ABSTRACT
To evaluate the traits and rheological properties of thermosensitive in situ gel of Yihuang Decoction and its common gel for vaginal use, and predict the release behavior of Yihuang Decoction in situ gel in vitro. Poloxamer was used as thermosensitive material to prepare Yihuang Decoction vaginal in situ gel, and Yihuang Decoction common gel was prepared with carbopol. Then the differences of the two gels before and after diluting with vaginal fluid were compared. The rheological parameters of Yihuang Decoction in situ gel and its common gel were determined with Anton Paar MCR102 rheometer. In addition, berberine hydrochloride was selected as an index component to evaluate the in vitro release properties of Yihuang Decoction vaginal thermosensitive in situ gel. Yihuang Decoction vaginal thermosensitive in situ gel was Newtonian fluid under low-temperature conditions, which was yellow and transparent. After reaching the gelling temperature of 24.5 ℃, it became semi-solid, pseudoplastic fluid. The gelling temperature was predicted to be 37 ℃, and the phase transition time was 30 s after diluting with simulated vaginal fluid. However, the rheological properties of Yihuang Decoction common gel had no significant changes with temperature. Compared with in situ gel, the color of common gel was darker and more translucent. Besides, its mobility was stronger after diluting with simulated vaginal fluid. The in vitro release study showed that the kinetic behavior of berberine hydrochloride in Yihuang Decoction vaginal thermosensitive in situ gel was matched with the Higuchi equation. Through simulation of vaginal administration, physical properties and dynamic rheological parameters were used to intuitively and scientifically evaluate the two gels. Compared with the common gel, the thermosensitive in situ gel could quickly attached to the vaginal mucosa and release drug, and thus was more suitable for developing vaginal administration of Yihuang Decoction, which also provides references for studying new vaginal preparation of Yihuang Decoction.
Subject(s)
Female , Humans , Administration, Intravaginal , Drugs, Chinese Herbal/chemistry , Gels/chemistry , Poloxamer , Rheology , Temperature , ViscosityABSTRACT
Paclitaxel (PTX) is a complex secondary metabolite isolated from Taxus brevifolia, which widely used as chemotherapentic agent with a broad spectrum of actinity against cancer in the world. Its water solubility was poor and oral bioavailability was low. Cremophor-EL was used in traditional PTX injections to improve the solubility of PTX, and resulted in several adverse side effects such as severe hypersensitivity. Pre-desensitization treatment was needed before clinical use. Recently, a variety of non-injection drug delivery systems (DDS) of PTX have been developed. In this paper, the research progress of non-parenteral PTX was reviewed, including oral administration systems, vaginal administration systems, transdermal DDS, implantable DDS, transdermal DDS, intranasal administration and inhalation DDS, so as to provide references for future study and clinical applications.
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Objective: A selective and sensitive ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method was employed to study the pharmacokinetics of ginsenoside Re (GRe) in rabbits after vaginal administration of Xiaomi suppository to evaluate the systemic exposure of the suppository for the local treatment. Methods: Chromatographic separation was on an ACQUITY UPLC® BEH C18 column, and acetonitrile-0.1% formic acid was used as mobile phase in gradient elution. The plasma samples were deproteinized by acetonitrile, and the pharmacokinetic parameters were calculated by Winnonlin 6.4. Results: Calibration curve of GRe showed a good linearity over the concentration range from 5 ng/mL to 500 ng/mL (r = 0.9999). The low limit of quantification of 5 ng/mL could satisfy the experimental requirement. The intra-day and inter-day precision of GRe at three concentrations were less than 1.96%, and the average recoveries of GRe were more than 64.0%. The pharmacokinetic parameters for vaginal administration were as follows: Tmax, 0.5 h; Cmax, 20.88 ng/mL; AUC0-t, 64.71 h · ng/mL and the residence time was 3.06 h. By using deconvolution calculation method, the cumulative absorption fraction of GRe was about 0.89%. Conclusion: The systemic exposure of GRe was minimal after vaginal administration of Xiaomi suppository.
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Vaginal delivery system has a unique therapeutic advantage. In recent years, the rapid development of dosage forms shows a good prospect of development. The related literatures at home and abroad in recent years were analyzed and summarized. The research progress in the drug absorption model of various vaginal administrations was reviewed. The review provided reference for the research of new drug preparations and drug absorption mechanisms of vaginal administration.
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Curcumin is the main active component in turmeric, which possesses many pharmacologic effects, including anti-in-flammatory, antioxidant, anti-tumor, anti-atherosclerosis, liver and kidney protection and so on. However, due to its poor bioavail-ability, its clinical application is limited. Therefore, the methods for improving the bioavailability of curcumin were reviewed by refer-ring to a large number of literatures. The bioavailability of curcumin can be improved by different administration routes and various dos-age forms. The review provides theoretical basis and research ideas for the development of new drugs.
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OBJECTIVE:To investigate therapeutic efficacy and recurrence rate of vaginal administration of lactobacillus com-bined with chlorquinaldol-promestriene for senile patients with atrophic vaginitis. METHODS:150 senile patients with atrophic vag-initis were selected and divided into group A,B,C according to random number table,with 50 cases in each group. Group A was given Lactobacillus vaginal capsules,2 capsules,qd (at bedtime);group B given Chlorquinaldol-promestriene vaginal tablets,1 tablet,qd(at bedtime);group C given Chlorquinaldol-promestriene vaginal tablets,1 tablet,qd(at bedtime),and Lactobacillus vaginal capsules,2 capsules,qd,next morning,implanting into vagina. 3 groups received treatment for 18 d. Clinical efficacy, vaginal health score,vaginal symptom score and vaginal pH value were observed in 3 groups,and the occurrence of ADR and re-currence rate during follow-up period (12 months) were recorded. RESULTS:The total effective rate of group C was 94.00%, which was significantly higher than group A(72.00%)and B(74.00%),with statistical significance(P0.05). After treatment,vaginal health score of 3 groups were increased significantly,while vaginal symptom score and vaginal pH value were decreased significantly;and the improvement of above indexes in group C were significantly better than in group A and B,with statistical significance(P<0.05). No obvious ADR was found in 3 groups during treatment. The recurrence rate of group C during follow-up period(4.00%)was significantly lower than that of group A(18.00%)and group B(20.00%),with statistical significance(P<0.05). CONCLUSIONS:Vaginal administration of lactobacillus combined with chlorquinaldol-promestriene for se-nile patients with atrophic vaginitis can effectively relieve clinical symptoms and signs,improve vaginal cleanliness,regulate the lo-cal pH value and reduce the risk of recurrence,with good safety.
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OBJECTIVE: To compare the effectiveness of oral misoprostol with vaginal misoprostol administration in mid-trimester pregnancy termination after pretreatment with serial laminarias tenting. METHODS: This study was made in 50 patients for mid-trimester pregnancy termination at Department of Obstetrics and Gynecology, Chonbuk National University Hospital from January 1999 through December 2002. Twenty five women received misoprostol orally in a dose of 200 micro gram every hour for 3 doses followed by 400 micro gram every 4 hours after serial laminarias tenting. Twenty five women received misoprostol vaginally in a dose of 400 micro gram every 4 hours after serial laminarias tenting. Side effects of drug, induction to delivery interval, delivery numbers within 24 hours, curettage numbers for retained placenta, and the length of hospital stay were compared. RESULTS: The mean time of induction to delivery interval was significantly shorter in the vaginal group (15.5 +/- 12.7 vs 24.2 +/- 14.3 hours, p<0.01). The length of hospital stay was also shorter in the vaginal group (38.9 +/- 13.1 vs 47.2 +/- 14.5 hours, p<0.01). The number of patients delivered within 24 hours was more in the vaginal group (92 vs 72%, p<0.05). The side effects of misoprostol were slightly more common in the oral group than the vaginal group without statistical significance. CONCLUSION: We suspect that after serial tenting of laminarias, intravaginal misoprostol appears to be more safe and effective than oral misoprostol for mid-trimester termination.