Study of pharmacodynamic interaction of Phyllanthus emblica extract with clopidogrel and ecosprin in patients with type II diabetes mellitus.

BACKGROUND: Diabetes mellitus is associated with oxidative stress which impairs the platelet function. Phyllanthus emblica extract a rich source of vitamin C plays an important role in scavenging free radicals. The effect of vitamin C on platelet aggregation in healthy and coronary artery disease patients has been demonstrated. The present study attempts to study the pharmacodynamic interactions of P. emblica extract with clopidogrel and ecosprin. MATERIALS AND METHODS: This was a randomized open label crossover study of 10 type II diabetic patients. The dosage schedules were either single dose of 500 mg P. emblica extract or 75 mg clopidogrel or 75 mg ecosprin or 500 mg P. emblica+75 mg clopidogrel or 500 mg P. emblica+75 mg ecosprin. After single dose study and washout period, patients received either 500 mg P. emblica extract twice daily or 75 mg clopidogrel or 75 mg ecosprin once daily or combinations for 10 days. Platelet aggregation was measured at baseline and at 4h of treatment after single and multiple dose study along with recording of bleeding and clotting time. RESULTS: After single and multiple dose administration of the three treatments and with combinations there was statistically significant decrease of platelet aggregation compared to baseline. Further, the mean percent inhibition of platelet aggregation was significant, when compared between single and multiple doses of P. emblica. The bleeding and clotting time was prolonged with single and multiple dose administration of all treatments compared to baseline. All treatments were well tolerated. CONCLUSION: P. emblica extract demonstrated significant antiplatelet activity with both single and multiple dose administration.

Antinociceptive and anti-inflammatory activity of a flavonoid isolated from Caralluma attenuata.

Luteolin-4'-O-neohesperidoside, i.e. luteolin-4'-O-[alpha-(L-rhamnopyranosyl-(1-->2)-beta-D-glucopyranoside)] has significant anti-inflammatory action. It is more potent than ibuprofen. Its antinociceptive activity is less pronounced when compared with its anti-inflammatory activity.

Involvement of receptors in IDPH-791 induced prolongation of pentobarbitone hypnosis.

IDPH-791, when injected (ip) to mice potentiated the pentobarbitone sleeping time in a dose dependent manner. Involvement of neurotransmitters and receptors in this effect was studied using various receptor blockers, enzyme inhibitors, agonist and an amine depletor. Pretreatment with high dose of yohimbine (0.5 mg/kg), haloperidol, cyproheptadine, atropine and a combination of atropine and yohimbine significantly reversed the activity. Physostigmine, diethyldithiocarbamate and high dose of apomorphine (2.5 mg/kg) potentiated the subminimal effect of IDPH-791, whereas low dose of apomorphine (0.1 mg/kg) failed to potentiate. However, reserpine significantly reversed this response. Prazosin, phenoxybenzamine, low dose of yohimbine (0.25 mg/kg), propranolol, methysergide, mepyramine and cimetidine did not produce any change, thus ruling out the involvement of adrenergic, serotonergic and histaminergic systems. There seems to be simultaneous involvement of muscarinic receptors and postsynaptic dopamine (D2) receptors in IDPH-791 induced potentiation of pentobarbitone hypnosis.

A rapid method for evaluation of analgesic and anti-inflammatory activity in rats.

Carrageenin (2%) was used to produce edema and hyperalgesia; indomethacin, phenylbutazone, aspirin, ibuprofen, analgin, paracetamol and phenacetin were tested at different doses for anti-inflammatory and analgesic activity in the same rats as the peak for the edema reached at the end of 3rd hr and for the hyperalgesia at the end of 4th hr. Indomethacin, phenylbutazone and ibuprofen reduced edema and increased the pain threshold. Analgin and aspirin increased the pain threshold relatively at a low dose. Paracetamol and phenacetin were inactive in the doses tested. Carrageenin (2%) was observed to possess both phlogistic and allogenic properties.