DESC:FIELD OF THE INVENTION
The present invention relates to method development to improve precompression parameter of phytoconstituents and process for preparation thereof. The present disclosure comprises processes to improvement in precompression parameters without using additives/ excipients/ chemicals. This invention further improves the therapeutical effect of dosage form by incorporating active ingredients instead of additives replaced by this process.

BACKGROUND OF THE INVENTION
In Herbal, Botanical & Phytopharmaceutical industry, micromeritics properties include precompression parameters of standard raw material/ extract are not suitable for direct compression due to their high hygroscopic and amorphous nature. Gelatine capsule is not safe for long-term, and another drawback is dose dumping. Compressing a precise quantity of powder or granules to shape a uniform tablet has a challenge in pharmaceutical companies. Technical innovation in dosage modifying, target delivery and fast disintegration to 24 hours of release time able to set with or without additives by unique technology. For precise dose and to avoid weight variation, precompression parameter should be good and flowable as per pharmacopeial limits. Here with we develop a process to improve overall flow property parameters without adding excipients/ additives/chemicals/polymers. It’s a totally unique OEM process, economic, highest yield process. By these techniques almost 50% improvement is found in micromeritics, flow property, and precompression parameters. Standard phytochemical and modifying phytochemical studies for physical evaluation, characterization, and organoleptic evaluation, conclude that without interaction, tremendous improvement is found in all parameters listed in detail study.
The proposed process begins with the selection of appropriate raw materials, followed by rigorous characterization to assess their physical and chemical properties. Subsequently, optimization studies are conducted to identify the most suitable processing techniques and formulation strategies for improving precompression parameters. This may involve the use of advanced analytical tools such as particle size analyzers, powder rheometers, and moisture sorption analyzers to evaluate the impact of process variables on the properties of phytoconstituent powders. Finally, the optimized formulation and process parameters are validated through comprehensive studies including in vitro dissolution testing, stability testing, and pharmacokinetic evaluation to ensure the desired performance and quality of the final dosage forms.
The method development process involves a systematic investigation of various factors influencing precompression parameters of phytoconstituents. This includes optimization of particle size distribution through milling or micronization techniques, enhancement of flow properties using granulation or coating methods, and control of moisture content through drying or moisture equilibration processes. Furthermore, the development of novel excipients or formulation additives can aid in improving compressibility and lubrication properties, thus facilitating better tablet formation during compression.
US10674154B2, Apparatus and methods for recompression of digital images discloses system and method for generating a second reduced size digital image from a first digital image, the method including iteratively compressing the first digital image to an extent determined by a quality measure comprising at least a blockiness measure quantifying added artifactual edges along coding block bom1daries of the second image and/or use of a quantization matrix generated by computing a weighted average of the quantization matrix of the first digital image and a scaled second quantization matrix.
US20210275458A1, Tablet formulation comprising a glp-1 peptide and a delivery agent discloses the present invention relates to solid compositions comprising a GLP-1 peptide and a delivery agent, such as SNAC, as well as uses thereof.
Case Studies in Construction Materials (Volume 15, December 2021, e00575) Pre-compression and capillarity effect of treated expansive subgrade subjected to compressive and tensile loadings (Aneke, Frank Ikechukwu et al.) Pavement structures often are under tension and compression mobilised by the coupled effects of traffic loads and swelling stress. Seasonal moisture variations cause capillarity rise and volumetric movement within the subgrade. The objective of this investigation is to evaluate the pre-compression and capillarity effect of expansive subgrades stabilised with activated fly ash (a-FA), and sisal fibre, analysed for tensile and compressive strengths.
International Journal of Current Pharmaceutical Research (Vol 14, Issue 3, 2022) phytochemical profile, fabrication, and evaluation of herbal tablets (deka, s., prasad, s. et. al) The present study investigates the qualitative and quantitative phytoconstituents and to develop and optimize herbal tablets from the methanolic leaves extract of Xanthium indicum J. Koenig ex Roxb and their evaluation
OBJECTIVE OF INVENTION
Flow property is very important as a precompression parameters in pharmaceutical industry for manufacturing of tablet dosage form whether it is conventional or modifying. In phytopharmaceutical, Phytochemical/ Phytoconstituent are isolated/manufactured by different extraction process and then solidifying by spray drying, lyophilization, or by vacuum drying.

In drying steps, for uniform flow maltodextrin or dextrin (8-12%) should be added. Even after addition of maltodextrin as a lubricant, standard extract/ standard Phytochemical/ standard Phytoconstituent derive poor flow property. Hence difficult to incorporate in capsule and difficult to convert in tablet without an excipient or granulation process. In this invention, unique excipientless granulation with only aqueous phase developed to improve flow property (Micromeritics property) and precompression parameters. Post compression basic parameters also studied to confirm organoleptic, physical and uniformity of dosage form.

SUMMARY OF THE INVENTION
The present invention relates to method development to improve precompression parameter of phytoconstituents and process for preparation thereof. The present disclosure comprises processes to improvement in precompression parameters without using additives/ excipients/ chemicals.

This invention further improves the therapeutical effect of dosage form by incorporating active ingredients instead of additives replaced by this process.
In present investigation Standard phytochemicals are selected to check precompression parameters such as bulk density, tapped density, porosity, angle of repose, Hausner ratio, compressibility index, physical nature etc.

In particular, the present disclosure relates to the polyherbal composition comprising of Allicin, Gymnemic acid, Hydroxycitric acid, Curcumin, Ginsenosides, Chlorogenic acid, bacoside, fulvic acid, piperine, boswellic acid, withanolides, sennosides, glycyrrhizin, Guggulsterone, Andrographolides to improve precompression parameters.

Then it converted in to granules by improve precompression parameters by unique granulation. Without excipients, significant improvement found in overall precompression parameters.

DETAILED DESCRIPTION OF THE INVENTION:
Detailed Description of the Invention While this specification concludes with claims particularly pointing out and distinctly claiming that, which is regarded as the invention, it is anticipated that the invention can be more readily understood through reading the following detailed description of the invention and study of the included examples.
The following is a detailed description of embodiments of the present disclosure. The embodiments are in such detail as to clearly communicate the disclosure. However, the amount of detail offered is not intended to limit the anticipated variations of embodiments; on the contrary, the intention is to cover all modifications, equivalents, and alternatives falling within the spirit and scope of the present disclosure as defined by the appended claims.

Unless the context requires otherwise, throughout the specification which follow, the word “comprise” and variations thereof, such as, “comprises” and “comprising” are to be construed in an open, inclusive sense that is as “including, but not limited to.”

Reference throughout this specification to “one embodiment” or “an embodiment” means that a particular feature, structure or characteristic described in connection with the embodiment is included in at least one embodiment. Thus, the appearances of the phrases “in one embodiment” or “in an embodiment” in various places throughout this specification are not necessarily all referring to the same embodiment. Furthermore, the particular features, structures, or characteristics may be combined in any suitable manner in one or more embodiments.

The headings and abstract of the invention provided herein are for convenience only and do not interpret the scope or meaning of the embodiments.

Various terms are used herein. To the extent a term used in a claim is not defined below, it should be given the broadest definition persons in the pertinent art have given that term as reflected in printed publications and issued patents at the time of.
Phytochemistry is an emerging branch, globally accepted by regulatory and nowadays Natural Phytochemical, Botanical, and Herbal market size rise at top most level. In Herbal industry, the demand of extract either Phytoconstituent or Phytochemical are growing gradually. Some Pharmaceutical merge Phyto Pharma, Herbal, and Nutraceutical division in existing. A Clinical studies, Patent work and stability study also running well. For precise, effective, and stable dosage form, Tablet is mostly acceptable oral dosage form. Nowadays various leading Pharma engage with modifying tablet dosage forms with single phytochemical or with synergy form.

In this field, this process invention is most crucial before tableting to discard undesirable excipients and processing steps. This invention comprises processes to improvement in precompression parameters without using additives/ excipients/ chemicals. This invention improves the therapeutical effect of dosage form by incorporating active ingredients instead of additives replaced by this process.
Phytochemicals play a vital role as an active ingredient either alone or synergy. Standard phytochemicals are selected to check precompression parameters like bulk density, tapped density, porosity, angle of repose, Hausner ratio, compressibility index, physical nature etc. Standard phytochemicals include Allicin, Gymnemic acid, Hydroxycitric acid, Curcumin, Ginsenosides, Chlorogenic acid, bacoside, fulvic acid, piperine, boswellic acid, withanolides, sennosides, glycyrrhizin, Guggulsterone, Andrographolides studied for all precompression parameters and then it converted in to granules by improve precompression parameters by unique granulation. Without excipients, significant improvement found in overall precompression parameters. Results are shown in detail of the invention.

Precompression study
Bulk Density- It is the ratio of mass of the blend to bulk volume. It is measured by pouring powder in measuring cylinder and measuring the volume occupied by powder.
Bulk density is measured using following equation:
Bulk density = Mass/Volume
Tapped Density-Tapped density is the ratio of mass of the blend to tapped volume. It can be evaluated by mechanically tapping a measuring cylinder containing adequate gram of powder sample. After observing the initial volume, the cylinder is mechanically tapped, and volume reading can be taken after 100 tapping of powder.
Hausner’s ratio- Hausner’s ratio is measured using following equation:
Hausner’s ratio = Tapped density/ Bulk density
Carr’s Index- Carr’s Index is measured using following equation:
Carr’s Index = Tapped density – Bulk density/ Tapped density X 100

Table 1. Carr’s Index and Hausner’s ratio as an indication of powder flow
Type of flow Carr’s Index (%) Hausner’s Ratio
Excellent = 10 1.00 – 1.11
Good 11-15 1.12 – 1.18
Fair 16 – 20 1.19 – 1.25
Passible 21 – 25 1.26 – 1.34
Poor 26 – 31 1.35 – 1.45
Very Poor 32 – 37 1.46 – 1.59
Extremely Poor >38 >1.60

Angle of Repose- The pile can be carefully built up by dropping the material through a funnel till the tip of the funnel (height, 2 cm) and measured the radius of the pile. The angle of repose is calculated by inversing tangentially the ratio of height and radius of the formed pile using following equation:

Angle of repose ? = tan-1 (h/r)
Where, h = Height of pile,
r = Radius of pile
Table 2. Correlations between angle of repose & flow property
Angle of repose (?) Predicted flow property
5 – 15 Excellent
12 – 16 Good
18 – 21 Fair
23 – 28 Poor
28 – 35 Poor
35 – 38 Very poor
>40 Extremely poor

Results
Table 3. Precompression Parameter of Standard Phytochemical
Formulation Angle of repose (0) Bulk density (gm/ml) Tapped density (gm/ml) Carr's index (%) Hausner's ratio
Allicin 38.15 ± 0.81 0.331 ± 0.04 0.431 ± 0.32 24.13 ± 0.82 1.36 ± 0.02
Gymnemic acid 39.47 ± 1.13 0.407 ± 0.01 0.462 ± 0.36 25.43 ± 0.87 1.39 ± 0.02
HCA (60%) 37.29 ± 0.56 0.349 ± 0.03 0.458 ± 0.39 27.38 ± 0.90 1.31 ± 0.03
Curcumin (95%) 36.25 ± 0.22 0.378 ± 0.03 0.411 ± 0.34 24.35 ± 0.74 1.39 ± 0.04
Ginsenosides 39.23 ± 0.12 0.398 ± 0.08 0.440 ± 0.37 26.63 ± 1.41 1.32 ± 0.05
Chlorogenic acid 40.39 ± 1.41 0.359 ± 0.02 0.441 ± 0.33 27.14 ± 1.26 1.39 ± 0.04
Bacoside 37.44 ± 0.43 0.352 ± 0.03 0.462 ± 0.38 23.52 ± 1.23 1.36 ± 0.17
Fulvic acid 38.29 ± 0.75 0.338 ± 0.02 0.454 ± 0.31 24.03 ± 0.28 1.39 ± 0.06
Piperine 39.21 ± 0.23 0.484 ± 0.10 0.503 ± 0.38 23.80 ± 1.72 1.38 ± 0.12
Boswellic acid 37.81 ± 0.61 0.377 ± 0.01 0.466 ± 0.46 25.11 ± 0.61 1.38 ± 0.02
Withanolides 39.24 ± 0.65 0.394 ± 0.03 0.420 ± 0.28 24.50 ± 1.32 1.38 ± 0.19
Sennoside 37.23 ± 0.62 0.412 ± 0.08 0.451 ± 0.37 23.53 ± 1.25 1.29 ± 0.12
Glycyrrhizin 38.35 ± 0.23 0.419 ± 0.07 0.451 ± 0.29 27.74 ± 0.45 1.31 ± 0.04
Guggulsterone 37.34 ± 0.09 0.340 ± 0.07 0.449 ± 0.29 27.71 ± 0.91 1.29 ± 0.01
Andrographolides 40.27 ± 0.11 0.398 ± 0.04 0.419 ± 0.21 26.09 ± 0.63 1.29 ± 0.03

Table 4. Precompression Parameter of Modifying Phytochemical by unique granulation
Formulation Angle of repose (0) Bulk density (gm/ml) Tapped density (gm/ml) Carr's index (%) Hausner's ratio
Allicin 27.26 ± 0.62 0.513 ± 0.03 0.811 ± 0.22 14.11 ± 0.86 1.06 ± 0.02
Gymnemic acid 27.39 ± 2.23 0.512 ± 0.01 0.801 ± 0.30 15.37 ± 0.84 1.07 ± 0.02
HCA (60%) 30.19 ± 0.33 0.521 ± 0.03 0.767 ± 0.39 17.18 ± 0.90 1.10 ± 0.06
Curcumin (95%) 28.15 ± 0.39 0.524 ± 0.03 0.817 ± 0.32 14.25 ± 0.71 1.11 ± 0.07
Ginsenosides 28.26 ± 0.62 0.543 ± 0.08 0.739 ± 0.35 15.42 ± 1.46 1.09 ± 0.06
Chlorogenic acid 26.32 ± 1.33 0.523 ± 0.02 0.806 ± 0.35 16.08 ± 1.26 1.10 ± 0.03
Bacoside 27.03 ± 0.67 0.527 ± 0.08 0.820 ± 0.38 14.52 ± 1.23 1.07 ± 0.09
Fulvic acid 27.52 ± 0.79 0.528 ± 0.02 0.804 ± 0.39 14.95 ± 0.78 1.09 ± 0.10
Piperine 28.48 ± 0.56 0.529 ± 0.10 0.783 ± 0.22 12.01 ± 1.22 1.11 ± 0.11
Boswellic acid 27.59 ± 0.39 0.517 ± 0.0 l 0.776 ± 0.36 13.18 ± 0.81 1.03 ± 0.02
Withanolides 28.78 ± 0.38 0.534 ± 0.08 0.770 ± 0.58 14.56 ± 1.12 1.04 ± 0.12
Sennoside 26.30 ± 0.16 0.542 ± 0.08 0.796 ± 0.47 13.26 ± 1.2 1.05 ± 0.12
Glycyrrhizin 28.34 ± 0.18 0.541 ± 0.07 0.835 ± 0.33 15.27 ± 0.92 1.05 ± 0.02
Guggulsterone 30.54 ± 0.44 0.548 ± 0.07 0.824 ± 0.69 15.70 ± 0.92 1.06 ± 0.03
Andrographolides 28.27 ± 0.42 0.608 ± 0.08 0.829 ± 0.42 16.15 ± 0.65 1.10 ± 0.04

Precompression parameters play an important role in tablet compaction and compression. Poor characteristics in density, particle size, and porosity is a drawback of tablet compression, hence weight variation, tablet capping, fragment, harness & friability issue will create in post compression parameters, it will directly connect with disintegration, dissolution to therapeutical effect of dose. Our invention comprises a process of unique granulation with distilled water with the same phytochemical. Ex- for Allicin, Standard allicin (0.1-0.5% w/v) concentration is selected for granulation fluid in Standard Allicin. Then mix it for 30-45 min. Wet mixed granules then convert to dry granules at 50-600 C in the tray dryer by passing it on sieve no-80-100. Add 1% of Talc in dry granules and mix it for 15-20 min. These granules characterized with standard phytochemicals by XRPD, FTIR, and DSC show no interaction found. Same process is done with other phytochemicals mentioned in the table.

Table 5. Basic Post compression Parameters in Modifying Phytochemical
Phytochemical Weight Variation Hardness (Kg/cm2) % Friability Appearance Disintegration time (sec)
Allicin 500 ± 0.03 5.3 ± 0.11 0.244 Complies 210
Gymnemic acid 500 ± 0.25 5.4± 0.23 0.259 Complies 234
HCA (60%) 552 ± 0.22 5.5 ± 0.14 0.304 Complies 151
Curcumin (95%) 499 ± 0.18 5.5 ± 0.12 0.319 Complies 130
Ginsenosides 499 ± 0.26 4.8 ± 0.14 0.419 Complies 160
Chlorogenic acid 500 ± 0.32 4.7 ± 0.08 0.515 Complies 155
Bacoside 502 ± 0.26 5.2 ± 0.23 0.421 Complies 144
Fulvic acid 502 ± 0.19 5.1 ± 0.38 0.432 Complies 168
Piperine 501 ± 0.37 5.3 ± 0.14 0.394 Complies 153
Boswellic acid 499 ± 0.22 5.4 ± 0.21 0.428 Complies 150
Withanolides 500 ± 0.31 5.1 ± 0.11 0.532 Complies 320
Sennoside 502 ± 0.12 5.2 ± 0.09 0.278 Complies 140
Glycyrrhizin 504 ± 0.04 5.2 ± 0.07 0.435 Complies 165
Guggulsterone 501 ± 0.26 5.4 ± 0.12 0.432 Complies 180
Andrographolides 498 ± 0.15 5.8 ± 0.22 0.399 Complies 122
,CLAIMS:1. A polyherbal composition to improve precompression parameter of phytoconstituents and process for preparation thereof.
2. The polyherbal composition as claimed in claim 1, wherein polyherbal composition processes to improvement in precompression parameters without using additives/ excipients/ chemicals.
3. The polyherbal composition as claimed in claim 1, wherein polyherbal composition improves the therapeutical effect of dosage form by incorporating active ingredients instead of additives replaced by this process.
4. The polyherbal composition as claimed in claim 1, wherein polyherbal composition comprising of Allicin, Gymnemic acid, Hydroxycitric acid, Curcumin, Ginsenosides, Chlorogenic acid, bacoside, fulvic acid, piperine, boswellic acid, withanolides, sennosides, glycyrrhizin, Guggulsterone, Andrographolides to improve precompression parameters.
5. The polyherbal composition as claimed in claim 1, wherein standard phytochemicals are selected to check precompression parameters such as bulk density, tapped density, porosity, angle of repose, Hausner ratio, compressibility index, physical nature.
6. A method of preparation of polyherbal blend of sugar free dry syrup composition comprises of;
a. Polyherbal composition converted in to granules by improve precompression parameters by unique granulation.
b. Process of unique granulation with distilled water with the same phytochemical.
c. Then mix it for 30-45 min.
d. Wet mixed granules then convert to dry granules at 50-600 C in the tray dryer by passing it on sieve no-80-100.
e. Add 1% of Talc in dry granules and mix it for 15-20 min.
f. These granules characterized with standard phytochemicals by XRPD, FTIR, and DSC.