Design and Evaluation of Rectal Suppositories of Carvedilol

DOI:

https://doi.org/10.37285/ijpsn.2009.2.3.9

Authors

  • P. V. Swamy
  • Laeeq Farhana
  • S. B. Shirsand
  • Md.Younus Ali
  • Ashokgoud Patil

Abstract

Carvedilol (non-cardio selective b-blocker) is an antihypertensive used in management of hypertension, angina pectoris and heart failure.  But its oral bioavailability is about 25-35% only due to significant degree of first pass metabolism.  It has gastrointestinal side effects such as diarrhea, gastric pain and irritation.  Hence, rectal suppositories of carvedilol were developed by using different water-soluble polymeric bases like gelatin and agar-agar using propylene glycol as plasticizer. The gelatin suppositories were disintegrating/dissolving type while gelatin–agar based suppositories were non-disintegrating/non-melting. All the formulations were evaluated for various physical parameters like weight variation,  drug content uniformity, liquefaction time, micro-melting range, in vitro dissolution, short-term stability and drug-excipient interaction (FTIR).  The mechanism of drug release was diffusion controlled and follows first order kinetics in majority of cases. The results suggested that when gelatin is replaced up to 25% w/w with agar, liquefaction time and drug release were not appreciably affected; higher proportions of agar exhibited incomplete and slow release.  Stability studies conducted at 25±3º C and 60±5% relative humidity for three months indicated that the formulations were stable in the drug-content and in vitro drug release rate (p<0.05).

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Keywords:

Carvedilol, rectal suppository, melting/ non-melting, gelatin, agar-agar

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Published

2009-11-30

How to Cite

1.
Swamy PV, Farhana L, Shirsand SB, Ali M, Patil A. Design and Evaluation of Rectal Suppositories of Carvedilol. Scopus Indexed [Internet]. 2009 Nov. 30 [cited 2024 Jun. 16];2(3):654-60. Available from: https://www.ijpsnonline.com/index.php/ijpsn/article/view/636

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Section

Research Articles

References

Basvaraj BV and Nanjundaswamy NG. 2005. Formulation and evaluation of paracetamol suppositories adapting various bases and adjuvants. Indian Drugs, 42(5): 305-8 (2005).

Carter SJ. Cooper and Gunn’s Dispensing for Pharmaceutical Students, 12th edition, CBS Publishers, New Delhi, 2008. pp. 232-52.

Coben LJ and Lieberman HA. Suppositories. In: Lachman L, Lieberman HA and Kanig JL (eds.), Theory and Practice of Industrial Pharmacy, 3rd edition, Varghese Publishing House, Mumbai, 1989. p. 580.

Coben LJ and Lieberman HA. Suppositories. In: Lachman L, Lieberman HA and Kanig JL (eds.), Theory and Practice of Industrial Pharmacy, 3rd edition, Varghese Publishing House, Mumbai, 1989. p. 586.

Gowthamrajan K, Giriraj Kulkarni T, Venkateswaran G, Samanta MK and Suresh B. Formulation and dissolution of meloxicam solid dispersion incorporated suppositories. Indian J. Pharm. Sci. 64(6): 525-28 (2002).

Hermann TW. Recent research on bioavailability of drugs from suppositories. Int. J. Pharm. 123: 1-11 (1995).

Indian Pharmacopoeia. 1996. vol II, 4th edition. Controller of Publications, Ministry of Health and Family Welfare, Govt of India, New Delhi, p. 572.

Jawahar N, Jayaprakash S, Maria GRNS, Nagarajan M, Dhachina Moorthi D, Jubie S and Manivannan R. Design and evaluation of sustained release suppositories of nimesulide. Indian J. Pharm. Sci. 67(5): 558-61 (2005).

Rawlins EA. Bentley’s Text Book of Pharmaceutics, 8th edition, All India Traveler Book Seller, Delhi, 2002, pp. 347-50.

Rytting JH and Fix JA. Suppositories. In: James Swarbrick and Boylan JC (eds.), Encyclopedia of pharmaceutical technology, vol I, 2nd edition, Marcel Dekker Inc, New York, 2002, pp. 932-43.

Svein Oie and Leslie ZB. The effect of route of administration and distribution on drug action. In: Banker GS and Rhodes CT (eds.), Modern Pharmaceutics. 3rd edition, Marcel Dekker Inc, New York, 1996, p.167.

Sweetman SC (ed.), Martindale: The Complete Drug Reference, 33rd edition, Pharmaceutical Press, London,2002, p. 855.