Abstract
The acquisition and the development of knowledge on how drugs exert their pharmacological effect, particularly information such as dose response, onset, and duration of action and pharmacodynamic and pharmacokinetic relationships has demanded attention to and stimulated interest in delivering drugs at rates (and to locations) that optimize their effects. Controlling drug release from the medication has accordingly evolved as a multidisciplinary science, requiring expertise spanning such disciplines as polymer science, engineering technologies, and awareness of the complexities and vagaries of gastrointestinal conditions that affect transit of dosage forms. Much has been achieved but there is still much to learn. This chapter outlines the historical evolution of concepts, practices, and achievements in providing better delivery systems for drugs so that they are better medications.
Access this chapter
Tax calculation will be finalised at checkout
Purchases are for personal use only
References
Noyes AA, Whitney WR (1897) The rate of solution of solid substances in their own solutions. J Am Chem Soc 19:930–934
Martindale WH, Wescott WW (1924) The extra pharmacopoeia, vol 1, 18th edn. H.K. Lewis, London, pp 682–683
de Gennes P-G (2004) La Memoire du College de France. “Ce n’est pas en perfectionnant la bougie que l’on invente l’électricité”
Bell B (1858) The therapeutic relations of opium and belladonna to each other. Edinb Med J 4:1–7
Fiset P, Cohane C, Browne S, Brand SC, Shafer SL (1995) Biopharmaceutics of a new transdermal fentanyl patch. Anesthesiology 83:459–469
Folkman J (1990) How the field of controlled-release technology began, and its central role in the development of angiogenesis research. Biomaterials 11:615–618
Hoffman AS (2008) The origins and evolution of “controlled” drug delivery systems. J Control Rel 132:153–163
Lazarus J, Cooper J (1961) Absorption, testing and clinical evaluation of oral prolonged-action drugs. J Pharm Sci 50:715
Florence AT (1992) Generic medicines: a question of quality. In: Wells FO (ed) Medicines: responsible prescribing. Queen’s University Press, Belfast, pp 63–83
Florence AT (1987) Sustained release theophylline preparations: pitfalls in generic prescribing. In: Fairfax AJ (ed) Therapeutics in respiratory medicine. Royal Society of Medicine Symposium Series 117, pp 23–32
Jonkmann JHG (1989) Food interactions with sustained release theophylline preparations. Clin Pharmacokinet 16:162–179
Brockedon T (1843) Shaping pills, lozenges and black lead in dies. GB Patent 9977
Brockedon’s Patent. Process Pharm J 3:1843–1844
Pariente L (1996) Comprimés Chap. 6 in Naissance et Evolution de Quinze Formes Pharmaceutiques. Editions Louis Pariente, Paris, pp 94–118
Dunton J (1875) Improvement in the manufacture of pills. US Patent 168,240
Carter C (1878) Improvement in coated compressed medicaments. US Patent 207,013
Ellzey EF (National Aniline Company) (1931) Device for administering medicaments. US Patent 1,815,902
Kraus F (1870) Improvements in putting up medicines. US Patent 108,034
Bird JC (American Cyanamid) (1948) Casting gelatin tablets. US Patent 2,552,027
Ritchie J (1893) Brief notes of several cases of acute diarrhoea treated with keratin-coated carbolic acid pills. Lancet 142:1305–1306
Dumez AG (1921) A contribution to the history of the development of enteric capsules. J Am Pharm Assoc 10:372–376. cited by B.E. Jones (2004), The history of the medicinal capsule, in Podczeck F, Jones BE (eds) Pharmaceutical capsules, 2nd edn. Pharmaceutical Press, London
Lille DG, Shepheard S (1917) A report on the treatment of Entamoeba histolytica “carriers” with emetine bismuth iodide giving a comparison between keratin coated and salol-coated pills. Lancet 190:418–419
Cowen DL (2002) Swallowing the pill. Apothecary’s Cabinet 4, p 6
Gorley JT, Lee CO (1938) A study of enteric coatings. J Am Pharm Assoc 27:379–384
Praetorius E, Faber JH (1950) Om tabletters henfald og passage geenem esophagus af ventrikel. Ugeskrift for Laeger 112:628–631
Freestone DS (1969) Formulation and therapeutic efficacy of drugs used in clinical trials. Lancet 294:98–99
Evans KT, Roberts GM (1976) Where do all the tablets go? Lancet 308:1237–1239
Channer KS (1990) Adverse reactions to the transit of dosage forms. In: Florence AT, Salole EG (eds) Formulation factors in adverse reactions. Wright, London, pp 75–95 (and references therein)
Thompson HO, Lee CO (1944) History, literature and theory of enteric coatings. J Am Pharm Assoc Sci Ed 34:135–138
Grönberg J (1919) Acta Med Scand 52:227–268
Thompson HO, Lee CO (1944) A study of enteric coatings. J Am Pharm Asssoc Sci Ed 27:138–142
Jack D (1962) Prolongation of drug action. Pharm J 188:581–585
Riseman JF, Altman G, Koretsky S (1958) Nitroglycerin and other nitrates in the treatment of angina pectoris. Circulation 17:22–39
Russek HI, Zohman BL, Drumm AE et al (1955) Long-acting coronary vasodilating drugs: Metamine, Paveril, Nitroglyn and Peritrate. Circulation 12:169–175
Genung LB (1938) (Eastman Kodak) US Patent 2,123,460
Greminger GK et al (1959) (Dow Chemical Co) US Patent 2,887,440
Rowe RC (1984) Material used in the film coating of oral dosage forms. In: Florence AT (ed) Critical reports on applied chemistry, Materials used in pharmaceutical formulation. Blackwells, Oxford
Theeuwes F (1975) Elementary osmotic pump. J Pharm Sci 64:1987–1991
Rose S, Nelson JF (1955) A continuous long term injector. Aust J Exp Med 33:415–429
Theeuwes F, Higuchi T, Zaffaroni A, Michaels AS (1973) Belgian Patent 800,485
Theeuwes F, Higuchi T(1974) (Alza Corp) US Patent 3,845,770
Bjarnason I, Macpherson AJS (1994) Intestinal toxicity of non-steroidal anti-inflammatory drugs. Pharmacol Ther 62:145–157
The Committee on Safety of Medicines (Aug 1983) Osmosin (Controlled release indomethacin) Current Problems, No 11
Cree IA, Walker MA et al (1985) Osmosin and ileal ulceration: a case report. Scott Med J 30:40–41
Day TK (1983) Intestinal perforation associated with osmotic slow release capsules. Br Med J 287:1671–1672
Celin A (1984) Intestinal perforation associated with osmotic slow release capsules. Br Med J 288:240–241
Laidler P, Maslin SC, Gilhome RW (1985) What’s new in Osmosin and intestinal perforation? Pathol Res Pract 180:74–76
Malaterre V, Ogorka J, Loggia N, Gurny R (2009) Oral osmotically driven systems: 30 years of development and clinical use. Eur J Pharm Biopharm 73:311–323
Santus G, Baker RW (1995) Osmotic drug delivery: a review of the patent literature. J Control Rel 35:1–21
Abrahams A, Linnell WH (1957) Oral depot therapy with a new long-acting dexamphetamine salt. Lancet 27:1317–1318
Chaudhry NC, Saunders L (1956) Sustained release drugs from ion-exchange resins. J Pharm Pharmacol 8:975–986
Elder DP (2005) Pharmaceutical applications of ion-exchange resins. J Chem Ed 82:575–587
Mahore JG, Wadher KJ et al (2010) Ion exchange resins: pharmaceutical application and recent advancement. Int J Pharm Sci Rev Res 1:8–13
Anon (1949) Prolonged penicillin action. Lancet 253:872–873
Romansky MJ, Rottman GE (1944) A method of prolonging the action of penicillin. Science 100:196–198
Romansky MJ, Rottman GE (1945) Penicillin blood levels for twenty four hours following a single intramuscular injection of calcium penicillin in beeswax and peanut oil. N Engl J Med 233:577–582
Monash S (1947) The use of bismuth, silver and mercury salts of penicillin for the prolongation of penicillin blood levels. J Invest Dermatol 9:157
Sullivan NP, Symmes AT, Millar HC, Rhodehamel HW Jr (1948) A new penicillin for prolonged blood levels. Science 107:169–170
Salivar CJ, Hedger FH, Brown EV (1948) Crystalline procaine penicillin. J Am Chem Soc 70:1287
Boger WP, Flippin HF (1949) Penicillin plasma concentrations. J Am Med Assoc 139:1131
Young MY, Andrews GWS, Montgomery DM (1949) Procaine penicillin. Lancet 253:863–865
Emery JL, Rose IM, Stewart SM, Wayne EJ (1949) The use in children of procaine penicillin with aluminium monostearate. Br Med J 1:1110–1112
Thomas EW, Lyons RH et al (1949) Newer repository penicillin products. J Am Med Assoc 137:1517–1519
Crommelin DJA, de Blaey CJ (1980) In vitro release studies on drugs suspended in non-polar media. I. Release of sodium chloride from suspensions in liquid paraffin. Int J Pharm 5:305–316 (see also idem. II. The release of paracetamol and chloramphenicol from suspensions in liquid paraffin. Int J Pharm 6:29–42
Szabo JL, Edwards CD, Bruce WF (1951) N.N’ dibenzylethylene diamine penicillin: preparation and properties. Antibiot Chemother 1:499
Seifter J, Glassman JM, Begany AJ, Blumenthal A (1951) Antibiot Chemother 1:504–508
Minto CF, Howe C et al (1997) Pharmacokinetics and pharmacodynamics of nandrolone esters in oil vehicle: effects of ester, injection site and injection volume. J Pharmacol Exp Ther 281:93–102
Junkman K (1957) Long acting steroids in reproduction. Recent Progr Horm Res 13:380–419
Kelly M (1947) Failure of oil-soluble anaesthetics to give prolonged analgesia. Lancet 249:710–711
Larsen SW, Thomsen AE, Rinvar E, Friis GJ, Larsen C (2001) Effect of drug lipophilicity on in vitro release from oil vehicles using nicotinic acid esters as model prodrug derivatives. Int J Pharm 216:83–93
Curry SH, Whelpton R, de Schipper PJ, Vranckx S, Schiff AA (1979) Kinetics of fluphenazine after fluphenazine dihydrochloride, enanthate and decanoate administration to man. Br J Clin Pharmacol 7:325–331
Larsen SW, Larsen C (2009) Critical factors influencing the in vivo performance of long-acting lipophilic solutions- impact on in vitro release method design. AAPS J 11(4):762–770
Honrath WL, Wolff A, Meli A (1963) The influence of the amount of solvent (sesame oil) on the degree and duration of action of subcutaneously administered testosterone and its propionate. Steroids 2:425–428
Deanesly R, Parkes AS (1937) Factors affecting the effectiveness of administered hormones. Proc R Soc B Med 124:279–298
Deanesly R, Parkes AS (1943) Further experiments on the administration of hormones by the subcutaneous implantation of tablets. Lancet 242:500–502
Noble RL (1938) Effect of synthetic oestrogenic substances on the body growth and endocrine organs of the rat. Lancet 232:192–195
Bishop PMF (1938) A clinical experiment in oestrin therapy. Br Med J 1:939–941
Parkes AS (1942) Administration of non-steroid substances by the implantation technique. J Endocinol 3:220–233
Folkman J, Long DM (1964) The use of silicone rubber as a carrier for prolonged drug therapy. J Surg Res 4:139–142
Dzuik PJ, Cook B (1966) Passage of steroids through silicone rubber. Endocrinology 78:208
Mischell DR (1975) Intravaginal rings for contraceptive use. An editorial comment. Contraception 12:249–251
Hutchinson FG, Furr BJA (1990) Biodegradable polymer systems for the sustained release of polypeptides. J Control Rel 13:279–294
Furr BJA, Hutchinson FG (1992) A biodegradable delivery system for peptides; preclinical experience with the gonadotrophin-releasing hormone agonist Zoladex™. J Control Rel 21:117–128
Parkes AS (1938) Effective absorption of hormones. Br Med J 1:371–373
Anon. (1941) Absorption of implanted hormone tablets. Lancet 238:318
Dang W, Daviau T, Ying P et al (1996) Effects of Gliadel wafer initial molecular weight on the erosion of wafer and release of BCNU. J Control Rel 42:83–92
Langer R (1983) Implantable controlled release systems. Pharm Ther 21:35–51
Li Y, Shawgo RS, Tyler B et al (2004) In vivo release from a drug delivery MEMS device. J Control Rel 100:211–219
Grüntzig A, Senning A, Siegenthaler WE (1979) Nonoperative dilatation of coronary-artery stenosis: percutaneous transluminal coronary angioplasty. New Engl J Med 301:61–68
Muller DWM, Topol EJ (1991) Implantable devices in the coronary artery. Trends Cardiovasc Med 1:225–232
Anon. (1949) Aerosols by inhalation. Lancet 254:660
Rooth G (1949) Inhalation of liquid aerosols. Acta Med Scand 133(Suppl. 228)
Beigel H (1865) On the inhalation of atomized fluids. Lancet 86:35–36
Beigel H (1865) On the inhalation of atomized fluids. Lancet 86:114–116
Mutch N (1944) Inhalation of chemotherapeutic substances. Lancet 244:775–780
Heubner W (1920) Z ges Exp Med 10:35
Hückel R (1925) Z ges Phys Ther 30:317
Anon. (1984) The Nebuliser epidemic. Lancet 324:789–790
Edwards DA, Hanes J, Caponetti G et al (1997) Large porous particles for pulmonary delivery. Science 276:1868–1872
Anon. (1929) Atopham administered by inunction. Lancet 2:413–414
Rothman S (1943) The principles of percutaneous absorption. J Lab Clin Med 28:1305–1321
For example: Telfer SV (1923) The administration of insulin by inunction. Br Med J 1:715
Major RH, Delp M (1936) Cutaneous absorption of insulin. Proc Soc Exp Biol Med 35:429
Zondek B, Bromberg YM, Shapiro B (1942) Percutaneous application of sulfonamides in animals and men. Proc Soc Exp Biol Med 50:116
Hadgraft J, Lane M (2005) Skin permeation: the years of enlightenment. Int J Pharm 305:2–12
Shelmire JB (1958) Observations on the role of vehicles in percutaneous absorption. AMA Arch Derm 78:191–195
Sarkany I, Hadgraft JW, Caron GA, Barret CW (1965) The role of vehicles in the percutaneous absorption of corticosteroids. Br J Dermatol 77:569–575
Herrmann F, Salzberger MB, Baer RL (1942) New penetrating vehicles and solvents. Science 96:451–452
Gemmell DHO, Morrison JC (1957) The release of medicinal substances from topical applications and their passage through the skin. J Pharm Pharmacol 9:641–656
Smith CC (1955) Failure to demonstrate absorption of hydrocortisone when topically applied to the human skin. Ann NY Acad Sci 61:517–519
Malkinson FD, Ferguson EH (1955) Percutaneous absorption of hydrocortisone-4-C14 in two human subjects. J Invest Dermatol 25:281–283
Leduc S (1900) Introduction des substances medicamenteuses dans la profondeur des tissus par le courant electrique. Ann d’Electrobiol 3:545–560
Erlanger G (1929) Iontophoretic medication in ophthalmology. Arch Phys Ther 20:16
Fleming N (1943) Iontotherapy (Ionic medication, iontophoresis, ionization) as an aid in ophthalmic therapeutics. Br J Ophthalmol 27:354–360
Deutsch D (1934) Device for inserting medicaments into the body by iontophoresis. US Patent 1,967,927
Abramson HA, Engel MG (1942) Skin reactions. XII. Patterns produced in the skin by electrophoresis of dyes. Arch Dermatol Syph 44:190
Clark WG, Strakosch EA, Nordlum C (1942) Penetration of sulfonamides through intact skin by iontophoresis and other means of local application. Proc Soc Exp Biol Med 50:43
Hoogstraate AJ, Srinivasan V, Simms SM, Higuchi WI (1994) Iontophoretic enhancement of peptides: behaviour of leuprolide versus model compounds. J Control Rel 31:41–47
Guy RH, Kalia YN, Delgado-Charro MB et al (2000) Iontophoresis: electrorepulsion and electroosmosis. J Control Rel 64:129–132
Yang RK et al (2008) (Monosol Rx) Process for making an ingestible film. US Patent 7,357,891
Zaffaroni A (1971) (Alza Corporation). Bandage for administering drugs. US Patent 3,598,122
Zaffaroni A (1971) (Alza Corporation) Bandage for administering drugs. US Patent 3,598, 123
Gerstel MS, Place VA (1976) Drug delivery device, US Patent 3,964,482
Henry S, McAllister D, Allen MG, Prausnitz MR (1998) Microfabricated microneedles: a novel method to increase transdermal drug delivery. J Pharm Sci 87:922–925
Prausnitz MR (2004) Microneedles for transdermal drug delivery. Adv Drug Deliv Res 56:581–587
Sedlácek J (1965) Possibility of the application of ophthalmic drugs with the use of gel contact lenses. Ceskoslovenska oftalmologie 21:509–512
Wichterle O, Lim D (1960) Hydrophilic gels in biological use. Nature 185:117–118
Ness RA (Alza Corporation) Ocular insert, US Patent 3,618, 604
Armaly MF, Rao KR (1973) The effect of pilocarpine Ocusert with different release rates on ocular pressure. Invest Ophthalmol 12:491–496
Wadleigh JC (1883) Gelatine eye-disk. US Patent 273,410
Chang TMS (1964) Semipermeable microcapsules. Science 146:524–525
Orive G, Hernández RM et al (2004) History, challenges and perspectives of cell microencapsulation. Trends Biotechnol 22:87–91
Brynko C, Scarpelli JA (1961) (National Cash register Company) Process of making dual-walled oil-containing capsules. US Patent 2,969,331
Figge FHJ et al (1969) (AMP Inc) Method of administering therapeutic agents. USP 3,474,777
Kitajama M et al (1972) (Fuji Photo Film Co. and Toyo Jozo Co.) Encapsulation method. US Patent 3,691,090
Kitajima M, Kondo A, Arai F (1976) (Fuji Photo Film Co.) Process of producing aspirin-containing capsules. US Patent 3,951,851
Kramer PA (1974) Albumin microspheres as vehicles for achieving specificity in drug delivery. J Pharm Sci 63:1646–1647
Eckman B, Sjöholm I (1975) Use of macromolecules in microparticles. Nature 257:825–826
Kato T, Nemoto R, Mori H, Kumagai I (1978) Microencapsulated mitomycin C therapy in renal cell carcinoma. Lancet 314:479–480
see also Kato T, Nemoto R (1978) Preparation and properties of microencapsulated mitomycin C. IRCS Med Sci 6:311
Lee TK, Sokolski TD, Royer GP (1981) Serum albumin beads: an injectable biodegradable system for sustained release of drugs. Science 213:233–235
Okada H et al (1987) Prolonged release microcapsule production, US Patent 4,652,441
Okada H, Heya T, Ogawa Y, Shimamoto T (1988) One-month release injectable microcapsules of a luteinizing hormone-releasing hormone agonist (leuprolide acetate) for treating experimental endometriosis in rats. J Pharmacol Exp Ther 244:744–750
Okada H, Doken Y, Ogawa Y, Toguchi H (1994) Preparation of three-month depot injectable microspheres of leuprorelin acetate using biodegradable polymers. Pharm Res 11:1143–1147
Chen Y, Willmott N, Anderson J, Florence AT (1988) Haemoglobin, transferrin and albumin/polyaspartic acid microspheres as carriers for the cytotoxic drug adriamycin. I. Ultrastructural appearance and drug content. J Control Rel 8:93–101
Bungenberg de Jong BH (1949) Crystallisation-coacervation-flocculation. In: Kruyt HR (ed) Complex colloid systems. Colloid Science, Vol 2. Elsevier, Amsterdam, pp 232–255, 335–429
Burgess DJ, Carless JE (1985) Manufacture of gelatin/gelatin coacervate microcapsules. Int J Pharm 27:61–70
Dapper T, Thies C (1978) Statistical models for controlled release microcapsules: rationale and theory. J Membr Sci 4:99–113
Kreuter J (2007) Nanoparticles: a historical perspective. Int J Pharm 331:1–10
Speiser P (1976) Controlled release of drugs from microcapsules and nanocapsules. Acta Pharm Suec 13(Suppl):35
Couvreur P, Kante B, Roland M et al (1979) Polycycanoacrylate nanocapules as potential lysosomotropic carriers: preparation, morphological and sorptive properties. J Pharm Pharmacol 31:331–332
Hanes J, Cleland JL, Langer R (1997) New advances in microsphere-based single-dose vaccines. Adv Drug Deliv Rev 28:97–119
Higuchi T (1963) Mechanism of sustained-action medication. Theoretical analysis of rate of release of solid drugs dispersed in solid matrices. J Pharm Sci 52:1145–1149
Higuchi WI (1967) Diffusional models useful in biopharmaceutics. Drug release rate processes. J Pharm Sci 56:315–324
Singh P, Desai SJ, Simonelli AP, Higuchi WI (1967) Release rates of solid drug mixtures dispersed in inert matrices: I. Non-interacting drug mixtures. J Pharm Sci 56:1542–1547
Peppas N (1984) Mathematical modelling of diffusion processes in drug delivery polymeric systems. In: Smolen VF, Ball L (eds) Controlled drug bioavailability, vol 1. Wiley, New York, pp 203–237
Acknowledgments
I thank Mrs. Michelle Wake and Mr. Peter Field of the Library of The School of Pharmacy, University of London for retrieving copies of some of the older literature. I am also indebted to all those who have written historical reviews on many of the topics covered here.
There have been two Schools of Pharmacy with which I have been associated, at the University of Strathclyde, Glasgow, and in the University of London. In the former I began my research in 1962, so as both a student and researcher have seen some of the history discussed above unfold. My interest in pharmaceutics was piqued by the work that had been done in Glasgow, in wartime on transfusion and pyrogens, on transdermal absorption, atracurium, not to mention the work of my mentor Peter Elworthy on surfactant systems. In London its pedigree included the work of Prof Leonard Saunders in the 1960s with proto-liposomes, diffusion and ion-exchange drug resonates, formed a little part of the history, not all of it recounted here.
Author information
Authors and Affiliations
Corresponding author
Editor information
Editors and Affiliations
Rights and permissions
Copyright information
© 2011 Controlled Release Society
About this chapter
Cite this chapter
Florence, A.T. (2011). A Short History of Controlled Drug Release and an Introduction. In: Wilson, C., Crowley, P. (eds) Controlled Release in Oral Drug Delivery. Advances in Delivery Science and Technology. Springer, Boston, MA. https://doi.org/10.1007/978-1-4614-1004-1_1
Download citation
DOI: https://doi.org/10.1007/978-1-4614-1004-1_1
Published:
Publisher Name: Springer, Boston, MA
Print ISBN: 978-1-4614-1003-4
Online ISBN: 978-1-4614-1004-1
eBook Packages: Biomedical and Life SciencesBiomedical and Life Sciences (R0)