See discussions, stats, and author profiles for this publication at: https://www.researchgate.

net/publication/236213513

The film coating potential of grewia gum: Some physicochemical properties

of paziquantel tablets

Article · April 2011

CITATIONS READS

18 440

2 authors:

Ikoni Joshua Ogaji Ignatius Sylvester Okafor

University of Jos University of Jos
32 PUBLICATIONS   214 CITATIONS    16 PUBLICATIONS   118 CITATIONS   

SEE PROFILE SEE PROFILE

Some of the authors of this publication are also working on these related projects:

Excipient from local sources View project

Phytotherapy View project

All content following this page was uploaded by Ikoni Joshua Ogaji on 21 May 2014.

The user has requested enhancement of the downloaded file.

 International Journal of Pharmaceutical Research
2011, Volume 3, Issue 2, 16-19.
ISSN 0975-2366

Research Article
Potential of Grewia Gum as Film Coating Agent: Some physicochemical properties of
Coated Praziquantel Tablets
Ikoni Ogaji*1,2 and Ignatius S. Okafor1
1
.Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, University of Jos,
PMB 2084 JOS 930003
2.
Currently in School of Pharmacy, University of Maryland, 20 N Pine Street, Baltimore, MD 21201
* Corresponding author:ikoniogaji@gmail.com
Received: 17/08/2010, Revised: 06/09/2010, Accepted: 10/10/2010
ABSTRACT
The purpose of this work was to study the film coating potential of grewia gum, extracted from the stem bark of Grewia
mollis, using praziquantel as a model drug. Core tablets of praziquantel were prepared by wet granulation method and the
physicochemical properties such as weight, hardness, friability and disintegration time were evaluated. Aqueous coating
suspensions of grewia gum extract (2.5%w/w) with or without plasticizers were prepared and used to coat the tablets in an
improvised coating pan. The coated tablets were evaluated for weight uniformity, diameter, thickness, hardness, friability,
and disintegration time and moisture uptake at controlled humidity. The coating remained intact, durable and resistant to
chipping when challenged to catastrophic fall or rubbed on a white paper. Hardness of coated tablets improved by 40% and
the disintegration time was extended five- fold compared to the core tablets. There were changes in the amount of moisture
absorbed, which was dependent on the formulation and the environmental condition. The formulation of grewia gum without
plasticizer and that containing polyethylene glycol 4000 were of better quality compared to those with glycerin and propyl-
ene glycol.

KEYWORDS: Grewia gum, film coating, potential, physicochemical properties

INTRODUCTION the Middle East[6-8]. Due to the bitter taste of praziquantel

The application of coatings to pharmaceutical solids
has been practiced for a while now and coating has been
used in a variety of pharmaceutical products such as tablets,
beads, pellets, granules, capsules, and drug crystals[1] Tab-
let coating, whether sugar or film coating, offers many ad-
vantages, namely, improving aesthetic qualities of dosage
forms, masking unpleasant odor or taste, easing digestion,
improving product stability, and modifying the release
characteristics of the drug, for example, the enteric coated,
colonic delivery systems, controlled release systems and
osmotic pump systems[2, 3].
Film coating is a complex and multi-step process in-
volving the application of thin polymer- based layer to a
substrate under conditions that permit parallel computation
between the addition rate of the coating liquid and the dry-
ing, uniformity of distribution of the coating liquid across
the surface of the substrate, and optimization of the quality
of the process and final coat[4]. Film layer may be formed
from either polymeric solution (organic- solvent or aqueous
based) or aqueous polymeric dispersion (commonly called
latex). Polymer is the main ingredient in the majority of
film-coated formulations, and it may be from different ori-
gins, including cellulosics, acrylics, vinyl, and combination
polymers. Natural polymers have advantages over synthetic
and semi synthetic polymers in that they are cheap and
easily available, nonirritant, biodegradable, biocompatible,
and ecofriendly[5]
Praziquantel is a white to nearly white crystalline
powder with bitter taste and it is formulated as a 600mg
tablet for treatment of schistosomiasis, liver flukes and tape
worms. Human schistosomes, in which this drug is most
useful currently infect more than 200 million people in 74
countries worldwide in the endemic areas of Africa, the
Caribbean, Central America, South America, East Asia, and
it is usually film coated to increase patient compliance.
These coatings are usually accomplished with synthetic
polymers which may increase the cost of the drug.
Grewia gum is a polysaccharide derived from the inner
bark of the edible plant Grewia mollis,Juss (family Tiliace-
ae). The plant is a savanna shrub that grows wildly but is
usually cultivated[9]. The leaves and bark of the plant con-
tain mucilage[10]. In Nigeria the dried and pulverized inner
stem bark is used as a thickening agent in some local dish-
es[11]. The binding effect of grewia mollis gum has been
investigated on salicylic acid as a model drug and it was
demonstrated that grewia gum has a good binding proper-
ty[12]. Some scientists[13] also investigated the effect of
the gum on the mechanical properties of paracetamol tablet
formulation using the density measurements and compres-
sion equations of Heckel and Kawakita as assessment pa-
rameters. Grewia gum was found to improve the fluidity of
paracetamol granulation than pvp and the conclusion of
another study carried out by Okafor and Chukwu was that
gum might find application in film coating of tablets, cap-
sules and granules[14].
The purpose of this work was to carry out some pre-
liminary investigations on the potential of grewia gum as a
film coating agent using praziquantel as a model drug.
MATERIAL AND METHODS
Materials
Grewia gum was obtained from the stem bark of a
wild Grewia mollis in the locality and mucilage was ex-
tracted with ethanol 96%. Praziquantel powder was re-
ceived as a gift from Baka’I Helvetica Pharmaceutical
Company, Minna, Nigeria; Pregelatinized starch (Ro-
quette),Microcrystalline cellulose (FMC, Biopolymer,
USA), titanium dioxide (Whittaker, New Jersey USA and

16 | IJPR | April-June
 Ogaji and Okafor / International Journal of Pharmaceutical Research 2011 3(2) 16-19

talcum powder (Roquette). Chemicals were of the analyti- environment was measured by means of OM-44 Omega
cal or British Pharmacopoeia grade. data logger (Omega, USA). The core praziquantel tablets
were weighed and charged into the coating pan and warmed
Core Tablet Production to 40-45 oC before the coating process. The suspension was
The core tablets with target weight of 650mg consisted atomized in Kumas airless electric sprayer (Kumas Compa-
of praziquantel (92.3%w/w), pregelatinized starch as binder ny, Germany) and sprayed on to the tablets while the drying
and microcrystalline cellulose as a disintegrant were was achieved with the aid of a hand held dryer. The coat-
3.1%w/w each while talcum powder was used at 1.5%w/w ing was stopped after a uniform coat was observed on the
level as a lubricant. Core tablets of praziquantel were made tablets. The tablets were discharged from the coating pan
using the wet granulation method[15]. The wet granulation and dried in a hot air oven at 50 oC for 30-45 minutes. The
was performed in a Diosna mixer (Dierks and Sohne, dried tablets were stored in double airtight polythene bags
GmbH, Germany) by adding sufficient quantity of water as for 48hrs before evaluation
the granulating fluid. The wet mass was screened through a
no.16 mesh sieves (Humboldt, USA) and was dried in hot Evaluation of coated tablets
air circulating oven (Genlab Limited, UK) for 24 hrs at 50 Generally the coating remained intact, durable and
o
C. The dried granules were passed through no.40 mesh resistant to chipping when challenged to catastrophic fall or
sieves (Humboldt, USA) and blended before compression rubbed on a white paper. The coated tablets were evaluated
on SVIAC tabletting machine (SVIAC,France) at a com- for weight uniformity, hardness, percent friability, disinte-
pression of 70N using 13.0mm punches and dies. The com- gration time, dimensions, moisture absorption at different
pressed tablet were evaluated on the following parameters: relative humidity conditions and rate of water uptake.
average weight; hardness; friability, disintegration time and Weight uniformity: Twenty tablets were individually
the dimensions (thickness and diameter). weighed and the standard deviation determined
Harness: Ten tablets were used for this test using Mo-
Preparation of coating suspension santo hardness tester
Grewia gum (2.5%w/v) coating suspensions were Friability: The friability of ten tablets was determined
prepared according to the formulation in Table 1. The on a Roche friabilator from the percent difference in weight
choice of concentration of grewia was informed by the before and after 4 minutes catastrophic fall on the friabila-
observations from pre formulation experiments. Grewia tor.
gum was dispersed in about 50 ml of water at 60-70oC. Disintegration time: The time it took six tablets in
Other components were added stepwise and the volume Erweka disintegration time machine to break into non-
was made up with water. The density of the coating suspen- palpable mass in water maintained at 37oC was taken as the
sions was 1.18-1.22gcm-3 and viscosity  271.7centipoise. disintegration time.
Moisture sorption: Five tablets of known weight were
Table 1: Coating formulations of grewia gum with dif- placed in desiccators maintained at relative humidity condi-
ferent plasticizers tions of 20-97%RH and weight of the tablets was taken at
24 hourly initially and the interval was increased up to 30
Formulation days. Increase in weight of the tablet was taken as the
Description amount moisture absorbed.
1 2 3 4
Water uptake and water uptake rate. The methods of
Grewia gum (g) 2.5 2.5 2.5 2.5 Gohel et al[16] and Zhang et al[17] were used with modifi-
Glycerin (g) B.P 10 cation. A whatman filter paper supported by glass slide was
placed on a petri-dish that was partially filled with water. A
Propylene Glycol (g) 10 tablet was placed on the filter paper and uptake of water
Polyethylene Glycol 4000 (g) 10 occurred from the lower surface of the tablet. The tablet
was removed and assessed change in weight. The percent-
Titanium dioxide B.P (g) 1.2 1.2 1.2 1.2
age water uptake by the tablet was calculated by:
Talcum powder B.P (g) 1.0 1.0 1.0 1.0
Water (g) qs. 100 100 100 100 % water uptake = (wt-wo/wo) X100 ……………[1]

where wt is the wet weight of the tablet at 5minutes and wo

Relative humidity conditions is the initial weight of the dry coated tablet. Changes in the
Saturated salt solutions were prepared by dissolving
dimensions (diameter and thickness) of the coated tablet
the salt in distilled water at 60oC until crystal deposit of the
were measured using venier caliper and the results were the
salt was seen. Desiccators of 9500-9800ml were used with
average of five determinations.
portions of 500ml saturated salt solutions at 20-25oC. No-
mad RH/Temp 2X external OM-44 (Omega, USA) was
RESULTS AND DISCUSSION
used to measure the relative humidity, temperature and dew
Polymers used in film coating are mostly amorphous
point in the desiccators and the data was read out on a com-
in nature; therefore, glass transition temperature (Tg) plays
puter with the aid of the Omega software (Logsoft).
an important role in the formation of the coat layer and its
stability[18].Below Tg polymer is brittle, while it becomes
Film coating rubbery and flexible above Tg, which indicates an increase
Film coating was done in an improvised coating pan
in the temperature coefficient of expansion[18]. To lower
(internal and outer diameter respectively were 15.2 and
Tg and impart flexibility, platicizers are added. In this study
15.4mm) placed about 75cm away from the spray gun noz-
water, glycerin, propylene glycol and polyethylene glycol
zle. The relative humidity and temperature of the coating
4000 were used as plasticizer at 10% w/w of the coating

IJPR | April-June | 17
 Ogaji and Okafor / International Journal of Pharmaceutical Research 2011 3(2) 16-19
suspension to gain insight on their effects on the physico-
chemical properties of the coated tablets. The role of titani-
um dioxide was as an opacifier while talcum powder served
as the anti tacky agent to prevent tackiness during the coat-
ing process and storage.
Table 2. Some Physicochemical Properties of Coated Praziquantel Hydrochloride Tablets
Description
1 2
Weight uniformity (mg) 652 (8.3*) 653.1.7(7.9*)
Hardness (kgf) 6.5 7.0
Friability (%) 0.001 0.001
Thickness (mm) 4.20 (0.2*) 4.15 (0.2)
Diameter (mm) 13.10 13.10
Disintegration time (min) 5 12
Water uptake in 5min (%) 84.10 68.18
Rate of water uptake (g/s) 0.28 0.23
* Standard deviations.
Film coating is deposition of a thin film of polymer
surrounding the tablet core. It is more favored than sugar
coating because weight increase is 2-3%, single stage pro-
cess, easily adaptable to controlled release, it retains color
of original core, and high adaptability to GMP and automa-
tion is possible[19, 20]. Some film coats do not significant-
ly change physicochemical properties such as hardness and
disintegration of core tablets, making them ideal for taste
masking and improvement of appearance of tablets. Table2
shows some physicochemical properties of coated pra-
ziquantel tablets. There was a marginal increase of 0.6% in
weight of the coated tablet over that of the core. Applica-
tion of coating material resulted in a 30-40% improvement
in the hardness of tablets and their friability was reduced
by 99.5% compared to the core tablets. Similarly the disin-
tegration time of coated tablets was prolonged 2-5 fold that
of the core tablets depending on the formulation. Although
the official limit for disintegration time of oral uncoated
tablets is 15 minutes while coated tablets could be up to
2hrs[21], and it could be concluded that both the uncoated
and coated tablets passed the official test for uncoated tab-
lets making this type of coating suitable for decorative,
taste and odor masking without affecting the pharmacoki-
netic profile of the tablet. One of the objectives for film
coating tablets is to facilitate swallowing of tablets by pa-
tients[3]. Friable and soft tablets may be difficult to handle
during transfers, transport and storage. The improvement in
hardness and friability of the coated tablets suggest that the
polymer could be useful in improving the mechanical prop-
erties of tablet formulations that are inherently soft and
friable, thereby improving patient compliance and reduction
in damages that might arise during transport. The diameter
and thickness of the coated tablets did not vary much from
batch to batch as suggested by the low standard deviations
indicating that the coating suspension evenly covered the
tablets during the coating process.
Plasticizers are usually non-volatile, high boiling or-
ganic solvents used to impart flexibility to otherwise hard
or brittle polymeric material[22]. Polymeric films use plas-
18 | IJPR | April-June
ticizers to impart flexibility, improve flow and reduce brit-
tleness and different plasticizers achieve this to different
extent. In this study water, propylene glycol, glycerin and
polyethylene glycol 4000 were used as plasticizers and
formulation containing them were designated as Formula-
Formulation
3 4 Core
653.6 (9.2*) 652.4 (7.3*) 649.6(7.3*)
6.5 6.5 5.0
0.001 0.001 0.2
4.15 (0.2) 4.15(0.3) 4.10
13.10 13.05 13.0
4 4.5 2.5
67.24 101.40 89.1
0.22 0.34 0.3
tion 1, 2, 3 and 4 respectively. The effects of the plasticiz-
ers used in the coating suspension are also shown in Ta-
ble2. Tablets containing glycerin (formulation 2) had an
average hardness of 7.0kfg while those tablets containing
water (Formulation1), propylene glycol (Formulation3) and
polyethylene glycol 4000 (Formulation4) had the same
average hardness of 6.5kgf.The disintegration times were of
the order: Formulation2 > 1 >4 > 3. These increases in the
disintegration times of the coated formulation were proba-
bly due to the effect of the coating material and the type of
plasticizer used. The profile of these coated tablets showed
that glycerin imparted better mechanical properties on the
coated tablets when used as plasticizer compared to water,
propylene glycol or polyethylene glycol.
Water uptake experiment gives an idea of the level of
protection that a film coat offers to the core tablet when
challenged with substantial amount of fluid. The values of
the water uptake by different formulations of the coated
tablets as shown in the table indicate that formulation con-
taining polyethylene glycol had the highest water uptake
capacity while those of propylene glycol had the least water
uptake. The general order of water uptake was Formulation
4 > S >1 >2 > 3
One of the factors that affect the stability of pharma-
ceutical products is moisture. Deterioration is faster when a
pharmaceutical product comes in contact with moisture and
relative humidity is key to the amount of moisture present
in an environment[21, 23]. Effect of varying the relative
humidity conditions on the amount of moisture absorbed by
the tablets over time was also studied. Except the first 4
days all the formulations maintained a moisture sorption of
less than 0.0025g at 22% RH. The amount of moisture ab-
sorbed remained minimal and almost the same in all formu-
lation at below 55% RH except few surges seen in uncoated
(S). It was observed that above 55%RH Formulations 2
tablets tended to be sticky with storage, a situation that can
pose stability problem. Increase in the percent relative hu-
midity resulted in pronounced changes in the moisture sorp-
tion and desorption in the formulations. Neither absorption
nor disorption is good for the integrity of the tablets be-
 Ogaji and Okafor / International Journal of Pharmaceutical Research 2011 3(2) 16-19
cause this could lead to instability of the tablet by being
susceptible to hydrolysis in the presence of moisture or
cracking of the films. In this study tablets in all the formu-
lations absorbed moisture. The amount of moisture ab-
sorbed at lower relative humidity were similar but began to
differ with increase in relative humidity conditions. At 95%
relative humidity, for example, fewer fluctuations were
seen in Formulation1 and 4 when compared to 2, 3 and ST.
This data showed that grewia gum may be a film former
that can be used with or without plasticizers in aqueous film
coating operations. Should this turns out to be true it will
overcome the disadvantage that the most widely used aque-
ous film former, hydroxylpropyl methylcellulose suffers
but this is yet to be confirmed, a scope beyond the present
work. When the coated tablets from these formulations
were subjected to abrasion on a white paper, there was no
evidence of peel indicative of adhesiveness of the coat to
the tablets. The changes that were observed in friability,
disintegration, and water uptake and moisture sorption to
our mind are due to the effects of the coats conferred on the
tablets and more work is being done to verify this initial
observation. No physical changes were observed on any of
the formulations to suggest incompatibility of the plasticiz-
ers with the film former.
CONCLUSION
The potential of grewia gum (2.5%w/w) as a film-
coating agent was investigated using praziquantel tablets as
model drug. Aqueous coating suspensions of the gum with
or without plasticizers were prepared and used to coat the
tablets. The tablets were evaluated for some physicochemi-
cal properties and effect of environmental conditions on
their stability. It was observed that the friability, hardness
and disintegration time changed compared to those of the
uncoated. Changes were also observed in the response of
the tablets in these formulations to environmental condi-
tions, which was dependent on the formulation and we
conclude that the observed changes were due to the effects
of plasticizers and the mechanical properties of the grewia
gum films deposited and formed on these tablets during the
coating process.
REFERENCE
1. Rhodes CT, Porter SC: Coating for controlled release
drug delivery systems. Drug Development and Indus-
trial Pharmacy 1998, 24(12):1139-1154.
2. Rowe RC: The effect of some formulation and process
variables on the surface roughness of film coated tab-
lets. Journal of pharmacy and Pharmacology 1978,
30:669-672.
3. Kwok TSH, Sunderland VB, Heng WP: An investiga-
tion on the influence of a vinyl pyrrolidone/vinyl ace-
tate copolymer on the moisture permeation, mechani-
cal and adhesive properties of aqueous-based hydrox-
ypropyl methylcellulose film coatings. Chemical and
Pharmaceutical Bulletin 2004, 52(7):790-796.
4. Rowe RC: Tablet-tablet contact and mutual rubbing
within a coating drum-an important factor governing
the properties and appearance of tablet film coatings.
International Journal of Pharmaceutics 1988, 43:155-
159.
View publication stats
5. Singh K, Kumar A, Langyan N, Ahuja M: Evaluation
of Mimosa pudica seed mucilage as sustained release
excipient. In: AAPS PharmSciTech AAPS
PharmSciTech 2009.
6. Salvana EM, King CH: Schistosomiasis in travelers
and immigrants. Current Infectious Disease Report
2008, 10(1):42-49.
7. Chitsulo L, Engels D, Montresor A, Savioli L: The
global status of schistosomiasis and its control. Acta
Tropica 2000, 77(1):41-51.
8. Yosry A: Schistosomiasis and neoplasia. Contributions
to Microbiology 2006, 13:81-100.
9. Keay FW, Onoche CFA, P SD: Nigeria trees. Ibadan:
Department of Forestry; 1964.
10. Gill LS: Ethnomedical uses of plants in Nigeria. Be-
nin: UniBen press, University of Benin, Benin City;
1992.
11. Okafor IS, Chukwu A, Udeala OK: Some physico-
chemical properties of grewia gum. Nigeria Journal of
Polymer Science and Technology 2001, 2(1):161-168.
12. Okafor IS, Chukwu A: Water vapor permeability of
aqueous based grewia gum film. Nigeria Journal of
Polymer Science and Technology 2003, 3(1):178-185.
13. Emeje M, Isimi C, Kunle O: Effect of grewia gum on
the mechanical properties of paracetamol tablet formu-
lations. In: African Journal of Pharmacy and Pharma-
cology. vol. 2; 2008: 1-6.
14. Okafor IS, Chukwu A: The mechanical properties of
aqueous based grewia gum films. Nigeria Journal of
Polymer Science and Technology 2004, 4(1):305-309.
15. Omlo IG, Ghaly ES: Evaluation of two dextrose-based
directly compressed excipients. Drug Development
and Industrial Pharmacy 1998, 24(8):771-778.
16. Gohel MC, Patel PD, shah NK, Jani GK: Evaluation of
synthesized cross-linked tragacanth as a potential dis-
integrant. Indian Journal of Pharmaceutical Sciences
1996, 59:113-118.
17. Zhang X, Wang Y, Wang J, Wang Y, Li s: Effect of
pore former on the properties of casted film prepared
from blends of Eudragit NE30D and Eudragit L30D-
55. Chemical and Pharmaceutical Bulletin 2007,
55(8):1261-1263.
18. Missaghi S, Fassihi R: A novel approach in the as-
sessment of polymeric film formation and film adhe-
sion on different pharmaceutical solid substrates.
AAPS PharmSciTech 2004, 5(2 art 29):1-8.
19. Cole G, Aulton ME, Hogan J: Pharmaceutical coating
technology: Informa HealthCare; 1995.
20. Hogan JE: Tablet coating. In: Pharmaceutics: The
science of dosage form design. Edited by Aulton ME.
New York: ChurchhillLivingstone; 1988: 734.
21. Pharmacopoeia: British Pharmacopoeia. London: Her
Majesty Stationary Office; 1998.
22. Morflex: Influence of plasticizers on the dissolution
and physical properties of ethyl-cellulose films and
coated beads. In: Pharmaceutical Coatings Bulletin.
USA: Morflex Inc; 1995: 102-103.
23. Application note on SHTXX humidity and tempera-
ture sensmitter introduction to relative humidity [
www.sensirion.com ]
IJPR | April-June | 19