ABSTRACT
Objective: To prepare 1% voriconazole ( VCZ) sulfonated butyl ether- β-cyclodextrin ( SBE-β-CD) inclusion com-pound eye drop and study the quality. Methods: VCZ SBE-β-CD inclusion compound was prepared with the molar ratio of VCZ to SBE-β-CD of 1 :1. Sodium chloride was used as the osmotic pressure regulator and benzalkonium bromide was employed as the pre-servative in the preparation of VCZ SBE-β-CD inclusion compound eye drop. The appearance, pH value, content stability and irritation of the eye drop were studied as well. Results:The eye drop was colorless and transparent solution with the pH value of 6. 44 ± 0. 20, 6. 50 ± 0. 15,6. 48 ± 0. 22 the osmotic pressure of (320 ± 4. 62),(316 ± 2. 88),(322 ± 2. 60)MOsm and the VCZ content of 1. 02% g ·ml-1 . The results of accelerated testing and long-term testing showed no notable changes in the quality indices. The eye drop exhibi-ted no significant irritation to the rabbit eyes. Conclusion:VCZ SBE-β-CD inclusion compound eye drop shows the properties of high VCZ content, stable quality and promising safety in eye application, which is worthy of further studies.
ABSTRACT
OBJECTIVE:To prepare the Carboprost methyl-hydroxypropyl-β-cyclodextrin (HP-β-CD) clathrate sublingual tab-lets,and conduct quality evaluation. METHODS:Wet granulation method was used to prepare Carboprost methyl-HP-β-CD clath-rate sublingual tablets. Using the appearance,calving time,wetting time and main drug content as investigation indexes,mass ratio of mannitol-lactose,povidone volume fraction and amount of low-substituted hydroxypropylcellulose(L-HPC)as factors,orthogo-nal test was used to screen the formulation. The calving time,wetting time,main drug content,content uniformity,dissolution de-gree of sublingual tablets with optimal formulation were evaluated. RESULTS:The optimal formulation was as follow as 78.82 mg of carboprost methyl-HP-β-CD clathrate (containing carboprost methyl 1 mg),100 mg of mannitol-lactose (mass ratio of 9:1) mixed powder,appropriate amount of 2% povidone solution,30 mg of L-HPC,and 1 mg of magnesium stearate. The calving time of prepared 3 batches of sublingual tablets was(25.30±3.21)-(26.53±2.69)s;wetting time was(64.65±8.07)-(65.54±7.21)s;main drug content was (96.13 ± 0.43)%-(97.06 ± 0.82)%;content uniformity was 5.95-7.68;the cumulative dissolution degree within 10 min was more than 50%,and it can completely dissolute within 30 min. CONCLUSIONS:Carboprost methyl- HP-β-CD clathrate sublingual tablets,which are up to requirements,are prepared successfully.
ABSTRACT
Objective: To prepare 1% voriconazole ( VCZ) sulfonated butyl ether- β-cyclodextrin ( SBE-β-CD) inclusion com-pound eye drop and study the quality. Methods: VCZ SBE-β-CD inclusion compound was prepared with the molar ratio of VCZ to SBE-β-CD of 1 :1. Sodium chloride was used as the osmotic pressure regulator and benzalkonium bromide was employed as the pre-servative in the preparation of VCZ SBE-β-CD inclusion compound eye drop. The appearance, pH value, content stability and irritation of the eye drop were studied as well. Results:The eye drop was colorless and transparent solution with the pH value of 6. 44 ± 0. 20, 6. 50 ± 0. 15,6. 48 ± 0. 22 the osmotic pressure of (320 ± 4. 62),(316 ± 2. 88),(322 ± 2. 60)MOsm and the VCZ content of 1. 02% g ·ml-1 . The results of accelerated testing and long-term testing showed no notable changes in the quality indices. The eye drop exhibi-ted no significant irritation to the rabbit eyes. Conclusion:VCZ SBE-β-CD inclusion compound eye drop shows the properties of high VCZ content, stable quality and promising safety in eye application, which is worthy of further studies.