Glibenclamide

One of the most common metabolic diseases during pregnancy period is gestational diabetes mellitus (GDM). It is associated with several perinatal complications, especially in those who have risk factors such as obesity, polycystic ovary syndrome, and a family history of type 2 diabetes mellitus (DM). Some research has shown that physical exercise and medical nutrition treatment can give beneficial effects to control glycemic and body weight for GDM affected women. Furthermore, pharmacological agents such as insulin and a specific oral antidiabetic can be prescribed safely during pregnancy to decrease maternal glucose blood. Therapy of GDM is needed to control blood for the wellness of the patient during and after the pregnancy. The main treatment therapy for GDM is lifestyle modification, which includes medical nutritional therapy and daily physical exercise. In the special case of disorder glucose level, drug therapy will be given to the patient. Insulin is the chosen drug because ...

Introduction: Therapeutic equivalence of medications is carried out through in vitro and in vivo studies called bioequivalence studies. Objective: To determine the in vitro therapeutic equivalence of the 5 mg glibenclamide multi-source tablets respecting the reference medicine. Materials and methods: Both, the multi-source drug 5 mg glibenclamide and the reference 5 mg Glidiabet are made in Peru, and were acquired in a drugstore of Ica city (Peru). Reagents and an analytical grade standard were used. The Ultraviolet absorption method at 300 nm was used on each of the three dissolution media. Results: Neither the multi-source drug T nor the reference R dissolved by 85% at pH 1.2 and at pH 4.5, during 15 or 30 minutes. However, at pH 6.8 dissolution occurs. These results correspond to Food and Drug Administration and United States Pharmacopoeia criteria. The similarity factor value was within the acceptance range (50-100) for the three tested pHs. Dissolution efficiency was 68.66% (pH...

Context: Sustained release drug delivery systems are more preferred than the conventional drug delivery systems due to its enhanced bioavailability and patient compliance. Earlier studies reported on glibenclamide (GBCM) were not clear and hence, the step has been taken to explore the sustained release drug delivery system of GBCM.

Aims: To evaluate the sustained release microspheres obtained of GBCM.

Methods: Microspheres were prepared by ionic gelation method using the polymers like Eudragit RS 100 and xanthan gum. Polymers can sustain the drug release from microspheres. The prepared microspheres were subjected to micromeritic studies like Carr’s index, Hausner’s ratio and angle of repose.

Results: Micromeritic studies confirmed that the microspheres possessing acceptable flow properties. It was observed from the in vitro release studies, formulations F8 and F9 showed sustained drug release for desired time of 12 h and when compared to F9, formulation F8 showed maximum drug release for 12 h.

Conclusions: Results confirmed the formulation F8 consist of the polymers such as Eudragit RS 100 about 150 mg and xanthan gum about 100 mg showed desired sustained release of 12 h with 96.07% and kinetic studies confirmed that the release from microspheres followed non-Fickian diffusion mechanism. Due to its sustained release property, it could enhance the bioavailability of drug thereby improves the patient compliance and expect better treatment than conventional dosage forms.

The objective of the present study was to improve solubility, dissolution rate and therapeutic efficacy of a BCS Class II drug, glibenclamide by using oral self nano emulsifying powder. The powder was prepared by adsorbing the mixture of oil, surfactant and co-surfactant onto a carrier with large surface area; Aerosil 200. The ratios of oil and S mix (surfactant/co-surfactant mixture) required to produce an emulsion was optimized based on percentage transmittance studies and particle size determinations. The optimized formulation was subjected to in vitro dissolution study and in vivo therapeutic efficacy in rabbits by monitoring blood glucose levels. Scanning electron microscopy, differential scanning calorimetry and X-ray powder diffraction studies revealed that the drug was present in amorphous form in the final formulation. The in vivo study in rabbits indicated the improved therapeutic efficacy of glibenclamide in self-nanoemulsifying powder compared to plain drug.

Syzygium cumini is commonly known as insulin plant in India. Consumption of leaves of this plant are believed to lower blood glucose level in healthy normal and diabetic individuals. The present study was planned to evaluate the effect of the leaves of syzygium cumini leaves on dexamethasone induced hyperglycemic rats. MaleWistar rats (n=6) were treated with 10mg/kg of dexamethasone subcutaneously for 20 days from 11 th day to 20 days. Different groups received 100mg/kg plant extract in distill water and glibenclamide 500µg/kg per orally on plasma blood glucose level, serum total cholesterol, triglyceride level, HDL, LDL and Serum VLDL were observed. Dexamethasone caused an increase blood glucose level, serum total cholesterol, serum triglyceride level, Serum HDL ,Serum LDL and Serum VLD and compare with normal control[ **P<0.01]. In the dexamethasone model 100mg/kg p.o. of Ethanolic extract of syzygium cumini leaf showed significant decrease in blood glucose level, serum total cholesterol , serum triglyceride level, Serum HDL ,Serum LDL and Serum VLDL when compared to dexamethasone control[l.**P<0.01]. The study results concluded Syzygium cumini proved to be effective in treatment of Type-II Diabetes mellitus owing to its ability to decrease insulin resistance.

RP-HPLC method was developed and applied for the simultaneous determination of enalapril and hypoglycemics in bulk, pharmaceutical formulations and human serum. A Hypersil ODS, C18 (150×4.6mm, 5micron) column was used. Eluents were monitored at 230 nm, on mobile phase consisting of methanol: water (70:30 v/v, pH 2.8) with flow rate of 1.0 mL min -1 .

Aim of present study was to develop solid self micro emulsifying drug delivery system (S-SEDDS) with Aerosil 200 for enhancement of dissolution rate of model drug Glibenclamide (GBM). SEDDS was prepared using Capmul MCM C8 TM , Cremophor RH 40 TM , and Transcutol P TM as oil, surfactant and cosurfactant respectively. For formulation of stable SEDDS, micro emulsion region was identified by constructing pseudo ternary phase diagram containing different proportion of surfactant: co-surfactant (1:1, 2:1 and 3:1), oil and water. Prepared SEDDS was evaluated for turbidity measurement, globule size and zeta potential, viscosity determination and % transmittance. S-SEDDS was prepared by adsorption technique using Aerosil 200 as solid carrier. Prepared S-SEDDS was evaluated for flow properties, drug content, FTIR, SEM, DSC and in-vitro dissolution study. Results showed that prepared liquid SEDDS passed all evaluation tests. Globule size was found to be 142.8 nm with polydispersity index 0.396. S-SEDDS showed good flow property and drug content. From the experiment, it is clear thateven after conversion of the liquid SEDDS into the solid one there was no significant alteration in the properties of solid SEDDS.in-vitro dissolution studies showed that there was enhancement of dissolution rate of GBM as compared with that of plain drug and marketed formulation. From the results it is concluded that, Aerosil 200 can be used to develop S-SEDDS by adsorption technique to enhance dissolution rate of poorly water soluble model drug GBM

More than 100 million people worldwide are affected by a complex and heterogeneous disorder of Type 2 diabetes causing serious socio-ecologic problems. The different extracts of the bark of Cuscuta reflexa (Cuscutaceae – Dodder family) were tested for anti-diabetic activity, by alloxan induced diabetic rats and glucose tolerance test in normal rats. The blood glucose level of normal and experimental animals after oral administration of glucose (2 g/kg) the extract as well as standard drug treated animals showed more significant decrease in peak blood glucose level after 1 h. After 2 h, the extract treated animals tended to bring the values near normal. The extract produced significant decrease in the blood glucose level when compared with the controls in alloxan induced hyperglycemic rats in the single dose experiment at the tested dose level and are comparable with the standard drug glibenclamide. The ethanolic extract reversed the weight loss of the diabetic rats and they returned to near normal. This study gave a clear view that the ethanolic extract prevented significant elevation of glycosylated hemoglobin in vitro, with IC50 value being 11.25 μg/ml that is comparable with the reference drug α- tocopherol, since the non-enzymatic glycosylation of hemoglobin is an oxidative reaction.
Keywords: Cuscuta reflexa, hypoglycemic activity, alloxan, glibenclamide, α- tocopherol.

A simple, rapid, and precise reversed-phase high-performance liquid chromatographic method for simultaneous analysis of metformin hydrochloride, pioglitazone hydrochloride, and glibenclamide in a tablet dosage form has been developed and validated. Chromatography was performed on a 25 cm × 4.6 mm i.d., 5-μm particle, C 18 column with 55:45 (v/v) acetonitrile-potassium dihydrogen phosphate buffer (pH adjusted to 3.0 ± 0.1 with 5% orthophosphoric acid) as mobile phase at a flow rate of 1.5 mL min −1 . UV detection was performed at 230 nm. Total run time was 10 min; metformin hydrochloride, pioglitazone hydrochloride, and glibenclamide were eluted with retention times of 1.362, 3.418, and 7.395 min, respectively. The method was validated for accuracy, precision, linearity, specificity, and sensitivity in accordance with ICH guidelines. Validation revealed the method is specific, rapid, accurate, precise, reliable, and reproducible. Calibration plots were linear over the concentration ranges 200-1000 μg mL −1 for metformin hydrochloride, 200-1000 μg mL −1 for pioglitazone hydrochloride, and 50-300 μg mL −1 for glibenclamide. Limits of detection were 6.3, 15.4, and 8.2 ng mL −1 and limits of quantification were 19.09, 46.66, and 24.84 ng mL −1 for metformin hydrochloride, pioglitazone hydrochloride, and glibenclamide, respectively. The high recovery and low coefficients of variation confirm the suitability of the method for simultaneous analysis of the three drugs in tablets. The validated method was successfully used for quantitative analysis of triglycomate tablets.

Abstract: The suspensions of sulfonylurea glyburide (glibenclamide) are compounded extemporaneously for patients suffering from transitional and Permanent Neonatal Diabetes mellitus (PND). The purpose of this study is to compare the stability of three different galenic liquid formulations compounded from tablet containing glibenclamide. The samples were stored at refrigerated (2-8°C) and room temperature and analyzed at different times. All formulations analysed are stable for at least 90 days, but only two guarantee the administration responding to prescription, especially when it comes to giving dosages very small.

Worldwide prevalence of diabetes mellitus has become an issue of great concern in current decades. This life threatening disease is associated with worsening of glycemic control and progressive metabolic dysfunctions. Objective: Current study aimed to investigate the effect of hydroxychloroquine (HCQ) as an adjunct to glibenclamide or metformin on glycemic control in alloxan induced diabetic rats. Methods: HCQ was combined separately with two conventional anti-diabetic drugs; glibenclamide and metformin. At first, alloxan (120 mg/kg) induced diabetic rats were treated with single dose of metformin (850 mg/70 kg BW), glibenclamide (10 mg/70 kg BW) and HCQ (300 mg/70 kg BW) intraperitoneally once daily for two weeks. Then non fixed dose combinations of glibenclamide (5 mg/70 kg BW) with HCQ (150 mg/70 kg BW) and metformin (425 mg/70 kg BW) with HCQ (150 mg/70 kg BW) were injected along with those of the three drugs alone once daily for four weeks. Results: In alloxan induced diabetic rats, glibenclamide, metformin and their combination therapies reduced blood glucose level significantly but combination therapies are the most effective. Glibenclamide or metformin in combination with HCQ also significantly (P < 0.05) reduced the elevated levels of total cholesterol, triglycerides, and low density lipoprotein cholesterol (LDL-C) level and increased high density lipoprotein cholesterol (HDL-C) level. Moreover, HCQ potentiates the liver glycogen synthesis of metformin or glibenclamide. Conclusion: Outcomes of this investigation indicate that combination of glibenclamide or metformin with HCQ improves glycemic control and provides additional metabolic benefits, not achieved * Corresponding author.

Talinum triangulare is used by some traditional healers to manage preterm labour and prevent preterm birth. The effect of T. triangulare on uterine contractility is so far unknown. This study was therefore aimed at: the investigation of the pharmacological and physiological effect of T. triangulare leaf extract (MTT) on the isolated mouse uterus; investigation of possible mechanisms of activity and identification of significant metabolites present in the leaves. Longitudinal uterine segments from non-pregnant mice were isolated and mounted in a continuously aerated organ bath containing physiological salt solution and maintained at 37°C. The effect of MTT (0.0007 -7.777 µg/ml) on spontaneous contractions, 11.82 nM oxytocin, and 40 mM KCl was investigated. Additionally, MTT (3.43 mg/ml) in the presence of 95.34 nM amiodarone, 5.06 nM glibenclamide and 11.57 nM propranolol was investigated. High resolution mass spectrometric (HRMS) analysis was performed on MTT. MTT exerted a biphasic effect on spontaneous uterine contractility, with low concentrations inhibiting and high concentrations stimulating contraction. MTT also increased oxytocin and KCl-induced contraction. The effect on oxytocin was reduced in the presence of amiodarone but not glibenclamide or propranolol. HRMS identified high levels of oestrogenic compounds which may play a role in the activity of the plant on female reproductive health

The study was designed to evaluate antidiabetic activity on methanolic extracts of Rotula aquatica Lour roots in Streptozotocin induced diabetic rats. The roots of Rotula aquatica Lour were extracted with methanol and evaluated for their antidiabetic activity in Streptozotocin induced diabetic rats at doses levels of 100, 200 and 400 mg/kg body weight. The lowering of blood sugar levels as well as percent blood glucose reduction were calculated and compared with the standard glibenclamide (0.45 mg/kg b.w.). Preliminary phytochemical screening was also conducted for occurrence of compounds. The oral administration of 400 mg/kg b.w. of methanolic extract of roots of Rotula aquatica showed more significant (P<0.01) decrease in blood glucose levels at 4 and 8 th hrs and highly significant (P<0.001) decrease in blood glucose levels at 8 th hr. The methanolic extracts of Rotula aquatica roots showed good activity at a dose of 400 mg/kg body weight .Phytochemical screening revealed presence of triterpenes and tannins in plant extracts.

Abstract
BACKGROUND: Severe hypoglycemia is a frequent cause of hospi- talization in Mexico.
OBJECTIVE: To identify the clinical and laboratory characteristics as- sociated to severe hypoglycemia in consecutive patients with severe hypoglycemia and normal creatinine serumvalues.
PATIENTS AND METHOD: A prospective study was done from August 11, 2011 to May 31, 2013, including patients with severe hypoglyce- miaandnormal creatinine serumvalues.Age, sex, timeof evolutionof diabetesmellitus2,antidiabetictreatment,comorbiditiesand24-hour urine creatinine clearance wererecorded.
RESULTS: From 234 patients with severe hypoglycemia admitted, 21 (9%)hadnormalcreatinine:13women(62%)and8(38%)men,with
amean age of 64.76 years (range: 42-84); 13 (62%)were older than
60 years; 15 (71%) hadmore than 5 yearswithDM2(mean evolution
of 9.2 years); 15 received glibenclamide (71%),4 in combinationwith insulin(19%)and8withmetformin(38%).Tworeceivedrosiglitazone plusinsulin.Fourpatientshadnotcomorbidities(19%);16hadarterial hypertension (71%) and 3, neoplasms (adenocarcinoma, gastric carci- nomaandesophagealcarcinoma).Elevenpatients(52%)wereadmitted with syncope, 5 with disorientation (24%), 4 with conduct disorders (19%)andonewithdyslalia(5%);15of21patients(71%)hadadvanced degreesofrenalimpairment,despitenormalcreatinineserumvalues.
CONCLUSIONS: It is important to perform creatinine clearance at all levels of care, the only guide for safe treatments according to kidney function. Glibenclamide should be cautiously prescribed in older adults with a history of more than 10 years of diabetesmellitus 2 and should be avoided in those with documented chronic renal failure.
KEYWORDS: hypoglycemia; diabetes mellitus 2; oral antidiabetic drugs; chronic kidney failure

A large number of oral antidiabetic agents are available today. This article provides a short review of the pharmacology and some clinical aspects of various oral antidiabetic drugs. It focuses mainly on the newest developing drugs (therapy of the near future) and on the most commonly used older groups for the common approach of everyday practice (sulphonylureas). The primary goal of this review is to compare the electrophysiological effects of glibenclamide in isolated normal and streptozotocin induced diabetic rats and alloxan induced rabbits ventricular preparations, while on the other hand to differentiate the hypoglycaemic sulphonylureas (0.1-1000 mmol/kg) according to their cardiovascular activity in healthy and diabetic animals. In vitro (1-100 mmol/l) as well as chronically treated (5 mg/kg for 10 weeks) glibenclamide prolonged the action potential duration in normal but failed to affect it in diabetic ventricular preparations. Our results suggest that the sensitivity to glibenclamide of KATP channels in diabetic ventricular fibers is drastically decreased. The effects of different sulphonylureas (tolbutamide, glibenclamide, gliclazide, glimepiride) on ventricular ectopic beats as well as the duration of ventricular fibrillation induced by 10 min ischemia/50 min reperfusion in healthy and diabetic rats were compared. Tolbutamide and gliclazide dose-dependently enhanced both parameters both in healthy and diabetic groups. Glibenclamide in healthy rats increased, while in diabetic rats it decreased the arrhythmogenicity. Glimepiride depressed the arrhythmogenicity in both healthy and diabetic animals. Glimepiride proved to dose-dependently enhance the myocardial tissue flow in dog in contrast to glibenclamide. These results confirm that glimepiride has less cardiovascular actions than other sulphonylureas. From the newest oral antidiabetics this review tries to emphasize the most important basic pharmacological properties, mechanism of action, therapeutic use.

Agglomerates were prepared using methanol, chloroform and water as good solvent, bridging liquid and poor solvent, respectively. Direct compressible tablets of the agglomerates showed appropriate hardness, friability, weight variation and disintegration time with improved drug release than conventional marketed tablets. Tablets were adequately stable as per regulatory guidelines. Pharmacokinetic study indicated rapid absorption with higher bioavailability of the drug from the prepared tablets of agglomerates than marketed tablet (Glyburide; Sandoz). Hence, the tablets prepared with the agglomerates of glibenclamide may reduce the total dose of drug and could improve the patient compliance by reducing the dose-related side effects.

The objective of this study was to evaluate the antitumor effect of glibenclamide (Gli) alone or in combination with tamoxifen (Tam) on experimental mammary tumors induced by N-Nitroso-N-methylurea (NMU) in non-diabetic and diabetic rats. For experimental diabetes induction, Sprague-Dawley rats were injected with streptozotocin (STZ) on the second day of life. For experimental mammary tumor induction, non-diabetic and diabetic rats were intraperitoneally injected with NMU at 50, 80 and 110 days of life. Non-diabetic and diabetic rats bearing mammary tumors were treated with 0.06 mg/day of Gli orally, Tam 1 mg/kg/day sc, or with the combined treatment (Gli+Tam). After 20 days of treatment, different responses were observed. In non-diabetic rats, 64% of tumors were responsive to Gli treatment: they regressed or remained stable, whilst 57% of tumors under treatment with Tam exhibited a response. Results of the combined Gli+Tam treatment indicated that all tumors were responsive: 58% regressed and 42% remained stable. Diabetic rats receiving Gli treatment did not show response to this treatment, whilst 65% of the tumors of Tam treated diabetic rats showed regression. Histopathologic observation indicated an important intratumor secretion in all tumors of Gli, Tam or Gli+Tam treated rats. No secondary toxic effect was observed after treatment at any assayed doses. In conclusion, the present data demonstrate the in vivo antitumor action of Gli treatment on the experimental mammary tumors employed, indicating that Gli exerted a direct effect on tumor cells in non-diabetic rats. The combined Gli+Tam treatment potentiates the antitumor effect of each drug alone. Future research will examine the molecular aspects of these findings.

Hyperglycemia exerts toxic effects on the pancreatic β-cells. This study investigated the hypothesis that the antidiabetic drugs glibenclamide and metformin, in combination with hydroxychloroquine (HCQ) offer additional protection for the pancreas against oxidative stress and produce hepatoprotective effect in alloxan-induced diabetic rats. Diabetes was induced in male Long-Evans rats by a single dose of alloxan (120 mg/kg; i.p.). Different groups of diabetic animals were treated with glibenclamide (10 mg/70 kg, i.p.), metformin (850 mg/70 kg, i.p.), HCQ (300 mg/70 kg, i.p.) and combination of both glibenclamide and metformin with HCQ, separately for a period of 28 days. Diabetic rats had significantly elevated levels of serum glutamate oxaloacetate transaminase (SGOT) and serum glutamate pyruvate transaminase (SGPT), while catalase (CAT) and superoxide dismutase (SOD) activity were significantly reduced. Glibenclamide and metformin produced no significant effects on antioxidant enzymes but both showed significant (p<0.05) result in reducing SGOT and SGPT level in diabetic rats. In contrast, the combination of glibenclamide or metformin with HCQ showed better effect on up-regulation of CAT and SOD activity and down-regulation of SGOT and SGPT activity in comparison with the antidiabetic drug alone. These findings suggest that, HCQ potentiates the effect of glibenclamide and metformin to protect pancreas against oxidative stress and produce hepatoprotective effect in diabetic rats.

Context: Diabetes mellitus (DM) is a metabolic hyperglycemia disease caused by abnormalities in insulin secretion and the highest increase in diabetes sufferers that occurred in Southeast Asian countries, including Indonesia. The sikkam leaf (Bischofia javanica) ethanolic extract contains many secondary metabolites, and some of them are quercetin and gallic acid, which have the potential to be used as antidiabetic.

Aims: To analyze apoptosis via cytochrome c in aortic tissue of DM after giving B. javanica leaves.

Methods: The treatment group consisted of G0: Negative control, G1: Positive control (alloxan induction + standard feed), G2: Alloxan induction + 300 mg/kg BW of B. javanica leaves ethanol extract, G3: Alloxan induction + 600 mg/kg BW of B. javanica leaves ethanol extract, G4: Induction of alloxan + ethanol extract of B. javanica leaves 900 mg/kg BW and G5: Induction of alloxan + glibenclamide 0.5 mg/kg BW. Fourteen days later, the rats were dissected, and the aortic tissue was analyzed for apoptosis by tunnel assay and cytochrome c by immunohistochemistry.

Results: There was a statistically significant difference (p<0.01) in the apoptotic value and cytochrome c. Increasing the dose of B. javanica leaves, the cytochrome c expression, and apoptotic value decreases in the aorta of DM rats. The cell shape returned to normal after being given B. javanica ethanol extract 900 mg/kg BW than glibenclamide.

Conclusions: Bischofia javanica ethanolic extract reduced apoptosis via cytochrome c in aortic histology, and this plant can be developed into a diabetic drug candidate.

Background: The leaves of Thaumatococcus danielli (Benth.) have been traditionally used in folk medicine to treat malaria in Nigeria. However, there is no report on whether these leaves contain Nephroprotective activity. Thus, the ethanol leaf extract was investigated for Nephronprotective activity in Streptozotocin induced diabetic rats.

Methods: First, the LD50 of the leaf was determined using standard procedure. Rats were assigned to 5 groups (A-E) of five rats. Except for the control group, each group was made
diabetic using Streptozotocin (65 mg/kg/b.wt. i p). The treated groups received 0.5 ml of glibenclamide (25 mg/kg/b.wt, o.p), 250 and 500 mg/kg/b.wt, o.p of Thaumatococcus danielli respectively. After 14 days of treatment, animals were sacrificed under light anaesthesia. Data expressed as Means ± S.D (n=5) and was analyzed using one-way ANOVA followed by Dunnet’s test. Values were considered significant at p<0.05.

Results: The plant showed a LD50 greater than 5000 mg/kg/b.wt in albino rats observed for 72 hours. A significant (p<0.05) decrease in serum Na+, Cl-, HCO-
3, total protein, and an insignificant increase in K+, urea and creatinine level were observed in the diabetic group when
compared with the normal group. Oral administration of plant extract and glibenclamide significantly (p<0.05) restored the electrolytes to near normal. Histological alterations such as glomerulonephritis and tubules infiltration by inflammatory cells observed in diabetic control
were also reversed.

Conclusion: This study suggests renal protective ability of the plant against impairment due to hyperglycemia.

Keywords: Streptozotocin, Thaumatococcus danielli, Nephroprotective, Glibenclamide, serum electrolytes.

Introduction: Studies suggest that ATP-sensitive potassium (KATP) channels are a potential
pharmacotherapeutic target for neuroprotection in neurodegenerative diseases. The current
study aimed at evaluating the effect of pretreatment with glibenclamide (Glib) and B vitamins
supplement on the severity of behavioral symptoms in 6-hydroxydopamine (OHDA)-induced
Parkinsonism. Also malondialdehyde (MDA) concentration was measured in the blood and brain
suspensions to find probable neuroprotective mechanism of Glib.
Methods: The 6-OHDA was injected into striatum of rats by stereotaxic surgery. Treatment
with Glib and B vitamins was started before the surgery and continued up to 3 weeks after that.
Development and severity of Parkinsonism were evaluated by conventional behavioral tests.
MDA values were measured spectrophotometrically using thiobarbituric acid and MDA standard
curve.
Results: Pretreatments with Glib, at both doses of 1 and 5 mg/kg or B vitamins significantly
ameliorated severity of the behavioral symptoms. Pretreatment with a combination of Glib and B
vitamins was more effective than pretreatment with Glib or B vitamins alone. Also, pretreatment
with B vitamins, Glib, or a combination of them reduced MDA concentration in the brain
suspensions. Decrease in MDA concentration in the group of rats that received a combination of B
vitamins and Glib was more prominent than that of the Glib groups.
Conclusion: As severity of the behavioral symptoms in the 6-OHDA-induced Parkinsonism
reflects the degree of the lesion in Substantia Nigra (SN) dopaminergic neurons, it is suggested
that Glib pretreatment has neuroprotective effect against 6-OHDA-induced neurotoxicity. The
current study data also showed that this effect may be mediated by antioxidant effect of Glib.

Objectives: The present study was undertaken to determine the interaction of glibenclamide with methanolic extract of bark of Ficus glomerata Roxb. (FBME).
Methods: The interaction was evaluated in normal and alloxan-induced diabetic rats using the parameters such as glucose tolerance test, acute and subacute levels of antidiabetic study and body weight estimations at various intervals. Glibenclamide was administered orally at two different doses of 300 µg/kg (low dose) and 600 µg/kg (high dose) and FBME was co-administered at the dose of 200 mg/kg. Individual treatments of above drugs were also carried out.
Results: The combination therapy of glibenclamide and FBME showed significant (P<0.01) hypoglycemic effect compared to their individual treatments in the parameters studied and it also showed more percentage increase in body weight than the individual treatments.
Conclusion: The present herb-drug interaction was found to be beneficial as it was observed that FBME showed synergistic effect with glibenclamide. This could provide an opportunity to reduce the dose of glibenclamide to achieve an enhanced therapeutic effect with minimal side effects.

Diabetes mellitus, often simply referred to as diabetes, is a group of metabolic diseases in which a person has high blood sugar, either because the body does not produce enough insulin, or becausecells do not respond the insulin that is produced. 1 This high blood sugar produces theclassicalsymptoms of polyuria (frequent urination), polydipsia (increased thirst) and polyphagia (increased hunger). The global increase in the prevalence of diabetes is due to population growth, aging, urbanisation and an increase of obesity and physical inactivity. It is estimated that there are currently 285 million people with diabetes worldwide and this number is set to increase to 438 million by the year 2030. 2 The study was conducted on 4 groups of 6 rats each to evaluate the hypoglycaemic effect of Atorvastatin. Glibenclamide was used as a standard drug and the results were compared in reference to it. Tween 80 was given for both normal and diabetic control groups. The fasting blood sugar levels were recorded on 1 st ,3 rd ,5 th ,7 th ,10 th days by Glucometer. The results indicate that the test compound Atorvastatin has significant and sustained oral hypoglycaemic activity, comparable with the hypoglycaemic effect of Glibenclamide, a sulfonylurea. The hypoglycaemic potential of Atorvastatin is found to be comparable with that of the standard drug Glibenclamide.

Aims This study compared the effects of 52 weeks' treatment with pioglitazone, a thiazolidinedione that reduces insulin resistance, and glibenclamide, on insulin sensitivity, glycaemic control, and lipids in patients with Type 2 diabetes. Methods Patients with Type 2 diabetes were randomized to receive either pioglitazone (initially 30 mg QD, n = 91) or micronized glibenclamide (initially 1.75 mg QD, n = 109) as monotherapy. Doses were titrated (to 45 mg for pioglitazone and 10.5 mg for glibenclamide) to achieve glycaemic targets during the next 12 weeks: fasting blood glucose of ≤ 7 mmol /l and 1-h postprandial blood glucose of ≤ 10 mmol / l. Patients were maintained on the titrated dose for 40 weeks. Results Pioglitazone significantly increased insulin sensitivity compared with glibenclamide, as assessed by homeostasis model assessment (17.0% vs. − 13.0%; P < 0.001), quantitative insulin sensitivity check index (0.011 vs. − 0.007; P < 0.001) and fasting serum insulin (− 1.3 pmol /l vs. 23.8 pmol /l; P = 0.007). The glibenclamide group had significantly lower HbA 1c than the pioglitazone group after 12 weeks of therapy (7.8% vs. 8.3%, P = 0.015), but significantly higher HbA 1c after 52 weeks of therapy (7.8% vs. 7.2%, P = 0.001). Pioglitazone significantly (vs. glibenclamide) increased mean HDL-C (P < 0.001), decreased mean triglycerides (P = 0.019), and decreased mean atherogenic index of plasma (AIP; P = 0.001) and mean total cholesterol / HDL-C (P = 0.004), without significantly elevating mean total cholesterol or mean LDL-C compared with glibenclamide. Conclusions These data suggest that the effects of pioglitazone are more sustained than those of glibenclamide for improving insulin sensitivity in patients with Type 2 diabetes, and that 52 weeks' treatment with pioglitazone has favourable effects on glycaemic control and lipoprotein profile.

Purpose: To examine body mass index (BMI), occupation, sex, age, and duration of therapy as contributory factors in treatment failure in type 2 diabetic patients taking metformin and glibenclamide in a tertiary hospital in Northwestern Nigeria. Method: A retrospective case control study was employed where variables (age, sex, body mass index, tribe, duration of therapy, glycaemic profile and occupation) for a total of 520 type 2 diabetic patients that took metformin and glibenclamide for a minimum of 1 year were examined. Patients were classified into two groups based on progression to triple oral therapy or a switch from metformin and glibenclamide therapy. Results: Of the 520 patients analysed, 276 failed treatment. Over 90 % of the patients were&gt; 40 years while 61 % had been on treatment for&gt; 4 years. The subjects ’ mean age was 53.22 ± 9.03 years. The mean population body mass index (BMI) was 27 kg/m2. Housewives comprised more than half of the population (55.5 %). The mea...

Diabetic patients, habitually, use plants and plant products those assumed to have an anti-hyperglycemic desire often combined with the oral anti-diabetic medication given. The subsequent interaction between the ingested plant and the medication taken may affect the pharmacology and toxicology profile of which either component 298 leads to number of categorizing effects. This study designed to investigate the anti-diabetic properties of the mixture of Swietenia macrophylla seeds and endocarps aqueous extract in STZ-induced diabetic rats, and also to assess the possible plant-medication interaction with glibenclamide. Twenty four male rats (Sprague Dawley) made diabetic, they were orally force-fed with glibenclamide, mixture of seeds and endocarps aqueous extract and combination of full strength extract with half of the previous glibenclamide dosage, daily for three weeks. Body weight and FBG levels were determined at treatment intervals of 0, 7, 14 and 21 days. Both glibenclamide and plant extract showed hypoglycemic effect. Highest significance found in the group with combined treatment of plant extract plus glibenclamide. We concluded that the use of the aqueous extract of Swietenia macrophylla King seeds and endocarps in combination with glibenclamide can exhibit potent additive anti-diabetic effect in rats.