|Year : 2023 | Volume
| Issue : 3 | Page : 223-229
Pharmaceutical development of Lekhaniya Mahakashaya into dispersible tablet–A polyherbal formulation
Sakshi1, Rajendraswami S Hiremath1, Vinod Shrishaila Mannur2
1 Department of Rasashastra and Bhaishajya Kalpana, KAHER’s Shri BMK Ayurveda Mahavidyalaya, Belagavi, Karnataka, India
2 Department of Quality Assurance, KAHER’s College of Pharmacy, Belagavi, Karnataka, India
|Date of Submission||14-May-2022|
|Date of Acceptance||15-Feb-2023|
|Date of Web Publication||16-Aug-2023|
Dr. Rajendraswami S Hiremath
Department of Rasashastra and Bhaishajya Kalpana, KAHER’s Shri B.M.K. Ayurveda Mahavidyalaya, Shahapur, Belagavi, Karnataka 590003
Source of Support: None, Conflict of Interest: None
BACKGROUND: Lekhaniya Mahakashaya (LM) is indicated in Ayurveda for obesity. Its classical dosage form is Kashaya (decoction), which involves time-consuming preparation and has a low shelf-life. The aim of the study was, therefore, to modify the dosage form of LM into a dispersible tablet (DT), a unit solid dosage form close to decoction, due to its conversion into aqueous solution during administration. METHODS: Raw materials were authenticated as per API standards. To develop and optimize the DT, totally six trials for each of the 30 tablets were carried out by direct compression method using two super disintegrants, viz., Sodium Starch Glycolate (SSG) and Croscarmellose Sodium, with the effervescent agents, tartaric acid, and sodium bicarbohydrate. The developed formulation was analyzed for its pre- and post-compression parameters besides Fourier transform infrared (FTIR). RESULTS: The formulation made using Anhydrous Lactose (AL) as a binding agent and SSG as a super disintegrant passed all the quality parameters of a DT. The average weight was 500 mg. The angle of repose was 0.600, Carr’s index was 19.40, and Hausner’s ratio was 1.24. Disintegration time was 2.5 min, friability was less than 1%, hardness was 2.5, and weight variation was less than 5%. FTIR revealed the presence of functional groups such as phenolics, alcohol, alkene, and nitride. CONCLUSION: LM can be modified into a DT using AL as a binding agent and SSG as a super disintegrant. Further studies are warranted to fix the clinical dose and assess efficacy.
Keywords: Direct compression, dispersible tablet, FTIR, Lekhaniya Mahakashaya
|How to cite this article:|
Sakshi &, Hiremath RS, Mannur VS. Pharmaceutical development of Lekhaniya Mahakashaya into dispersible tablet–A polyherbal formulation. J Drug Res Ayurvedic Sci 2023;8:223-9
|How to cite this URL:|
Sakshi &, Hiremath RS, Mannur VS. Pharmaceutical development of Lekhaniya Mahakashaya into dispersible tablet–A polyherbal formulation. J Drug Res Ayurvedic Sci [serial online] 2023 [cited 2023 Sep 23];8:223-9. Available from: http://www.jdrasccras.com/text.asp?2023/8/3/223/383701
| Introduction|| |
Ayurveda has a chest of polyherbal formulations and among the valuable gems are Mahakashayas—groups of 10 drugs that possess similar action. Among them, Lekhaniya Mahakashaya (LM) is a group of drugs mentioned in the Ayurvedic classics for the management of obesity. The classically prescribed dosage form is “Kashaya” (decoction), wherein the drugs are soaked, boiled in potable water, reduced in volume by evaporation, filtered, and administered. Over time, decoctions have exhibited unquestionable efficacy. However, decoctions have a very minimal shelf life, and it is not possible to preserve their therapeutic action for a long time in this dosage form. To render these wonder drugs in a user-friendly form without breaching the fundamental principles of Ayurveda, the aim of the present study was to modify the dosage form of LM from decoction (liquid) to dispersible tablet (DT), which despite being a unit solid dosage form can essentially be considered as a liquid because the tablet is dissolved in water prior to administration and the end product consumed is an aqueous solution.
Furthermore, solid unit dosage forms are stable, easy to administer, portable, cost-effective, and consumer-friendly. DTs dissolve quickly in water to form a homogeneous solution instantly. When administered thus, there is greater bioavailability and lesser absorption period owing to disintegration into smaller readily absorbable particles. DTs are compatible with almost everyone, right from the pediatric population to the geriatric age group.
| Materials and Methods|| |
Instruments and equipment
Raw materials and Authentication: Raw drugs that constitute LM [Table 1]Mustaka (Cyperus rotundus L.), Kushtha (Saussurea costus (Falc.) Lipsch., Haridra (Curcuma longa L.), Daruharidra (Berberis aristata DC.), Ativisha (Aconitum heterophyllum Wall. ex Royle), Katurohini (Picrorhiza kurroa Royle ex Benth.), Chitraka (Plumbago zeylanica L.), Chirbilwa (Holoptelea integrifolia Planch.), and Vacha (Acorus calamus L.) were procured from Good manufacturing practices certified KLE Ayurveda Pharmacy, Belagavi, Karnataka, India. The dried drugs were authenticated by the Drug Testing Laboratory for Ayurveda, Siddha, Unani drugs approved by AYUSH and GOI, KAHER’s Shri BMK Ayurveda Mahavidyalaya, Belagavi, Karnataka, India.
Excipients for DT preparation: Potassium bromide (KBr) was procured from M/s Hi Media Laboratories Pvt. Ltd., Mumbai, India. The excipients, viz., sodium starch glycolate (SSG) and croscarmellose sodium (CCS), were procured from M/s Ozone International Mumbai, India. Anhydrous lactose (AL), tartaric acid, talc, sodium bicarbonate and magnesium stearate were procured from M/s Hi Media Laboratories Pvt. Ltd. M/s RIMEK Mini press, India single rotary machine was used for tablet punching.
Instruments for analysis: Standard instruments were used for all the analyses. Shimadzu Infrared (IR) for Affinity-1 DRS system was used for Fourier transform infrared (FTIR) analysis and IR solution application was used to navigate and analyze the sample. Kubelka-Munk function was used for the reflectance and finally, peak picking in the fingerprint region and functional group region was done.
Lekhaniya Mahakashaya preparation
In an open stainless-steel vessel, coarse powder of the raw drugs of LM was initially soaked with 16 times potable water and allowed to rest overnight. The next day, the mixture was boiled till the water level was reduced to 1/8th. This resultant decoction [Figure 1] was then filtered using a clean cloth and stored for analysis and further processing in Ghana.
Lekhaniya Mahakashaya Ghana preparation
The filtered decoction was taken in a stainless-steel vessel and subjected to heat. When the consistency started to thicken, the contents were transferred to another vessel to avoid burning of the contents, and this vessel was placed over boiling water, and indirect heat was, thus, provided till a semisolid consistency was obtained. The temperature was maintained at 60°C–70°C. Upon attainment of semisolid consistency, the contents were kept aside to cool. When the mass became lukewarm, it was transferred into a plate on which butter paper was spread. It was then placed under sunlight for drying. This semisolid content was labeled as LM Ghana (LMG). Dried LMG was pounded to remove the adhesions and lumps formed. The resultant powder was labeled as LMG powder [Figure 2] and stored in an airtight container for further processing. A part of LMG was taken for analytical evaluation.
During the preparation of LMG, precautions were taken to check the consistency through its adhesion to the ladle and formation of 1–2 thread consistency. Throughout the duration of heating, the contents were continuously stirred to avoid charring and to prevent the contents from sticking to the base of the vessel.
Development of Lekhaniya Mahakashaya dispersible tablet
The general method for the formulation of DT was adopted and is as follows:
Step 1: Milling and sieving—All ingredients should be powdered with no lumps and sieved.
Step 2: Mixing—The powders should be homogenously blended and the lubricants (talc, magnesium stearate) should then be added.
Step 3: Sieving the powder blend—The above blend is to be again sieved by Mesh number 80.
Step 4: Tablet compression: The sieved blend is compressed through the direct compression method into the desired size and shape.
Using the above method, a total of six trials were performed—three using each of SSG and three using CCS along with effervescent agents. For each trial, LMG powder was passed through sieve number 80 superimposed on 100. The excipients [Table 2] were sieved and weighed separately in the required quantities. Tartaric acid and sodium bicarbonate were made into a fine powder and mixed, followed by the addition of SSG, and finally, the extract already mixed with AL was added and mixed homogeneously, followed by the addition of permissible quantities of talc and magnesium stearate before compression. The blend was then subjected to direct compression in the tablet compression machine (M/s RIMEK Mini press single rotary), and the LM dispersible tablet (LMDT) with an average weight of 500 mg was punched (shown in [Figure 3]).
FTIR analysis of LMG and LMDT
Fourier Transform Infrared Spectroscopy of polyherbal aqueous extracts is usually performed to identify the functional groups present in the LMG and LMDT. It is a quality parameter to detect the active components in the developed formulation.
KBr was placed in a hot air oven for 3 h at 75°C prior to use. One part of LMG powder was triturated with 99 parts of KBr and subjected to analysis. The sample for LMDT was prepared in the same way.
Shimadzu IR for Affinity-1 DRS system was used, and IR solution application was used to navigate and analyze the sample. The Kubelka-Munk function was used for the reflectance of both samples, and finally, peak picking in the fingerprint region (400–1,450 cm−1) and functional group region (1,450–4,000 cm−1) was done.
| Results|| |
Preparation of Lekhaniya Mahakashaya Ghana
LMG was prepared at a room temperature of 26°C. The weight of Ghana obtained was 6.17% in comparison with the decoction used.
Lekhaniya Mahakashaya dispersible tablet
The pH for 10% solution of LMDT in distilled was found to be 4.63.
| Discussion|| |
Raw drugs were as per the standard limits. The classics of Ayurveda have stated that the Mahakashayas are groups of drugs that exhibit similar therapeutic action and can be selected in combinations for formulation of polyherbal compounds. In other words, one may choose any combination of drugs among the 10 drugs of a Mahakashaya, or all the 10 may also be taken together. With this concept, nine drugs have been selected, excluding Haimavati (Iris versicolor L.) whose botanical name was ambiguous. As Chakrapani has stated Haimavati is Shwetavacha, its absence was compensated by taking Vacha in double the prescribed quantity.
To develop DT from LMG, totally six trials were carried out based on quality parameters applied for DTs as per standards. The prescribed limit for disintegration time for DTs is 3 min. Among the trials performed, F1, F2, F4, F5, and F6 did not meet this requirement. F3 passed this parameter with a disintegration time of 150.9 ± 1.0 s. On this basis, all trials other than F3 were rejected. The prepared blend of LM was subjected to precompression analysis. Results showed that the angle of repose was the lowest in F3 (i.e., 30.96°), from which it may be inferred that the flow property of F3 is greater than the rest. When analyzed as a ratio, bulk density and tapped density give the value of Hausner’s ratio and Carr’s index, both of which are indicative of the quality of flow character. Hausner’s ratio was found to be the lowest in F3, being 1.24 ± 0.005, and Carr’s index in F3 was 19.40 ± 0.005, indicating the fair flow character of F3. All the precompression parameters supported that F3 was better in terms of flow property, which aids the compression of LMDT better than the other formulations. By these inferences, it was concluded that F3 could be taken up further for punching.
After punching, the tablets were subjected to postcompression analysis [Table 4]. The hardness value for F3 was 2.5, which is neither too hard for disintegration nor too soft to be broken easily while processing. The permissible friability for any tablet is less than 1%, and these criteria were fulfilled by trials F1 and F2. In thickness and diameter, the difference was minimal. Disintegration time was minimum in F3 (2 min, 30 s, or 150.9 s), which could have been due to the synergistic effect of super-disintegrant SSG and effervescent agent tartaric acid and sodium bicarbonate. Overall, F3 passed all the parameters required for a DT and, hence, was finalized as the ideal formulation based on all the precompression and postcompression parameters discussed above. In the organoleptic study, the color of F3 was light brown, odor was characteristic, and taste was bitter and astringent.
|Table 4: Postcompression evaluation parameters for Lekhaniya Mahakashaya dispersible tablet|
Click here to view
The precompression parameters of LMDT blend in [Table 3]. LMDT was punched using a Mini press Single Rotary Tablet Compression Machine such that each tablet weighed 500 mg, and care was taken to avoid any defects during the manufacturing processes such as lamination, chipping, and capping.
FTIR analysis of polyherbal aqueous extracts is usually performed to identify the functional groups. The analysis revealed the presence of functional groups such as phenols, alkenes, alcohols, carbonyl group, aromatic rings, and nitrile group in both samples [Figure 4] and [Figure 5]. Cyprene I and Cyprene II are the alkenes present in Musta. Essential oils present aromatic rings in Kushtha. Beta-sitosterol is present in almost all the drugs of this group, having O-H group, which is responsible for mimicking cholesterol and lowering the absorption of cholesterol into blood and excreting it into feces. LMG and LMDT showed similar peaks of the major active ingredients in FTIR indicative of the preservation of the active botanicals of the formulation [Table 5].
LM has drugs that are already proven for their antihyperlipidemic action. Preliminary phytochemical analysis of LM showed the presence of flavonoids and tannins, which are showing hypolipidemic actions. Flavonoids act on body lipid constituents that influence lipid metabolism and, thereby, reduce cholesterol levels in the body. Tannins prevent obesity by virtue of their lipase-inhibiting properties, thus preventing the digestion and absorption of oils and fat.
The pH of 10% solution of LM was 4.42 and that of LMDT was 4.63, respectively. This is indicative of the moderately acidic nature of both LM and LMDT. Not much change was found in the pH of LM and LMDT, suggesting no interaction between the Active pharmaceutical ingredient and the excipients.
| Conclusion|| |
In the study, LMDT weighing 500 mg was successfully formulated by the direct compression method. Therefore, it can be concluded that DTs that have properties standing within the evaluation limits can be developed out of LM by direct compression method using AL as a binding agent and SSG as a super disintegrant. Further studies may be carried out using additives and excipients other than the ones used in the present study. Further, in vitro and in vivo comparative studies may be taken up with respect to LMG Vati (tablet punched directly with LMG) and LMDT. Safety and efficacy studies may be carried out on a clinical level in order to determine the appropriate dose and to evaluate the therapeutical action of LMDT.
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Conflicts of interest
There are no conflicts of interest.
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[Figure 1], [Figure 2], [Figure 3], [Figure 4], [Figure 5]
[Table 1], [Table 2], [Table 3], [Table 4], [Table 5]