ABSTRACT
OBJECTIVE: Research has shown that polycystic ovary syndrome (PCOS) is a common cause of infertility in women. The drugs used to treat PCOS tend to manage the symptoms rather than cure the disease. Furthermore, these drugs have severe side-effects and influence the quality of life for the patients. There is therefore a need for natural medicine that can effectively treat PCOS without side-effects. METHOD: PCOS was induced in adult female Wistar rats by daily oral administration of letrozole (1 mg/kg) for 21 days. From day 22 until the end of the experiment (day 36), these rats were given a daily oral dose of either Prunus dulcis (walnut) or Salvia hispenica (chia seed) alone, or in combination. Animals were subsequently examined for morphological, biochemical, and histopathological changes. RESULT: When compared with the control and standard groups, rats who had consumed P. dulcis and S. hispenica, either as individual agents or in combination, had significantly lower body and ovarian weights, and hormone concentrations were maintained at healthy levels. The presence of polyphenolic compounds in these substances induced ovulation in the PCOS model animals. CONCLUSION: This study demonstrated that animals fed with P. dulcis and S. hispenica either individually or in combination were able to overcome infertility. Hormone levels and metabolism were restored in these animals. Therefore, P. dulcis and S. hispenica can be used as therapeutic agents to treat patients who are infertile due to suboptimal oocyte competence and anovulation.
ABSTRACT
Metformin/Gliclazide extended release tablets were formulated with Eudragit NE30D by wet granulation technique. Two batches were prepared in order to study influence of drug polymer ratio on the tablet formation and in vitro drug release. The formulated tablets were characterized by disintegration time, hardness, friability, thickness, weight variation, and in vitro drug release. The percentage of polymer, with respect to Metformin/Gliclazide, required to produce tablets with acceptable qualities was 9 to 13.45. The percentage of polymer below this range released the drug immediately and above this range produced granules not suitable for tablet formation. The quantity of Metformin/Gliclazide present in the tablets and the release medium were estimated by a validated HPLC method. The formulated tablets had acceptable physicochemical characters and released the drug over 6-8 h. The data obtained from in vitro release studies were fitted with various kinetic models and was found to follow Higuchi kinetics.
Subject(s)
Gliclazide/pharmacokinetics , Metformin/pharmacokinetics , Polymethacrylic Acids/pharmacokinetics , Chemistry, Pharmaceutical , Delayed-Action Preparations/pharmacokinetics , TabletsABSTRACT
In the present study, a series of 1-substituted-4-hydroxyphthalazines were synthesized and characterized by IR, 1H-NMR and Elemental analysis. The compounds were assayed against seizures induced by maximal electroshock (MES) and pentylenetetrazole (scMet). Neurologic deficit was evaluated by the rotarod test. The decrease in the elevated motor activity by introceptive chemical stimuli (amphetamine antagonistic activity) was studied at the dose level of 25 and 50 mg kg(-1) and cardiac activity was also studied. All the compounds exhibited significant anticonvulsant activity. Compounds 4, 12, 13 and 17 were most active of the seriesagainst MES-induced seizures. Compounds 2, 4, 13 and 17 exhibited significant decrease in the elevated motor activity at the dose of 50 mg kg(-1). Remarkable sympathetic blocking activity was observed with 3, 5, 6, 7, 9 and 15 only.
Subject(s)
Anticonvulsants/chemistry , Anticonvulsants/pharmacology , Phthalazines/chemistry , Phthalazines/pharmacology , Amphetamine/antagonists & inhibitors , Animals , Anticonvulsants/chemical synthesis , Dose-Response Relationship, Drug , Drug Interactions , Epinephrine/pharmacology , Heart/drug effects , Magnetic Resonance Spectroscopy , Mice , Motor Activity/drug effects , Myocardial Contraction/drug effects , Pentylenetetrazole/toxicity , Phenobarbital/pharmacology , Phthalazines/chemical synthesis , Ranidae , Seizures/chemically induced , Structure-Activity RelationshipABSTRACT
In the present study, a series of 2-substituted-4-methyl-7-amino/4,7-dimethyl-1,8-naphthyridines were synthesized and characterized by IR, 1H-NMR and elemental analysis. The compounds were investigated for anticonvulsant (125, 250 mg/kg), cardiac and antimicrobial activities. The compounds were screened for antibacterial activity against gram (+) bacteria (Staphylococcus epidermidis, Bacillus subtilis, Enterococcusfaecalis and Micrococcus luteus) and gram (-) bacteria (Proteus vulgaris, Pseudomonas aeruginosa, Escherichia coli and Salmonella typhi). All the compounds except 2-(3'-phenylaminopropyloxy)-4-methyl-7-amino-1,8-naphthyridine exhibited significant anticonvulsant activity. The anticonvulsant activity of 2-(3-morpholino-2'-hydroxypropyloxy)-4-methyl-7-amino-1,8-naphthyridine, 2-(3'-diphenylamino-2'-hydroxypropyloxy)-4-methyl-7-amino-1,8-naphthyridine and 2-(3'-diethanolamino-propyloxy)-4,7-dimethy-1,8-naphthyridine at the dose of 250 mg/kg were found to be equivalent to diazepam (5 mg/kg). Sympathetic blocking activity was observed with 2-(3'-phenylamino-2'-hydroxypropyloxy)-4-methyl-7-amino-1,8-naphthyridine, 2-(3'-diethanolamino-2'-hydroxypropyloxy)-4-methyl-7-amino-1,8-naphthyridine and 2-(3'-diphenylamino-2'-hydroxypropyloxy)-4-methyl-7-amino-1,8-naphthyridine only. All the compounds were devoid of antibacterial activity against the tested bacteria.