Design and evaluation of matrix diffusion controlled transdermal patches of Diltiazem hydrochloride

S.L. Prabu, A. Shirwaikar, A. Shirwaikar, A. Kumar, A. Jacob

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

A matrix dispersion type transdermal drug delivery system of Diltiazem Hydrochloride was developed using different ratios of rosin with Eudragit RL PM and polyvinyl pyrrolidone. The patch prepared by the combination of rosin and polyvinyl pyrrolidone was not transparent one, and shows an uneven distribution of polyvinyl pyrrolidone, which may be due to the hydrophilic nature of polyvinyl pyrrolidone. The effect of the polymers on the technological properties, i.e., drug release, water vapor transmission rate, percentage moisture loss and thickness were investigated. The patch containing rosin: Eudragit RL PM (6:4) showed a release of 2651 mcg in 24 h. In order to improve the release various proportions of camphor was included in the formulation. The patch containing rosin: Eudragit RL PM (6:4) with 5% w/v of camphor showed a sustained release of the drug extending over a period of 24 h. Formulation F8 emerged as the most satisfactory formulation as far as the technological properties were concerned. Further skin permeation and skin irritation studies were carried out on rat skin and rabbit respectively. Therefore it can be concluded that the patch containing rosin: Eudragit RL PM in the ratio 6:4 with 5%w/v of camphor achieved the desired objectives of transdermal drug delivery systems, such as overcoming of first pass effect, extended release and reduced frequency of administration.
Original languageEnglish
Pages (from-to)211-227
Number of pages17
JournalArs Pharmaceutica
Volume49
Issue number3
Publication statusPublished - 2008

Fingerprint

Transdermal Patch
Diltiazem
Polyvinyls
Pyrrolidinones
Camphor
Drug Delivery Systems
Skin
Steam
Polymers
rosin
Drugs
Controlled
Evaluation
Rabbits
Eudragit RL

Cite this

Prabu, S. L., Shirwaikar, A., Shirwaikar, A., Kumar, A., & Jacob, A. (2008). Design and evaluation of matrix diffusion controlled transdermal patches of Diltiazem hydrochloride. Ars Pharmaceutica, 49(3), 211-227.
Prabu, S.L. ; Shirwaikar, A. ; Shirwaikar, A. ; Kumar, A. ; Jacob, A. / Design and evaluation of matrix diffusion controlled transdermal patches of Diltiazem hydrochloride. In: Ars Pharmaceutica. 2008 ; Vol. 49, No. 3. pp. 211-227.
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title = "Design and evaluation of matrix diffusion controlled transdermal patches of Diltiazem hydrochloride",
abstract = "A matrix dispersion type transdermal drug delivery system of Diltiazem Hydrochloride was developed using different ratios of rosin with Eudragit RL PM and polyvinyl pyrrolidone. The patch prepared by the combination of rosin and polyvinyl pyrrolidone was not transparent one, and shows an uneven distribution of polyvinyl pyrrolidone, which may be due to the hydrophilic nature of polyvinyl pyrrolidone. The effect of the polymers on the technological properties, i.e., drug release, water vapor transmission rate, percentage moisture loss and thickness were investigated. The patch containing rosin: Eudragit RL PM (6:4) showed a release of 2651 mcg in 24 h. In order to improve the release various proportions of camphor was included in the formulation. The patch containing rosin: Eudragit RL PM (6:4) with 5{\%} w/v of camphor showed a sustained release of the drug extending over a period of 24 h. Formulation F8 emerged as the most satisfactory formulation as far as the technological properties were concerned. Further skin permeation and skin irritation studies were carried out on rat skin and rabbit respectively. Therefore it can be concluded that the patch containing rosin: Eudragit RL PM in the ratio 6:4 with 5{\%}w/v of camphor achieved the desired objectives of transdermal drug delivery systems, such as overcoming of first pass effect, extended release and reduced frequency of administration.",
author = "S.L. Prabu and A. Shirwaikar and A. Shirwaikar and A. Kumar and A. Jacob",
note = "Cited By :4 Export Date: 10 November 2017 Correspondence Address: Prabu, S. L.; Dept. of Pharmaceutical Quality Assurance, Manipal College of Pharmaceutical Sciences, Manipal University, Madhav Nagar, Manipal - 576 104, Karnataka, India; email: slaxmanvel@gmail.com Chemicals/CAS: camphor, 464-49-3, 76-22-2, 8008-51-3; diltiazem, 33286-22-5, 42399-41-7; eudragit, 24938-16-7, 51822-44-7, 9065-11-6; povidone, 9003-39-8; rosin, 8050-09-7 Tradenames: eudragit rl pm, Roehm Pharma, Germany Manufacturers: Roehm Pharma, Germany; SD, India; Torrent, India; yucca enterprises References: Ghosh, T.K., Pfister, W.F., Transdermal and Topical Delivery Systems: An overview and future trends (1997) Transdermal and Topical Drug Delivery Systems, pp. 1-32. , Ghosh TK, Pfister WF ed, CRC Press, Boca Raton, FL; Verma, P.R.P., Iyer, S.S., Transdermal delivery of propranolol using mixed grades of Eudragit: Design and in vitro and in vivo evaluation (2000) Drug Dev Ind Pharm, 26 (4), pp. 471-476; Hadgraft, J., Guy, R.H., Selection of drug candidates for transdermal delivery (1989) Transdermal Drug Delivery, pp. 60-120. , 1st ed, Marcel Dekker Inc, New York; Devi, V.K., Saisivam, S., Maria, G.R., Deepti, P.U., Design and evaluation of matrix diffusion controlled transdermal patches of verapamil hydrochloride (2003) Drug Dev Ind Pharm, 29 (5), pp. 495-503; Chaffman, M., Brogden, R.N., Diltiazem: A review of its pharmacological properties and therapeutic efficacy (1985) Drugs, 29 (5), pp. 387-454; Kim, H., Fassihi, R., New ternary polymeric matrix system for control drug delivery of highly soluble drugs (1997) Pharm Res, 14, pp. 1415-1421; Sheorey, D.S., Dorle, A.K., Preparation and study of release kinetics of rosin pentaerythritol ester microcapsules (1994) J. Microen, 11 (1), pp. 11-17; Shirwaikar AA, Reddy N. Rosin, a polymer for micro encapsulation of Diltiazem Hydrochloride for sustained release by emulsion solvent evaporation technique. Ind J Pharm Sci 2000; 62(4): 308-310; Pathak, Y.V., Dorle, A.K., Rosin and rosin derivatives as hydrophobic matrix materials for controlled release of drugs (1990) Drug Dev Ind Pharm, 6 (3), pp. 223-227; Ramani, C.C., Puranik, P.K., Dorle, A.K., Study of maleoabietic acid as matrix forming material (1996) Int J Pharm, 1, pp. 344-352; Satturwar, P.M., Fulzele, S.V., Mandaogade, P.M., Mundhada, D.R., Gogte, B.B., Dorle, A.K., Evaluation of new rosin derivative for pharmaceutical coating (2004) Int J Pharm, 270 (1-2), pp. 27-36; Fulzele, S.V., Satturwar, P.M., Dorle, A.K., Polymerized rosin: Novel film forming polymer for drug delivery (2002) Int. J. Pharm, 249 (1-2), pp. 175-184; Satturwar, P.M., Fulzele, S.V., Dorle, A.K., Evaluation of polymerized rosin for the formulationand evelopment of transdermal drug delivery system. A technical note (2005) AAPSPharmSciTech, 6 (4), p. 81. , article; Balestrieri, F., Magri, A.D., Magri, A.L., Marini, D., Sacchini, A., Application of differential scanning calorimetry to the study of drug-excipient compatibility (1996) Thermochimica Acta, 285, pp. 337-345; British Pharmacopoeia (1996) Addendum 1996, p. 1761. , British Pharmacopoeia Commission, London, UK: British Pharmacopoeia Commission;; Rao PR, Ramakrishna S, Diwan PV. Drug release kinetics from polymeric films containing propranolol hydrochloride for transdermal use. Pharm Dev Techno 2000; l5: 465-472UR - https://www.scopus.com/inward/record.uri?eid=2-s2.0-58949097899&partnerID=40&md5=7f1408de6177379491ae4f1486bef337",
year = "2008",
language = "English",
volume = "49",
pages = "211--227",
journal = "Ars Pharmaceutica",
issn = "0004-2927",
publisher = "Editorial Universida de Granada",
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}

Prabu, SL, Shirwaikar, A, Shirwaikar, A, Kumar, A & Jacob, A 2008, 'Design and evaluation of matrix diffusion controlled transdermal patches of Diltiazem hydrochloride', Ars Pharmaceutica, vol. 49, no. 3, pp. 211-227.

Design and evaluation of matrix diffusion controlled transdermal patches of Diltiazem hydrochloride. / Prabu, S.L.; Shirwaikar, A.; Shirwaikar, A.; Kumar, A.; Jacob, A.

In: Ars Pharmaceutica, Vol. 49, No. 3, 2008, p. 211-227.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Design and evaluation of matrix diffusion controlled transdermal patches of Diltiazem hydrochloride

AU - Prabu, S.L.

AU - Shirwaikar, A.

AU - Shirwaikar, A.

AU - Kumar, A.

AU - Jacob, A.

N1 - Cited By :4 Export Date: 10 November 2017 Correspondence Address: Prabu, S. L.; Dept. of Pharmaceutical Quality Assurance, Manipal College of Pharmaceutical Sciences, Manipal University, Madhav Nagar, Manipal - 576 104, Karnataka, India; email: slaxmanvel@gmail.com Chemicals/CAS: camphor, 464-49-3, 76-22-2, 8008-51-3; diltiazem, 33286-22-5, 42399-41-7; eudragit, 24938-16-7, 51822-44-7, 9065-11-6; povidone, 9003-39-8; rosin, 8050-09-7 Tradenames: eudragit rl pm, Roehm Pharma, Germany Manufacturers: Roehm Pharma, Germany; SD, India; Torrent, India; yucca enterprises References: Ghosh, T.K., Pfister, W.F., Transdermal and Topical Delivery Systems: An overview and future trends (1997) Transdermal and Topical Drug Delivery Systems, pp. 1-32. , Ghosh TK, Pfister WF ed, CRC Press, Boca Raton, FL; Verma, P.R.P., Iyer, S.S., Transdermal delivery of propranolol using mixed grades of Eudragit: Design and in vitro and in vivo evaluation (2000) Drug Dev Ind Pharm, 26 (4), pp. 471-476; Hadgraft, J., Guy, R.H., Selection of drug candidates for transdermal delivery (1989) Transdermal Drug Delivery, pp. 60-120. , 1st ed, Marcel Dekker Inc, New York; Devi, V.K., Saisivam, S., Maria, G.R., Deepti, P.U., Design and evaluation of matrix diffusion controlled transdermal patches of verapamil hydrochloride (2003) Drug Dev Ind Pharm, 29 (5), pp. 495-503; Chaffman, M., Brogden, R.N., Diltiazem: A review of its pharmacological properties and therapeutic efficacy (1985) Drugs, 29 (5), pp. 387-454; Kim, H., Fassihi, R., New ternary polymeric matrix system for control drug delivery of highly soluble drugs (1997) Pharm Res, 14, pp. 1415-1421; Sheorey, D.S., Dorle, A.K., Preparation and study of release kinetics of rosin pentaerythritol ester microcapsules (1994) J. Microen, 11 (1), pp. 11-17; Shirwaikar AA, Reddy N. Rosin, a polymer for micro encapsulation of Diltiazem Hydrochloride for sustained release by emulsion solvent evaporation technique. Ind J Pharm Sci 2000; 62(4): 308-310; Pathak, Y.V., Dorle, A.K., Rosin and rosin derivatives as hydrophobic matrix materials for controlled release of drugs (1990) Drug Dev Ind Pharm, 6 (3), pp. 223-227; Ramani, C.C., Puranik, P.K., Dorle, A.K., Study of maleoabietic acid as matrix forming material (1996) Int J Pharm, 1, pp. 344-352; Satturwar, P.M., Fulzele, S.V., Mandaogade, P.M., Mundhada, D.R., Gogte, B.B., Dorle, A.K., Evaluation of new rosin derivative for pharmaceutical coating (2004) Int J Pharm, 270 (1-2), pp. 27-36; Fulzele, S.V., Satturwar, P.M., Dorle, A.K., Polymerized rosin: Novel film forming polymer for drug delivery (2002) Int. J. Pharm, 249 (1-2), pp. 175-184; Satturwar, P.M., Fulzele, S.V., Dorle, A.K., Evaluation of polymerized rosin for the formulationand evelopment of transdermal drug delivery system. A technical note (2005) AAPSPharmSciTech, 6 (4), p. 81. , article; Balestrieri, F., Magri, A.D., Magri, A.L., Marini, D., Sacchini, A., Application of differential scanning calorimetry to the study of drug-excipient compatibility (1996) Thermochimica Acta, 285, pp. 337-345; British Pharmacopoeia (1996) Addendum 1996, p. 1761. , British Pharmacopoeia Commission, London, UK: British Pharmacopoeia Commission;; Rao PR, Ramakrishna S, Diwan PV. Drug release kinetics from polymeric films containing propranolol hydrochloride for transdermal use. Pharm Dev Techno 2000; l5: 465-472UR - https://www.scopus.com/inward/record.uri?eid=2-s2.0-58949097899&partnerID=40&md5=7f1408de6177379491ae4f1486bef337

PY - 2008

Y1 - 2008

N2 - A matrix dispersion type transdermal drug delivery system of Diltiazem Hydrochloride was developed using different ratios of rosin with Eudragit RL PM and polyvinyl pyrrolidone. The patch prepared by the combination of rosin and polyvinyl pyrrolidone was not transparent one, and shows an uneven distribution of polyvinyl pyrrolidone, which may be due to the hydrophilic nature of polyvinyl pyrrolidone. The effect of the polymers on the technological properties, i.e., drug release, water vapor transmission rate, percentage moisture loss and thickness were investigated. The patch containing rosin: Eudragit RL PM (6:4) showed a release of 2651 mcg in 24 h. In order to improve the release various proportions of camphor was included in the formulation. The patch containing rosin: Eudragit RL PM (6:4) with 5% w/v of camphor showed a sustained release of the drug extending over a period of 24 h. Formulation F8 emerged as the most satisfactory formulation as far as the technological properties were concerned. Further skin permeation and skin irritation studies were carried out on rat skin and rabbit respectively. Therefore it can be concluded that the patch containing rosin: Eudragit RL PM in the ratio 6:4 with 5%w/v of camphor achieved the desired objectives of transdermal drug delivery systems, such as overcoming of first pass effect, extended release and reduced frequency of administration.

AB - A matrix dispersion type transdermal drug delivery system of Diltiazem Hydrochloride was developed using different ratios of rosin with Eudragit RL PM and polyvinyl pyrrolidone. The patch prepared by the combination of rosin and polyvinyl pyrrolidone was not transparent one, and shows an uneven distribution of polyvinyl pyrrolidone, which may be due to the hydrophilic nature of polyvinyl pyrrolidone. The effect of the polymers on the technological properties, i.e., drug release, water vapor transmission rate, percentage moisture loss and thickness were investigated. The patch containing rosin: Eudragit RL PM (6:4) showed a release of 2651 mcg in 24 h. In order to improve the release various proportions of camphor was included in the formulation. The patch containing rosin: Eudragit RL PM (6:4) with 5% w/v of camphor showed a sustained release of the drug extending over a period of 24 h. Formulation F8 emerged as the most satisfactory formulation as far as the technological properties were concerned. Further skin permeation and skin irritation studies were carried out on rat skin and rabbit respectively. Therefore it can be concluded that the patch containing rosin: Eudragit RL PM in the ratio 6:4 with 5%w/v of camphor achieved the desired objectives of transdermal drug delivery systems, such as overcoming of first pass effect, extended release and reduced frequency of administration.

M3 - Article

VL - 49

SP - 211

EP - 227

JO - Ars Pharmaceutica

JF - Ars Pharmaceutica

SN - 0004-2927

IS - 3

ER -

Prabu SL, Shirwaikar A, Shirwaikar A, Kumar A, Jacob A. Design and evaluation of matrix diffusion controlled transdermal patches of Diltiazem hydrochloride. Ars Pharmaceutica. 2008;49(3):211-227.