丹参益肝自微乳滴丸的制备工艺研究
|
摘要
目的研究丹参益肝自微乳滴丸的制备工艺。方法考察丹参酮提取物在不同油相中的溶解度,利用微乳外观等级评分及伪三元相图法优化自微乳处方,进一步固化制备丹参益肝自微乳滴丸,并对丹参益肝自微乳滴丸的释放度进行考察。结果丹参益肝自微乳的最佳处方为:EO为油相,Cremophor RH40为乳化剂,无水乙醇为助乳化剂。Km值为2:1;选择油相和混合乳化剂比例为3:7。将制备成的载药油状物,按1:2.5比例加入PEG 6000,于70℃熔融,以6 cm滴距、30 d/min滴速滴入二甲基硅油中,制备成滴丸。丹参益肝自微乳滴丸在不同释放介质中10 min内的累积释放率均在90%左右。结论该制备工艺稳定可行,适合大工业生产。
Objective To study the preparation technology of Danshen Yigan microemulsion dropping pill.Methods The solubility of tanshinone extracts in different oil phases was investigated. The microemulsion appearance grade and pseudo-ternary phase diagram were used to optimize the selfmicroemulsion formulation, and the Danshen Yigan microemulsion pills were further solidified. The release of microemulsion dropping pills was investigated. Results The best prescription of Danshen Yigan microemulsion was EO as oil phase, Cremophor RH40 as emulsifier and absolute ethanol as emulsifier. Km value of 2:1; select the oil phase and mixed emulsifier ratio of 3:7. The prepared oilcontaining oil was added into PEG 6000 at a ratio of 1:2.5, melted at 70 ℃ and dripped into dimethyl silicone oil at a dropping rate of 6 cm and a rate of 30 d/min. The cumulative release rate of Danshen Yigan microemulsion dropping pills in different release media was about 90 % within 10 min.Conclusion The preparation process is stable and feasible, suitable for large-scale industrial production.
Objective To study the preparation technology of Danshen Yigan microemulsion dropping pill.Methods The solubility of tanshinone extracts in different oil phases was investigated. The microemulsion appearance grade and pseudo-ternary phase diagram were used to optimize the selfmicroemulsion formulation, and the Danshen Yigan microemulsion pills were further solidified. The release of microemulsion dropping pills was investigated. Results The best prescription of Danshen Yigan microemulsion was EO as oil phase, Cremophor RH40 as emulsifier and absolute ethanol as emulsifier. Km value of 2:1; select the oil phase and mixed emulsifier ratio of 3:7. The prepared oilcontaining oil was added into PEG 6000 at a ratio of 1:2.5, melted at 70 ℃ and dripped into dimethyl silicone oil at a dropping rate of 6 cm and a rate of 30 d/min. The cumulative release rate of Danshen Yigan microemulsion dropping pills in different release media was about 90 % within 10 min.Conclusion The preparation process is stable and feasible, suitable for large-scale industrial production.
引文
[1]中国药典[S].一部.2015.
[2]马丙祥,董宠凯.丹参的药理作用研究新进展[J].中国药房,2014,25(7):663~665.
[3]Patel AR,Vavia PR.,Preparation and in vivo evaluation of SMEDDS(self-microemulsifying drug delivery system)containing fenofibrate.AAPS J,2007,9:E344-E352.
[4]Kommuru TR,Gurley B,Khan MA,Reddy IK.Self-emulsifying drug delivery systems(SEDDS)of coenzyme Q10:formulation development and bioavailability assessment.Int J Pharm,2001,212:233~246.
[5]Tang B,Cheng G,Gu JC,Xu CH.Development of solid self-emulsifying drug delivery systems:preparation techniques and dosage forms.Drug Discov Today,2008,13:606~612
[6]Serratoni M,Newton M,Booth S,et al.Controlled drug release from pellets containing water-insoluble drugs dissolved in a self-emulsifying system[J].Eur J Pharm Biopharm,2007,65(1):94~99.
[7]Amri A,Le Clanche S,Therond P,BonnefontRousselot D,Borderie D,Lai-Kuen R,et al.Resveratrol self-emulsifying system increases the uptake by endothelial cells and improves protection against oxidative stress-mediated death.Eur J Pharm Biopharm.2014,86(3):418~26.
[8]Weerapol Y,Limmatvapirat S,KumpugdeeVollrath M,Sriamornsak P.Spontaneous emulsification of nifedipine-loaded self-nanoemulsifying drug delivery system.AAPS Pharm Sci Tech.2014,1-9.doi:10.1208/s12249-014-0238-0.
[9]Patel D,Sawant K K.Self micro-emulsifying drug delivery system:formulation development and biopharmaceutical evaluation of lipophilic drugs[J].Curr Drug Deliv,2009,6(4):419~424.
[2]马丙祥,董宠凯.丹参的药理作用研究新进展[J].中国药房,2014,25(7):663~665.
[3]Patel AR,Vavia PR.,Preparation and in vivo evaluation of SMEDDS(self-microemulsifying drug delivery system)containing fenofibrate.AAPS J,2007,9:E344-E352.
[4]Kommuru TR,Gurley B,Khan MA,Reddy IK.Self-emulsifying drug delivery systems(SEDDS)of coenzyme Q10:formulation development and bioavailability assessment.Int J Pharm,2001,212:233~246.
[5]Tang B,Cheng G,Gu JC,Xu CH.Development of solid self-emulsifying drug delivery systems:preparation techniques and dosage forms.Drug Discov Today,2008,13:606~612
[6]Serratoni M,Newton M,Booth S,et al.Controlled drug release from pellets containing water-insoluble drugs dissolved in a self-emulsifying system[J].Eur J Pharm Biopharm,2007,65(1):94~99.
[7]Amri A,Le Clanche S,Therond P,BonnefontRousselot D,Borderie D,Lai-Kuen R,et al.Resveratrol self-emulsifying system increases the uptake by endothelial cells and improves protection against oxidative stress-mediated death.Eur J Pharm Biopharm.2014,86(3):418~26.
[8]Weerapol Y,Limmatvapirat S,KumpugdeeVollrath M,Sriamornsak P.Spontaneous emulsification of nifedipine-loaded self-nanoemulsifying drug delivery system.AAPS Pharm Sci Tech.2014,1-9.doi:10.1208/s12249-014-0238-0.
[9]Patel D,Sawant K K.Self micro-emulsifying drug delivery system:formulation development and biopharmaceutical evaluation of lipophilic drugs[J].Curr Drug Deliv,2009,6(4):419~424.