Narrative review of guggulu formulations of ayurveda reflecting their percentage of guggulu, pharmaceutics and pharmacology

Introduction

Ayurvedic medicine involves use of various types of formulations. The formulations include basic formulations [juice, decoction, paste, powders, cold and hot infusions], and advance formulations like medicated ghee, medicated oil, semisolid avaleha preparations, fermentation products of acidic and alcoholic nature, pills of various sizes and guggulu formulations [specialised preparations of oleo gum resin of guggulu], and many more.

Various types of formulations in Ayurvedic system of medicine

The basic formulations include herbal fresh juice, decoction, paste, cold infusion, hot infusion. Further formulations are modified and advanced versions of these basic dosage forms. The need for modifications was observed when these basic formulations missed the mark to fulfil criteria like shelf life, palatability and stability. Most patients cannot prepare drugs freshly due to practical issues. Palatability issues arise in infants and pregnant females due to the smell and taste of the medicine. The shelf life of these dosage forms is only couple of hours after they are prepared i.e., they become unstable for consumption as microorganisms grow in them and they get contaminated due to high moisture content. If they are preserved, the adverse effects of preservation come into picture.

Therefore, to overcome and to fulfil the above-mentioned criteria, pill formulations emerged. The preparation of pills requires a binding agent like sugar, jaggery, gum resin of commiphora wightii (guggulu) to bind the ingredients and for uniform shape of guti-vati. These are the natural binders.^[1] 

S.No.	Kalpa	Dose according to classical ref	Percentage of guggulu	Indications
1.	Sinhanad guggulu [2]	2-3 gm in divided dose	11.11%	Rheumatoid arthritis, skin disease, gout, tumour, painful condition, rejuvenation, etc (anupan-ghruta, taila, mansarasa, shaali)
2.	Gokshuradi guggulu [3]	[1 shaan=3gm]  3gm divided dose.	12.5%	Diabetes, Burning sensation on urination (mutrakruchra), Menorrhagia (pradar), Anuria (mutraaghat), gout (vatarakta), Renal calculi (ashmari).
3.	Amrutaakhya guggulu [4]	2-3 gm	13.7%	Gout, skin disorder (kushta), treatment of wound (dustavrana), diabetes (prameha), Rheumatoid arthritis (aamvata), Fistual (bhagandar), pilonidal sinus (naadivrana).
4	Panchatiktak guggulu [5]	6-12gm divided dose.	14.2%	Skin disorders involving toxicity or rashes, Anti- toxic activity, vata related disorders (vatavyadhi), tumour (gulma), diabetes (meha), Anemia (pandu)
5	Punarnava guggulu [6]	2-3gm divided dose.	16.6%	Skin disorder (Twacharoga), swelling (shotha), Anemia (pandu), obesity (sthaulya), Kapharoga.
6	Vatari guggulu [7]	early in morning with warm water for a month 2-3gm divided dose.	16.6%	Vata vyadhi, painful conditions like sciatica, RA, gout, burning sensation at extremities.
7	Loha guggulu [8]	1 karsha = 12 gm	17.6%	Rejuvenator.
8	Kaishor guggulu [9]	3gm	18.13%	Gout (Vatarakta), Skin disorder (kustha), Wound (vrana), Diabetic wounds (prameha pitika), Diabetes (prameha), Ascitis (udar), Anemia (pandu), rejuvenation (rasyana), improves skin health, eye diseases (netraroga), vranakushthaghna (to be consumed with khadir kwatha).
9	Chandraprabha [10]	125mg to 500 mg	20.51%	Disorders of teeth (dantaroga), eye disorder (netraroga), aartavadushti, shukradushti, mandagni, Anorexia (aruchi), Dyspnea (shwas), cough (kaas), skin disorders (kushtha), Diabetes (prameha), burning sensation on urination (mutrakruchra), anuria (mutraghata), renal calculi (ashmari), tumour (granthi), pain in lower back (katishoola), ascites (udar),fistula (bhagandar), rejuvenation (rasayana)
10	Amruta guggulu [11]	3 gm	21.7%	Gout (Vatarakta), skin disorder(kushta), haemorrhoids (arsha), wound(dushtavrana), Diabetes (prameha), rheumatoid arthritis (aamvata), fistula (bhagandar).
11.	Amrutadi guggulu [12]	3 gm	22.22%	Diabetic wound (Pramehapidika), fistula (bhagandar), obesity (sthaulya)
12.	Mahayograj guggulu [13] (sha)	3 gm	25.86%	Vata disorders (Vatavyadhi), skin disorders (kushta), arsha, Diabetes (prameha), Fistula (bhagandar), Tuberculosis (kshaya), Epilepsy (apasmar), anorexia (aruchi), Anemia(Pandu)
13.	Loha guggulu [14]	1 karsha= 12gm with ushnodaka	33.3%	Anemia (pandu), Jaundice (kamala)
14.	Yograj guggulu [15]	2-3gm in divided dose.	50%	Rheumatoid arthritis (Amavata), worms (krumi), Wound (dushtavrana), Tumour (gulma), Haemorroids (arsha).
15.	Tryushnadi guggulu [16]	Desha-kala-bala anusar	50%	Diabetes (Prameha), urinary system related disorders (mutradosha), in certain paediatric disorders (balaroga).
16.	Kanchanar guggulu [17]	2-3gm divided dose	50%	Enlargement of glands/nodes in neck region, tumour (granthi), wound (vrana), skin disorders (kustha), Fistula (bhagandar).
17.	Navaka guggulu [18]	3 gm	50%	Rheumatoid arthritis (amavata)
18.	Abha guggulu [19]	3 gm	50 %	Fracture healing (chakradatta), arthritis (Bhagnasandhi prasadaka)
19.	Vidangadi guggulu [20]	1 Vatak i.e., 10 gm (to be consumed with cow ghee) with meal.	50%	Wound (Dushtavrana), Diabetes (prameha), Skin disorder (kushtha).
20.	Amruta guggulu [21]	5gm	50%	Wound (Vrana), Gout (vatarakta), Tumour (gulma), Anemia (pandu).
21.	Varadi guggulu [22]	10gm [1 vatak]	50%	Gonorrhoea, Blood related disorder (raktadosha), Wound (dushtavrana).
22.	Swayambhuakhya guggulu [23]	3 gm	50%	Skin related disorder (Mahakushta.)
23.	Aabha guggulu [24]	3 gm	50%	Used in union of fractures. (Bhagnasandhiprasadaka).
24.	Laksha guggulu	2-3gm divided dose	50%	Used in union of fractures (Bhagnasandhiprasadak), relieves pain (rujahar), strengthens the body.
25.	Chitrakadi guggulu	At morning meals with ghee	50%	Skin disorders (kushta), Worms (krumi), Wound (ushtavrana),Haemorroids (arsha),diseases of buccal cavity (mukharoga), Disorder of lyrynx-phyrnx (galaroga),Scitica (grudhrasi),Fractures (bhagna).
26.	Panchamrut Loha Guggulu [25]	125-250mg twice a day.	50%	Sciatica (Grudhrasi), frozen shoulder (avabahuk), lower back ache (katishoola), knee joint pain (janushoola), Headache (vataj shirahshoola), insomnia (anidra), Anemia (pandu).
27.	Trayodashanga guggulu [26]	5 gm 2-3gm in divided dose.	50%	Lower back stiffness (Katigraha),Scitica (gridhrasi), Arthritis (sandhigatavta),useful in healing of fracture.
28.	Aditya Paka guggulu [27]	5gm	50%	Vata related disorders (Vatavyadhi)- related with joints, bones.
29.	Navakarshik Guggulu [28]	3 gm	55.55%	Fistula (Bhangandar), tumour (gulma), swelling (shotha), haemorrroids (arsha).
30.	Ekvinshati guggulu [29]	3 gm	50%	Skin disorder (Kushta), Worms(krumi), wounds (vrana), grahani,arsha,mukharoga.
31.	Triphala guggulu [30]	3 gm	55.55%	Treatment of Wounds Bhagandar, gulma, shotha, arsha.
32.	Saptang guggulu [31]	3 gm	50%	Pilonidal sinus, fistula, infected wounds, painful wounds
33	Saptavinshati guggulu [32]	6 gm	66.66%	Wide range of indications including Fistula in ano, constipation, pain in chest, Haemorroids, renal calculi, burning micturition etc.
34	Rasna Guggulu	3 gm	83%	Sciatica

Table 1 Percentageof Guggulu In Various Guggulu Formulations-

Jaggery and sugar being part of diet are specifically used for palatability and vata alleviating action and soothing action in throat, making it easy for consumption. The shelf life of the vati prepared using jaggery is less thus very few formulations like ‘bahushala guda’, ‘marichadi gutika’, ‘suranavatak’ etc are prepared using jaggery and sugar. The tablets such as ‘vyoshadi vataka’ made using jaggery as a binder are hygroscopic, and they may stick to one another when packed. Hence there are challenges in large scale manufacturing of such tablets. Research and development are needed to convert these into marketable products.

In modern pharmaceutical practices chemical binding agents are used which are inert and their purposes vary, like used as binders, lubricants, disintegrants etc. On the contrary Guggulu formulations are special; as Guggulu is of medicinal value, it is good as a binding agent, and possesses various properties to eliminate diseases. Considering the Ayurvedic properties and actions of guggulu it has been primarily chosen as a gum for binding the tablets. It has a wide range of usefulness in indigenous medicine. It is astringent and antiseptic and acts as a bitter, promotor of appetite, and relieves flatulence when taken internally. It acts as a diaphoretic, expectorant, diuretic, uterine stimulant. Inhalation of the fumes from burnt guggulu is recommended as it is praised as ‘Devadhupa’. ^[33]

Speciality of Guggulu formulations 

Guggulu is the oily-gummy resinous substance extracted from the bark of Commiphora wightii.

As per the general guideline^[1] the quantity of Guggulu is 50 % and that of other ingredients is 50 %. In various guggulu kalpana like trayodashang guggulu and kanchnar guggulu the quantity of guggulu was 50 percent, however while we review the ancient literature of Ayurveda it was evident that in various other guggulu formulations [eg Gokshuradi guggulu, Vatari Guggulu] the quantity of guggulu is not 50 %. This has been reviewed and compiled in [Table 1].  The table mentions only main indications; however, the drugs are also indicated in medical conditions only after complete assessment by an Ayurvedic physician

Fresh guggulu [Nava Guggulu] is supposed to be the one collected and used within a year. Mature Guggulu [Purana guggulu] is the one used after storing for a year or more. Fresh one should be used where nourishing or anabolic and aphrodisiac function is expected and mature guggulu should be used where intense catabolic action is expected. Critical analysis of the percentage of guggulu, used in preparation of guggulu formulations is carried out here.

As per agryasangraha [best drug index] of the Ayurvedic classical text ‘Ashtangahruday’, Guggulu is the primarily most important drug for treatment of ailments involving fat tissue [Meda dhatu].

The dose adjustment of the formulation is dependent on many factors including strength of the patient, his age, his body constitution, region, season. However classical dose must be taken into consideration while treatment.

In some classical formulations, there are many indications, here not only dose but time of drug administration [aushadhi sevan kala] also matters. A drug can be effectively used for many conditions by correct choice of drug delivery time, such as – early in morning [for rejuvenation], before lunch [for vyana vayu disorders] etc.

From the above list it is clear that the quantity of guggulu in these guggulu formulations varies with respect to other ingredients, this may be due to the expected synergistic activity of the formulation and role of guggulu in it. Ayurvedic formulations are complex drugs based on the principles of synergism and antagonism in order to achieve desired effect of the formulation. To avoid the adverse drug reactions due to its extreme pitta aggravating action; processing of guggulu is carried out by dissolving it in liquid media like decoction of Adhatoda vasica, decoction of triphala [Terminalia chebula, Terminalia belerica. Emblica officinalis], or cow milk, followed by straining and condensation which is known as purification.^[34]

When the quantity of guggulu is 50% or more, it is used for its own therapeutic effects predominantly synergistically with other drugs whereas when this percentage is lesser [eg – 12.5% guggulu in Gokshuradi Guggulu], it may have been added for its yogavahi action [carrier/ supporting accompanying medicament]. The mechanism of action of the guggulu formulation is influenced by the other drugs present in it, this process in modern medicines/pharmaceutics is called synergistic action. Considering this process, the selection of guggulu i.e., fresh and mature should be done according to the effects expected such as anabolism or catabolism respectively. Following are some examples of most commonly used formulations of guggulu and the critical analysis of their composition and action with few examples below.

Significance of percentage of guggulu in its formulations in view of pharmaceutics -

Guggulu formulations are manufactured by following methods. 

Somapaka (preparations by intense pounding only, no heat is applied.

Agnipaka (preparations using heat.

Aditya paka (preparations using sunlight.

Compression (preparations using tablet compression machine.  

When we consider the option of compression at industry level manufacturing, the quantity of excipients would depend upon the percentage of guggulu in the formulation. Guggulu itself is a gum resin and hence additional binders may not be required. The combination of excipients is important as there is always a challenge of exceeding the normal limits of disintegration time in case of guggulu tablets. Disintegrators and lubricants need to be used in proper proportions. 

It has been reported in a study conducted for triphala guggulu vati, four types of samples were prepared by direct compression, somapaka (pounding), agnipaka (by heat) and aditya paka (by sunlight). This formulation contains guggulu in 55.55% hence no additional binder was required. The powder of triphala guggulu was directly compressed to get good quality tablets. Excipients like binder, glidant, lubricant, and anti-adherent were not used. ^[35]

A General note on excipients

Excipients are the additives used to convert pharmacologically active compounds into pharmaceutical tablets suitable for administration to patients.

International pharmaceutical excipients council (IPEC) defined excipients as the other substances in pharmaceutical formulation other than the active pharmaceutical ingredients which have been appropriately evaluated for the safety in order to help in processing, manufacturing, protection and give support or to enhance stability or to assist in product identification [by use of colourants] or improve any features of safety or effectiveness of drug delivery system during storage or use. ^[36]

Excipients for tableting includes following different substances.

Guggulu as a binder for allopathic drug

It’s interesting to know that gum from guggulu was extracted and used as a binder for paracetamol tablet in 4 different concentrations [2%, 4%, 6%, 8%] and gum guggulu exhibited good binding property in uncoated tablets with 90% of drug release in 70 mins of dissolution.[40] However, such use of guggulu as a binder in allopathy is rare. Considering its action against diabetes and arthritis, it may be used as an effective binder synergistically assisting the action of other drugs.

In the recent times there have been important developments in the field of pharmaceutics regarding different dosage forms for the ones existing as well as new designed drugs, synthetic, semi synthetic and natural excipients need to be used for different purposes. Synthetic excipients might cause harm to the body and that’s the reason researchers are interested and looking for excipients from natural resources. Excipients from natural resources possess own properties which can enhance the efficacy of the drug. The natural excipients have an edge over synthetic excipients for, the natural excipients are biodegradable, non-toxic, low cost, environment friendly, having abundant availability, acceptance-palatability.

For guggulu formulations these excipients can be used as follows- Traditionally the guggulu formulations are made by rolling the pills by hands or by pill making machine. It would be appropriate to add some modern disintegrants while formulating guggulu formulations by compression method so that we can reduce the disintegration time; which is reported to be above 1 hour for traditionally made guggulu pills. ^[35]. As a lubricant the Ayurvedic physicians use ghee to prevent adhesion to hands. ^[36] The challenges in traditionally prepared guggulu pills are related to its quality control. More research is needed in this area.

Conclusion

Guggulu formulations of Ayurveda are unique, as Guggulu is a natural binder as well as an excellent medicine itself. There are many challenges in manufacturing high quality Guggulu formulations. Hence the formulations were reviewed for their constitutions so that addition of proper disintegrants, and skipping additional binders can be employed while small- and large-scale production of Guggulu formulations. The percentage of this gum resin has been reviewed for assisting the drug research in this field.

Acknowledgements

The authors are sincerely grateful to the Bharati Vidyapeeth (Deemed to be University).

Conflicts of Interest

All contributing authors declare no conflicts of interest.

Source of Funding

None.