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ARTICLES
Year : 1979  |  Volume : 27  |  Issue : 4  |  Page : 61-65

Ocular penetration of hydrocortisone and dexamethasone in aqueous humour after subconjunctival injection


R.N.T. Medical College, Udaipur, India

Correspondence Address:
M R Jain
Professor of Ophthalmology, R.N.T. Medical College, Udaipur
India
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Source of Support: None, Conflict of Interest: None


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How to cite this article:
Jain M R, Srivastava S. Ocular penetration of hydrocortisone and dexamethasone in aqueous humour after subconjunctival injection. Indian J Ophthalmol 1979;27:61-5

How to cite this URL:
Jain M R, Srivastava S. Ocular penetration of hydrocortisone and dexamethasone in aqueous humour after subconjunctival injection. Indian J Ophthalmol [serial online] 1979 [cited 2020 Nov 30];27:61-5. Available from: https://www.ijo.in/text.asp?1979/27/4/61/32578

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Table 1

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Table 1

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The study was undertaken to estimate the time and quantity of intraocular penetration of hydrocortisone acetate and dexamethasone sodium phosphate as estimated in human aqueous. Though these are widely used steroids in ocular inflammations the literature is practi­cally silent on such studies in human subject.


  Materials and Methods Top


125 cases of uncomplicated cataract were selected for this study and divided into following three groups.­

Group I-Comprised 20 cases in which double blind study was conducted by injecting subconjunctivally normal saline in 10 cases, hydrocortisone acetate in 5 cases and dcxamethasone sodium phosphate in 5 cases.

Group II:-Comprised 70 cases (including 5 cases of double blind study). In these cases 0.5 ml. of 2.5 per cent hydiecortisone acetate (Wycort) was injected subconjurctivally. This group was subdivided into 7 sub groups. Each subgroup consisted of 10 separate cases in which aqueous was collected after 10, 20, 30, 60, minutes, 24 hours; 3 days and 7 days following the subccnjunctival injection.

Group III:- Comprised 45 cases (including 5 cases of double blind study). In these cases 0.5 ml, of 0.4 percent dexamethasone sodium phosphate (Dexona) was injected subconjunctivally. The group was sub­divided into 5 subgroups. First 4 subgroups considered of 10 separate cases in which aqueous was collected after 10, 20, 3o and 60 minutes following subccnjunctival injection. Fifth sub group had 5 separate cases in which aqueous was collected 24 hours after the conjunctival injection.

After subconjunctivai injections of 0.5 ml. of steroids, aqueous samples of 0,1 to 0.2 ml. were collec­ted at various time intervals, mostly at the time of cataract operation.

These samples were mixed with ethanol (for hydrocortisone) or methanol (for dexamethasone) to make I ml. of solution. The samples were stored in the refrigerator at 4 centigrade till they were estimated.

For estimation purposes-a Systronics type 103 spectrocalorimeter which provided continuouly variable wave length of 400 to 700 mm. was used.

Hydrocortisone acetate estimation was done at the wave length of 650 nm by the method of Pesez and Robin[13] and dexametbasone sodium phosphate at the wave length of 410 nm. by method of Porter and Silber[12] modified by Lewbart and Mattox[9].

Observations

Average age in group II was 59.87 years with a range of 36 to 79 years, while in group III the average age was 59.57 years with a range of 40. to 70 years. The maximum number of cases belonged to age group of 60 to 69 years in both the groups. In group II, the male and female ratio was 3.25: 1.125 and in group 111, the male and female ratio was 4:5. None of the control case (group 1) showed presence of steroids. Group II results are shown in [Table - 1] and [Figure - 1]. Peak con­centration of 214.39 ug/ml. of Hydrocortisone acetate was noted at 10 minutes interval. Subsquently, it shows gradual decline from the peak level to 131.75 microgram/ ml. in 20 minutes and 117.24 microgram/ml. in 30 minutes. After 30 minutes there were no signifincant variations in the concentration of hydrocortisone in the aqueous humor upto 24 hours (103.84 microgram/ml). Then it gradually declined to 63.41 ug/ml. in 3 days. Seventh day sample indicated the presence of hydrocorti­sone acetate in aqueous humor to the extent of 20.54 ug/ml.

[Table - 2] and [Figure - 2] shows that dexamethasone sodium phosphate also attained peak level with in 10 minutes with conentration of 268 ug/ml. Subsequently there is a gradual fall in concentration to 238.20 ug/ml. at 20 minutes. 220.00 ug/ml. at 30 minutes and 179.00 ug/mI. at 60 minutes. At the end of 24 hours, the concentration was reduced markedly to 123.00 ug/mI. [Figure - 3] shows the comparative concentration of hydrocortisone and dexamethasone.


  Discussion Top


Distinct advantage of subconjunctivally injected corticosteroids as compared to topical and parentral therapy have been amply demons­trated in the clinical and experimental work done by (2, 10, ) and many other workers.

Some how, none of the earlier worker has tried to estimate steroid in normal human aqueous though its presence in rabbit's aqueous in quantities varying from 0.018 to 0.4 ug/ml. have been demonstrated by[8],[4]. Our double blind study in normal human being has demonstrated complete absence of steroids in human aqueous.

Hydrocortisone

Penetration of topically instilled hydrocor­tisone has been studied by[7] where they noted maximum concentration of 2 ug/ml. and by[3]. Who noted varying concentration of 6 to 30 ug/ml. in the rabbit aqueous. Isolated signi­ficant study is available where Wine et al[16] used radioactive hydrocortisone (C14 hydro­cortisone) in rabbit eyes and noted its concen­tration in the eye to be 176.7 ug/ml. in 30 minutes after the subconjunctival injection in rabbit eye. While comparing the results, we observed that we recorded maximum concentra­tion of 213.30 ug/ml. of aqueous within 10 minutes. The concentration declined rapidly within another 10 minutes 131.75 ug/ml). but thereafter declined gradually till it maintained concentration of 103.84 ug/ml. upto 24 hours. Seventh day sample also showed steroid concen­tration of 20.54 ug/ml. Rodger[14] has stated that therapeutic active steroid may last in subconjunctival space upto 3 weeks but whether it is sufficient to provide therapeutic active concentration in aqueous is not stated. Crystal­loid deposit under the conjunctiva after subcon­junctival injection was noticed by us for 2 to 4 weeks.

Dexamethasone

Clinical effectiveness of dexamethasone in the form of subconjunctival injection has been recognised by various workers (Gordon,[1],­Neelsen,[11]) and is thought to be due to better penetration of the drug. But some how not even a single study is reported where dexa­methasone concentration in human aqueous has been estimated after its subconjunctival injection. Studies of estimation conducted mostly by radio­active counting after topical instillation of drops reveal varying strength from nil to 4.27 ug/ml. of aqueous in rabbit eyes (Shert et al, [15] Kupferman et al,[5] and Krupin,[6]) when :compared, our results show remarkably high concentration of the drug with maximum concentration of 268.0 ug/ml. within 10 minutes; 239.20 ug/ml. within 20 minutes and 179.0 ug/ml. within 60 minutes. Interestingly a significantly high concentration of 123.0 ug/ml. was noticed even at the interval of 24 hours.

Normal anti-inflammatory activity of dexamethasone is 25 times that of hydrocorti­sone. But clinical effectiveness of dexamethasone becomes far more intensified due to its better penetration. Our results indicate that in bet­ween 20 to 30 minutes dexamethasone becomes 47 times more effective than hydrocortisone and within 24 hours the effectiveness of dexamethas­one varies from 29.5 to 47 times.


  Summary Top


125 eyes of either sex undergoing cataract surgery were studied for steroid concentration in aqueous at various time intervals by calorimetric technique after subconjunctival injections. Steroids used were 0.5 ml. of 2.5 percent hydro­cortisone acetate (Wycort)and 0.5 ml. of 0.4 percent of dexamethasone sodium phosphate (Dexona). Both steroids attained maximum con­centration within 10 minutes and it was 214.39 ug/ml. and 268.0 ug/ml. respectively. Clinical effectiveness of dexamethasone within 24 hours of subconjunctival injection varied from 29.5 to 47 times more than hydrocortisone.


  Acknowledgement Top


We are extremly thankful to John Wyeth laboratory for the liberal supply of wycort and Cadila laboratories for the supply of dexona.

 
  References Top

1.
Gordan, D. M., 1959, Afner. J. Ophthal., 48, 656.  Back to cited text no. 1
    
2.
Hogan, M.J., Thygeson, P. and Kimura, S., 1955, Arch, Ophthal., 53, l65.  Back to cited text no. 2
    
3.
Hamashige, B.S. and Potts, A.M. 1955, Amer. Jour. Ophthal., 40, 211.  Back to cited text no. 3
    
4.
Kircher, H. 1963, 'Klin. Mbl. Augenheilk', 143, 264, Cited in International Ophthalmology clinics 6, 4, 1966.  Back to cited text no. 4
    
5.
Kupferman, A. and Leibowitz, H.M, 1974, Arch. Jour Ophthal., 91, 373.  Back to cited text no. 5
    
6.
Krupin, T., Waltman, S.R. and Becker, 1974, Arch. Ophthal., 92, (4), 312.  Back to cited text no. 6
    
7.
Leopold and Weimer, 1954, Arch. Ophthal., 52, 769.  Back to cited text no. 7
    
8.
Leopold and Green, 1965, Amer. M, and Aesoe Arch. Ophthal., 54, 916,  Back to cited text no. 8
    
9.
Lewart and Mattox, 1964, Jour. Org. Chem., 29, 513, Cited in book of calorimetric and fluori­metric analysis of organic compounds and drugs (Steroids) by Pesez and Bartos 1, 505, 1974.  Back to cited text no. 9
    
10.
McDonald, P.R, Leopold, I.H. Vogal, A.W., and Mulberger, R.D. 1953, Amer. and Assoc. Arch. J. Ophthal.; 49, 400.  Back to cited text no. 10
    
11.
Neelson, R. H., 1959, Arch. Ophthal.. 62, 118.  Back to cited text no. 11
    
12.
Porter, C.C. and Silber, R.H., 1950, Jour. Bio. Chem. 185, 201, Cited in book of Colorimetric and fluorimetic analysis of organic compounds and drugs (Steroids)-Pesez and Bartos, 505. Vol. 1, 1974.  Back to cited text no. 12
    
13.
Pesez, M. and Robin, J., 1959, Ann. Pharm. Pr. 17, 627, Cited in the book of colorimetric and fluorimetric analysis of organic compounds and drugs (Steroids)-Pesez and Bartos, 501.503, Vol. I. 1974.  Back to cited text no. 13
    
14.
Rodger, P.C. 1965, Brit. J. Ophthal , 49, 218.  Back to cited text no. 14
    
15.
Shert et al, 1966, Amer. and Assoc. Arch. Ophthal., 75, 689.  Back to cited text no. 15
    
16.
Wine, N.A., Gornal, A.G., and Basu, P.K., 1964, Amer. J. Ophthal., 58, 362.  Back to cited text no. 16
    


    Figures

  [Figure - 1], [Figure - 2], [Figure - 3]
 
 
    Tables

  [Table - 1], [Table - 2]



 

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