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Publication
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| Title of Article |
EFFECTS OF FORMULATION PARAMETERS ON PROPERTIES OF GASTRIC
FLOATING TABLETS CONTAINING POORLY SOLUBLE DRUG: DICLOFENAC
SODIUM |
| Date of Acceptance |
17 August 2018 |
| Journal |
| Title of Journal |
International Journal of Applied Pharmaceutics |
| Standard |
SCOPUS |
| Institute of Journal |
Elsevier B.V. |
| ISBN/ISSN |
0975-7058 |
| Volume |
10 |
| Issue |
6 |
| Month |
November |
| Year of Publication |
2018 |
| Page |
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| Abstract |
Objective: The objective of this study was to prepare and investigate the effects of formulation
parameters on the properties of gastric floating tablets containing diclofenac sodium (DICL) as a
model of poorly soluble acidic drug, sodium bicarbonate (NaHCO3) or calcium carbonate
(CaCO3) as gas-forming agent, hydroxypropyl methylcellulose (HPMC) K100M or K15M as
swelling polymer and sodium lauryl sulfate (SLS) as wetting agent.
Methods: DICL floating tablets were prepared using direct compression method. The compressed
tablets were evaluated for tablet properties, swelling index, and in vitro buoyancy. The in vitro
release under non-sink condition was determined. Molecular interaction was studied using
differential scanning calorimetry and fourier transform infrared spectroscopy.
Results: The tablet properties of all DICL floating tablets were within the acceptance criteria. The
molecular interaction between DICL and excipients in formulation was excluded. Depends on the
formulation compositions, the swelling index at 3 h (SI) ranged from 44±11 to 1158±33 %,
whereas the buoyancy properties namely floating lag time (FLT) and total floating time (TFT)
were 0.33±0.03 to 10.04±0.04 min and 10.0±0.0 to >12 h, respectively. NaHCO3 showed higher
swelling, buoyancy and release properties compared to those of CaCO3. NaHCO3 at 20% gave
sufficient swelling (SI of 1074±16 %), buoyancy (FLT of 0.39±0.03 min, TFT of >12 h) and
release properties (cumulative release of 5.83±0.02 %). HPMC K100M showed better swelling
property of which its initial swelling rate was 1412±25 %/h compared to HPMC K15M (1042±31
%/h). HPMC K100M at 20% showed better buoyancy and release properties compared to those
obtained from HPMC K100M at 30%. The release testing under non-sink conditions was able to
distinguish the effect of formulation parameters on the DICL release profiles. Incorporation of
SLS at 0.25% could enhance both release rate and cumulative release of DICL from the floating
tablets. Nevertheless, it showed unacceptable adverse effect on swelling and buoyancy properties
of DICL floating tablets. The TFT of DICL floating tablets containing 0.25% SLS was only
0.5±0.0 h.
Conclusion: DICL floating tablets were successfully prepared. Tablets possessing suitable
swelling and buoyancy properties were obtained using NaHCO3 at 20% as gas-forming agent,
with HPMC K100M at 10 and 20% as floating matrix and swelling polymer. Addition of SLS as
wetting and solubilizing agent showed unacceptable adverse effect on the swelling and buoyancy
properties of DICL floating tablets. The release under sink conditions and/or in vivo
pharmacokinetic studies shall be further performed. |
| Keyword |
Diclofenac sodium, Floating tablet, HPMC, SLS |
| Author |
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| Reviewing Status |
มีผู้ประเมินอิสระ |
| Status |
ได้รับการตอบรับให้ตีพิมพ์ |
| Level of Publication |
นานาชาติ |
| citation |
false |
| Part of thesis |
true |
| ใช้สำหรับสำเร็จการศึกษา |
ไม่เป็น |
| Attach file |
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| Citation |
0
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