In vitro and in situ absorption studies of vasicine in rats

H.N.A. Ram, A. Shirwaikar

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

Vasicine is a pyrralazoquinazoline monobasic alkaloid obtained from the plant Adhatoda zeylanica. In the current experiment, we have made an attempt to determine the sites of absorption for the bioactive component vasicine from the various segments of small intestine (duodenum, jejunum and ileum) and colon. Everted intestinal sac method was used to assess the in vitro absorption of vasicine. The absorption of standard vasicine, vasicine from methanol and ethanol extracts of vasaka from the small intestine of rats was studied using the Doluisio technique. Maximum absorption of 87.3±5.256% of vasicine was observed in the duodenal region, whilst the colon showed the minimum absorption of 42.6±7.314%. The jejunum and ileum showed 77.2±3.415% and 46.9±3.271% absorption of vasicine respectively. The luminal disappearance of vasicine by Doluisio technique was determined from the standard curve. Absorption of vasicine was found to be better from the ethanol extract than from the methanol extract. Standard vasicine has revealed steady absorption as evidenced by a typical sigmoidal curve. The absorption rate was found to be of the first order for the tested samples.
Original languageEnglish
Pages (from-to)365-369
Number of pages5
JournalIndian Journal of Pharmaceutical Sciences
Volume69
Issue number3
Publication statusPublished - 2007

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Jejunum
Ileum
Small Intestine
Methanol
Justicia
Colon
Ethanol
In Vitro Techniques
vasicine
Duodenum
Alkaloids

Cite this

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title = "In vitro and in situ absorption studies of vasicine in rats",
abstract = "Vasicine is a pyrralazoquinazoline monobasic alkaloid obtained from the plant Adhatoda zeylanica. In the current experiment, we have made an attempt to determine the sites of absorption for the bioactive component vasicine from the various segments of small intestine (duodenum, jejunum and ileum) and colon. Everted intestinal sac method was used to assess the in vitro absorption of vasicine. The absorption of standard vasicine, vasicine from methanol and ethanol extracts of vasaka from the small intestine of rats was studied using the Doluisio technique. Maximum absorption of 87.3±5.256{\%} of vasicine was observed in the duodenal region, whilst the colon showed the minimum absorption of 42.6±7.314{\%}. The jejunum and ileum showed 77.2±3.415{\%} and 46.9±3.271{\%} absorption of vasicine respectively. The luminal disappearance of vasicine by Doluisio technique was determined from the standard curve. Absorption of vasicine was found to be better from the ethanol extract than from the methanol extract. Standard vasicine has revealed steady absorption as evidenced by a typical sigmoidal curve. The absorption rate was found to be of the first order for the tested samples.",
author = "H.N.A. Ram and A. Shirwaikar",
note = "Cited By :3 Export Date: 10 November 2017 CODEN: IJSID Correspondence Address: Department of Pharmacognosy, Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal - 576 104, India; email: arunshirwaikar@yahoo.co.in Chemicals/CAS: alcohol, 64-17-5; methanol, 67-56-1; vasicine, 6159-55-3 References: The Wealth of India. Publication and Information Directorate, CSIR: New Delhi; 1948; Nadakarni, K.M., (1976) Indian Materia Medica, , Mumbai; Popular Prakashan; Atal, C.K., Chemistry and Pharmacology of Vasicine (1980) Director, RRL: Jammu Tawi; Tukker, J.J., In vitro methods for the assessment of permeability (2000) Oral drug absorption, prediction and assessment, pp. 51-72. , Dressman JB, Lenernas H, editors, New York; Marcel Dekker Inc; Indian Herbal Pharmacopoeia. IDMA and RRL (CSIR): Jammu Tawi; 1998; Kulkarni, S.K., (1999) Hand book of Experimental Pharmacology, , 3rd ed. Delhi; Vallabh Prakashan; Wilson, T.H., Wiseman, G., The use of sacs of everted small intestine for the study of the transference of substances from the mucosal to the serosal surface (1954) J Physiol, 123, pp. 116-125; Yamamoto, A., Kawaratani, T., Kawashima, K., Hashida, M., Sezaki, H., Intestinal transport of sulfanilic acid in rats immunised with protein-sulfanilic acid conjugate (1990) Pharm Res, 7, pp. 767-771; Komiya, I., Park, J.Y., Kamani, A., Ho, N.F., Higuchi, W.I., Quantitative mechanistic studies in simultaneous fluid flow and intestinal absorption using steroids as model solutes (1980) Int J Pharmaceut, 4, pp. 249-262; Lennernas, H., Human jejunal effective permeability and its correlation with preclinical drug absorption models (1997) J Pharm Pharmacol, 49, pp. 627-638; Fagerholm, U., Johansson, M., Lennernas, H., Comparison between permeability coefficients in rats and human jejunum (1996) Pharm Res, 13, pp. 1335-1341; Amidon, G.L., Sinko, P.J., Fleisher, D., Estimating human oral fraction dose absorbed: A correlation using rat intestinal membrane permeability for passive and carrier-mediated compounds (1988) Pharm Res, 5, pp. 651-654; Lennernas, H., Ahrenstedt, O., Hallgren, R., Knutson, L., Ryde, M., Paalzow, L.K., Regional jejunal perfusion, a new in vivo approach to study oral drug absorption in man (1992) Pharm Res, 9, pp. 1243-1251; Lennernas H, Lee ID, Fagerholm U, Amidon GL. A RTD analysis of the hydrodynamics within the human intestine during a regional single-pass perfusion: In vivo permeability estimation. J Pharm Pharmacol 1997;49:682-6; Leppert, P.S., Fix, J.A., Use of everted intestinal rings for in vitro examination of oral absorption potential (1994) J Pharm Sci, 83, pp. 976-981; Pento, J.T., Mousissian, G.K., Time-dependent deterioration of active transport in duodenal segments of rat intestine (1988) J Pharmacol Met, 20, pp. 9-14; Sim, S.M., Back, D.J., Intestinal absorption of oestrone, oestrone glucuronide and oestrone sulphate in the rat in situ - II. Studies with the Doluisio technique (1986) J Steroid Biochem, 24, pp. 1085-1089; Park, J.Y., Ho, N.F., Morozowich, W., Physical model approach to gastrointestinal absorption of prostaglandins II: In situ rat intestinal absorption of dinoprost (1984) J Pharm Sci, 73, pp. 1588-1594; Lennernas, H., Human intestinal permeability: An overview (1998) J Pharm Sci, 87, pp. 403-410; Amidon, G.L., Lennernas, H., Shah, V.P., Crison, J.R., A theoretical basis for a biopharmaceutic drug classification: The correlation of in vitro drug product dissolution and in vivo bioavailability (1995) J Pharm Res, 12, pp. 413-420",
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In vitro and in situ absorption studies of vasicine in rats. / Ram, H.N.A.; Shirwaikar, A.

In: Indian Journal of Pharmaceutical Sciences, Vol. 69, No. 3, 2007, p. 365-369.

Research output: Contribution to journalArticle

TY - JOUR

T1 - In vitro and in situ absorption studies of vasicine in rats

AU - Ram, H.N.A.

AU - Shirwaikar, A.

N1 - Cited By :3 Export Date: 10 November 2017 CODEN: IJSID Correspondence Address: Department of Pharmacognosy, Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal - 576 104, India; email: arunshirwaikar@yahoo.co.in Chemicals/CAS: alcohol, 64-17-5; methanol, 67-56-1; vasicine, 6159-55-3 References: The Wealth of India. Publication and Information Directorate, CSIR: New Delhi; 1948; Nadakarni, K.M., (1976) Indian Materia Medica, , Mumbai; Popular Prakashan; Atal, C.K., Chemistry and Pharmacology of Vasicine (1980) Director, RRL: Jammu Tawi; Tukker, J.J., In vitro methods for the assessment of permeability (2000) Oral drug absorption, prediction and assessment, pp. 51-72. , Dressman JB, Lenernas H, editors, New York; Marcel Dekker Inc; Indian Herbal Pharmacopoeia. IDMA and RRL (CSIR): Jammu Tawi; 1998; Kulkarni, S.K., (1999) Hand book of Experimental Pharmacology, , 3rd ed. Delhi; Vallabh Prakashan; Wilson, T.H., Wiseman, G., The use of sacs of everted small intestine for the study of the transference of substances from the mucosal to the serosal surface (1954) J Physiol, 123, pp. 116-125; Yamamoto, A., Kawaratani, T., Kawashima, K., Hashida, M., Sezaki, H., Intestinal transport of sulfanilic acid in rats immunised with protein-sulfanilic acid conjugate (1990) Pharm Res, 7, pp. 767-771; Komiya, I., Park, J.Y., Kamani, A., Ho, N.F., Higuchi, W.I., Quantitative mechanistic studies in simultaneous fluid flow and intestinal absorption using steroids as model solutes (1980) Int J Pharmaceut, 4, pp. 249-262; Lennernas, H., Human jejunal effective permeability and its correlation with preclinical drug absorption models (1997) J Pharm Pharmacol, 49, pp. 627-638; Fagerholm, U., Johansson, M., Lennernas, H., Comparison between permeability coefficients in rats and human jejunum (1996) Pharm Res, 13, pp. 1335-1341; Amidon, G.L., Sinko, P.J., Fleisher, D., Estimating human oral fraction dose absorbed: A correlation using rat intestinal membrane permeability for passive and carrier-mediated compounds (1988) Pharm Res, 5, pp. 651-654; Lennernas, H., Ahrenstedt, O., Hallgren, R., Knutson, L., Ryde, M., Paalzow, L.K., Regional jejunal perfusion, a new in vivo approach to study oral drug absorption in man (1992) Pharm Res, 9, pp. 1243-1251; Lennernas H, Lee ID, Fagerholm U, Amidon GL. A RTD analysis of the hydrodynamics within the human intestine during a regional single-pass perfusion: In vivo permeability estimation. J Pharm Pharmacol 1997;49:682-6; Leppert, P.S., Fix, J.A., Use of everted intestinal rings for in vitro examination of oral absorption potential (1994) J Pharm Sci, 83, pp. 976-981; Pento, J.T., Mousissian, G.K., Time-dependent deterioration of active transport in duodenal segments of rat intestine (1988) J Pharmacol Met, 20, pp. 9-14; Sim, S.M., Back, D.J., Intestinal absorption of oestrone, oestrone glucuronide and oestrone sulphate in the rat in situ - II. Studies with the Doluisio technique (1986) J Steroid Biochem, 24, pp. 1085-1089; Park, J.Y., Ho, N.F., Morozowich, W., Physical model approach to gastrointestinal absorption of prostaglandins II: In situ rat intestinal absorption of dinoprost (1984) J Pharm Sci, 73, pp. 1588-1594; Lennernas, H., Human intestinal permeability: An overview (1998) J Pharm Sci, 87, pp. 403-410; Amidon, G.L., Lennernas, H., Shah, V.P., Crison, J.R., A theoretical basis for a biopharmaceutic drug classification: The correlation of in vitro drug product dissolution and in vivo bioavailability (1995) J Pharm Res, 12, pp. 413-420

PY - 2007

Y1 - 2007

N2 - Vasicine is a pyrralazoquinazoline monobasic alkaloid obtained from the plant Adhatoda zeylanica. In the current experiment, we have made an attempt to determine the sites of absorption for the bioactive component vasicine from the various segments of small intestine (duodenum, jejunum and ileum) and colon. Everted intestinal sac method was used to assess the in vitro absorption of vasicine. The absorption of standard vasicine, vasicine from methanol and ethanol extracts of vasaka from the small intestine of rats was studied using the Doluisio technique. Maximum absorption of 87.3±5.256% of vasicine was observed in the duodenal region, whilst the colon showed the minimum absorption of 42.6±7.314%. The jejunum and ileum showed 77.2±3.415% and 46.9±3.271% absorption of vasicine respectively. The luminal disappearance of vasicine by Doluisio technique was determined from the standard curve. Absorption of vasicine was found to be better from the ethanol extract than from the methanol extract. Standard vasicine has revealed steady absorption as evidenced by a typical sigmoidal curve. The absorption rate was found to be of the first order for the tested samples.

AB - Vasicine is a pyrralazoquinazoline monobasic alkaloid obtained from the plant Adhatoda zeylanica. In the current experiment, we have made an attempt to determine the sites of absorption for the bioactive component vasicine from the various segments of small intestine (duodenum, jejunum and ileum) and colon. Everted intestinal sac method was used to assess the in vitro absorption of vasicine. The absorption of standard vasicine, vasicine from methanol and ethanol extracts of vasaka from the small intestine of rats was studied using the Doluisio technique. Maximum absorption of 87.3±5.256% of vasicine was observed in the duodenal region, whilst the colon showed the minimum absorption of 42.6±7.314%. The jejunum and ileum showed 77.2±3.415% and 46.9±3.271% absorption of vasicine respectively. The luminal disappearance of vasicine by Doluisio technique was determined from the standard curve. Absorption of vasicine was found to be better from the ethanol extract than from the methanol extract. Standard vasicine has revealed steady absorption as evidenced by a typical sigmoidal curve. The absorption rate was found to be of the first order for the tested samples.

M3 - Article

VL - 69

SP - 365

EP - 369

JO - Indian Journal of Pharmaceutical Sciences

JF - Indian Journal of Pharmaceutical Sciences

SN - 0250-474X

IS - 3

ER -