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      Formulation and Evaluation of Aceclofenac Injection Made by Mixed Hydrotropic Solubilization Technique

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          Abstract

          Aceclofenac is a non-steroidal anti-inflammatory drug (NSAID) that exhibits analgesic, antipyretic and anti-inflammatory activities. It is practically insoluble in water. The effect of hydrotropes such as urea and sodium citrate and blends (urea + sodium citrate) on the solubility of aceclofenac was investigated. The enhancement in the solubility of aceclofenac was more than 5 and 25 folds in 30% sodium citrate solution and 30% urea solution, respectively, as compared to its solubility in distilled water. The enhancement in the solubility of aceclofenac in a mixed hydrotropic solution containing ≥ 20% urea and 10% sodium citrate solution was more than 250 folds (compared to its solubility in distilled water). This proved a synergistic enhancement in solubility of a poorly water- soluble drug due to mixed hydrotropy. Synergistic combination of hydrotropic agents can minimize the amount of hydrotropic agents employed, minimizing the chances of their toxicities. Aqueous injection of aceclofenac, using the mixed hydrotropic solubilization technique, was developed and by using the lyophilization method, the problem of inadequate stability of aceclofenac in aqueous solution was overcome. The developed formulation was studied for physical and chemical stability.

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          Design of freeze-drying processes for pharmaceuticals: practical advice.

          Xiaolin (Charlie) Tang, Michael J. Pikal (2004)
          Design of freeze-drying processes is often approached with a "trial and error" experimental plan or, worse yet, the protocol used in the first laboratory run is adopted without further attempts at optimization. Consequently, commercial freeze-drying processes are often neither robust nor efficient. It is our thesis that design of an "optimized" freeze-drying process is not particularly difficult for most products, as long as some simple rules based on well-accepted scientific principles are followed. It is the purpose of this review to discuss the scientific foundations of the freeze-drying process design and then to consolidate these principles into a set of guidelines for rational process design and optimization. General advice is given concerning common stability issues with proteins, but unusual and difficult stability issues are beyond the scope of this review. Control of ice nucleation and crystallization during the freezing step is discussed, and the impact of freezing on the rest of the process and final product quality is reviewed. Representative freezing protocols are presented. The significance of the collapse temperature and the thermal transition, denoted Tg', are discussed, and procedures for the selection of the "target product temperature" for primary drying are presented. Furthermore, guidelines are given for selection of the optimal shelf temperature and chamber pressure settings required to achieve the target product temperature without thermal and/or mass transfer overload of the freeze dryer. Finally, guidelines and "rules" for optimization of secondary drying and representative secondary drying protocols are presented.
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            Solubility enhancement of some water-insoluble drugs in the presence of nicotinamide and related compounds.

            Alaa Abdul Rasool, Anwar A Hussain, Lewis Dittert (1991)
            The solubilities of five poorly water-soluble drugs, diazepam, griseofulvin, progesterone, 17 beta-estradiol, and testosterone, were studied in the presence of nicotinamide. All solubilities were found to increase in a nonlinear fashion as a function of nicotinamide concentration. The K1:1 and K1:2 stability constants were as follows: for diazepam, K1:1 = 5.23 M-1 and K1:2 = 8.6 M-2; for griseofulvin, K1:1 = 5.54 M-1 and K1:2 = 8.82 M-2; for progesterone, K1:1 = 5.48 M-1 and K1:2 = 42.47 M-2; for 17 beta-estradiol, K1:1 = 5.38 M-1 and K1:2 = 36.9 M-2; and for testosterone, K1:1 = 5.07 M-1 and K1:2 = 27.47 M-2. Two aliphatic analogues of nicotinamide (nipecotamide and N,N-dimethylacetamide) were studied as ligands with diazepam and griseofulvin and were found to increase the solubilities of both drugs in a linear fashion. The aromatic analogue, N,N-diethylnicotinamide, showed a nonlinear solubilization relationship similar to that seen with nicotinamide. In addition, three other aromatic analogues (isonicotinamide, 1-methylnicotinamide iodide, and N-methylnicotinamide) were studied. These ligands were not soluble enough in water to be studied over the wide range of concentrations used for nicotinamide and N,N-diethylnicotinamide; however, in the concentration range studied, these ligands solubilized diazepam and griseofulvin to a degree similar to that observed with comparable concentrations of nicotinamide. These results suggest that the aromaticity (Pi-system) of the pyridine ring is an important factor in complexation because the aromatic amide ligands were found to enhance the aqueous solubilities of the test drugs to a greater extent than the aliphatic amide ligands.(ABSTRACT TRUNCATED AT 250 WORDS)
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              Enhanced chartreusin solubility by hydroxybenzoate hydrotropy.

              G.K. Poochikian, J.C. Cradock (1979)
              The apparent aqueous solubility of the water-insoluble cytotoxic agent, chartreusin, was increased at neutral pH in the presence of hydroxybenzoates. Water molecules play an important role in the chartreusin conformation. Studies included solubility and spectral examinations. The weakest and strongest interactants with chartreusin were sodium benzoate and sodium trihydroxybenzoate, respectively, while the effect of mono- and dihydroxybenzoates was intermediate. A plane-to-plane orientation of chartreusin and the ligand molecules brought together by electrostatic and hydrophobic interactions is postulated. The dramatic chartreusin aqueous solubility increase relative to its aglycone, chartarin, under similar conditions was best rationalized by micellization.
              Article 0 comments Cited 13 times – based on 0 reviews     Review now
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                Author and article information

                Journal
                Journal ID (nlm-ta): Iran J Pharm Res
                Journal ID (iso-abbrev): Iran J Pharm Res
                Journal ID (publisher-id): IJPR
                Title: Iranian Journal of Pharmaceutical Research : IJPR
                Publisher: Shaheed Beheshti University of Medical Sciences (Tehran, Iran )
                ISSN (Print): 1735-0328
                ISSN (Electronic): 1726-6890
                Publication date (Print): Summer 2010
                Volume: 9
                Issue: 3
                Pages: 233-242
                Affiliations
                [1] Department of Pharmacy, Shri Govindram Seksaria Institute of Technology and Science, Indore, India.
                Author notes
                [* ]Corresponding author: E-mail: rkrkmaheshwari@yahoo.co.in
                Article
                Publisher ID: ijpr-09-233
                PMC ID: 3863437
                PubMed ID: 24363732
                SO-VID: d4068a35-e850-40a1-bbf9-5bae40d8087e
                Copyright © © 2010 by School of Pharmacy, Shaheed Beheshti University of Medical Sciences and Health Services
                License:

                This is an Open Access article distributed under the terms of the Creative Commons Attribution License, ( http://creativecommons.org/licenses/by/3.0/) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

                History
                Date received : February 2009
                Date accepted : March 2010
                Categories
                Subject: Original Article

                Keywords: mixed-hydrotropy,solubilization,aceclofenac,aqueous injection,urea,sodium citrate,synergistic enhancement
                Data availability:
                Keywords: mixed-hydrotropy, solubilization, aceclofenac, aqueous injection, urea, sodium citrate, synergistic enhancement

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