DESC: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
25 anticipated variations of embodiments; on the contrary, the intention is to cover all
7
modifications, equivalents, and alternatives falling within the spirit and scope of the
present disclosure as defined by the appended claims.
[0021] Unless the context requires otherwise, throughout the specification which
follow, the word “comprise” and variations thereof, such as, “comprises” and
5 “comprising” are to be construed in an open, inclusive sense that is as “including,
but not limited to.”
[0022] 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,
10 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.
15 [0023] The headings and abstract of the invention provided herein are for
convenience only and do not interpret the scope or meaning of the embodiments.
[0024] 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
20 time of filing.
[0025] The present disclosure relates to a process for preparing aqueous transparent
coating of phytochemical mixtures for taste masking of drugs.
[0026] In the preferred embodiment of the present disclosure, a process for
25 preparing an aqueous transparent coating of phytochemical mixtures further
comprises of phytochemical mixtures like Curcumin, Guar gum and Okra gum,
8
HPMC as film former with binding property in aqueous coating and distilled water
as the aqueous medium.
[0027] In an embodiment of the present disclosure, powdered extract of Curcumin
and Guar gum was purchased from the local market while okra pods were purchased
5 from the local market and later powdered extract was prepared while HPMC was
obtained
[0028] In an embodiment of the present disclosure, powdered extract of okra pods
has been prepared by cutting the okra pods into thin slices, drying the slices and
further milling the dried slices into the powder.
10
[0029] In an embodiment of the present disclosure, a process for preparing aqueous
transparent coating of phytochemical mixtures for taste masking of drugs comprises
of;
- taking the powdered extract of Curcumin, Guar gum, Okra gum and HPMC
15 in a beaker and adding distilled water to the said mixture to form aqueous
medium;
- allowing to set the aqueous medium by keeping it aside for few hours;
- stirring the aqueous medium containing the said phytochemical mixture in
the magnetic stirrer under a constant speed and if needed, increasing the
20 speed accordingly for forming vortex;
- the stirring speed is reduced momentarily to avoid foaming and trapping of
air;
- after 24 hours of continuous magnetic stirring, sieving the aqueous
transparent coating solution to obtain clear solution;
25 - spraying of the aqueous transparent coating solution on the tablets for taste
masking for 30 to 45 mins;
- drying of coated tablets in tray dryer at 40-650C for 30 to 45mins.
9
[0030] In another embodiment of the present disclosure, disclosed herein is a
process wherein, spraying of the aqueous transparent coating solution on the tablets
for taste masking for 30 to 45 mins further involves stopping of the continuous
stirring for one minute at every interval of 5 minutes, the same is repeated until 30
5 to 45 mins.
[0031] In another embodiment of the present disclosure, disclosed herein in a
process wherein, drying of coated tablets in tray dryer at 40-650C for 30 to 45 mins
further involves removing the aqueous transparent coated tablets for one minute
from tray dryer at every interval of 10 mins, the same is repeated until 30 to 45
10 mins.
[0032] In another embodiment of the present disclosure, 150 grams of powder
extract is used for preparing aqueous transparent coating solution that has been
prepared by mixing of Curcumin, Guar gum, Okra gum and HPMC together per
one litre of distilled water.
15
[0033] In another embodiment of the present disclosure, in 150 grams of powder
extract used for preparing aqueous transparent coating solution the quantity of
HPMC is 90-95 %, curcumin powder is 0.1-0.5 %, Guar gum powder is 2.5-4 %
and Okra gum powder is 2-5 %.
20
[0034] In another embodiment of the present disclosure, an aqueous coating
solution prepared by the said process of using phytochemical mixtures has been
evaluated further with respect to parameters like threshold bitterness, weight
variation, % cumulative release after coating, spraying time and stability; the said
25 aqueous coating solution has been used as a coating for tablet for evaluation of
palatability, friability, disintegration, patient’s compliance and appearance and
comparing the same evaluation factors with the coated tablets currently available in
the market .
10
[0035] In yet another embodiment of the present disclosure, a process for preparing
aqueous transparent coating of phytochemical mixtures for taste masking of drugs,
does not involve addition of excipients like synthetic preservatives, flavors and
5 colors.
[0036] In yet another embodiment of the present disclosure, an aqueous transparent
coating prepared by the said process has advantages including, improves poor
characteristic of drugs like unpleasant taste, odour, patient compliance and aesthetic
10 appearance; derived from natural source and is stable, is free from excipients such
as preservatives, diluents, flavors etc; no weight reduction during tablet coating and
enhances the bioavailability of drugs.
The following examples further describe certain specific aspects and embodiments
15 of the invention and a better understanding of present invention may be obtained
through the following examples and displayed process for manufacturing and it
demonstrates the practice and advantages thereof. It is to be understood that the
examples are given by way of illustration only and are not intended to limit the
scope of invention in any manner.
20 EXAMPLES:
a) Preparation of powder extract:
In the present invention, powdered extract of Curcumin and Guar gum was
purchased from the local market while okra pods were purchased from the local
market and later powdered extract was prepared while HPMC was obtained
25 Preparation of powder extract from okra pods:
Okra pods were washed sliced into about 2-3 cm thickness and dried at about 50 °C
in locally fabricated cabinet dryer for up to 3-4 hours. Drying okra at this
11
temperature gives high quality dried slices. The dried slices were milled and then
sieved through Sieve no 80 to give okra powder. The okra powder was thinly spread
on stainless steel trays for drying in a cabinet dryer thermostatically set at a
temperature of 60 °C until the moisture contents were below 12% (wet basis). The
5 dried flakes were then cooled, pulverized and packaged in sealed high-density
polythene bags and kept under a dry cool condition.
b) Process for preparing an aqueous transparent coating from taste masking of
drugs:
10 Accurately weigh curcumin, guar gum, okra gum and HPMC and mix all the
powders together in a beaker to form 150 grams of total weight. In 150 grams of
total mixture, the quantity of HPMC is 90-95 %, curcumin powder is 0.1-0.5 %,
Guar gum powder is 2.5-4 % and Okra gum powder is 2-5 % as indicated in table
1 below. To 150 grams of powder mixture, add one litre of distilled water to form
15 aqueous medium. Allow the aqueous medium to set by keeping it aside for one to
three hours. Stir the aqueous medium containing the said mixture in the magnetic
stirrer under a constant speed and if needed, increase the speed accordingly for
forming vortex. The stirring speed is reduced momentarily to avoid foaming and
trapping of air. After 24 hours of continuous magnetic stirring, sieve the aqueous
20 transparent coating solution to obtain clear solution. Spray the aqueous transparent
coating solution on the tablets for taste masking for 30 to 45 mins. While spraying
the aqueous transparent coating solution on the tablets, after 5 mins of continuous
spraying, the spraying is stopped for one minute and the same is repeated until 30
to 45 mins. The coated tablets are dried in tray dryer at 40-650C for 30 to 45mins.
While drying the coated tablets, after 10 mins of continuous drying at 40-650
25 C, the
coated tablets are removed from tray dryer for one minute and are again exposed to
continuous drying at 40-650C for 10 mins, the same is repeated until 30 to 45 mins
as indicated in Table 2.
Table 1: Quantity of Phytochemical mixture for aqueous transparent coating in
30 150 grams of powder mixture
12
Table 2: Process of aqueous transparent coating for taste masking of tablets
c) Evaluation of Aqueous Transparent Coated tablets
5
Table 3.1: Evaluation of Aqueous Transparent Coated Ashwagandha tablets
Table 3.2: Evaluation of Aqueous Transparent Coated Ashwagandha tablets
Formulation Palatability in
(10 Sec)
Friability
(%)
Disintegration
(Sec)
Patient’s
Compliance
Appearance
Ashwagandha
Coated Tab
No 0.763 102 Sec Yes Excellent
HPMC 90-95 %
Curcumin powder 0.1-0.5 %
Guar Gum powder 2.5-4 %
Okra Gum powder 2-5 %
Coating
solution
Spraying Time
(30-45 Min)
Drying temp
(30-45 Min & 40-65 0
C)
Concentration
of powder
mixture
Aqueous
Transparent
Coating
Stop 1 minute after
each 5 minutes of
interval
Stop 1 minute after
each 10 minutes of
interval
150gm/1-liter
distilled water
13
Marketed Tab Yes 0.980 1230 Sec Poor Poor
Marketed Tab Yes 1.002 945 Sec Poor Poor
Ashwagandha
Uncoated Tab
Yes 0.802 120 Sec Poor Poor
Determination of Threshold bitterness concentration of Aqueous Transparent
Coated tablets (in vitro taste masking evaluation study)
Threshold value of Aqueous Transparent Coated tablets is determined based on the
5 bitter taste recognized by eight volunteers in the age group of 21–28 years. Aqueous
Transparent Coated tablet is placed at the centre of the tongue of volunteer for 10-
30 seconds. The Tablet is spat out after 30 seconds, and the mouth is thoroughly
rinsed with distilled water. The same procedure is repeated for all volunteers. A gap
of 30 minutes is maintained in between tasting two different solutions. The
10 threshold value is selected on the basis of the lowest concentration that had a bitter
taste.
Aqueous Transparent Coated tablets are placed in a volumetric flask with 50?mL of
phosphate buffer (pH 6.8) and is stirred for 1 minute. The mixture is filtered, and
the filtrate is analysed for Aqueous Transparent Coated tablet concentration at
15 Appropriate (nm) by UV-Visible spectrophotometer and that is compared with the
threshold value.
20
14
Table 4: Taste Evaluation of Aqueous Transparent Coated tablets
Score Inference
5
0-Pleasant, 1-Tasteless, 2-Slightly bitter, 3-Moderately bitter, 4-Extremely bitter
The taste recognition threshold of Aqueous Transparent Coated tablets is
determined on the basis of taste evaluation mentioned in table 4 above. The
10 threshold is found to be 28?µg/mL under in vitro taste masking evaluation study, in
pH 6.8 phosphate buffer.
Table 5: Parameters compared with other marketed products to be considered after
coating of tablets
Sr.
No.
Parameters
Tablets after
Aqueous
transparent coating
Marketed
Tablet 1
Marketed Tablet
2
1 Excipients use for coating Excipient less Uncoated HPMC Coated
15
2 Threshold bitterness 10-14 sec Bitter 2-3sec
3 Weight Variation 1-5 mg 10-30 mg 4-16 mg
4 % cumulative release after
coating
99.98% in 45min Not
disintegrant till
45 min
Not disintegrant
till 45 min
5 Coated / Uncoated Aqueous
transparent
Uncoated Solvent Coated
6 Spraying Time 30-45min - Not mentioned
Above table 5 concludes that aqueous coating threshold bitterness concentration is
10-14 seconds whereas uncoated marketed tablet 1 is bitter and HPMC coated tablet
2 has 2 seconds of bitterness perception. Apart from other parameters, there is no
5 fluctuation in weight variation as compared to other marketed tablets and
Cumulative release after 45 min is near to 100% depicting greater advantage over
marketed tablets.
DSC, XRPD and FTIR studies indicates no interaction between the tablet and
aqueous transparent coating as depicted in Fig 1, Fig 2 and Fig 3 respectively.
10 Stability:
16
The purpose of coating is also the stability testing that provides a proof of the
quality of a finished product which might vary with time, under the influence of a
variety of environmental factors such as temperature, humidity and light.
Stability study has been conducted at 40°C±2°C/75% ± 5% RH in a humidity
chamber indicates that no significant changes occurred during six months. ,CLAIMS:1) A process for preparing aqueous transparent coating of phytochemical
mixtures for taste masking of drugs comprises of following steps;
- taking the powdered extract of Curcumin, Guar gum, Okra gum and HPMC
5 in a beaker and adding distilled water to the said mixture to form aqueous
medium;
- allowing to set the aqueous medium by keeping it aside for few hours;
- stirring the aqueous medium containing the said phytochemical mixture in
the magnetic stirrer under a constant speed and if needed, increasing the
10 speed accordingly for forming vortex;
- the stirring speed is reduced momentarily to avoid foaming and trapping of
air;
- after 24 hours of continuous magnetic stirring, sieving the aqueous
transparent coating solution to obtain clear solution;
15 - spraying of the aqueous transparent coating solution on the tablets for taste
masking for 30 to 45 mins;
- drying of coated tablets in tray dryer at 40-650C for 30 to 45mins.
2) The process for preparing aqueous transparent coating of phytochemical
mixtures for taste masking of drugs as claimed in claim 1 wherein, in the
20 said process, spraying of the aqueous transparent coating solution on the
tablets for taste masking for 30 to 45 mins further involves stopping of the
continuous stirring for one minute at interval of 5 minutes, the same is
repeated until 30 to 45 mins.
3) The process for preparing aqueous transparent coating of phytochemical
25 mixtures for taste masking of drugs as claimed in claim 1 wherein, in the
said process, drying of coated tablets in tray dryer at 40-650C for 30 to 45
mins further involves removing the aqueous transparent coated tablets for
one minute from tray dryer at interval of 10 mins, the same is repeated until
30 to 45 mins.
18
4) The process for preparing aqueous transparent coating of phytochemical
mixtures for taste masking of drugs as claimed in claim 1 wherein, the
amount of powder extract for preparing aqueous transparent coating
solution is 150 grams per one litre of distilled water, comprising mixture of
5 Curcumin, Guar gum, Okra gum and HPMC together.
5) The process for preparing aqueous transparent coating of phytochemical
mixtures for taste masking of drugs as claimed in claim 1 wherein, 150
grams of powder extract used for preparing aqueous transparent coating
solution further comprising 90-95 % of HPMC, 0.1-0.5 % of curcumin
10 powder, 2.5-4 % of Guar gum powder and 2-5 % of Okra gum powder.
6) The process for preparing aqueous transparent coating of phytochemical
mixtures for taste masking of drugs as claimed in claim 1 wherein, an
aqueous transparent coated tablet remained stable even after 6 months.
7) The process for preparing aqueous transparent coating of phytochemical
15 mixtures for taste masking of drugs as claimed in claim 1 wherein, the
threshold bitterness concentration of the aqueous transparent coated tablet
is 10-14 seconds compared to marketed coated tablets.
8) The process for preparing aqueous transparent coating of phytochemical
mixtures for taste masking of drugs as claimed in claim 1 wherein, in the
20 said process no excipients like synthetic preservatives, flavors and colors
have been used.
9) The process for preparing aqueous transparent coating of phytochemical
mixtures for taste masking of drugs as claimed in claim 1 wherein, aqueous
transparent coated tablets improves poor characteristic of drugs like
25 unpleasant taste, odour, patient compliance and aesthetic appearance