Drug – bio-affecting and body treating compositions – Plant material or plant extract of undetermined constitution...
Reexamination Certificate
2003-03-26
2004-12-21
Tate, Christopher R. (Department: 1654)
Drug, bio-affecting and body treating compositions
Plant material or plant extract of undetermined constitution...
Reexamination Certificate
active
06833143
ABSTRACT:
FIELD OF THE INVENTION
The present invention relates to an improved process for the preparation of stable bacosites enriched fraction in non-hygroscopic form from the herb
Bacopa monniera.
BACKGROUND AND PRIOR ART
Plant based drugs and formulations are showing a rising trend globally for the health care due to the biosafe attributes they possess over modern synthetic medicines. Amongst the numerous traditional Indian medicinal herbs, standardized extract of
Bacopa monniera
known as ‘Brahmi’ in Hindi is finding increasing use as a constituent of modern herbal nutraceuticals aimed at supporting brain and nerve function and enhancing memory, alertness & mental concentration (Ray Sahelian, M.D. “Mind Boosters”, 1999, Amazon Publishing House, USA).
Bacopa monniera
has been used in India since ancient times in Ayurvedic preparations as a brain and a nerve tonic (Chunekar K C, “Bhav Prakasha Nighantu”, Hindi translation, Varanasi, 1960: 372). In a clinical trial carried out at the Banaras Hindu University. (Singh R H and Singh Lallan, “Studies on the Anti-anxiety effect of the Medhya Rasayana Drug, Brahmi
Bacopa monniera
Wettst. Part 1
, Journal of Res. Ayurveda
&
Sidha
Vol 1: 133-148, 1980).
Bacopa monniera
in the form of brahmi syrup when administered to 35 patients suffering from anxiety neurosis, it was concluded that 4 weeks of treatment with brahmi significantly reduced the level of anxiety amongst the patients with improvement in the mental performance and memory of the treated patients. The beneficial effects of
Bacopa monniera
on the intelligence and mental performance were further investigated at Banaras Hindu University in a trial carried out on 20 school children over a period of three months. (Sharma R, Chaturvedi C, Tewari P V, “Efficacy of
Bacopa monniera
in revitalizing intellectual functions in Children”
Journal Res. Edu, Ind Med
, Jan-Jun.: 1-12, 1987).
Systematic Chemical Examination of
Bacopa monniera
was first reported by N Chatterjee, R P Rastogi & M L Dhar, (
Indian Journal of Chemistry
, Vol 1, May 1963). They reported the occurrence of two saponins designated as Bacoside A & B which are present in a concentration of over 2% in the dry plant. The molecular structure of the bacosides A & B was subsequently elucidated. (Chatterjee N, Rastogi R P and Dhar M L,
Indian J Chem
, Vol 3: 24, 1965 and Basu N, Rastogi P and Dhar M L,
Indian J Chem
Vol 5: 84, 1967). These studies also reported the physical properties of the bacosides A&B:
Bacoside A,
Melting Point = 250.6° C. (decomposition),
Optical Rotation &agr;
D
= (−) 42° in Ethanol
Bacoside B,
Melting Point = 203° C. (decomposition),
Optical Rotation &agr;
D
= (+) 8° in Ethanol
An analytical method based on high performance thin layer chromatography (HPTLC), for the determination of bacoside-A content in
Bacopa monniera
has been reported by Gupta et al (A P Gupta, S Mathur, M M Gupta & Sushil Kumar, “Effect of the method of drying on the bacoside-A content of the harvested
Bacopa monniera
shoots revealed using a high performance thin layer chromatography method”,
Journal of Medicinal and Aromatic Plants
Vol, 20: 1052-1055, 1998). The bioactivity of
Bacopa monniera
extract has been studied by evaluating the avoidance responses in Rats in an extensive trial carried out at the Central Drug Research Institute, Lucknow, India (H K Singh, R P Rastogi, R C Srimal and B N Dhawan,
Phytotherapy Research
, Vol 2 (2): 70-75, 1988). It has been concluded in this study that Bacosides A & B are the active constituents of
Bacopa monniera
which are responsible for the enhanced mental performance and retention capacity.
The authentication of the traditional claims of brahmi was investigated at the Central Drug Research Institute by studying the effect of alcoholic extract of this plant on acquisition, consolidation and retention of the three memory related behavioral responses in albino rats. (Singh H K and Dhawan B N, “Neuropsychopharmacological effects of the Ayurvedic nootropic
Bacopa monniera
Linn (Brahmi)”,
Indian Journal of Pharmacology
, Vol 29 (5): S359-S365, 1997). In this study, bacosides were also found to be safe in regulatory, pharmacological and toxicological studies carried out on normal healthy male volunteers. This study was designated as Phase-I clinical trial.
Bacopa
extract was administered to human volunteers for 4 weeks in single and multiple doses in double blind placebo controlled and non-crossover regulatory clinical trial. The mechanism of action of the facilitatory effect of bacosides was attributed to their enhanced protein kinase activity and production of an increased level of protein in hippocampus. Another conclusion of this study was that the bacosides attenuated the retrograde amnesia produced by immobilization induced stress and scopolamine. P A Thakurdesai, P L Kole and A. N Nagappa (www.Pharmabiz.com
ewsfeat/feat/112.com) have stressed the necessity of using standardized extracts for achieving desired efficacy.
Considering the great importance and potential of bacosides, derived from
Bacopa monniera
, in human health, the information about an efficient process suitable for industrial production is not available in the literature. Patent literature also does not disclose any information on the subject of efficient production technology of bacosides. The literature contains a few lab scale methods for the preparation of an extract of
Bacopa monniera
containing bacosides. The method of isolation adopted by Chatterjee et al (N Chatterjee, R. P. Rastogi & M. L. Dhar,
Indian Journal of Chemistry
, Vol 1, May 1963; Chatterjee N, Rastogi R P and Dhar M L,
Indian J Chem
, Vol 3: 24, 1965) and further modified by Singh et al (H K Singh, R P Rastogi, R C Srimal and B N Dhawan,
Phytotherapy Research
, Vol 2 (2): 70-75, 1988), describes the extraction of the
Bacopa monniera
dried herb with alcohol, wherein the dried herb material is first moistened with water and then extracted with alcohol, which is concentrated under reduced pressure and repeatedly macerated with benzene for defatting. The filtrate is diluted to 60% concentration of alcohol and is treated with an excess of lead acetate. The lead salts are filtered and the residual lead was removed from the filtrate with hydrogen sulphide. The pH of the filtrate is adjusted to 6.4 with sodium carbonate and concentrated at 50° C. under vacuum to one third of its volume and partitioned repeatedly with butanol & water. The butanol fraction on concentration under vacuum deposits a powder containing bacosides A&B. The powder is then crystallized from alcohol as colourless needles. An additional amount of bacosides is obtained from the filtrate by freeing it from solvent and macerating the residue with acetone. This method apart from being very tedious and time consuming involves the use of benzene (potentially carcinogenic) and lead salt (highly poisonous). Although the process attempts to remove the residual lead with hydrogen sulphide gas, the complete removal is doubtful in view of involvement of gas-liquid mass transfer where high efficiencies are difficult to achieve. The presence of these toxic chemicals even in traces will make the quality of the final product questionable. This method is not suited for scaling up to industrial production due to being tedious and health hazardous. In the method adopted for the study carried out by H K Singh and B N Dhawan (Journal of Ethanopharmacology, Vol 5: 205-214, 1982), to evaluate the effect of brahmi extract on avoidance responses in rats, the air dried plant material is extracted with 90% ethanol by soxhlet extraction apparatus and the extract obtained is mixed with 10% gum acacia for feeding the rats. In this study no attempt was made to monitor the bacosides contents of the extracts. In an another study carried out at the University of Madras on the anti cancer activity of
Bacopa monniera
(V. Elangovan, S Govindasamy, N Ramamoorthy and K. Balasubramanian, “In vitro studies on the anticancer activity of
Bacopa monniera, Fi
Gupta Madan Mohan
Kahol Atul Prakash
Singh Tarun
Tandon Sudeep
Perkins Coie LLP
Tate Christopher R.
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