New and traditional ayurvedic dosage forms

New & Traditional Ayurvedic Dosage Forms

K V GOPINATH M Pharm PhD,CPhTTirumala Tirupati Devasthanams

TIRUPATIe-mail:[email protected]

Definitions

Ayurvedic medicines are medicines intended for internal or external use, for or in the diagnosis ,treatment, mitigation or prevention of disease or disorder in human beings or animals.

Ayurvedic Drugs are obtained from the natural source that is from animal, plants and minerals.

Dosage form: It is a finished product of a drug contain the active drug in association with excipients.

Ayurvedic Dosages forms are classified in to four groups

- Solid Dosage Forms: Pills, Gutika, Vatika.- Semi-solid Dosage Forms: Avleha, Paka, Lepa, Ghrta.- Liquid Dosage Forms: Asava, Arista, Arista, Arka, Taila, Dravaka.- Powder Dosage Forms: Bhasma, Satva, Mandura, Pisti, Parpati, Lavana, Kshara, Churna.

Different Types of herbal NDDS

Liposomes

Microspheres

Nanoparticles

Phytosomes

Transferosomes

Ethosomes

Polymeric micelle formulations

Transdermal systems

Implants

Micro pellets

Complexation

Nano / micro emulsions

Advantages of New Ayurveda Dosage forms

Enhancement of solubility and bioavailability

Protection from toxicity

Enhancement of pharmacological activity

Enhancement of stability

Improving tissue macrophages distribution

Sustained drug delivery systems

Increased compliance , less total drug administration, increased outcome from the patient

Liposomes

Liposomes Microspheres Nanoparticles Phytosomes Transferosomes Ethosomes Nano /

micro emulsions Polymeric micelle

formulations Transdermal

systems Implants Micro pellets Complexation

These are colloidal and spherical vesicles (0.05 – 5.0 μm in diameter) composed of a bilayer membrane entrapping an aqueous core.

There are constructed with polar lipids which are made up of lipophilic and hydrophilic group on the same molecules.

Enhance product performance by increased solubility , bioavailability, targeting at site of action and prolonged release of drug.

Topical application of the capsaicin liposomal formulation increase in the skin permeation as well as increased duration of action , inclusion of taxanes (antitumor activity) into the liposomes led to decreased tissue related toxicities of the drug with the increase in the efficacy of drug.

Limitations: Low encapsulation efficiency, Rapid leakage of water-soluble drug in the presence of blood components and Poor storage stability.

Microspheres





It consists of spherical particles of size ideally 1-300 um. Each particle is matrix of the drug dispersed in the polymer

and drug is released as a first order process. Polymers used for fabrication of micro particulate carriers

such as albumin, gelatin, modified starch, polypropylene, dextran, polylactic acid and polylactide-co-glycolide etc

Plant active ingredients such as rutin, camptothecin, zedoary oil, tetrandrine, quercetine and cynara scolymus extract has been made into microspheres.

Immune microspheres and magnetic microspheres Limitations: - poor entrapment

- premature release.

Nanoparticles





These are colloidal systems with particles varying in size from 10 nm to 1000nm.

Advantages: - Increasing compound solubility

- Reducing doses

- Relatively increasing the absorbency of herbal medicines.

Limitations: - particle-particle aggregation

- Difficult in handling liquid and dry forms

Phytosomes





It is a emerging trends in delivery of herbal drugs and nutraceuticals.

It is a formulation that incorporates standardized plant extracts or water soluble phyto constituents into phospholipids to produce lipid compatible molecular complexes.

It improves absorption and bioavailability of herbals.

It is useful as in case of flavanoids, tannins, and terpenoids.

Limitation is their bioavailability when administered orally or topically.

Transferosomes





It is a phospholipid vesicle which acts as powerful carriers.

It is a potential Transdermal delivery of the cur cumin.

It is chemically unstable and its purity is under question.

They are very expensive.

Ethosomes





It is a vesicle composed of phospholipids and high concentration of ethanol.

Improved drug delivery to deeper layer of the skin and even to blood.

It is useful for topical delivery of alkaloids

Unstable and skin poor permeation limits their utility.

Nano/micro emulsions





These are O/W or multiple emulsion having the size range of several microns.

Useful in trans dermal delivery system,

Non-toxic and non irritant

Nanoemulsions useful in delivering drugs to cell culture, cancer therapy and as disinfectants.

It increases solubility and bioavailability of the drug.

Palatability and compatibility with other excipients is a limiting factor in the case of oral drug therapy.

Polymeric micelle formulations





Polymeric micelle consists of an inner hydrophobic core capable of solubilizing lipophilic substances and an outer hydrophilic corona which serves as the stabilizing interface.

It is used to carry a number of drugs like Artemisinin form Artemisia annua L and Curcumin form the roots of Curcuma longa L are used as antimalarial drug.

Polymer Sodium dodecyl sulfate led to 25 fold increase in solubility.

Poor physical stability and potential for embolism.

Transdermal Systems





These are the devices in which drug present in the formulation permeates into the systemic circulation by diffusion to stratum corneum and further to the effected organ.

These devices use polymer matrix, adhesive bandage and permeation enhancers.

Advantage: controlled drug delivery, enhanced bioavailability, reduction in side effects and easy application.

Transdermal delivery of herbal drugs are to increase the penetration and sustained action.e.g.transdermal films containing boswellic acid ( Boswellia serrate) and curcumin (Curcuma longa) were formulated for the treatment of inflammation (synergistic effect).

Limitations are hepatic first pass metabolism, increased therapeutic effect, and maintenance of steady state concentration in the serum.

Implants





It is used for controlled and sustained action of the drug Devices are directly placed in the body fluids/cavities by

mean of a microsurgery They are fabricated by using biodegradable polymers e.g.

chitosan and gelatin. Non biodegradable polymers may cause irritation. Implants of the extract of danshen (Radix salvia Miltiorrhizae)

used for healing of muscles and tissues in the abdominal cavities.

Activity may last for 28 days, that prevents the patient from frequent dosing.

Micropellets





These are used for the delivery of drugs (1-1000 µm) to specific sites and for the extended period of time

Used for the delivery of the two incompatible drugs simultaneously.

Pellets are used for the coating and taste masking of the formulations.

Pectin-hydroxypropyl methylcellulose (HPMC) coated curcumin pellets were prepared for delivery of the curcumin in the colon to treat the inflammatory disease.

Pectinolytic enzymes helps in releasing drug in the colon, and avoids vomiting, loss of appetite and nausea

The limitations are bioavailability and site specific drug delivery.

Complexation





It is the association between two or more molecules to form a non bonded entity with well defined stoichiometry.

Various complexing agents such as EDTA, cyclodextrins and polymers have been used for the complexation

The solubility of the curcumin was increased by the formation of the Curcumin soya lecithin complex and evaluated for the hapato-protective activity.

Traditional Ayurvedic Dosage Forms

Asava and AristaThese are the medicinal preparations prepared by soaking the drugs in the powdered forms or in the form of their decoction, in a solution of sugar or jaggery as may have intended for a specific period of time.

- It may produce self generated alcohol on fermentation and have sedation . Arka

It is the liquid preparation obtained by distillation of certain liquids or curde – drugs soaked in water using the distillation unit, (Arkayantra)

Avleha or Leha and PakaAvleha or Leha is a Semi-solid preparations of drugs prepared by addition of sugar, jaggery or sugar candy and boiled with prescribed drug juice or decoction.

2)


Kvatha CurnaThe coarse powder of crude drugs or the combination of drugs in powder form, kept ready for preparation of decoction (Kasaya) are known as Kvath Curna.e.g.: Dasmula Kvath Curna, Rasanadi Kvath Curna.

Curna (Churna)Fine powder of drug or drugs is known as Curna, Drugs mentioned in yoga are cleaned, properly, dried thoroughly, Pulversied and then sieved.

DravakaThe liquid preparations obtained from lavanas or ksharas are known as Dravakas. They are prepared by distillation process with or without addition of any fluids.e.g.: Sankha Dravaka.


KsarasAlakaline substances obtained from the ash of drugs are known as Ksaras. Drugs are cut in to small pieces and burnt to get ash. Ash is dissolved in water, stained again evaporated to get rid of water while salty solid obtained is known as Ksar.e.g.: Yav Ksara, Palsa Ksara.

LepaThe preparations in the form of paste meant for external applications on the body are known as Lepa.e.g.: Sinduradi Lepa, Pathyadi Lepa.

Vati or GutikaMedicaments in the form of Tablets or pills are known as vati or Gutika.e.g.: Muktadi Mahanjana and Chandroday Vartti.


Netrabindu and Anjan: Netrabindu is made by dissolving the specified drugs in water or kasaya or honey and used as eye drops. Anjans are very fine powders of medicaments to be applied with netrasalaka.e.g.: Muktadi Mahanjana and Chandroday Vartti.

Sattva: Water extractable solid substances obtained from drugs are known as Sattva.e.g.: Gulvel Sattva.

Pisti: These are obtained by triturating the drug with the specified liquids and exposing to sun or moon light.e.g.: Praval Pisti, Mukta Pisti.

Rasa-Yoga: The Medicinal Preparations containing mineral drugs as their main ingredients in the form of powder or pills are known as Rasa Yoga.e.g.: Kapura Rasa, Laghu Malini Vasant Rasa.


Greta (Snehkalapa)These are preparations in which ghee in boiled with the prescribed quantity of the decoction and fine paste of the drug as specified in the formula.

Taila (Oils)Tailas are the preparations in which tailas (Fixed Oils) is boiled with specified decoction and fine paste of the drug as mentioned in the prescribed formula.e.g.: Bhrangaraja Taila, Maha Narayan Taila.

BhasmaThe powdered form of the substances, obtained by calcinations of metals minerals or animal products by a special process in closed crucibles in pits covered with cow dung cake (Puta) is known as Bhasma.e.g.: Godanti Bhasma, Lauha Bhasma.


Kupipakva-Rasayana: These are the drugs prepared as: The minerals and drugs of metallic origin in the powdered form are mixed together and placed in glass flask occupying about one third of volume. The glass flask is closed with clay smeared pieces of cloth around the bottle in seven consecutive layers. The flask is dried and buried in sand (Valukayantra) up to neck. The flask in Valukayantra is then heated gradually in three that is Mrdu-agni, Madyamgni and tiksnagni for specified period of time as mentioned in process. Then the red hot iron rod about 5cm in diameter is inserted in glass flask through the opening and stirred properly, do that opening of flask is not chocked due to the coating formed by sublimed Sulphur. When the process is over, the glass flask is cooled and broken to collect the content carefully without the contamination of any glass pieces therein.e.g.: Makaradhvaja, Swarna sindura.

Conclusion

NDDS system of herbal drugs have a potential future of enhancing the activity and overcoming problems associated with plant medicines.

New and traditional ayurvedic dosage forms

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