studies on the preparation, characterization, and solubility of 2-hp-β-cyclodextrin-meclizine hci...

220 Journal of Young Pharmacists Vol 4 / No 4

p m

antiemetic, antispasmodic, and local anesthetic effects in

INTRODUCTION

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DOI: 10.4103/0975-1483.104365

Studies on the Preparation, Characterization, and Solubility of

George SJ, Vasudevan DT

Department of Pharmaceutics, Amrita School of Pharmacy, AIMS Health Care Campus, Kochi, Kerala, India

Address for correspondence: Dr. Deepa T Vasudevan; E-mail: [email protected]

ABSTRACT

An in vitro study showed that the

From the results of dissolution study, it was found that the prepared formulation was showing better release, which P < t

Key words:

Pharmaceutics

Journal of Young Pharmacists Vol 4 / No 4 221

other antihistamines of its class and also has longer duration

particular

and dissolution properties.

but toroidal or cone shaped. Based on this architecture, the

and their derivatives have been of considerable interest in

inclusion complexes formulation.

of the formulation is to attain faster dissolution rates, the

drug.

forms.

in vitro

MATERIALS AND METHODS

Chemicals

Phase solubility studies


Kc

K S0 (1

Preparation of solid inclusion complexes

Physical mixture

Kneading method

Co-precipitation method

at ambient temperature until complete evaporation of

Differential scanning calorimetrydifferential scanning calorimetry

Fourier transform infrared spectroscopy

.

In vitro dissolution studies

Formulation of tablets by direct compression method

Evaluation of precompression parameters of powder blend

evaluated.

Evaluation of postcompression parameters of tablets


RESULTS

Phase solubility study

Kc, obtained from the slope of

studies.

Differential scanning calorimetry

Fourier transform infrared spectroscopy

2 2

Table 1: Formulae of fast dissolving tablets of binary

Ingredients F1 (mg)Eq. blend of Meclizine HCl

97.63

Pearlitol SD200 58.57MCC (Avicel pH 102) 30Sodium starch glycolate 4Aspartame 1.5

1.5Aerosil (0.4%) 0.8Talc (3%) 6Total 200 mg

Figure 1: Phase solubility diagram of Meclizine HCl with -CD and HP- -CD


to the restriction of bending and stretching vibration of

due

indicating noncovalent interaction in inclusion complex.

Drug content

In vitro dissolution studies

release on the y x

Figure 2: DSC thermogram of Meclizine HClFigure 3: DSC thermogram of HP- -CD

Figure 4: DSC thermogram of physical mixtures

Figure 5: DSC thermogram of the co-precipitation complex


Evaluation of precompression parameters of powder blend

,

Evaluation of postcompression parameters of tablets

2

in vitro

in

DISCUSSION

Figure 6: DSC thermogram of the kneading complex

Figure 7: FT-IR spectra of Meclizine HCl

Figure 8: FT-IR spectra of HP- -CD

581.

81756.

22851.

71

942.

85

1032

.28

1157

.93

1245

.86

1335

.75

1373

.21

1413

.39

1645

.73

2929

.13

-10 0

10 20 30 40 50 60 70 80 90

%T

5001000150020002500300035004000Wavenumbers (cm-1)

Figure 9: FT-IR spectra of physical mixture

Time (min) % Release from prepared tableta

% Release from marketed tableta

5 44.44 ± 0.61 3.49 ± 0.3210 68.28 ± 0.46 9.87 ± 0.2315 72.34 ± 0.64 22.43 ± 0.9320 78.31 ± 0.48 28.98 ± 0.3425 84.12 ± 0.46 34.93 ± 0.9430 95.16 ± 0.64 53.39 ± 0.4545 - 70.39 ± 0.5060 - 81.39 ± 0.49aMean ± SD, n = 3


indicates the formation of true complex and conversion of

could be diagnosed as a superimposition of the bands of

formation of inclusion complex in the solid state. All the

inclusion complex. In vitro drug release from prepared tablets

technique and inclusion complex based fast dissolving tablets

ACKNOWLEDGMENTS

REFERENCES

Figure 10: FT-IR spectra of the kneading method

-10 0

10 20 30 40 50 60 70 80 90

%T

4000 3500 300026

36.0

5

2927

.63

2500

2202

.04

2450

.67

2513

.84

2000Wavenumbers (cm-1)

1430

.51

1644

.21

1155

.9612

41.7

7

1373

.27

1500

700.

3675

7.25

850.

39

941.

54

1000

581.

15

500

Figure 11: FT-IR spectra of co-precipitation

Figure 12: -CD systems

Figure 13:tablet and marketed tablet


How to cite this article: George SJ, Vasudevan DT. Studies on the

Source of Support: Nil, None declared.

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