盐酸普萘洛尔凝胶的制备及质量评价

Preparation and in vitro quality evaluation of hydrochloride propranolol gel

目的制备用于婴幼儿血管瘤的盐酸普萘洛尔(PPL.HCl)外用凝胶,并对其进行质量评价。方法以羟丙甲基纤维素(HPMC)为基质,用直接溶胀法制备PPL.HCl凝胶。以体外经皮累积渗透量(Q)为指标,筛选HPMC用量和载药量;并以锥入度、pH值、家兔皮肤刺激性等为指标,对凝胶进行评价。结果 HPMC用量为2.5%,载药量为5%时,PPL.HCl凝胶具有最高的经皮累积渗透量,凝胶外观呈乳白色半固态、细腻均匀,pH约为7.0,40℃恒温条件下保存30d稳定。单次、多次给予家兔正常及破损皮肤均无刺激性。结论所制PPL.HCl凝胶性质稳定,质量可控。该制剂为PPL.HCl外用治疗血管瘤的研究开发奠定了基础。

Objective To prepare hydrochloride propranolol （PPL · HCI） gel for infantile hemangioma and to evaluate its quality in vitro. Methods With HPMC as the matrix, PPL·HC1 gel was prepared by direct swelling method. The concentration of HPMC and PPL·HC1 was screened by accumulated permeation quantity in vitro. The cone penetra- tion, pH value and skin irritation were used as evaluation index. Results We found 2.5% HPMC and 5% PPL·HC1 were optimized, showing good appearance, optimum consistency, pH of about 7.0 and great enhancement of PPL· HC1 permeability. The PPL·HC1 gel was kept stable at 40℃ for 30 d. Both single or multiple doses of PPL· HC1 gel showed no irritation. Conclusion PPL·HC1 gel has been prepared with stable characteristics and quality control, which provides experimental basis for further research on topical infantile hemangioma.