NZ613666A - Process for preparation of a herbal extract - Google Patents

Abstract

613666 Disclosed is a process for preparing an extract of Momordica charantia comprising the following steps: a) preparing crude juice from crushed and chopped unripe Momordica charantia fresh fruit to which water is added intermittently; b) filtering the crude juice to obtain filtered juice; c) modifying the pH of the juice between 2.5 to 4 pH by adding an organic acid; d) allowing the pH modified juice to stabilise by allowing the pH added filtered juice to stand for 5 to 25-minutes; e) neutralising the stabilised juice with the help of alkali; f) allowing the neutralised juice to stand for a period of 20 to 30 minutes; g) rechecking the pH level of the juice for neutralisation; and h) drying the neutralised juice to obtain dried extract of Momordica charantia. c) modifying the pH of the juice between 2.5 to 4 pH by adding an organic acid; d) allowing the pH modified juice to stabilise by allowing the pH added filtered juice to stand for 5 to 25-minutes; e) neutralising the stabilised juice with the help of alkali; f) allowing the neutralised juice to stand for a period of 20 to 30 minutes; g) rechecking the pH level of the juice for neutralisation; and h) drying the neutralised juice to obtain dried extract of Momordica charantia.

Description

PROCESS FOR PREPARATION OF A HERBAL EXTRACT FIELD The present disclosure relates to a process for preparation of a herbal extract powder.

More particularly, the present disclosure s to a process for preparation of a herbal extract powder from Momordz'ca charantia.

BACKGROUND MomordicaecharantiariS'alsO’ca'l'ledrbitter‘m'el'on’or‘b‘itte’r—go—urdflt is a tro—pifil" and subtropical vine of the family Cucurbitaceae, widely grown in Asia, Africa and the ean for its edible fruit, which is among the most bitter of all fruits.

There are many ies that differ substantially in the shape and bitterness of the fruit.

Processes for extraction of the active constituents from s parts Momordica charantia and the formulations these constituents have been disclosed in Indian Patent 81887, GB1435664, IN156263, USSO98710, JP3112999, CN1180545, US6852695, US6831162 IN191582, CN1253734 CN1303698, IN188858, IN826/DEL/2000, IN768/MUM/2001, CN1418890, IP2005126370,CN1562340, CN1858223, IP2006314273, CN1709900, 134, 120701, TW200927139, CN101366806, CN101461514, CN101485429, CN101597389 and CN101637491.

The hitherto reported processes for extraction of the active constituents from various parts Momordl'ca tz'a suffer from several limitations which include : use of organic solvents for extraction, use of heat during processing, use of enzymes during the tion process, use of sophisticated equipments for the extraction s.

Also, the formulations comprising the Momordica constituents suffer from numerous short-comings which include lower shelf life, reduction in the potency and high cost on account of high processing.

There is therefore felt a need for a process for extraction of the active constituents from Momordica charantia which is simple, cost effective, which does not employ any harmful c solvents and which enhances the potency of the constituents.

A need is also felt for a formulation.comprisingacti-veconst-ituentsof-Momordica’ charantia which is simple, effective and potent as compared to the existing product.

OBJECT Some of the objects of the present sure are as follows: It is an object of the present disclosure to provide a process for preparation of an extract of Momordica charantz'a which has a longer shelf life.

It is another object of the present disclosure to provide a process for preparation of an extract of ica tia which does not employ any enzymes.

It is still another object of the present disclosure to provide a process for preparation of an t of Momordz'ca charantia which does not employ organic solvents.

It is yet another object of the present sure to provide a process for preparation of an extract of Momordica charantia which increases the potency of the extract.

It is yet another 'of the present disclosure to provide a process for ation of an extract of ’z'ca charantia wherein the end product is non- hygroscopic.

SUMMARY In accordance with the present disclosure there is provided a process for preparing an extract of Momordica charantz'a comprising_the_followingisteps:7 a) preparing crude juice from crushed and chopped unripe Momordica charantz'a fresh fruit to which water is added intermittently; b) filtering the crude juice to obtain filtered juice; c) modifying the pH of the juice between 2.5 to 4 pH by adding an organic acid; (1) allowing the pH modified juice to ize by allowing the pH added filtered juice to stand for 5 to 25 minutes; e) lizing the stabilized juice with the help of alkali; 0 allowing the neutralized juice to stand for a period of 20 to 30 minutes; g) rechecking the pH level of the juice for lization; and h) drying the neutralized juice to obtain dried extract of Momordica charantia.

Typically, the organic acid is at least one selected from the group consisting of citric acid, acetic acid, lactic acid, tartaric acid and oxalic acid.

Typically, the organic acid is citric acid.

Typically, the organic acid is lemon juice.

Typically, the acidic pH is adjusted to a value of 3.8.

Typically, the alkali used for neutralization is at least one alkali selected from the group consisting of sodium hydroxide, ium hydroxide, calcium ide and sodium onate.

Typically, the normality of the alkali used for neutralization is in the range of 0.1 Nto4N.

In accordance with the present'disclosure, during the step of neutralization the alkali is added dropwise in the stabilized acidic juice.

In ance with the present disclosure, the dried extract is obtained by treating the neutralized juice in at least one manner selected from the group consisting of spray , vacuum drying and freeze drying to obtain a dried extract of Momordz'ca chararztia.

There is also provided a ation containing the dried extract of Momordica charantia prepared in accordance with the present disclosure in a dosage form selected from the group consisting of powder, granule, capsule, tablet, sachet, suspension, , pastille, chewing gum, lozenges and pill.

DETAILED DESCRIPTION In one aspect, the present disclosure provides a process for preparation of a herbal extract powder from Momordz'ca charantz'a. The first and foremost consideration beforethe commencement of any herbal extraction process is the selection of the particular plant part for the purposes of extraction. Accordingly, the first step in ance of the process with the present disclosure is selection of the raw material.

In accordance with the process of the t disclosure, fruits are used as the raw material for the tion process. lly, green colored unripe fruits are used as the raw material.

Typically, the fruits that are used as the raw material are fresh.

A crude juice is prepared by crushing and ng the fruits with intermittent addition of water. The crude juice is then subjected to filtration to obtain a green coloured juice.

A pH modifying agent is added to render the green coloured juice acidic by adjusting the pH to a predetermined value.

Typically, a mild organic acid is used as the pH modifying agent.

Typically, the organic acid is at least one selected from the group consisting of citric acid, acetic acid, lactic acid, tartaric acid, oxalic acid and or the like, or the ations thereof.

In accordance with one embodiment, citric acid is used as the pH modifying agent.

The organic acid used as a pH modifying agent may be obtained from a natural source. Alternatively, the organic acid may be purely synthetic. In one embodiment, lemon juice is used as the pH modifying agent. In another embodiment, citric acid is used as the pH modifying agent.

Typically, the pre-determined pH value is selected from the values selected from the group consisting of 2.5, 3, 3.5 and 4.

In accordance with one embodiment of the disclosure, the predetermined value of pH is in the range of about 3.5 to about 4.0.

In accordance with still another embodiment of the present disclosure, the predetermined value of pH is 3.8.

It is believed that the addition of the organic acids in the clear juice converts the larger./zc.omplex_pr.oteinsgofifreshgfruits-of—Momordicaecharantiaato-sm'a'll—pepti'de' fractions, which help in reduction of blood glucose levels in ts.

The acidic juice extract with a predetermined pH is allowed to stabilize for a period in the range of about 5 min to 25 min, preferably, in the range of about 15 . to 20 minutes.

The stabilized acidic juice is lized by on of an alkali to obtain a neutralized juice extract with a pH in the range of about 6.5 to 7.

In accordance with a preferred embodiment of the present disclosure, the pH of the neutralized juice is about 7.

Typically, in the method step of neutralization of the acidic juice using an alkali, after the addition of the alkali to the acidic juice, the neutralized juice is kept aside for a period of about 20 to 30 minutes and the pH is cked. If necessary, additional alkali is added to ust the pH in a range of about 6.5 to about 7, preferably about 7.

Typically, the alkali used for the neutralization of the acid juice include but are not limited to sodium hydroxide, potassium hydroxide, calcium hydroxide, sodium bicarbonate or the like, or the ations thereof. lly, the normality of the alkali used for neutralization of the acid juice is in the range of 0.1N to about 4N.

Typically, the alkali is added in a drop~wise manner in the stabilized acidic juice for a time period ranging between 5 to 10 minutes.

Neutralizationiofiacidic—juicaensuresethe—prevention-of'furth'er-de‘gradatio’an* peptides in amino acids. Therefore, the fraction prepared from fresh green unripe fruits of Momordz‘ca charantia (bitter gourd) in accordance with the process of the present disclosure is found to be more potent as compared to the juice obtained from the whole fruit.

Theneutralizedjuiceext-ract thus~obtained—iSedried*by‘atrleastone manner‘selec't’ed from the group consisting of spray drying, vacuum drying and freeze drying to obtain a dried extract of Momordica charantia.

The Polypeptide—p, charantin and bitter constituents of Momordica charantia fruits show anti-diabetic activity.

In accordance with another aspect of the present disclosure, there is provided a herbal ition that comprises the dried t of Momordz’ca charantia prepared by the process in accordance with the present disclosure.

Typically, the herbal composition is formulated in a dosage form selected from the group consisting of powder, granule, capsule, tablet, sachet, suspension, liquid, pastille, chewing gum, lozenges and pill.

The present disclosure will now be described with the help of ing non- limiting examples.

Examples Preparation of Momordica charantia powder Example 1 — 5 Kg of fresh unripe green fruits along with seeds of Momordica tia Linn were subjected to, cleaning to remove the dust and other superfluous particles from the fruits. The cleaned fruits were chopped and grinded to obtain homologous slurry with the addition of approximately 500 ml of water.

The slurry was then filtered to separate the juice by using the nutch filter. The juice was then ed with 15% of citric acid under continuous stirring to adjust therpH to 4.0. Theistirringeofjuiceewascontinuedrfor-30 minutes an'd’a‘gain‘p'H wasi ‘ noted. After stabilization of pH, the pH of acidified juice was then neutralized with help of 15% sodium hydroxide solution to obtain pH to 7.0. The neutralized juice was then subjected to continuous stirring for 30 minutes and pH was once again noted to confirm the pH — 7.0. The juice with neutral pH was then concentrated under nt vacuum at 700 mm of Hg at temperature 55°C to ed juice with 18 brix (total solid content). The concentrated juice was dried using vacuum dryer adjusted at 60°C and reduced re, which gave 176 gm of the greenish brown coloured free flowing juice powder with characteristic taste and odour.

Analysis of the juice powder showed following constituents in Table 1.

Table 1.

Constituents .......... % by weight Proteins .......... 22.85 Bitters .......... 3.32 e 2 - 5 Kg of fresh unripe green fruits along with seeds of Momordica charantia Linn were subjected to cleaning to remove the dust and other superfluous particles from the fruits. The cleaned fruits were chopped and grinded to obtain homologous slurry with the addition of approximately 500 ml of water.

The slurry was then filtered to te the juice by using the high speed centrifiig‘e. The juice was then acidified with 15% of citric acid under continuous stirring to adjust the pH to 4.0. The stirring e was continued for 30 minutes and again pH was noted. After ization of pH, the pH of acidified juice was then neutralized with help of 15% sodium hydroxide solution to obtain pH to 7.0.

The neutralized juice was then subjected to continuous stirring for 30 minutes and pH was once again noted to confirm the pH — 7.0. The juice with neutral pH was then concentrated under constant vacuum at 700 mm of Hg at temperature 55°C to obtained juice with 16 brix (total solid content). The concentrated juice was dried using spray dryer at 155°C inlet temperature, 70°C to 80°C outlet temperature, which gave 159 gm of greenish brown ed free flowing juice powder with characteristic taste and odour. Analysis of the juice powder showed following constituents in Table 2.

Table 2. tuents .......... % by weight Proteins .......... 22 15 Bitters .... 2 76 e 3 - 5 Kg of fresh unripe green fruits along with seeds of Momordz’ca charantia Linn were subjected to cleaning to remove the dust and other superfluous particles from the . The cleaned fruits were chopped andzgrinded. to obtain homologous slurry with the addition of approximately 500 ml of water.

The slurry was then filtered to separate the juice by using the high speed centrifuge. The juice was then acidified with 15% of oxalic acid under continuous stirring to adjust the pH to 4.0. The stirring ofjuice was continued for 30 minutes and again pH was noted. After stabilization of pH, the pH of acidified juice Was then neutralized with help of 15% Calcium hydroxide solution to obtain pH to 7.0.

The neutralized juice was then subjected to continuous stirring for 30 minutes and pH was once again noted to confirm the pH — 7.0. The juice with neutral pH was then concentrated under constant vacuum at 700 mm of Hg at temperature 55°C to obtained juice with 18 brix (total solid content). The concentrated juice was dried using freeze dryer adjusted at -46°C and reduced pressure, which gave 165 gm of green coloured free flowing juice powder with characteristic taste and odour.

Analysis of the juice powder showed following constituents in Table 3.

Table 3.

Constituents .......... % by weight Proteins .......... 21.3 3 Bitters .......... 2. 85 Preparation of capsules of Momordica ‘z'a 400 mg.

Example 4 - The juice powder of Momordz'ca charantz'a, microcrystalline cellulose, aerosi_l,digflcjumphosphateaweresiftedthroughi40—U-Semesh*screen:bl'en'ded‘a’nd’ granulated using an aqueous on of Povidone (PVPK-30). The granules were then dried at temperature of 60 j: 5° C, sifted through 30 US mesh screen, lubricated and filled into hard gelatin capsule shells of suitable size.

The capsules had composition as given below in Table 4.

Table 4.

Ingredients .......... Quantity per mg in capsule Microcrystalline ose ........... 100 Aerosil ........... 3 Dicalcium phosphate ........... 40 Povidone (PVPK-30) ........... 5.5 ium stearate ..... 3 Talc ............ 3 Sodium starch glycolate ............ 15 Example 5 - The juice powder of Momordz'ca charantia, sodium carboxymethyl cellulose, sodium saccharin, citric acid and sodium glycyrrhizinate were sifted through 40 US mesh screen, d and granulated. The granules were then dried at temperature of 60 : 5° C, sifted through 30 US mesh screen filled either in bulk or in unit dose per pack.

The granules had composition as given below in Table 5.

Table 5. ients ty in mg Juice powderof Momordica charantz‘a of example 1 .......... 400 Sodium glycyrrhizinate .......... 10 Sodium citrate .......... 20 Mint flavour (0.1%) .......... 1 Sodium carboxy methyl cellulose .......... 2 Sodium saccharin .......... 1 Preparation of tablets ofMomordica charantia fraction 600 mg. e 6 - The juice powder of Momordica charantz’a of example 1, microcrystalline cellulose, aerosil, dicalcium phosphate were sifted through 40 US mesh screen, blended and granulated using an s on of Povidone (PVPK-30). The granules were then dried at temperature of 60 : 5° C, sifted through 30 US mesh screen and lubricated using talc, magnesium stearate and sodium starch glycolate. The lubricated granules were then compressed using suitable die and punches and coated.

The tablets had composition as given below in Table 6.

Table 6.

Ingredients .......... Quantity per mg in tablet Microcrystalline cellulose ........... 100 Aerosil ........... 20 Dicalcium phosphate ........... 50 Povidone (PVPK-30) ........... 10 ium stearate > ..... ...... 5 Talc ............ 5 Sodium starch glycolate ............ 25 y propyl methyl cellulose .......... 8 Titanium dioxide .......... 5 Propylene glycol .......... 3 Anecdotal studies: 1) A subject with uncontrolled type II es was administered three capsules of Momordica charantz'a ts in ance with the present disclosure per day containing 400 mg extract per capsule; as obtained from Example 4.

It was found that blood glucose level of the subject was reduced to 159 mg/dL from its base level — 249 mg/dL during one month of treatment at aidose of one capsule (400mg) administered three times a day. 2) A test was made of the hypoglycemic effect of the same juice powder of M charantz’a as employed in Example 4 upon a female patient of 56 years ‘of age and a body weight of 61 kg presenting with non n-dependent diabetes. The test subject exhibited a daily blood glucose level of 234 mg/dL, with administration of 500 mg of metformin; BID.

The subject continued stration of the same number of pills of metforrnin per day and commenced ingestion of 3 hard gelatin es containing 400 mg of Juice powder ofM charantia per capsule as obtained from example 4 for a period of 90 days. The practiced dosage regimen was 1 e before breakfast and 2 capsules before dinner.

The blood analysis of patient showed dramatic effect where the blood glucose level of the subject d to 170 mg/dL from its base level — 234 mg/dL during a three month of treatment. During the treatment, the patient was on_ _a very moderatediet and __she_ wasfiphysically,moderately active. 3) A test was made of the hypoglycemic effect of the same juice powder of M charantia as employed in Example 4 upon a non insulin-dependent uncontrolled diabetic male of 61 years of age and a body weight of 67 kg.

The t had long history of diabetes and was on oral medication from more than 5 years. The test subject exhibited a daily blood glucose level of 261 mg/dL, with administration of 500 mg of metformin; three tablets per day.

The subject continued administration of the same number of pills of metforrnin per day and commenced ingestion of 3 hard gelatin capsules containing 400 mg of Juice powder ofM charam‘ia per capsule as obtained from example 4 for a period of 90 days. The practiced dosage regimen was 1 capsule before breakfast and 2 capsules before dinner.

The blood analysis of the patient showed ic effect where the blood glucose level of the subject reduced to 159 mg/dL from its base level — 261 mg/dL during a three month of ent. 492A2malegsubject~ofi62~yearsiwithiuncontrolied-maturity'onsetrd'iabetW administered 3 capsules of commercially available ica charantia t per day containing 400 mg of commercial powder per capsule.

It was found that after a period of one month blood glucose level of the subject reduced from a base level of 249 mg/dL to 199 mg/dL consistently.

Thereafter under the same conditions, the t was administered one capsule as per example 4, three times a day. After one month treatment, the blood glucose level of the subject reduced to 159 mg/dL.

) A female subject of 70 years with uncontrolled maturity onset diabetes was administered 3 capsules of commercially available Momordica charantia extract per day containing 400 mg of commercial powder per capsule.

It was found that after a period of one month, the blood glucose level of the t reduced from a base level of 265 mg/dL to 215 mg/dL consistently.

Thereafter under the same conditions, the subject was administered one capsule as per example 4, three times a day. After one month treatment, the blood glucose level of the subject reduced to 145 mg/dL.

Safeg profile No toxic s or side effects were ascertained in the testings mentioned above.

The physical status of examined persons showed no sign of any harmful reaction to treatment. The dosage regimen as well as treatment were patient friendly and well tolerated by diabetics.

Other Benefits: Besides controlling the blood/urine sugar level the nutraceutical t(s) provide additional s in diabetes related human health problems like reduction in fatigue, weakness, drowsiness, numbing , nt urination, unusual thirst and hunger, weight loss, swellings on legs/ankles, burning sensation on feet, palms, relief in skin itching, skin dryness, black patches on skin, hypertension, increase in sleep comfort, energetic feeling, improvement in laziness, blurred vision, nt skin infections and slow g of wounds and sores.

A 20-35% reduction in blood glucose doses was also observed after 12 weeks in noninsulin-dependent diabetes mellitus (NTDDM) adult ics and can be also used as adjuvant therapy along with oral treatments.

The present disclosure thus provides the specific ition of Momordica charantz’a juice powder, the process for the preparation of juice powder and the medicinal benefits of the same.

Technical advancement: The process for preparation of Momordz'ca tia juice powder and the ation sized in accordance with the present disclosure has the following non—limited advancements: - The present disclosure provides a process for the preparation of a nutraceutical food supplement for diabetics without deteriorating the nutritional and pharmaceutical properties of the natural composition like enrichment of proteins and bitters that are responsible for hypoglycemic activity.

- The process for the preparation of Momordica charantia juice powder in -accordanc—eiw-ithithe*presentfdisclosure7iS’simple-and—cost—effectivei - The process for the preparation of Momordica charantz'a juice powder in accordance with the present disclosure is safe as it does not involve use of any harmful solvents.

- The Momordz'ca charantia juice powder ed in ance with the t disclosure is comparatively more effective against diabetes.

- The Momordica charantia juice powder prepared in accordance with the present disclosure is a natural food which is non toxic, easy to digest with optimum nutrition, health protective and promotive ties.

Throughout this specification the word ‘6comprise”, or variations such as “comprises” or “comprising”, will be understood to imply the inclusion of a stated element, integer or step, or group of elements, integers or steps, but not the exclusion of any other element, integer or step, or group of elements, integers or steps.

The use of the expression “at least” or “at least one” suggests the use of one or more elements or ingredients or quantities, as the use may be in the embodiment of the ion to achieve one or more of the desired objects or results.

Any discussion of documents, acts, materials, devices, articles or the like that has been included in this specification is solely for the purpose of providing a context for the ion. It is not to be taken as an admission that any or all of these matters form part of the prior art base or were common general knowledge in the field relevant to the invention as it existed anywhere before the priority date of this application.

The numerical values given for various physical parameters, dimensions and quantities are only approximate values and it is envisaged that the values higher than the cal value assigned to the physical parameters, dimensions and ties fall within the scope of the invention andthe claims unless there is a statement in the specification to the contrary.

The foregoing description of the specific ments will so fully reveal the general nature of the embodiments herein that others can, by applying current knowledge, readily modify and/or adapt for various applications such specific embodiments without departing from the generic concept, and, ore, such adaptations and modifications should and are ed to be comprehended within the meaning and range of equivalents of the disclosed ments. It is to be understood that the phraseology or terminology employed herein is for the purpose of description and not of limitation. Therefore, while the embodiments herein have been described in terms of red embodiments, those skilled in the art will recognize that the embodiments herein can be practiced with modification within the spirit and scope of the embodiments as described herein.

Claims (1)

1. Claims: 1. A process for ing an extract of Momora’ica tia comprising the following steps: a) preparing crude juice from crushed and chopped unripe Momordz'ca tia fresh fruit to which water is added intermittently; b) filtering the crude juice to obtain filtered juice; 0) modifying the pH of the juice between 2.5 to 4 pH by adding an organic acid; d) allowing the pH modified juice to stabilize by allowing the pH added firltered~juice—toestandefor—S-toa-S-minut-es;* e) neutralizing the stabilized juice with the help of alkali; t) allowing the neutralized juice to stand for a period of 20 to 30 minutes; g) rechecking the pH level of the juice for neutralization; and h) drying the neutralized juice to obtain dried t of Momora’ica charantz'a. !Q A process as claimed in claim 1, wherein the organic acid is at least one ed from the group consisting of citric acid, acetic acid, lactic acid, tartaric acid and oxalic acid. A process as claimed in claim 1, wherein the organic acid is citric acid. A process claimed in claim 1, wherein the organic acid is lemon juice. The process as claimed in any one of the preceding claims in which the acidic pH is adjusted to a value of 3.8. 6. The process as. claimed in any one of the preceding claims in which the alkali used for neutralization is at least one alkali selected from the group consisting of sodium hydroxide, potassium ide, m hydroxide and sodium bicarbonate. 7. The process as claimed in any one of the ing claims, wherein the normality of the alkali used for neutralization is in the range of 0.1 Nto4N. 8. The process as claimed in any one of the preceding claims, wherein during the step of neutralization the alkali is added dropwise in the stabilized acidic juice. 9. The process as claimed in any one of the preceding claims, wherein the dried extract is obtained by treating the neutralized juice in at least one manner selected from the group consisting of spray drying, vacuum drying and freeze drying to obtain a dried extract of Momordica tia. 10. A formulation ning the dried extract of Momordica charantia prepared in accordance with any one of the claims in a dosage form selected from the group consisting of powder, granule, capsule, tablet, sachet, suspension, liquid, pastille, g gum, lozenges and pill.