A novel method of extraction of bamboo seed oil (Bambusa bambos Druce) and its promising effect on metabolic symptoms of experimentally induced polycystic ovarian disease.

OBJECTIVE: To evaluate the potential effect of bamboo seed oil in decreasing the major metabolic symptoms associated with letrozole-induced polycystic ovarian disease using female rat model. MATERIALS AND METHODS: A new method of microwave-assisted extraction was developed. Female rats were grouped into four with six animals each. All rats were daily administered with letrozole (1 mg/kg b.wt.) for 21 days except control, and during this period, changes in estrous cycle were observed. After letrozole treatment, Group 2 was considered negative control, Groups 3 and 4 were treated orally with bamboo oil, 0.5 ml/kg b.wt. and 1 ml/kg b.wt., respectively, for 3 weeks (five consecutive estrus cycles). Various parameters such as estrus cycle, blood sugar level, lipid profile, and weights of reproductive system were determined. The characteristics of cystic ovaries were evaluated by histopathological studies. RESULTS: The isolated bamboo oil restored estrus cyclicity showed hypoglycemic and hypolipidemic effects. 1 ml/kg b.wt. of bamboo oil showed a marked glucose reduction from 254.04 ± 2.08 to 92.6 ± 1.63, and levels of total cholesterol, very low-density lipoprotein, triglyceride were reduced from 186.45 ± 2.28, 30.07 ± 2.36, 100.36 ± 2.35 to 152.14 ± 2.63, 25.94 ± 1.66, 93.32 ± 1.09, respectively. Histopathological results showed the presence of ovulation and recovery from cystic ovaries. CONCLUSION: A novel and promising drug was isolated in the treatment and maintenance of various metabolic symptoms associated with polycystic ovary disease.

Colon specific drug delivery of tramadol HCl for chronotherapeutics of arthritis.

OBJECTIVE: The objective of present work is to develop and evaluate a matrix system for Chronotherapeutic delivery of centrally acting of opioid analgesic (tramadol HCl) to treat nocturnal symptoms of arthritis using almond gum as carrier. MATERIALS AND METHODS: Matrix tablets of tramadol HCl were prepared by using 30, 40, 50, 60 and 70% w/w of tablet of gum badam as carrier by wet granulation technique. These tablets were compression coated with eudragit S100 to prevent drug release in stomach. All formulations were evaluated for hardness, friability, weight variation, drug content, in vitro and in vivo studies. The almond gum was characterized by viscosity measurements and Fourier transform infrared analysis. The coated (FC1 to FC5) and uncoated tablets (F1 to F5) were evaluated for in vitro release of tramadol HCl after sequential exposure to pH 1.2, pH 7.4 and pH 6.8 respectively for 2 h, 3 h and 19 h in the absence as well as presence of rat caecal content and the corresponding data was fitted to popular release kinetic equations in order to evaluate the release mechanisms-kinetics. The selected formulation was subjected to in vivo targeting efficacy studies by roentgenography technique. RESULTS AND DISCUSSION: In vitro release studies indicated that the matrix tablets (F1 to F5) failed to control the drug release in the physiological environment of stomach and small intestine. On the other hand, compression coated formulations were able to protect the tablet cores from premature drug release. Presence of rat caecal content enhances the drug release from the tablets as the concentration of polymer increased, drug release was found to be retarded. The release of tramadol from all the formulation followed zero order with non fickian diffusion. X-ray studies confirmed that the tablet successfully reached colon without getting disintegrated in upper gastrointestinal tract. CONCLUSION: Based on the results, selective delivery of tramadol HCl to the colon could be achieved using 60% w/w (FC4) of almond gum matrix tablets compression coated with eudragit S100.

GC-MS analysis of Cocus nucifera flower extract and its effects on heterogeneous symptoms of polycystic ovarian disease in female Wistar rats.

AIM: To evaluate the effect of Cocus nucifera L. flowers in reducing the major multiple symptoms of letrozole-induced polycystic ovarian disease (PCOD) in female rats. METHOD: Female, virgin Wistar rats were treated with letrozole (1 mg/kg body wt) to induce PCOD, and after 21 days of induction rats were administered orally with 100 and 200 mg·kg(-1) of Cocus nucifera flower aqueous extract, respectively. Estrus cycle and blood sugar were monitored once a week throughout the study. After scarification, various biochemical parameters, such as antioxidant status (superoxide dismutase (SOD) and glutathione reductase (GSH)) of the uterus homogenate, lipid profile (total cholesterol (TC), high density lipoprotein (HDL), low density lipoprotein (LDL), and triglycerides (TG)) of the serum were determined. Weights of the uterus and ovaries were separately monitored. The characteristics of changes in the ovary were evaluated by histopathological studies. RESULTS: GC-MS analysis of the aqueous extract showed the presence of volatile and pharmacologically active phytoconstituents. C. nucifera flower extract-treated groups showed estrus cyclicity and increased uterus weight which indicates the estrogenic effect. The improved blood sugar level, ideal lipid profile, good antioxidant status, and histopathology results revealed the recovery from poly cystic ovaries. CONCLUSION: The results indicate that C. nucifera flower is a potential medicine for the treatment of PCOD and this study supports the traditional uses of C. nucifera flower.

Mucoadhesive buccal films of glibenclamide: Development and evaluation.

BACKGROUND: Glibenclamide is an oral hypoglycemic drug completely metabolized in the liver, the principal metabolite being very weakly active, buccal delivery may be useful for the treatment of diabetes more effectively. The aim of the present study was to design formulations and systematically evaluate in vitro and ex vivo performances of buccal films of glibenclamide so that the required therapeutic plasma concentrations can possibly be achieved more rapidly using the different grades of hydroxypropyl methyl cellulose (HPMC) as the base matrix. MATERIALS AND METHODS: Mucoadhesive buccal films of glibenclamide were prepared by solvent casting technique using different grades of HPMC with different ratios. Prepared films were evaluated for weight, thickness, surface pH, swelling index (SI), folding endurance, drug content uniformity, in vitro release, and ex vivo permeation studies. RESULTS: The film thickness and weight were in the range of 0.213-0.4892mm and 22.25-39.83 mg, respectively. The films exhibited controlled release over more than 6 h. HPMC, HPMCK100, and HPMC3000 films exhibited satisfactory swelling. Surface pH of buccal films was found to be 6.4-6.8. SI observed to be highest for GF12 (275.3 ± 12.17) and lowest for GF1 (173.5 ± 5.65). The films exhibited controlled release over more than 6 h. HPMC exhibited satisfactory swelling, an optimum residence time, and promising drug release. The Higuchi plots were found to be linear with correlation coefficient values of 0.8933, 0.9138, and 0.9947 for GF4, GF8, and GF9, respectively. CONCLUSIONS: Among all the formulations, GF9 shows good controlled release results correlated with ex vivo permeation studies.

Pharmacokinetic evaluation of guar gum-based colon-targeted drug delivery systems of tinidazole in healthy human volunteers.

The aim of the present investigation was to determine the in vivo availability of guar gum-based colon-targeted tablets of tinidazole in comparison with immediate release tablets of tinidazole in human volunteers. Six healthy volunteers participated in the study, and a cross-over design was used. The plasma concentration of tinidazole was estimated by HPLC. The pharmacokinetic parameters were calculated from the plasma concentration of tinidazole versus time data. The immediate release tablets of tinidazole produced a peak plasma concentration (Cmax of 3239 +/- 428 ng/ml) at 1.04 +/- 0.32 hr (Tmax), whereas colon-targeted tablets produced peak plasma concentration (Cmax of 2158 +/- 78 ng/ml) at 14.9 +/- 1.6 hr. The delayed Tmax, decreased Cmax, and Ka, and unaltered bioavailability and elimination half-life of tinidazole from guar gum-based colon-targeted tinidazole tablets, in comparison with the immediate tablets, indicated that the drug was not released in the stomach and small intestine but delivered to the colon. Slow absorption of the drug from the less absorptive colon might result in the availability of the drug for local action in the colon. The guar gum-based colon-targeted tablets of tinidazole may be useful in providing an effective and safe therapy of intestinal amoebiasis.

Studies on the development of colon targeted oral drug delivery systems for ornidazole in the treatment of amoebiasis.

The aim of the present study is to develop colon-targeted drug delivery systems for ornidazole using guar gum as a carrier. The core formulation containing ornidazole was directly compressed. Compression-coated tablets of ornidazole containing various proportions of guar gum in the coat were prepared. All the formulations were evaluated for hardness and drug content uniformity and were subjected to in vitro drug release studies. The amount of ornidazole released from tablets at different time intervals was estimated by the HPLC method. The compression-coated formulations released less than 8% of ornidazole in the physiological environment of stomach and small intestine. The compression-coated tablets with 85%, 75%, and 65% of guar gum coat released about 21%, 38%, and 73% of ornidazole, respectively, in simulated colonic fluids indicating the susceptibility of the guar gum formulations to the rat caecal contents. The results of the study show that compression-coated ornidazole tablets with either 65% (OLV-65) or 75% (OLV-75) of guar gum coat are most likely to provide targeting of ornidazole for local action in the colon owing to its minimal release of the drug in the first 5 hr. The ornidazole compression-coated tablets showed no change in physical appearance, drug content, or in dissolution pattern after storage at 40 degrees C/75% relative humidity for 6 months.