Nghiên cứu điều chế hệ phân tán rắn itraconazol-hydroxybutyl-beta-cyclodextrin

• Nghien ciru - Ky thuat

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{Ngay nhan bai: 26/12/2013 - Ngay thong qua phin bien: 13/01/2014)

Nghien cmi dilu che he phan tan ran

itraconazol-hydroxybutyl-beta-cyclodextrin

Phung Dire Truyen'*, Nguyen Phu'O'c Trirfrng^

Huynh Van Hoa^ Sang Van Tinh^ ' Vien set ret-KST- CT TP. Hd Chi Minh

^ Dgi hoc YDuac TP. Ho ChiMinh

* E-mail:[email protected]

Summary

A bio-dosage form for Itraconazole (ITZ), a broad anti-fungal of triazole group, was developed.

Taking Itraconazole (ITZ) as one of the typical water-insoluble drugs, and this significantly challenges

the developing of ITZ's bio-dosage form, this study focused on overcoming this. Hydroxybutyl-beta￾cyclodextrin, a hydroxyalkyi derivative of pCD, showed capable of forming complex with ITZ at the

rate of 1:1; 1:2; 1:3. By IR. DSC, and ^H-NMR, the obtained ITZ-HB^CD complex was revealed to

have real interaction between ITZ and HBpCD. For all the tested samples, ITZ's dissolution from the

obtained complex by co-evaporation was much higher than other methods. ITZ's solubility in HCI 0. IN

was measured for itraconazol 10^, the ITZ-HB^CD complex at the rate of 1:1 (1.237 mg/ml), the ITZ￾HB^CD complex at the rate of 1:2 (3.218 mg/ml). and the ITZ-HB0CD complex at the rate of 1:3 (20.364

mg/ml). Ail proved HB^CD to be a potential substance for increasing the bioavailability of ITZ and other

poor water-soluble drugs.

Keywords: Itraconazole (ITZ). Hydroxybutyl-beta-cyciodextrin (HB^CD), the ITZ-HBpCD complex.

O a t vi n d e vu quan trgng trong phat trien dang bao ch i cua

Hydroxybutyl-beta-cyclodextrin (HB|3CD) la ^'^^- ^^ *^' "'^S'^'^" ^"^" ^^ " ^^® ^ ^ P^^" ^^" ^ "

mdt trong cac ddn chit hydroxyalkyi cua beta 'TZ-HBpCD" dugc thye hiOn lam ea sd de ung

cyclodextrin, hien nay tren th i gidi da bit di u dung tiep vao cac dang bao eh l d l lam tang dp

ung dung chdt nay tao HPTR vdi mgt so dugc ^^"^ ^^^

phim va cho thay kha nang lam tang dd tan vuat Va t Meu v a phu-an g pha p nghien

trgi cua no so vdi cdc ddn ehlt hydroxyalkyi khac cu>u'

cd cung do th i (DS) '^L

Itraconazol (ITZ), mgt thulc khang ni m pho ^^ * ''^ "

rgng nhom triazol, thuge nhdm II trong hO thong ITZ tidu chuan Eur. Ph/BP, Hang SIMS (Italia),

phan loai sinh dugc hgc, la mgt trong nhung loai hydroxybutyl-beta-cyclodextrin tong hgp tai Khoa

thulc khdng tan trong nude diln hinh (khoang 1 Dugc, OHYDTP. H i Chf Minh dgtTCCS, ethanol,

ng/ml d pH trung tinh va 6 pg/ml d pH 1). Dg tan may khuay tu co dilu nhiOt Stuart CB162 (Anh),

thip Id thach thuc dang ke trong viee xdy dyng mdy thu dg hda tan Enveka DT-700 {Q(rc), mdy

cdng thue bdo ch i eua ITZ. bi t k l dudng diing. ed quay BiJchi R210S (Thyy Sy), tu say chdn

Vi vay, tdng cudng ty lg hoa tan la mgt nhiOm khong Jeiotech OV-12/TRP-6 (Han Quoc), mdy

T^PCHi DUOC HQC - 2/2014 (S6 454 NAM 54)