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. 2005 Sep 22;7(1):E38–E42. doi: 10.1208/pt070106

In vivo characterization of monolithic matrix type transdermal drug delivery systems of pinacidil monohydrate: A technical note

Mohd Aqil 1,✉, Asgar Ali 1, Yasmin Sultana 2, Kiran Dubey 2, Abul K Najmi 2, Kollapa K Pillai 2
PMCID: PMC2750713  PMID: 16584165

Summary and Conclusions

The present work aimed to characterize transdermal drug delivery systems of pinacidil monohydrate in vivo by monitoring the effect of the TDDS on blood pressure of methyl prednisolone acetate induced hypertensive rats. The blood pressure of rats was measured using a noninvasive rat BP instrument based on cuff tail technique. A significant fall in rat BP (P<.01) was observed in treatment of hypertensive rats with all the formulations, which was maintained for 48 hours. Interformulation comparison revealed that formulation B-4 was the most effective with 37.96% reduction in BP (160.33±4.96 vs 99.44±4.46 mmHg). It was concluded that a single patch application of pinacidil TDDS (B-4) can effectively control hypertension in rats for 2 days. The system holds promise for clinical studies.

Keywords: hypertension, transdermal drug delivery system, methylprednisolone acetate, rat, pinacidil

Full Text

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Footnotes

Publised: January 13, 2006

References

  • 1.Ishii R, Tagawa T, Ishida T, Naruse T. Antihypertensive effects of a new TDS of clonidine in genetic and experimental rats. Arzneimittelforschung. 1996;46:261–268. [PubMed] [Google Scholar]
  • 2.Corbo M, Liu JC, Chien YW. Transdermal controlled delivery of propranolol from a multilaminate adhesive device. Pharm Res. 1989;6:753–758. doi: 10.1023/A:1015967329033. [DOI] [PubMed] [Google Scholar]
  • 3.Kommuru TR, Khan MA, Reddy TK. Effect of chiral enhancers on the permeability of optically active and racemic metoprolol across hairless mouse skin. Chirality. 1999;11:536–540. doi: 10.1002/(SICI)1520-636X(1999)11:7<536::AID-CHIR4>3.0.CO;2-H. [DOI] [PubMed] [Google Scholar]
  • 4.Aqil M, Sultana Y, Ali A. Monolithic matrix type transdermal drug delivery systems of metoprolol tartrate: in-vitro characterization. Acta Pharm. 2003;53:119–126. [PubMed] [Google Scholar]
  • 5.Spieker C, Vetter H, Liedtke R, Zidek W, Vetter W. Transdermal beta-blocker therapy in essential hypertension. Am J Hypertens. 1988;1:199S–200S. doi: 10.1093/ajh/1.3.199s. [DOI] [PubMed] [Google Scholar]
  • 6.Shah HS, Tojo K, Chien YW. Transdermal controlled delivery of verapamil: characterization of in vitro skin permeation. Int J Pharm. 1992;86:167–173. doi: 10.1016/0378-5173(92)90194-7. [DOI] [Google Scholar]
  • 7.Dubey BK. Lypophilzed aqueous-based polymer matrices for transdermal delivery of captopril. J Dermatol Sci. 1995;10:191–195. doi: 10.1016/0923-1811(95)00403-F. [DOI] [PubMed] [Google Scholar]
  • 8.Rao PR, Diwan PV. Formulation and in vitro evaluation of polymeric films of diltiazem hydrochloride and indomethacin for transdermal administration. Drug Dev Ind Pharm. 1998;24:327–336. doi: 10.3109/03639049809085627. [DOI] [PubMed] [Google Scholar]
  • 9.Thacharodi D, Rao KP. Transdermal absorption of nifedipine from microemulsions of lipophillic skin penetration enhancers. Int J Pharm. 1994;111:235–240. doi: 10.1016/0378-5173(94)90346-8. [DOI] [Google Scholar]
  • 10.Aqil M, Ali A. Effect of penetration enhancers on transdermal delivery of pinacidil monohydrate. J Sci Pharm. 2002;3:68–71. [Google Scholar]
  • 11.McBurney A, Farrow PR, Ainsworth S, Ward JW. Serum concentrations and urinary excretion of pinacidil and its major metabolite, pinacidil pyridine-N-oxide following iv and oral administration in healthy volunteers. Br J Clin Pharmacol. 1985;19:91–94. doi: 10.1111/j.1365-2125.1985.tb02618.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  • 12.Dollery C. Pinacidil Monohydrate (monograph) New York, NY: Churchill Livingstone; 1991. pp. 115–118. [Google Scholar]
  • 13.Aqil M, Ali A. Monolithic matrix type transdermal drug delivery systems of pinacidil monohydrate: in-vitro characterization. Eur J Pharm Biopharm. 2002;54:161–164. doi: 10.1016/S0939-6411(02)00059-0. [DOI] [PubMed] [Google Scholar]
  • 14.Krakoff LR, Selvadurai R, Sytter E. Effect of methylprednisolone upon arterial pressure and the renin angiotensin system in the rat. Am J Physiol. 1975;228:613–617. doi: 10.1152/ajplegacy.1975.228.2.613. [DOI] [PubMed] [Google Scholar]
  • 15.Plotz C, Knowlton A, Ragan C. The nature and history of Cushing’s syndrome. Am J Med. 1952;13:597–611. doi: 10.1016/0002-9343(52)90027-2. [DOI] [PubMed] [Google Scholar]
  • 16.Soffer LJ, Iannaccone A, Gabrilove JL. Cushing’s syndrome: a study of 50 patients. Am J Med. 1961;30:129–134. doi: 10.1016/0002-9343(61)90069-9. [DOI] [Google Scholar]
  • 17.David DS, Grieco MH, Cushman P. Adrenal glucocorticoids after 20 years: a review of their clinically relevant consequences. J Chronic Dis. 1970;22:637–648. doi: 10.1016/0021-9681(70)90078-0. [DOI] [PubMed] [Google Scholar]
  • 18.Ragan C. Corticotrophin, cortisone and related steroids in clinical medicine practical considerations. Bull-N. Acad Med. 1973;29:355–364. [PMC free article] [PubMed] [Google Scholar]
  • 19.Kotiyan PN, Vavia PR. Eudragits: role as crystallization inhibitors in drug-in-adhesive transdermal systems of estradiol. Eur J Pharm Biopharm. 2001;52:173–180. doi: 10.1016/S0939-6411(01)00174-6. [DOI] [PubMed] [Google Scholar]
  • 20.Rao PR, Reddy MN, Ramakrishna S, Diwan PV. Comparative in vivo evaluation of propranolol hydrochloride after oral and transdermal administration in rabbits. Eur J Pharm Biopharm. 2003;56:81–85. doi: 10.1016/S0939-6411(03)00038-9. [DOI] [PubMed] [Google Scholar]
  • 21.Guyot M, Fawaz F. Design and in vitro evaluation of adhesive matrix for transdermal delivery of propranolol. Int J Pharm. 2000;204:171–182. doi: 10.1016/S0378-5173(00)00494-4. [DOI] [PubMed] [Google Scholar]
  • 22.Mei Z, Chen H, Weng T, Yang Y, Yang X. Solid lipid nanoparticle and microemulasion for topical delivery of triptolide. Eur J Pharm Biopharm. 2003;56:189–196. doi: 10.1016/S0939-6411(03)00067-5. [DOI] [PubMed] [Google Scholar]
  • 23.Yoneto K, Ghanem AH, Higuchi WI, Peck KD, Li SK. Mechanistic studies of the 1-alkyl-2-pyrrolidones as skin permeation enhancers. J Pharm Sci. 1995;84:312–317. doi: 10.1002/jps.2600840310. [DOI] [PubMed] [Google Scholar]
  • 24.Yoneto K, Li SK, Higuchi WI, Shimabayashi S. Influence of the permeation enhancers 1-alkyl-2-pyrrolidones on permeant partitioning into the stratum corneum. J Pharm Sci. 1998;87:209–214. doi: 10.1021/js970190k. [DOI] [PubMed] [Google Scholar]

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