjects.

We studied the effect of a patient forgetting to take acarbose and also investigated whether there is any benefit in taking it within certain time periods after a meal. The subjects consisted of 10 volunteers and the tests were conducted during lunch periods. Over 6 test days the subjects ingested breakfast (100 kcal; carbohydrate 78%) and lunch (624 kcal; carbohydrate 56%) each day. On the first test day, as a control, no acarbose was given. Blood was drawn 7 times to determine the levels of plasma glucose and immunoreactive insulin (IRI) (just before and after a meal, and after 30 minutes, 45 minutes and 60 minutes, 90 minutes, and 120 minutes after a meal). The same 10 subjects then took 100 mg of acarbose just before a meal, and 30 minutes, 45 minutes and 60 minutes after starting a meal respectively on different days. The levels of plasma glucose and IRI were measured for the 7 blood drawing times. The levels of plasma glucose of the subjects who took acarbose just before a meal were significantly lower at the 5 times, from just after meal to 90 minutes after starting time of a meal, compared to the controls. The levels of IRI in the subjects who took acarbose just before meals were lower at all times compared to the controls and other intakes. There was no significant difference in the area under the blood concentration-time curve (AUC0-120) 1of plasma glucose during the 120 minute period after starting a meal between the subjects who took acarbose just before a meal, just after starting a meal, and 30 minutes after starting a meal. It was found that taking acarbose was therefore the most effecctive just before a meal but, if this is forgotten, it can still be effective if taken 15-30 minutes after starting a meal.

Effect of acarbose on postprandial lipid metabolism in type 2 diabetes mellitus

The effect of acarbose, an α-glucosidase inhibitor, on postprandial glucose and lipid metabolism was investigated in patients with type 2 diabetes mellitus. Twenty patients (10 men and 10 women) with type 2 diabetes mellitus were studied. A test meal was taken with or without 100 mg of acarbose. The levels of plasma glucose, and serum immunoreactive insulin, lipids, apolipoproteins, and remnant-like particle cholesterol were investigated. Acarbose inhibited the postprandial increase of both plasma glucose and serum immunoreactive insulin. Acarbose also significantly suppressed the increase of serum triglycerides at 60, 90, and 120 min ( P<0.05 to P<0.01), and the increase of serum remnant-like particle cholesterol at 60 and 120 min ( P<0.05). Acarbose inhibited the postprandial decline of apolipoprotein C-II, and decreased the postprandial serum apolipoprotein C-III level. These results suggest that acarbose may improve postprandial hyperlipidemia as well as postprandial hyperglycemia in patients with type 2 diabetes mellitus.

Carbohydrate malabsorption following acarbose administration.

Carbohydrate absorption was assessed during acarbose administration to investigate the actions of this drug. In 7 healthy volunteers, breath hydrogen concentration was measured at 15-min intervals after administration of 6 g of lactulose, and continued until 4 h after the breath hydrogen level exceeded its pretreatment value by > or =10 ppm, then the amount of undigested carbohydrate was calculated following administration of various doses of acarbose and Ensure Liquid. Breath hydrogen data were also obtained before and after administration of acarbose to 8 patients with Type 2 diabetes mellitus for 2 and 4 months. After administration of 50 mg of acarbose with 250 ml or 500 ml of Ensure, the mean amount of unabsorbed carbohydrate was 5.3 g and 7.7 g, respectively, while unabsorbed carbohydrate increased to 10.8 g after 100 mg of acarbose with 500 ml of Ensure. In the diabetic patients, breath hydrogen excretion decreased to 31.6% of baseline after 2 months of acarbose administration, indicating decreased carbohydrate malabsorption. Despite this, the haemoglobin A1c level remained stable after 5 months. In conclusion, the extent of carbohydrate malabsorption depended on the acarbose dose and the carbohydrate load. Although carbohydrate malabsorption decreased with continued acarbose administration, the improvement of glycaemic control was maintained.