Advertisement

AAPS PharmSciTech

, Volume 19, Issue 3, pp 1493–1499 | Cite as

Preparation of Controlled-Release Particles Based on Spherical Porous Silica Used as the Drug Carrier by the Dry Coating Method

  • Shohei Nakamura
  • Shihoko Kondo
  • Ayaka Mohri
  • Takatoshi Sakamoto
  • Hiroshi Yuasa
Brief/Technical Note
  • 125 Downloads

Abstract

A controlled-release formulation is a dosage form that could improve a patient’s quality of life by reducing the frequency of administration, while ensuring the continued effect of the medicine and reducing the side effects. To prepare these controlled-release particles, a wet coating method in which a drug is coated with a controlled-release material using water or an organic solvent is used, but with this method, the coating process is very time-consuming and requires large amounts of energy for the drying phase. In addition, contact with water or an organic solvent may cause problems such as alteration of the drug. Therefore, the use of a dry coating method has attracted attention as a means of overcoming these issues. However, since the drug is fixed to the surface of a core particle, it is necessary to further coat it with a water-soluble material. We used spherical porous silica (SPS) particles, considering that the drug fixation via a water-soluble material would not be necessary if the drug were to be placed in the pores of these particles. We used SPS filled with theophylline (TP), a model drug, as the core particles. To prepare controlled-release particles (CRP), a controlled-release layer consisting of hydrogenated castor oil (HCO) was applied to the core particle surface by a dry coating method. The paddle method using 1% w/v polysorbate 80 solution as the test medium was employed to estimate the TP dissolution rate of the resulting CRPs. The 50% dissolution time of TP extended from 14 to 405 min with increasing the amount of the coated HCO. The Korsmeyer-Peppas model applied to the TP dissolution behavior yielded an n value of around 1. Moreover, the K value was comparable with the case in which a zero-order model was applied. It is thought that the dissolution of TP from CRPs will conform to the zero-order model.

Keywords

Dry coating Controlled-release Spherical porous silica Hydrogenated castor oil Theophylline 

Notes

Acknowledgements

We thank Fuji Silysia Chemical Ltd. for kindly gifting the spherical porous silica and Freund Corp. for kindly gifting the hydrogenated castor oil.

Compliance with Ethical Standards

Conflict of Interest

The authors declare that they have no conflict of interest.

References

  1. 1.
    Miyagawa Y, Sato H, Okabe T, Nishiyama T, Miyajima M, Sunada H. In vivo performance of wax matrix particles prepared by a twin-screw compounding extruder. Drug Dev Ind Pharm. 1999;25(4):429–35.  https://doi.org/10.1081/DDC-100102192.CrossRefPubMedGoogle Scholar
  2. 2.
    Roy P, Shahiwala A. Multiparticulate formulation approach to pulsatile drug delivery: current perspectives. J Control Release. 2009;134(2):74–80.  https://doi.org/10.1016/j.jconrel.2008.11.011.CrossRefPubMedGoogle Scholar
  3. 3.
    Jono K, Ichikawa H, Miyamoto M, Fukumori Y. A review of particulate design for pharmaceutical powders and their production by spouted bed coating. Powder Technol. 2000;113(3):269–77.  https://doi.org/10.1016/S0032-5910(00)00310-7.CrossRefGoogle Scholar
  4. 4.
    Fujimoto S, Uemura T, Fukumori Y. A trial of dry process coating using a twin screw continuous kneader. Powder Sci Eng. 2006;38:57–62.Google Scholar
  5. 5.
    Kondo K, Ito N, Niwa T, Danjo K. Design of sustained release fine particles using two-step mechanical powder processing: Particle shape modification of drug crystals and dry particle coating with polymer nanoparticle agglomerate. Int J Pharm. 2013;453(2):523–32.  https://doi.org/10.1016/j.ijpharm.2013.06.028.CrossRefPubMedGoogle Scholar
  6. 6.
    Naganuma T, Nishida A, Sakamoto T, Kabasawa K, Imai K, Yuasa H. Preparation of dry-coated particles with controlled-release property using a new ultrahigh-speed mixer. J Pharm Sci Technol Japan. 2009;69:452–60.Google Scholar
  7. 7.
    Nakamura S, Sakamoto T, Ito T, Kabasawa K, Yuasa H. Preparation of controlled-release fine particles using a dry coating method. AAPS PharmSciTech. 2016;17(6):1393–403.  https://doi.org/10.1208/s12249-015-0475-x.CrossRefPubMedGoogle Scholar
  8. 8.
    Sayed E, Haj-Ahmad R, Ruparelia K, Arshad MS, Chang MW, Ahmad Z. Porous inorganic drug delivery systems—a review. AAPS PharmSciTech. 2017;18(5):1507–25.  https://doi.org/10.1208/s12249-017-0740-2.CrossRefPubMedGoogle Scholar
  9. 9.
    Konishi K. Pharmaceutical application of porous Ca silicate. Pharm Tech Japan. 2017;33:2197–202.Google Scholar
  10. 10.
    Ministry of Health, Labour and Welfare, “6.10 Dissolution,” In: The Japanese Pharmacopoeia, 17th edition, 2016. pp. 141–5.Google Scholar
  11. 11.
    Ministry of Health, Labour and Welfare, Guidance for Bioequivalence Studies of Generic Products, Attachment of Division-Notification 0229 No. 10 of the Pharmaceutical and Food Safety Bureau, February 29, 2012.Google Scholar
  12. 12.
    Higuchi T. Rate of release of medicaments from ointment bases containing drugs in suspensions. J Pharm Sci. 1961;50:874–5.CrossRefPubMedGoogle Scholar
  13. 13.
    Korsmeyer RW, Gurny R, Doelker EM, Buri P, Peppas NA. Mechanism of solute release from porous hydrophilic polymers. Int J Pharm. 1983;15(1):25–35.  https://doi.org/10.1016/0378-5173(83)90064-9.CrossRefGoogle Scholar

Copyright information

© American Association of Pharmaceutical Scientists 2018
corrected publication March/2018

Authors and Affiliations

  • Shohei Nakamura
    • 1
  • Shihoko Kondo
    • 1
  • Ayaka Mohri
    • 1
  • Takatoshi Sakamoto
    • 1
  • Hiroshi Yuasa
    • 1
  1. 1.Department of Pharmaceutical Technology, College of Pharmaceutical SciencesMatsuyama UniversityMatsuyamaJapan

Personalised recommendations