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      Pharmacokinetic profile of an intradeltoid diclofenac injection in obese Indian volunteers

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          Abstract

          Background

          A new propylene glycol-free and reduced-volume formulation of diclofenac sodium 75 mg/mL designed for intradeltoid administration has been found to be bioequivalent to a reference formulation of diclofenac sodium 75 mg/3 mL given via the intragluteal route in normal healthy volunteers. Standard needles may not reach the gluteus maximus muscle in many cases, especially in the obese. The objective of this study was to determine the pharmacokinetic parameters of the new formulation and compare the bioavailability of intradeltoid diclofenac sodium 75 mg/mL with that of the intragluteal 75 mg/3 mL reference formulation in obese volunteers.

          Methods

          A comparative, two-way, single-dose, bioavailability study was carried out in 10 obese (body mass index > 25) male Indian volunteers after a washout period of seven days. Blood samples were collected until six hours following drug administration and analyzed using a prevalidated high-pressure liquid chromatography method.

          Results

          The mean maximum plasma concentration and time to reach maximum plasma concentration for the test formulation were 1.30 μg/mL and 0.50 hours, respectively, versus 0.93 μg/ mL and 1.08 hours for the reference formulation. The mean areas under the curve from 0 to last measurable time point (AUC 0–t) for the test and reference formulations were 2.71 μg·h/mL and 2.73 μg·h/mL, respectively. The mean AUCs from 0 to infinity (AUC 0–∞) for the test and reference formulations were 3.71 μg·h/mL and 3.75 μg·h/mL, respectively.

          Conclusion

          The results suggest that the test formulation of diclofenac sodium 75 mg/mL has an AUC 0–t and AUC 0–∞ comparable with the reference intragluteal formulation of diclofenac sodium 75 mg/3 mL, but with an earlier time to reach maximum plasma concentration and a trend towards a higher maximum plasma concentration. This could be attributed to faster absorption from the deltoid region than from the gluteal region. The test formulation could be helpful in the management of pain in obese or overweight patients and those with dense subcutaneous fat in the gluteal area.

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          Most cited references 15

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          Nonsteroidal anti-inflammatory drug-induced hepatotoxicity.

          Nonsteroidal anti-inflammatory drugs are among the most common drugs associated with drug-induced liver injury, with an estimated incidence of between 3 and 23 per 100,000 patient years. Nimesulide, sulindac, and diclofenac seem to be associated with the highest risk and the only risk factor consistently identified is the concomitant use of other hepatotoxic drugs. Diclofenac-induced liver injury is a paradigm for drug-related hepatotoxicity. Recent studies suggest that genetic factors favoring the formation and accumulation of the reactive acylglucuronide metabolite of diclofenac and an enhanced immune response to the metabolite-protein adducts are associated with increased susceptibility to hepatotoxicity.
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            Determination of deltoid fat pad thickness. Implications for needle length in adult immunization.

            To measure deltoid fat pad thickness and determine the optimal needle length for deltoid intramuscular immunization in healthy adults. Prospective study of 220 healthy health care workers (126 women, 94 men) at the Mayo Medical Center, Rochester, Minn. Deltoid fat pad thickness determined by high-resolution ultrasound scanning, weight, height, and mid-deltoid arm circumference. We found a highly significant difference between women and men in deltoid fat pad thickness, with women having a thicker deltoid fat pad (11.7 vs 8.3 mm; P<.001). Women had a greater deltoid skin-fold thickness than men (34.7 vs 17.2 mm, P<.001) and an equal body mass index. According to the ultrasound findings, a standard 16-mm (5/8-in) needle would not have reached 5 mm into muscle in 17% (16/94) of men and 48.4% (61/126) of women in this study. Among healthy adults of the age range we studied, the following needle lengths appear to be appropriate for true deltoid intramuscular immunization: For men across the weight ranges we studied (59-118 kg), use of a 25-mm (1-in) needle would result in at least 5 mm of muscle penetration in all subjects. For women who weighed less than 60 kg, a 16-mm (5/8-in) needle would be sufficient to achieve muscle penetration of 5 mm. For women between 60 and 90 kg, a 25-mm (1-in) needle would be sufficient, and women greater than 90 kg would require a 38-mm (1.5-in) needle to ensure intramuscular administration.
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              Intramuscular injections into the buttocks: are they truly intramuscular?

              To radiologically determine if intramuscular (IM) injections into the buttocks are truly intramuscular. This was a prospective study conducted during a 6 month period beginning in October 2004. Fifty inpatients were recruited from a single tertiary referral hospital. Approval was obtained from the hospital research ethics committee and informed written consent was acquired from all participants. Prior to computerised tomography (CT), each patient received an IM injection of their prescribed medication along with 1 mL of air into the upper outer quadrant of the buttocks. CT images were subsequently analyzed by two radiologists to determine the position of the injected air bubble and to assess whether it was intramuscular or subcutaneous in position. Body mass index (BMI), distance to injection site, subcutaneous fat and muscle thickness were also measured. Overall, only 32% (n=16/50) of patients had intramuscular injections, with the majority of injections (68%, n=34/50) being subcutaneous. When analysed by gender, 56% (n=14/25) of males had intramuscular injections while in females, the efficacy rate was significantly lower at 8% (n=2/25). The majority of assumed intramuscular injections are actually subcutaneous.
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                Author and article information

                Journal
                J Pain Res
                Journal of Pain Research
                Journal of Pain Research
                Dove Medical Press
                1178-7090
                2010
                19 November 2010
                : 3
                : 235-240
                Affiliations
                [1 ] Medical Services, Troikaa Pharmaceuticals Ltd, Ahmedabad, India
                [2 ] Department of Bio-analytical, B.V. Patel Pharmaceutical Education and Research Development Centre, Ahmedabad, India
                [3 ] Department of Biostatistics, B.V. Patel Pharmaceutical Education and Research Development Centre, Ahmedabad, India
                [4 ] Department of Pharmacology and Toxicology, B.V. Patel Pharmaceutical Education and Research Development Centre, Ahmedabad, India
                [5 ] Director, B.V. Patel PERD Centre, and Project Director, NI PER, Ahmedabad, India
                Author notes
                Correspondence: Vijaya Jaiswal, Medical Services, Troikaa Pharmaceuticals Ltd., Commerce House-1, Satya Marg, Bodakdev, Ahmedabad 54, India, Tel +917 926 8562 4245, Fax +917 926 8562 4246, Email vijayajaiswal@ 123456troikaapharma.com
                Article
                jpr-3-235
                10.2147/JPR.S13894
                3033031
                21311716
                © 2010 Shep et al, publisher and licensee Dove Medical Press Ltd.

                This is an Open Access article which permits unrestricted noncommercial use, provided the original work is properly cited.

                Categories
                Original Research

                Anesthesiology & Pain management

                intradeltoid, pharmacokinetics, diclofenac, obese, bioavailability

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