Standardized extracts arose out of the need to create a uniform product for clinical trials. .. With the pharmaceutical companies in control, they have taken patients . of the herb's constituents are present to deliver an efficacious product. their multidimensional role in homeostatic management of inflammation, to support various standardized herbal extract phytosomes as a tool of drug delivery. of herbal medicines to be incorporated in novel drug delivery system, such as Controlled drug release and subsequent biodegradation are important for developing . Gugulipid is a standardized extract prepared from the oleo gum resin of.
CONTROL DELIVERS STANDARDIZED EXTRACTS PHARMACEUTICAL
The potential market is huge and growing incrementally. The next step, however, was how to realize enough profit to justify a costly campaign of research to increase credibility. Herbs unlike chemical drugs, themselves are not patentable. However, a standardized product used for research is patentable.
An herbalist who was one of the first to examine and pass judgment on standardized extracts and highly concentrated herbal preparations was Dr. Alfred Vogel of Bioforce Company of Switzerland.
In his laboratory at Roggwil, Switzerland, he concluded that tinctures of the whole plant were more effective than fluid extracts that were extra concentrated according to active principles. An overview of some of the main German companies that were among the first to produce standardized extracts may give us some intimation of the direction of the herbal movement in the United States.
Lichtwer-Pharma is in a suburb of Berlin. In they became established as a company to manufacture a small product range of herbs. These include garlic, valerian, St Johnswort, and hawthorn. The goal of the company has always been to make plant-based medicine that would be acceptable to conventional medical practice. To this aim, it has invested heavily in research and technology.
With heart disease in Germany and the US being the number one killer, they found that a high quality garlic product standardized to 1.
The venture was phenomenally successful worldwide, with the sale of Kwai garlic in at around 40 million dollars. Because of the huge money it spent in research while seeking a license for its garlic product, the company was able to aggressively market a prescription garlic product to doctors on the basis of its ability to strengthen the heart and counteract many of the conditions associated with aging.
The same formula for success occurred by targeting the most common mental illness, depression. To any vested pharmaceutical company the opportunity to validate the efficacy of a product leading to approval by investing sums of money for research is the formula for phenomenal success. In the case of hypericum this could be the case.
There may be an ancient reference for this use in the annals of Chinese medicine but essentially, this product sprang on the market with no reference to previous empirical data. As such it could be heralded as a triumph by western pharmacy over empiricism or traditional use. This was further underscored by the fact that based on their research, the most effective standardized form required 50 parts of the slightly yellowed autumn harvested leaves to be reduced to one part with further extraction with highly toxic solvents to arrive to produce this product.
Sales of this product is unprecedented if for no other reason than the fact that there are no synthetic drugs known to be effective for senile dementia. The pattern repeats itself, first launching it simultaneously as a prescription drug in Germany and France, total sales worldwide in of Gingko standardized extract was million dollars.
Most are not on these boards because of their clinical experience in the use of herbs but because of their academic standing. Many of these such as Varro Tyler scarcely less than a decade ago could barely be counted as a supporter of herbal medicine. As such, I find that the public media and various herb journals attempt to achieve credibility by including these unqualified individuals posing as having practical hands-on clinical herbal experience is very misleading.
Certainly one of the most misleading of all stances that is all to often advocated is the patently inaccurate statements that the use of standardized extracts are the only way to assure identity, quality and efficacy.
As briefly described, by definition, a standardized herbal extract involves predetermining one or a number of biochemical constituents as either active or as marker compounds. The result involves two very distinct types of extracts.
This type establishes that a specified amount of a marker compound is present in the finished product. It must be remembered that a marker does not represent the active constituents but is selected as a biochemical constituent characteristic of the plant.
In many cases, if this process uniformly increases all plant constituents to an intended level. In general, the insoluble compounds, such as cellulose and fiber, are excluded.
In some cases the concentrated extracts remain dried and powdered while in others they are mixed with a neutral material such as corn starch, and in still others, the extract is mixed with the fine granules of the whole herb. The most important distinction is that marker extracts are not based on the concentration of a proven active constituent, but are used for positive identification or to create a higher degree of uniform potency.
As for the latter, it as yet remains to be proven whether this is consistent with the potency of the whole herb. Considering the fact that all herbal preparations are to a degree an extract, a marker extract that equally regulates all constituents, retains more relationship to the traditional way herbalists use herbs. Another problem is the propensity to overly promote one use over many others that it may have.
Traditional herbal medicine uses herbs more functionally rather than for the treatment of specific pathology. There are some differences as to how each herb is treated but in general the following is a list of some of the better known Marker Extracts.
This regulates a specific biochemical constituent to a level that may not be naturally found in the plant. There are at least three specific and obvious problems with pumping up one constituent of a product at the expense of its other constituents:.
The problem of exclusively promoting an herb as a standardized extract overlooks the range of many of its other uses. For instance, Milk thistle seed extract is specifically sold as a liver protective agent while the Eclectics according to Felter and Lloyd as quoted in Ellingwood described a much wider use. These include a dull aching pain over the spleen that passes up to the left scapula associated with pronounced debility and despondency, splenic pain with or without enlargement.
Further uses indicate that it was known to improve blood circulation especially in the pelvis making it particularly useful for dysmenorrhea, amenorrhea and irregular passive uterine hemorrhages. It is known that in fact, very few herbs in trade are reliably standardized to known active constituents as opposed to possibly inactive markers? Joerg Gruenwald is one of the editors for the German Commission E Monographs, a recently published book that is regarded as the highest recognized standard in the western world on medicinal herbs and plant products.
Sennosides in senna are still regarded as the active constituent in senna but the kava lactones in kava or the ginsenosides in ginseng are questionable as to whether there are no other actives involved. This means that one who exclusively relies on using a standardized extract based on known active ingredients, except for a very few, might be just as well or even better served by using a quality non-analyzed herb product.
Certainly it will be cheaper in cost and even the quality of herb used is likely to be superior because the manufacturer would be selecting herbs based more on quality than quantity. Imagine telling a traditional Chinese herbalist that they should only use phytopharmaceuticals in the form of standardized extracts. They do not treat primarily by named diseases but conditions that give rise to disease. This is what traditional herbal medicine is best able to do.
Certainly concentrated extracts of all ingredients of high quality botanicals can be used in this practice and I use them a great deal in my practice as 5 to 1 dried extracts. They are not as effective as the nasty tasting herbs but there is better long-term patient compliance.
So we lose and gain something in the process. Except for researching the action of a specific or a limited group of plant constituents, why do we need them? What Rudy and Bonati are pointing to is that to truly standardize, every variable concerning the growth, harvest and preparation of a plant must be controlled.
From their perspective, it is disadvantageous to use wild herbs because they may not be up to standard. Herbalists have for centuries used highly effective methods of selecting and sorting herbs according to their quality. This is also standardization.
At the same time, there is a strong tradition that wild herbs are generally superior to cultivated. The opposite is advocated by the advocates of standardization. Again the recurring leitmotif, why?
This movement while attracting more consumers to herbs is really luring them to what I am afraid is the ultimate eclipse of herbal medicine as an alternative. Anything can happen at that point of evolution. Drugs go into obsolescence all the time. Once herbs are regarded as phytopharmaceuticals it is a short stretch for them to be considered as just another drug.
It seems that what we gain from this treatment of herbs is too little and what we lose, the ability to treat patients by a distinct medical paradigm encompassed by the term wholistic or traditional herbal medicine. He discovered that there were dozens of other constituents in whole unadulterated turmeric that also possessed anti-inflammatory properties. Some of these may be as potent or even more potent than curcumin. Again, there is nothing wrong with having both choices available turmeric high in the anti-inflammatory curcumin for joint and gall bladder inflammations and the whole root that can also be used for blood circulation and digestion.
The unanswered question based on lack of research is whether the whole herb is as effective for inflammation as the standardized extract. Herbalists may argue that it is so then why bother making a standardized extract based on the high concentration of curcumin? Again, the reason for the original development of the standardized extract of turmeric was not because it would be superior but because it is more appropriate for controlled study and research based on the high concentration of curcumin.
Plant chemistry is extremely complex representing a vast number of chemical compounds. The complexity of this issue raises serious concern of what might be gained or lost if we limit ourselves to a standard of exclusively using only standardized extracts. From this we see that curcumin, as the standardized marker for turmeric are effective for the widest number of applications. Further, it is a compound that is certainly unique to the herb.
There are a few conditions, such as the use of turmeric for skin conditions antidermatic and a lipoxygenase inhibitor where curcumin has no relevance.
Its professional membership, whose members are admitted through a process of peer review, represents a considerable number of years of collective clinical experience that should not be overlooked in any honest inquiry or discussion about the efficacy and safety of herbs. The primary reason standardized herbal extracts exist is because they are considered necessary to achieve as much control in double blind studies as is possible.
Researchers, however, never intended to establish that standardized extracts were superior to whole herbs or more conventional preparations. It produces a consistently strong product with guaranteed constituents.
When you consider the quality of most commercial herbs, this at least assures that they have something in it and that the correct herb is being used. The major proponents of standardized extracts view herbs as medicine in a way that is fundamentally different from herbalists.
Rudolf Bauer, one of the leading botanical research scientists in Germany states the three primary reasons for the standardization of herbs into phytopharmaceutical drugs. He states that 1. Also, in pharmacological, toxicological and clinical studies with herbal drugs, their composition needs to be well documented in order to obtain reproducible results, 3, The World Health Organization Who has recognized this problem and has published guidelines to ensure reliability and repeatability of research on herbal medicines, 4.
This concept should be followed not only in research, but also in the production and therapeutic application of phytopharmaceuticals. From the perspective of this paper, the question is what is involved in making a traditional medicinal herb conform to the standards of a drug i.
Who is it that needs herbs in this form and used in this way? Researchers attempting to get a grant or funding for research on the medicinal properties of plants, the pharmaceutical industry and the medical establishment, which is not interested in being transformed by wholistic herbal medicine but into changing it into something that will be acceptable within their paradigm, and the herb industry who through marketing, can capitalize on the union of science and herbal medicine to develop a competitive edge in the market.
It is understandable that this would not sit well with most clinical herbalists and the many who were drawn to the use of herbs based on a need to affirm their connection and interdependence with nature. The question really is whether this is necessary and to whom and for what? Is it necessary for effective herbal practice?
Hardly — imagine telling a Chinese herbalist that it is best for he or she to use only chemically standardized herbal extracts in the form of phytopharmaceuticals? It is a key point of this of this article, however, that standardized extracts, and I think we are mostly referring to active constituent extracts, have very specific applications as compared with commercial, non-analyzed whole herb products.
As such they might not always be the best choice. Studies comparing the effects of standardized biochemical extracts with whole herbs or conventional preparations would be very enlightening.
Unfortunately, so far there has been no enthusiasm for such a study because there is more profit to be made from the sale of standardized extracts. Another reason favoring the use of standard extracts is that they assure positive identification that the herb is what it is claimed to be. Cheating and misrepresentation has been endemic in the field of herbalism at least since the time of the Egyptians and Greeks. We read in ancient records complaints of receiving bogus herbs or herbs of inferior quality.
Therefore, while a standardized extract of a particular herb may offer a degree of assurance that the product is what it claims to be, even with this method, it is possible to be deceived and cheated, winding up with the wrong herb in an adulterated form of a standardized extract.
One consideration is that standardizing to a single biochemical compound requires exponentially higher quantities of herbs. Unless we are confident in the overriding importance of an isolated chemical constituent, as opposed to the use the whole herb, it is wasteful to support the harvest of tons of herbs for this purpose.
Furthermore, the harvest of such huge quantities of an herb invariably threatens quality. Part of the implied assumption is that before the availability of standardized herbal extracts most herbal products were inferior. The truth is that there are many herbal companies who make high-quality herbal products. Further, one advantage a smaller company has over a larger one is that it needs less quantity to achieve superior quality, while the manufacturer of standardized products is more likely to sacrifice quality of botanical material for quantity.
Other approaches to drug delivery are focused on crossing particular physical barriers, such as the blood—brain barrier, in order to better target the drug and improve its effectiveness; or on finding alternative and acceptable routes for the delivery of protein drugs other than via the gastrointestinal tract, where degradation can occur.
Presently novel drug delivery systems have been widely utilized only for allopathic drugs, but they have their own limitations hence, turning to safe, effective and time-tested Ayurvedic herbal drug formulation would be a preferable option. However, the drug delivery system used for administering the medicine to the patient is traditional and out-of-date, resulting in reduced efficacy of the drug. In case of herbal extracts, there is a great possibility that many compounds will be destroyed in the highly acidic pH of the stomach.
Other components might be metabolized by the liver before reaching the blood. As a result, the required amount of the drug may not reach the blood. Phytopharmaceuticals are pharmaceuticals using traditional compounds derived from botanicals instead of chemicals. Natural ingredients are more easily and more readily metabolized by the body. Therefore they produce fewer, if any, side effects and provide increased absorption in the bloodstream resulting in more thorough and effective treatments.
Pharmaceuticals made from chemical compounds are prone to adverse side effects. The human body will have a tendency to reject certain chemical compounds which do not occur naturally.
These rejections occur in the form of side effects; some as mild as minor headaches, and others as severe as to be potentially lethal. It is important to note while phytopharmaceuticals produce fewer to no side effects, chemical interactions with other prescription drugs can occur.
Furthermore, as they are single and purified compounds, they can be easily standardized making it easier to incorporate them in modern drug delivery systems compared to herbs. Lipid-based drug delivery systems have been investigated in various studies and have shown their potential in controlled and targeted drug delivery.
Pharmacosomes are amphophilic phospholipid complexes of drugs bearing active hydrogen that bind to phospholipids. They impart better biopharmaceutical properties to the drug, resulting in improved bioavailability. Phytosomes are novel compounds comprising of lipophilic complexes of components of plant origin like Silybum Marianum, Ginkgo Biloba, ginseng and so on, with phospholipid. They have high lipophilicity and improved bioavailability and therapeutic properties.
These are advanced form of herbal extract that have improved pharmacokinetic and pharmacological parameter, whose result can advantageously be used in treatment of acute liver diseases, either metabolic or infective origin. Phytosomes are produced by a patent process in which individual component of herbal extract like flavonolignans and terpenoids are bound on a molecular level to the phospholipids like phosphatidylcholine through a polar end.
Phytosomes are used as a medicament and have wide scope in cosmetology. Many areas of phytosomes are to be revealed in future in the prospect of pharmaceutical application.
Phytosomes forms a bridge between the convectional delivery system and novel delivery system. If the herbs themselves or the purified phytopharmaceuticals or phytosomes are incorporated in novel drug delivery systems, we can get the benefits of both. Thus it is important to incorporate the novel drug delivery system in Indian Ayurvedic medicines to combat serious diseases. As herbal novel drug delivery systems have lot of potential, several researchers are working towards developing novel drug delivery systems like mouth dissolving tablets, sustained and extended release formulations, mucoadhesive systems, transdermal dosage forms, microparticles, microcapsules, nanoparticles, implants etc.
Some of them are at the laboratory stage and some have reached to the marked. Some of the research work done in this area is summarized below. Asoka Life science Limited launched Res-Q, the world's first poly-herbal mouth dissolving tablet, fast mouth dissolving drug. It has a novel drug delivery system that imparts increased efficacy. In Ayurvedic medicine segment, this is the first attempt to make medicines more effective in managing chronic ailments. Res-Q is a poly-herbal medicine highly effective for lung problems and other respiratory ailments like asthma.
This unique mouth dissolving drug delivery system ensures that the drug reaches the blood directly and the first pass metabolism is bypassed. It dissolves in mouth by mixing with the saliva and get absorbed. This Res-Q provides relief from respiratory distress within fifteen minutes. This way, this drug resembles the efficacy of Sorbitrate, a revolutionary mouth dissolving drug used in cardiac distress.
The active ingredients are selected from the group consisting of hypericin, hyperforin and echinacosides. The invention seeks to provide improved herbal preparations, whose preparations offer a convenient oral dosage form of herbs for supplying optimum plasma concentrations of the biologically active compounds that facilitates user compliance. The oral-controlled and stable release dosage form of granulated herb is in either matrix formulations such as matrix tablets or in multi-particulate formulations like microcapsules put into two piece capsules that are done in order to obtain a drug delivery system, which will ensure a steady supply of the active components for a sustained period.
Another US patent invention is a new stable herbal drug formulation in the form of sustained-release microgranules containing Gingko Biloba extract as well as the process for preparing it. Plant extracts have poor flowability and compressibility properties. Thus, formulation of such extracts in the form of sustained release tablets is difficult, as it requires homogeneous mixtures of extracts with pharmaceutical excipients during all compression steps. Microgranules can be manufactured by a number of different processes, for example extrusion-spheronization, fluid air bed process or a coating-pan method.
Extrusion-spheronization is suitable for pellets with high content of active substance, but need more equipment. For the manufacture of the granules of the invention, the coating-pan method is preferred, as it requires only simple equipment and operation.
A study on palatal mucoadhesive tablet containing a herbal formulation showed the sustained release abilities of buccal adhesive tablets comprising of muco-adhesive polymers. The ingredients of the herbal formulation i. In the study, the herbal formulation comprised of these four herbal medicinals was incorporated into a slow dissolving mucoadhesive tablet, designed to fit the palate. Results indicated that the adhesive tablet containing the herbal formulation is effective in reducing oral malodor and VSC levels.
An investigation aimed to formulate transdermal films incorporating herbal drug components such as Boswellic acid Boswellia serrata and curcumin Curcuma longa is one of the first few attempts to utilize ayurvedic drugs through transdermal drug delivery system TDDS , which utilizes skin as a site for continuous drug administration into the systemic circulation.
Thus this delivery system avoids the first pass metabolism of the drug without the pain associated with injection; moreover, the system provides a sustained drug delivery with infrequent dosing via zero-order kinetics and the therapy can be easily terminated at any time. Use of turmeric in TDDS for the local action of the drug at the site of administration can also be considered as a new version of ayurvedic turmeric poultice or lepa.
The formulations selected for oral retention were from the group consisting of gels, pastes and chewing gums. The herbal ingredients are selected and prepared to provide a composition that is effective at causing human scalp and facial hair to darken, to reduce loss of scalp hair and to promote hair growth after a period of repeated usage. In a study by Ma and colleagues, the effect and mechanism of Shuanghua aerosol SHA was investigated on upper respiratory tract infections in children aged from 3 to 14 years.
The authors conclude that SHA has obvious anti-inflammatory and antiviral effects and has a good curative effect in treating infantile upper respiratory tract infections. Gugulipid is a standardized extract prepared from the oleo gum resin of Commiphora wightii been clinically proven to reduce the levels of harmful serum lipids in the blood stream.
Microparticles of gugulipid were formulated by different techniques using chitosan, egg albumin, sodium alginate, ethyl cellulose, cellulose acetate, gelatin and beeswax. The microparticles were evaluated for their physico-chemical characteristics.
The HPLC profile showed distinct separation of Guggulsterone-E and -Z; confirming entrapment of gugulipid in the prepared microparticles. Microcapsules with entrapped herbal water-soluble extracts of plantain Plantago major and calendula Calendula officinalis L. PCE were prepared by layer-by-layer adsorption of carrageenan and oligochitosan onto calcium carbonate microparticles with their subsequent dissolving after the treatment of EDTA.
Entrapment of PCE was performed by using adsorption and co-precipitation techniques. The co-precipitation provided better entrapment of PCE into the carbonate matrix compared to adsorption.
In vitro release kinetics was studied using artificial gastric juice. Using the model of acetate ulcer in rats, it has been demonstrated that PCE released from the microcapsules accelerates gastric tissue repair. Nanoparticles of TCH traditional Chinese herbs are helpful to improve their absorption and distribution in body, and therefore enhance their efficacies. Traditional Chineseherbs, including peach seed, safflower, angelica root, Szechwan lovage rhizome, Rehmannia root, red peony root, leech, gadfly, earth worm and ground beetle , were mixed and prepared through drying, mincing, extracting, crushing into liquid particles with ultrasonic wave, filtering and nanometerizing into nanoparticles soliquid with nanometer collider.
Nanoparticles of TCH s showed significant thrombolytic effects, resulting in quick recovery from arterial embolism and diminution of thrombi.
The thrombolytic effects of nanoparticles of TCHs are much intensified than their non-nanoparticle form. There are also some research works on integrative evaluation, pharmacokinetics and pharmacological activity of the oral prolonged-release preparations of traditional Chinese medicine.
Novel sustained-release implant of herb extract using chitosan has proved to be very useful. The extract of danshen Radix Salvia miltiorrhiza , a medicinal herbal, was developed with CS—gelatin as an implant for the promotion of anastomosing and healing on muscles and tissues at the organic incision site in abdominal cavities.
Measurements were made of the sustained release of tanshinone IIa, a marker component, from the material in vitro. The dissolution medium was assayed with a high-performance liquid chromatography method. Biodegradation studies of the material were also conducted both in vitro and in vivo. The film made of this material exhibited a sustained release effect. The release profile conforms to the Higuchi equation. Drug release was found to be effectively controlled by the drug-amount loaded in the matrix.
This film of 0. ArthriBlend-SR is a marketed formulation containing herbal extracts and nutrients to support healthy joints and connective tissues in the body. It is a proprietary clinically validated blend of natural actives for joint care applications. The composition has the added advantage of sustained release technology, which benefits the continuous management of symptoms of arthritis.
The blend contains Glucosamine sulfate, Boswellin Boswellia serrata extract and Curcumin C3 Complex Curcuminoids from Curcuma longa , ingredients that work synergistically to support the management of inflammatory conditions such as arthritis. The benefits of a sustained release formulation are particularly relevant to the bioavailability of glucosamine.
Why Standardized Herbal Extracts?
Mar 24, Formulations of herbal novel drug delivery system [33,36,38,47] Content uploaded .. phytoconstituents or standardized plant extracts. into phospholipids . control the release of drug from microsphere. The release of drug. Citation: Pawar HA, Bhangale BD () Phytosome as a Novel Biomedicine: A Microencapsulated Drug Delivery System. J Bioanal Biomed Phytosomes - A New Herbal Drug Delivery System standardized extract and active ingredients of an herb . compared to a group of controls (49 treated.