NZ613666B - 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 relates to a process for preparation of a herbal t powder from z'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 Caribbean for its edible fruit, which is among the most bitter of all fruits.

There are many varieties that differ substantially in the shape and ness of the fruit.

Processes for extraction of the active constituents from various parts Momordica tia and the ations 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, CN1872134, JP2008120701, TW200927139, 66806, CN101461514, CN101485429, CN101597389 and CN101637491.

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

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

There is therefore felt a need for a process for extraction of the active constituents from Momordica tia which is simple, cost effective, which does not employ any harmful Organic 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 disclosure 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 Momordica charantia which does not employ any enzymes.

It is still another object of the present disclosure to e a process for ation of an extract of Momordz'ca charantia which does not employ c solvents.

It is yet another object of the t disclosure 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 preparation of an extract of Momora’z'ca charantia wherein the end product is non- hygroscopic.

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 c acid; (1) allowing the pH modified juice to stabilize by allowing the pH added filtered juice to stand for 5 to 25 minutes; e) neutralizing the ized 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 neutralization; and h) drying the neutralized juice to obtain dried t of Momordica charantia.

Typically, the organic acid is at least one ed 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, potassium hydroxide, calcium hydroxide and sodium bicarbonate.

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

In accordance with the t'disclosure, during the step of neutralization the alkali is added dropwise in the stabilized acidic juice.

In accordance with the present sure, the dried extract is obtained by ng 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 Momordz'ca chararztia.

There is also ed a ation containing the dried extract of Momordica charantia prepared in accordance with the present disclosure in a dosage form ed from the group consisting of powder, granule, capsule, , sachet, suspension, liquid, 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 accordance of the process with the present disclosure is selection of the raw material.

In accordance with the process of the present disclosure, fruits are used as the raw material for the tion process.

Typically, green colored unripe fruits are used as the raw al.

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

A crude juice is ed by crushing and chopping the fruits with intermittent on 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 combinations thereof.

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

The organic acid used as a pH ing agent may be obtained from a natural source. atively, 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 ment 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 on 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 patients.

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 neutralized by addition of an alkali to obtain a lized juice extract with a pH in the range of about 6.5 to 7.

In ance with a preferred embodiment of the t 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 re-checked. If necessary, additional alkali is added to re-adjust 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 e but are not limited to sodium hydroxide, potassium hydroxide, calcium hydroxide, sodium bicarbonate or the like, or the combinations thereof.

Typically, 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 r gourd) in accordance with the process of the present disclosure is found to be more potent as ed 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 sure, there is provided a herbal composition that ses the dried extract of Momordz’ca charantia prepared by the process in accordance with the present disclosure.

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

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

Examples Preparation of Momordica charantia powder Example 1 — 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 separate the juice by using the nutch filter. The juice was then acidified 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 ization of pH, the pH of acidified juice was then neutralized with help of 15% sodium ide solution to obtain pH to 7.0. The neutralized juice was then subjected to continuous stirring for 30 s and pH was once again noted to confirm the pH — 7.0. The juice with neutral pH was then trated under constant vacuum at 700 mm of Hg at ature 55°C to obtained juice with 18 brix (total solid content). The concentrated juice was dried using vacuum dryer adjusted at 60°C and reduced pressure, 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 ica tia Linn were subjected to cleaning to remove the dust and other superfluous particles from the fruits. The cleaned fruits were chopped and d 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 centrifiig‘e. The juice was then acidified with 15% of citric 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 ed 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 coloured free flowing juice powder with characteristic taste and odour. Analysis of the juice powder showed following constituents in Table 2.

Table 2.

Constituents .......... % by weight Proteins .......... 22 15 Bitters .......... 2 76 Example 3 - 5 Kg of fresh unripe green fruits along with seeds of Momordz’ca charantia Linn were subjected to ng to remove the dust and other superfluous particles from the fruits. The d 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 ide solution to obtain pH to 7.0.

The neutralized juice was then subjected to continuous stirring for 30 s 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 ing constituents in Table 3.

Table 3.

Constituents .......... % by weight Proteins .......... 21.3 3 Bitters .......... 2. 85 Preparation of capsules of Momordica charam‘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 solution of Povidone (PVPK-30). The granules were then dried at ature 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 ition as given below in Table 4.

Table 4.

Ingredients .... Quantity per mg in capsule rystalline cellulose ........... 100 Aerosil ........... 3 Dicalcium phosphate ........... 40 Povidone (PVPK-30) ........... 5.5 Magnesium stearate ........... 3 Talc ............ 3 Sodium starch glycolate ............ 15 Example 5 - The juice powder of Momordz'ca charantia, sodium carboxymethyl ose, sodium saccharin, citric acid and sodium rhizinate were sifted through 40 US mesh screen, blended 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.

Ingredients Quantity 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 on 600 mg.

Example 6 - The juice powder of Momordica charantz’a of example 1, microcrystalline cellulose, aerosil, dicalcium ate were sifted through 40 US mesh screen, blended and ated using an aqueous solution 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 30) ........... 10 Magnesium stearate > ..... ...... 5 Talc ............ 5 Sodium starch glycolate ............ 25 Hydroxy propyl methyl cellulose .......... 8 Titanium e .......... 5 Propylene glycol .......... 3 Anecdotal studies: 1) A subject with uncontrolled type II diabetes was administered three capsules of Momordica charantz'a extracts in accordance 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 d to 159 mg/dL from its base level — 249 mg/dL during one month of ent 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 insulin-dependent es. The test subject exhibited a daily blood glucose level of 234 mg/dL, with administration of 500 mg of metformin; BID.

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 charantia per capsule as obtained from e 4 for a period of 90 days. The practiced dosage regimen was 1 capsule before breakfast and 2 capsules before dinner.

The blood is of patient showed dramatic effect where the blood glucose level of the subject reduced 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 subject had long y of diabetes and was on oral medication from more than 5 years. The test subject exhibited a daily blood e 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 ‘ia per capsule as obtained from e 4 for a period of 90 days. The ced dosage regimen was 1 capsule before breakfast and 2 capsules before dinner.

The blood analysis of the t showed dramatic 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 treatment. 492A2malegsubject~ofi62~yearsiwithiuncontrolied-maturity'onsetrd'iabetW 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 blood e level of the subject reduced from a base level of 249 mg/dL to 199 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 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 e.

It was found that after a period of one month, the blood glucose level of the subject 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 effects 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 ly and well tolerated by ics.

Other Benefits: Besides controlling the blood/urine sugar level the nutraceutical product(s) provide additional benefits in diabetes related human health problems like ion in fatigue, weakness, drowsiness, numbing effect, frequent urination, l thirst and hunger, weight loss, swellings on legs/ankles, burning ion 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, frequent skin infections and slow healing of wounds and sores.

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

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

Technical ement: The process for preparation of Momordz'ca charantia juice powder and the formulation synthesized 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 orating the nutritional and pharmaceutical properties of the natural composition like enrichment of proteins and bitters that are responsible for ycemic ty.

- The s 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 prepared in accordance with the present disclosure is comparatively more effective against diabetes.

- The ica charantia juice powder ed in ance with the present disclosure is a natural food which is non toxic, easy to digest with optimum nutrition, health protective and promotive properties.

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 invention to achieve one or more of the desired objects or results.

Any discussion of nts, 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 invention. 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 ties are only approximate values and it is envisaged that the values higher than the numerical value assigned to the physical parameters, dimensions and quantities fall within the scope of the invention andthe claims unless there is a statement in the cation to the ry.

The ing description of the specific embodiments 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 ments without departing from the generic concept, and, therefore, such adaptations and modifications should and are ed to be comprehended within the meaning and range of equivalents of the disclosed embodiments. 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 preferred embodiments, those skilled in the art will recognize that the embodiments herein can be practiced with ation within the spirit and scope of the embodiments as bed herein.

Claims (1)

1. A process for preparing an extract of Momora’ica charantia sing the following steps: a) preparing crude juice from d and chopped unripe Momordz'ca charantia fresh fruit to which water is added intermittently; b) filtering the crude juice to obtain d 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 extract of Momora’ica charantz'a. !Q A process as claimed in claim 1, wherein the organic acid is at least one selected 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 ide, potassium hydroxide, m ide and sodium bicarbonate. 7. The process as claimed in any one of the preceding 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 t of Momordica charantia. 10. A formulation containing 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 , granule, capsule, , sachet, suspension, liquid, pastille, chewing gum, lozenges and pill.