Bioavailability and factors influencing its rate
Authors:
Barbora Vraníková; Jan Gajdziok
Authors place of work:
Veterinární a farmaceutická univerzita Brno, Farmaceutická fakulta, Ústav technologie léků
Published in the journal:
Čes. slov. Farm., 2015; 64, 7-13
Category:
Přehledy a odborná sdělení
Summary
Bioavailability can be defined as the rate and range of active ingredient absorption, when it becomes available in the systemic circulation or at the desired site of drug action, respectively. Drug bioavailability after oral administration is affected by anumber of different factors, including physicochemical properties of the drug, physiological aspects, the type of dosage form, food intake, biorhythms, and intra- and interindividual variability of the human population. This article is the first from the series dealing with the bioavailability and methods leading to its improvement. The aim of the present paper is to provide an overview of aspects influencing the rate of bioavailability after oral administration of the active ingredient. Subsequentarticles will provide detailed descriptions of methods used for dug bioavailability improvement, which are here only summarized.
Keywords:
bioavailability • drug solubility • poorly soluble drugs • factors influencing bioavailability
Zdroje
1. Kawabata Y., Wada K., Nakatani M., Yamada S., Onoue S. Formulation design for poorly water-soluble drugs based on biopharmaceutics classification system: Basic approaches and practical applications. Int. J. Pharm. 2011; 420, 1–10.
2. Rasenack N., Müller B. W. Dissolution rate enhancement by in situ micronization of poorly water-soluble drugs. Pharm. Res. 2002; 19, 1894–1900.
3. Keck C. M., Müller R. H. Drug nanocrystals of poorly soluble drugs produced by high pressure homogenization. Eur. J. Pharm. Biopharm. 2006; 62, 3–16.
4. Vasconcelos T., Sarmento B., Costa P. Solid dispersions as strategy to improve oral bioavailability of poor water soluble drugs. Drug Discov. Today 2007; 12, 1068–1075.
5. Gursoy R. N., Benita S. Self-emulsifying drug delivery systems (SEDDS) for improved oral delivery of lipophilic drugs. Biomedicine and Pharmacotherapy. 2004; 58, 173–182.
6. Vraníková B., Gajdziok J., Vetchý D., Kratochvíl B., Seilerová L. Systémy kapalina v pevné fázi jako moderní trend zvyšování biologické dostupnosti léčiva. Chem. Listy 2013; 107, 681–687.
7. Lüllmann H., Mohr K., Wehling M. Farmakologie a toxikologie. 2. vydání Praha: Grada Publishing 2004.
8. Lincová, D., Farghali, H. Základní a aplikovaná farmakologie. 2. vydání. Praha: Galén 2007.
9. Allam A. N., El Gamal, S. S., Naggar V. F. Bioavailability: a pharmaceutical review. Int. J. Nov. Drug Deliv. Tech. 2001; 1, 80–96.
10. van de Waterbeemd H., Testa B., Mannhold R., Kubinyi H., Folkers G. Drug Bioavailability: Estimation of solubility, Permeability, Absorption and Bioavailability. 2nd Edition. Weinheim: John Wiley & Sons 2009.
11. Komárek P., Rabišková M. Technologie léků. 3. přepracované a doplněné vydání. Praha: Galén 2006.
12. Lipinski C. A., Lombardo F., Dominy B. W., Feeney P. J. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv. Drug Deliv. Rev. 2001; 46, 3–26.
13. Okáčová L., Vetchý D., Franc A., Rabišková M., Kratochvíl B. Zvýšení biodostupnosti těžce rozpustných léčivých látek jejich modifikací. Chem. Listy 2010; 104, 21–26.
14. Český lékopis 2009. 1. vydání. Praha: Grada Publishing 2009.
15. Yazdanian M., Briggs K., Jankovsky C., Hawi A. The „high solubility“ definition of the current FDA guidance on biopharmaceutical classification system may be too strict for acidic drugs. Pharm. Res. 2004; 21, 293–299.
16. Amidon G. L., Lennernäs 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. Pharm. Res. 1995; 12, 413–420.
17. Chavda H. V., Patel C. N., Anand I. S. Biopharmaceutics classification system. Syst. Rev. Pharm. 2010; 1: 62–69.
18. van De Waterbeemd H., Smith D. A., Beaumont K., Walker D. K. Property-based design: optimization of drug absorption and pharmacokinetics. J. Med. Chem. 2001; 44, 1313–1333.
19. Dostálek M. Farmakokinetika. Praha: Grada Publishing 2006.
2 0. Li X., Hu M. Oral bioavailability: basic principles, advanced concepts, and applivations. 1st edition. Weinheim: John Wiley & Sons 2011.
21. Farsa O. Terapeutické monoklonální protilátky v léčbě a ve vývoji. Chem. Listy 2013; 107, 464–470.
22. Kratochwil N. A., Huber W., Müller F., Kansy M., Gerber P. R. Predicting plasma protein binding of drugs: a new approach. Biochem. Pharmacol. 2002; 64, 1355–1374.
23. Lüllmann, H., Mohr, K., Hein, Lutz. Barevný atlas farmakologie. 3. vyd. Praha: Grada Publishing 2007.
24. Alhamami O. M. Delay in gastric emptying rate enhances bioavailability of sodium salicylates in rabbit. Arch. Pharm. Res. 2007; 30, 1144–1148.
25. Mearrick P. T., Wade D. N., Birkett D. J., Morris J. Metoclopramide, gastric emptying and L-dopa absorption. Aust. N. Z. J. Med. 1974; 4, 144–148.
26. Amir I., Anwar N., Baraona E., Lieber C. S. Ranitidine increases the bioavailability of imbibed alcohol by accelerating gastric emtying. Life Sci. 1996; 58, 511–518.
27. Dressman J. B., Berardi R. R., Dermentzoglou L. C., Russell T. L., Schmaltz S. P., Barnett J. L., Jarvenpaa K. M. Upper gastrointestinal (GI) pH young healthy men and women. Pharm. Res. 1990; 7, 756–761.
28. Augustijns P., Brewster M. Solvent systems and their selection in pharmaceutics and biopharmaceutics. Berlin: Springer Science & Business Media 2007.
29. Zhou D., Qiu Y. Oral Absorption and the Biopharmaceutics Classification System. Journal of validation technology 2009; 15, 62–72.
30. Fallingborg J. Intraluminal pH of the human gastrointestinal tract. Dan. Med. Bull. 1999; 46, 183–196.
31. Dvořáčková K., Franc A., Kejdušová M. Směrování léčiv do tlustého střeva. Chem. Listy 2013; 107, 522–529.
32. Kwan K. C. Oral bioavailability and first-pass effects. Drug Metab. Dispos. 1997; 25, 1329–1336.
33. Levy G., Gumtow R. H., Rutowski J. M. The Effect of Dosage form upon the Gastrointestinal Absorption Rate of Salicylates. Can. Med. Assoc. J. 1961; 85, 414–419.
34. Melander A. Influence of food on the bioavailability of drugs. Clin. Pharmacokinet. 1978; 3, 337–351.
35. Guidance for Industry: Food-Effect Bioavailability and Fed Bioequivalence Studies. http://www.fda.gov/downloads/Regulatory Information/Guidances/UCM126831.pdf. (12. 1. 2015).
36. Moses D. K., Charles B. G., Ravenscroft P. J., Whyte I. M. Food reduces the oral bioavailability of propantheline bromide in healthy subjects. Br. J. Clin. Pharmacol. 1983; 16, 758–759.
37. Lecaillon J. B., Godbillon J., Campestrini J., Naquira C., Miranda L., Pacheco R., Mull R., Poltera A. A. Effect of food on the bioavailability of triclabendazole in patients with fascioliasis. Br. J. Clin. Pharmacol. 1998; 45, 601–604.
38. Lemmer B. Relevance for chronopharmacology in practical medicine. Semin. Perinatol. 2000; 24, 280–290.
39. Griffett K., Burris T. P. The mammalian clock and chronopharmacology. Bioorg. Med. Chem. Lett. 2013; 23, 1929–1934.
40. Ptáček R., Bartůněk P. a kol. Etické problémy medicíny na prahu 21. století. 1. vydání. Praha: Grada Publishing 2014.
41. Kovarik J. M., Mueller E. A., van Bree J. B., Tetzloff W., Kutz K. Reduced inter- and intraindividual variability in cyclosporine pharmacokinetics from a microemulsion formulation. J. Pharm. Sci. 1994; 83, 444–446.
42. Lebbe C., Beyeler C., Gerber N. J., Reichen J. Intraindividual variability of the bioavailability of low dose methotrexate after oral administration in rheumatoid arthritis. Ann. Rheum. Dis. 1994; 53, 475–477.
43. Grahnén A., Hammarlund M., Lundqvist T. Implications of intraindividual variability in bioavailability studies of furosemide. Eur. J. Clin. Pharmacol. 1984; 27, 595–602.
44. Kataria M. K., Bhandari A. Solubility and dissolution enhancement: technologies and research emerged. Journal of Biological and Scientific Opinion 2013; 1, 105–116.
45. Kusumi S., Tomono S., Okuzawa S., Kaneko E., Ueda T., Sasaki K., Takahashi D., Toshima K. Total synthesis of vineomycin B2. J. Am. Chem. Soc. 2013; 135, 15909–15912.
46. Vishweshwar P., McMahon J. A., Bis J. A., Zaworotko M. J. Pharmaceutical Co-Crystals. J. Pharm. Sci. 2006; 95, 499–516.
47. Hetal T., Bindesh P., Sneha T. A review on techniques for oral bioavailability enhancement of drugs. International Journal of Pharmaceutical Sciences Review and Research 2010; 4, 203–223.
48. Offermanns S., Rosenthal W. Encyclopedia of molecular pharmacology. 2nd edition. Berlin: Springer Science & Business Media 2008.
49. Djokic S., Vajtner Z., Krnjevic H., Lopotar N., Kolacny-Babic L. Complexes and chelates of azithromycin with bivalent and/or trivalent metals and their use as antiulcer. 1990; US5498699A.
50. Hancock B. C., Parks M. What is the true solubility advantage for amorphous pharmaceuticals? Pharm. Res. 2000; 17, 397–404.
51. Pudipeddi M., Serajuddin A. T. M. Trends in solubility of polymorphs. J. Pharm. Sci. 2005; 94, 929–939.
52. Kaur J., Aggarwal G., Gurpreet S., Rana A. C. Improvement of drug solubility using solid dispersion. International Journal of Pharmacy and Pharmaceutical Sciences. 2012; 4, 47–53.
53. Gowardhane A. P., Kadam N. V., Dutta S. Review on enhancement of solubilisation precess. Journal of Pharmacy and Phytotherapeutics 2013; 2, 28–38.
54. Maheshwari M., Jahagirdar H., Paradkar A. Melt sonocrystallization of ibuprofen: Effect on crystal properties. European Journal of Pharmaceutical Sciences. 2005; 25, 41–48.
55. Chuchvalec P., Novák J. P. Kritické veličiny látek a jejich predikce. Chem. Listy 2007; 101, 989–993.
56. Kim J., Kim H., Ju C. Micronization and characterization of drug substances by RESS with supercritical CO2. Korean J. Chem Eng. 2010; 27, 1139–1144.
57. Sander J. R. G., Zeiger B. W., Suslick K. S. Sonocrystallization and sonofragmentation. Ultrason. Sonochem. 2014; 21, 1908–1915.
58. Nireesha G., Divya L., Sowmya C., Venkateshan N., Babu M. N., Lavakumar V. Lyophilization/freeze drying – an review. International Journal of Novel Trends in Pharmaceutical Sciences 2013; 3, 87–98.
59. Yasmin R., Tan A., Bremmell K. E., Prestidge C. A. Lyophilized silica lipid hybrid (SLH) carriers for poorly water-soluble drugs: physicochemical and in vitro pharmaceutical investigations. J. Pharm. Sci. 2014; 103, 2950–2959.
60. Sahoo N. G., Abbas A., Judeh Z., Li C. M., Yuen K. H. Solubility enhancement of a poorly water-soluble anti-malarial drug: Experimental design and use of a modified multifluid nozzle pilot spray drier. J. Pharm. Sci. 2009; 98, 281–296.
61. Sollohub K., Cal K. Spray drying technique: II. current applications in pharmaceutical technology. J. Pharm. Sci. 2010; 99, 587–597.
62. Walters R. H., Bhatnagar B., Tchessalov S., Izutsu K., Tsumoto K., Ohtake S. Next generation drying technologies for pharmaceutical applications. J. Pharm. Sci. 2014; 103, 2673–2695.
63. Vandana K. R., Raju Y. P., Chowdary V. H., Sushma M., Kumar V. N. An overview on in situ micronization technique – an emerging novel concept in advanced drug delivery. Saudi Pharm. J. 2014; 22, 283–289.
64. Joshi J. T. A review on micronization techniques. Journal of Pharmaceutical Science and Technology 2011; 3, 651–681.
65. Bansal K., Pant P., Rao P. R. T., Padhee K, Sathapathy A., Kochhar P. S. Micronization and dissolution enhancement of norethindrone. International Journal of Research in Pharmacy and Chemistry 2011; 1, 315–319.
66. Chen H., Khemtong C., Yang X., Chang X., Gao J. Nanonization strategies for poorly water-soluble drugs. Drug Discov. Today 2011; 16, 354–360.
67. Balakrishnan A., Rege B. D., Amidon G. L., Polli E. Surfactant-mediated dissolution: Contributions of solubility enhancement and relatively low micelle diffusivity. J. Pharm. Sci. 2004; 93, 2064–2075.
68. Bajaj H., Bisht S., Yadav M., Singh V. Bioavaolability enhancement: a review. International Journal of Pharma and Bio Sciences 2011; 2, 202–216.
69. Sikarra D., Shukla V., Kharia A. A., Chatterjee D. P. Techniques for solubility enhancement of poorly soluble drugs: an overview. Journal of Medical Pharmaceutical and Allied Sciences 2012; 1, 1–22.
70. Li P., Yhao L. Solubilization of flurbiprofen in pH-surfactant solutions. J. Pharm. Sci. 2003; 92, 951–956.
71. Rangel-Yagui C. O., Pessoa Jr. A., Taveres L. C. Micellar solubilization of drugs. J. Pharm. Pharm. Sci. 2005; 8, 147–163.
72. Zhu J., Bierwagen G. P. The surface chemistry of water-reducible polymer solutions/dispersions – 1. Surface tension behavior. Prog. Org. Coat. 1995; 26, 87–100.
73. Kawakami K., Oda N., Miyoshi K., Funaki T., Ida Y. Solubilization behavior of a poorly soluble drug under combined use of surfactants and cosolvents. Eur. J. Pharm. Sci. 2006; 28, 7–14.
74. Vemula V. R., Lagishetty V., Lingala S. Solubility enhancement techniques. International Journal of Pharmaceutical Sciences Review and Research 2010; 5, 41–51.
75. Jangher A., Griffiths P. C., Paul A., King S. M., Heenan R. K., Schweins R. Polymeric micelle disruption by cosolvents and anionic surfactants. Colloid and Surface A. 2011; 391, 88–94.
76. Patil A. E., Devtalu S. V., Bari M. M., Barthel S. D. A review on: novel solubility enhancement technique hydrotropy. Indo American Journal of Pharmaceutical Research 2013; 3, 4670–4679.
77. Kumar V. S., Raja C., Jayakumar C. A review on solubility enhancement using hydrotropic phenomena. International Journal of Pharmacy and Pharmaceutical Sciences 2014; 6, 1–7.
78. Terao K., Nakata D., Fukumi H., Schmid G., Arima H., Hirayama F., Uekama K. Enhancement of oral bioavailability of coenzyme Q10 by complexation with γγ-cyclodextrin in healthy adults. Nutr. Res. 2006; 26, 503–508.
79. Dvořáčková K. Principy uvolňování léčiv z perorálních matricových tablet obsahujících hypromelosu. Chem. Listy 2009; 103, 66–72.
80. Okáčová L., Vetchý D., Franc A, Rabišková M. Zvýšení biodostupnosti těžce rozpustných léčivých látek technologickými postupy usnadňujícími jejich rozpouštění. Chem. Listy 2011; 105, 34–40.
81. Sinha S., Ali, M., Baboota S., Ahuja A., Kumar A., Ali J. Solid dispersion as an approach for bioavailability enhancement of poorly water-soluble drug ritonavir. AAPS PharmSciTech. 2010; 11, 518–527.
82. Baek H. H., Kim D. H., Kwon S. Y., Rho S. J., Kim D. W., Choi H. G., Kim Y. R., Yong C. S. Development of novel ibuprofen-loaded solid dispersion with enhanced bioavailability using cycloamylose. Arch. Pharm. Res. 2012; 35, 683–689.
83. Zatloukal Z. Interaktivní práškové směsi. Čes. slov. Farm. 2004; 53, 165–171.
84. Allahham A., Stewart P. J. Enhancement of the dissolution of indomethacin in interactive mixtures using added fine lactose. Eur. J. Pharm. Biopharm. 2007; 67, 732–742.
85. Watano S., Imada Y., Hamada K., Wakamatsu Y., Tanabe Y., Dave R. N., Pfeffer R. Microgranulation of fine powders by a novel rotating fluidized bed granulation. Powder Technol. 2003; 131, 250–255.
86. Planinšek O., Kovačič B., Vrečer F. Carvediol dissolution improvement by preparation of solid dispersions with porous silica. Int. J. Pharm. 2011; 406, 41–48.
87. Krupa A., Jachowicz R., Kurek M., Figiel W., Kwiecień M. Preparation of solid self-emulsifying drug delivery systems using magnesium aluminometasilicates and fluid-bed coating proces. Powder Technol. 2014; 266, 329–339.
88. Yang H., Teng F., Wang P., Tian B., Lin X., Hu X., Zhang L., Zhang K., Zhang Y., Tang Y. Investigation of a nanosuspension stabilized by Soluplus® to improve bioavailability. Int. J. Pharm. 2014; 477, 88–95.
89. Kulkarni S. A., Aloorkar N. H., Mane M. S. Liquisolid systems: a review. International Journal of Pharmaceutical Sciences and Nanotechnology 2010; 3, 795– 802.
90. Kavitha K., Lova Raju K. N. S., Ganesh N. S., Ramesh B. Effect of dissolution rate by liquisolid compacts approach: an overview. Der Pharmacia Lettre 2011; 3, 71–83.
91. Shaikh J., Ankola D. D., Beniwal V., Singh D., Kumer M. N. Nanoparticle encapsulation improves oral bioavailability of curcumin by at least 9-fold when compared to curcumin administered with piperine as absorption enhancer. Eur. J Pharm. Sci. 2009; 37, 223–230.
92. Chen Y., Lu Y., Chen J., Lai J., Sun J., Hu F., Wu W. Enhanced bioavailability of the poorly water-soluble drug fenofibrate by using liposomes containing a bile salt. Int. J. Pharm. 2009; 376, 153–160.
93. Petersen S. B., Nolan G., Maher S., Rahbek U. L., Gultdbrandt M., Brayden D. J. Evaluation of alkylmaltosides as intestinal permeation enhancers: comparison between rat intestinal mucosal sheets and Caco-2 monolayers. Eur. J. Pharm. 2012; 47, 801–712.
94. Thanou M., Verhoef J. C., Junginger H. E. Chitosan and its derivatives as intestinal absorption enhancers. Adv. Drug Deliv. Rev. 2001; 50, S91–101.
Štítky
Farmácia FarmakológiaČlánok vyšiel v časopise
Česká a slovenská farmacie
2015 Číslo 1-2
Najčítanejšie v tomto čísle
- Biologická dostupnost léčiva a možnosti jejího ovlivňování
- Účinnost fytoterapie v podpůrné léčbě diabetes mellitus typu 2 Borůvka černá (Vaccinium myrtillus)
- Užívání vybraných OTC přípravků: srovnání Řecko a Česká republika
- K životnému jubileu pani doc. RNDr. Zuzany Vitkovej, PhD.