Design, Development and Rationalization of Sarpagandha Ghanvati.

Sarpagandha ghanvati is a classical Ayurvedic formulation widely prescribed for anxiety and insomnia. It contains Sarpagandha (roots of Rauwolfia serpentina L. (Benth.) Ex Kurz; Family: Apocyanaceae), Khurasani ajowan (Hyocyamus niger L.; Family: Solanaceae) seeds, Jatamansi (Nardostachys jatamansi DC. Family: Valerianaceae) roots and Pipplamul (root of Piper longum L.; Family: Piperaceae). The objective of this study was to make a comparative evaluation of Ghanvatis and tablets of this formulation. Two tablet formulations were prepared; one incorporating only powders of all ingredients; the other with ethanol extracts of the first three ingredients and powder of Piper longum root. Similarly, two types of Sarpagandha ghanvati pills were prepared; one as per Ayurvedic Formulary of India; the other with ethanol extracts of the first three ingredients and powder of Piper longum root. Alcohol extracted 0.22% w/w of total alkaloids as against 0.061% w/w extracted by water. Tablets prepared with powders of all the ingredients had friability more than 3.0% where as those prepared with ethanol extract had very low friability. Ghanvatis, prepared as per the Ayurvedic formulary, did not show reserpine although other alkaloids were present. They showed less content uniformity and lower drug release. Ethanol extracted reserpine along with other alkaloids. Ghanvatis made with the alcoholic extracts exhibited better content uniformity and drug release than the traditional formulation. Tablets prepared with powders or extracts of the ingredients exhibited good content uniformity but the release of alkaloids from the tablets of powders was only 80%. Tablets of the extracts had good content uniformity with 90% release of the total alkaloids. Tablets prepared with alcoholic extracts using 1% polyvinylpyrrolidone as binder and 5% dried starch powder as disintegrating agent confirmed to all the requirements. Thus, the study shows tablets made with the extracts are superior to Ghanvatis and powder tablets.

Development of carbamazepine transnasal microemulsion for treatment of epilepsy.

Carbamazepine is widely preferred therapy for the treatment of epilepsy. However, oral therapy results in slower brain uptake and systemic side effects. Intranasal route can achieve faster brain uptake, but poor aqueous solubility of carbamazepine is the main obstacle for administration by nasal route. The purpose of this study was to prepare and evaluate intranasal oil in water microemulsion of carbamazepine to improve its solubility and enhance the brain uptake. Intranasal microemulsion of carbamazepine was prepared by water titration method using oleic acid as oil, Tween 80 as surfactant and Transcutol® as cosurfactant. Microemulsions were evaluated for various physical parameters including globule size, viscosity, pH and conductivity. Toxicity study of microemulsion was carried out by employing sheep nasal mucosa. The microemulsion was also evaluated by maximal electric shock, and the brain uptake study was done using HPLC method. The microemulsion was stable and transparent with average globule size of 21.03 nm and did not show any toxic symptoms. It showed reduction in the hind limb extension phase and faster recovery from seizures in comparison to oral microemulsion and nasal solution. Higher brain/plasma ratio was obtained with nasal microemulsion in comparison to ratio obtained after intraperitoneal injection of carbamazepine solution.

Design and development of mixed film of pectin: ethyl cellulose for colon specific drug delivery of sennosides and triphala.

The present study was aimed at developing colon specific drug delivery system for sennosides and Triphala. These drugs are reputed Ayurvedic medicines for constipation in India. The proposed device explored the application of pectin and ethyl cellulose as a mixed film for colon specific delivery. This mixed film was prepared using non-aqueous solvents like acetone and isopropyl alcohol. A 32 factorial design was adopted to optimize the formulation variables like, ratio of ethyl cellulose to pectin (X1) and coat weight (X2). The rate and extent of drug release were found to be related to the thickness and the ratio of pectin to ethyl cellulose within the film. Statistical treatments to the drug release data revealed that the X1 variable was more important than X2. Under simulated colonic conditions, drug release was more pronounced from coating formulations containing higher proportions of pectin. The surface of the device was coated with Eudragit S100 to ensure that the device was more pH dependent and trigger the drug release only at higher pH. The final product is expected to have the advantage of being biodegradable and pH dependant. This type of a film effectively releases the drug while maintaining its integrity.

In vitro studies on guar gum based formulation for the colon targeted delivery of Sennosides.

PURPOSE: The objective of the present study is to develop colon targeted drug delivery systems for sennosides using guar gum as a carrier. METHODS: Matrix tablets containing various proportions of guar gum were prepared by wet granulation technique using starch paste as a binder. The tablets were evaluated for content uniformity and in vitro drug release study as per BP method. T(50) % value from the dissolution studies was taken for selecting the best formulation. RESULTS: Guar gum matrix tablets released 4-18% sennosides in the physiological environment of gastrointestinal tract depending on the proportion of the guar gum used in the formulation. The matrix tablets containing 50% of guar gum were found to be suitable for targeting of sennosides for local action in the colon. Compared to tablets having 30% and 40% of guar gum, those with 50% guar gum gave better T(50)% (11.7 h) le and fewer amounts (5-8%) of drug release in upper GIT. These tablets with 50% guar gum released 43% and 96% sennosides with and without rat caecal fluids. This suggests the susceptibility of matrix to the colonic micro flora. The similarity factor (f2 value) for drug release with and without rat caecal fluids was found to be less than 30. When hydroxy propyl methylcellulose phthalate (10%) was used as a coat material on the matrix tablets, the initial loss of 5-8% sennosides in stomach could be completely averted. These tablets showed no change in physical appearance, content and dissolution profile upon storage at 45 degrees C / 75% relative humidity for 3 months. CONCLUSION: The results of our study indicates that matrix tablets containing 50% guar gum and coated with 10% hydroxy propyl methylcellulose phthalate are most suitable for drugs like sennosides which are mainly active in the lower GIT.

Anti-bacterial activity of Galega officinalis L. (Goat's Rue).

Alcoholic extracts of Goat's Rue (Galega officinalis L.; Papilionaceae) were tested on Gram +ve and Gram -ve bacteria as the plant was claimed to hasten skin healing after surgery. Ethanolic (60%) extract exhibited significant inhibition on growth of both Gram +ve and Gram -ve bacteria.