Enhancement of Solubility of Diclofenac Sodium by Pastillation Method

Abstract

The Diclofenac Sodium is BCS class II drug which comes under the antipyretic class drug, and has a wide range of use. But due to its low solubility it has low dissolution rate and hence reduced bioavailability. There are several methods for the enhancement of solubility and dissolution rate. Pastillation technique is widely employed in chemical industry for solidification and better handling. Pastilles are solidified discrete units, acquired directly from the melt mass. However, this method of pastillation has not been explored for the drug delivery system yet. Literature revels that it can be used as a novel, effective and easiest method for the enhancement of solubility and dissolution rate. The selection of polymer was done by the solubility studies and Kolliphor HS 15 was used to make the pastilles of Diclofenac Sodium. Formation of pastilles were confirmed by FT-IR and further evaluated for % yield, drug contents, solubility study and dissolution test. From the results it was concluded that, solubility of Diclofenac Sodium was increased by pastillation method by 2-fold and dissolution rate was also enhanced by double than that of the drug. Thus, pastillation can be an effective and easiest method to enhance the solubility, dissolution rate and bioavailability of poorly water-soluble drugs having good permeability. 
 Keywords: Diclofenac Sodium, Pastillation, Kolliphor HS 15, Solubility enhancement, Solid dispersion.

The development of ternary and quaternary solid dispersion based hydrotropic blends of atorvastatin calcium

“…For instance, Pund et al, employed muslin cloth to calculate the percentage of drug release from pastillated diclofenac sodium solid dispersion. 42 In (Table 3) and (Figure 3. A), respectively, the cumulative percentage of drugs released from all ATV formulations, and a pure sample of ATV were displayed.…”

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“…However, active cosmetic ingredients used in anti-ageing therapy such as CoQ10 and AMSC-MP, among others, suffer from skin penetration-related drawbacks including low water solubility and large molecular weight. The use of transfersomes and protransfersomes may facilitate the penetration by active cosmetic ingredients of the deep skin layers, i.e., the dermis, which is composed of almost 70% collagen [103]. "…”

“…This is probably due to its promotion of cyclooxygenase inhibition which reduces melanin transfer to the epidermal keratinocytes [101,102]. Diclofenac itself has come to be regarded as a low water soluble substance with good permeability [103]. El Zaafarany et al (2010) [104] studied a comparison of the characteristics of the Diclofenac topical transfersome prepared by means of two manufacturing methods, active ingredient content, phospholipid-EA ratio, and using five variations of surfactants as EAs.…”

“…Page 15 line 46: "Interestingly, the topical use of 3% diclofenac sodium with hyaluronic acid greatly repairs signs of skin damage due to chronic UV exposure including irregular pigmentation and coarsenes, which are probably due to its activity on cyclooxygenase inhibition decreasing melanin transfer to epidermal keratinocytes[101,102]. Diclofenac itself has been known to be low water soluble substance with good permeability[103]. "Page 16 line 53:"The use of Tween 80 in transfersome loading diclofenac sodium effectively improves deformability of the vesicles thus increasing skin delivery in non-occlusive topical application."…”