Fluocinolone Acetonide   中文名称: 醋酸氟轻松

使用氟轻松（0.1-50 μg/mL，两天）可以提高泡沫细胞的存活率[1]。氟轻松（0.1–50 μg/mL，2 天）可降低胆固醇酯的积累并抑制炎症细胞因子的释放 [1]。 Fluocinolone（0.1-100 μmol/L，24 小时）刺激 DPC 生长 [2]。 Fluocinolone（1-10 μmol/L，7 天）上调牙本质特异性标记物牙本质唾液酸磷蛋白的表达，并上调 BSP、OCN、DSPP 和 Wnt4 [2]。

在 PTX 产生的小鼠模型中，氟轻松（500 μg/kg，腹腔注射，每天一次，持续两周）抑制严重周围神经病变的发展 [3]。

细胞增殖检测[2]
细胞类型： DCP
测试浓度： 0.1 μmol/L、1 μmol/L、10 μmol/L、20 μmol /L、40 μmol/L、60 μmol/L、100 μmol/L
孵育时间： 24 h
实验结果： 显着促进生长速度低浓度的 DPC。

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蛋白质印迹分析[2]
细胞类型： DCP
测试浓度： 1 μmol/L、10 μmol/L
孵育时间：7天
实验结果：表明DSPP和Wnt4蛋白的表达高于阴性对照。

Animal/Disease Models: PTX-induced peripheral neuropathy model [3]
Doses: 500 μg/kg
Route of Administration: intraperitoneal (ip)injection
Experimental Results: Prevented a marked reduction in intraepidermal nerve fibers density in the plantar surface of the hind paws.

Absorption, Distribution and Excretion
When administered as an eye implant, fluocinolone acetonide presents a sustained delivery for even 12 months in which there can be observed a sustained release. The concentration of fluocinolone acetonide are generally higher in the vitreous and retina with a little dispersion to the aqueous humor. There are reports indicating that topical administration of fluocinolone acetonide produces a percutaneous absorption which is determined by the vehicle, integrity of the epidermal barrier and the use of occlusive dressing. Independently of the route of administration, the systemic absorption of fluocinolone acetonide is below 0.1 ng/ml which indicates that the systemic distribution is very minimal and the effect of fluocinolone is mainly local.
Fluocinolone acetonide is mainly excreted by the kidneys. It is important to mention that the systemically absorbed dose is very minimal.
This pharmacokinetic parameter is not relevant as the systemic absorption of fluocinolone acetonide is very minimal.
This pharmacokinetic parameter is not relevant as the systemic absorption of fluocinolone acetonide is very minimal and the concentration in urine is lower than the minimum quantitation limit.
METABOLISM OF CORTICOSTEROIDS IS GREATLY SLOWED BY INTRODUCTION OF THE 1,2 DOUBLE BOND OR A FLUORINE ATOM INTO MOLECULE, & HALF-LIFE IS CORRESPONDINGLY PROLONGED. /CORTICOSTEROIDS/
(14)C WAS RAPIDLY & MAINLY EXCRETED IN 48-HR FECES (90%), VIA BILE (70% IN 24 HR), & IN URINE (8%). AFTER DERMAL APPLICATION OF CREAM CONTAINING [(14)C]FLUOCINOLONE ACETONIDE TO MICE, GREATER THAN 7% OF (14)C WAS ABSORBED.
...WITHIN 1 HR OF SC DOSE OF [(14)C]FLUOCINOLONE ACETONIDE TO MICE, LARGE AMT...PRESENT IN LIVER & INJECTION SITE, LOWER AMT IN PANCREAS, KIDNEYS, SALIVARY GLANDS, MYOCARDIUM, PITUITARY, & LACRIMAL GLANDS. TISSUE (14)C DECR FAIRLY RAPIDLY DURING 24 HR, EXCEPT IN LIVER & INTESTINES, BECAUSE OF BILIARY SECRETION...
PENETRATION OF...FLUOCINOLONE ACETONIDE...TOPICALLY APPLIED, THROUGH HUMAN ABDOMINAL SKIN WAS OPTIMAL WHEN CONCN OF DRUGS WAS MAXIMAL WHILE MAINTAINING FAVORABLE PARTITION COEFFICIENT BETWEEN SKIN BARRIER & VEHICLE.
For more Absorption, Distribution and Excretion (Complete) data for FLUOCINOLONE ACETONIDE (6 total), please visit the HSDB record page.

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Metabolism / Metabolites
Following absorption, fluocinolone acetonide metabolism is primarily hepatic. It is important to mention that the systemically absorbed dose is very minimal.
...IT IS GENERALLY ASSUMED THAT METAB OF /CORTISOL &/ ITS CONGENERS & SYNTH DERIV IS QUALITATIVELY SIMILAR. ...METABOLIZED PRINCIPALLY BY REDN OF RING A, REDN OF KETONE AT C 20, & CLEAVAGE OF SIDE CHAIN. METABOLITES ARE EXCRETED...AS GLUCURONIDES, SULFATES, & UNCONJUGATED COMPOUNDS. /CORTICOSTEROIDS/

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Biological Half-Life
The reported half-life of fluocinolone acetonide ranges between 1.3-1.7 hours.

Protein Binding
This pharmacokinetic parameter is not relevant as the systemic absorption of fluocinolone acetonide is very minimal.

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Interactions
REVERSAL OF CORTICOSTEROID-INDUCED IMPAIRMENT OF WOUND HEALING HAS BEEN REPORTED AFTER TOPICAL APPLICATION OF VITAMIN /VITAMIN A/. /CORTICOSTEROIDS/

[1]. The potential of fluocinolone acetonide to mitigate inflammation and lipid accumulation in 2D and 3D foam cell cultures . BioMed Research International, 2018, 2018.

[2]. Fluocinolone acetonide promotes the proliferation and mineralization of dental pulp cells . Journal of endodontics, 2013, 39(2): 217-222.

[3]. Identification of fluocinolone acetonide to prevent paclitaxel‐induced peripheral neuropathy . Journal of the Peripheral Nervous System, 2016, 21(3): 128-133.

[4]. Glucocorticoids with different chemical structures but similar glucocorticoid receptor potency regulate subsets of common and unique genes in human trabecular meshwork cells . BMC medical genomics, 2009, 2(1): 1-14.

[5]. http://en.wikipedia.org/wiki/Fluocinolone_acetonide.

[6]. Glucocorticoids with different chemical structures but similar glucocorticoid receptor potency regulate subsets of common and unique genes in human trabecular meshwork cells. BMC Med Genomics, 2009. 2: p. 58.

Therapeutic Uses
Glucocorticoids, Synthetic; Glucocorticoids, Topical
WITH EXCEPTION OF SUBSTITUTION THERAPY, USE OF CORTICOSTEROIDS & THEIR CONGENERS IN DISEASE IS EMPIRICAL. ...FOR ANY DISEASE, IN ANY PT, APPROPRIATE DOSE TO ACHIEVE GIVEN THERAPEUTIC EFFECT MUST BE DETERMINED BY TRIAL & ERROR & MUST BE REEVALUATED FROM TIME TO TIME AS STAGE & ACTIVITY OF DISEASE ALTER... /CORTICOSTEROID/
GLUCOCORTICOID WITH POTENT ANTI-INFLAMMATORY & METABOLIC ACTIONS & NEGLIGIBLE MINERALOCORTICOID ACTIONS.
IT IS EMPLOYED TOPICALLY IN TREATMENT OF VARIOUS DERMATOSES. IN RESISTANT NUMMULAR DERMATITIS, PSORIASIS, OR CHRONIC NEURODERMATITIS USUALLY USED UNDER OCCLUSIVE DRESSINGS.
For more Therapeutic Uses (Complete) data for FLUOCINOLONE ACETONIDE (7 total), please visit the HSDB record page.

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Drug Warnings
...AS CORTICOSTEROID THERAPY IS PROLONGED OVER PERIODS OF MO, & TO EXTENT THAT DOSE EXCEEDS EQUIV OF SUBSTITUTION THERAPY, INCIDENCE OF DISABLING & POTENTIALLY LETHAL EFFECTS INCR; EXCEPT IN ADRENAL INSUFFICIENCY, ADMIN...IS NEITHER ETIOLOGICAL OR CURATIVE THERAPY BUT ONLY PALLIATIVE...ANTI-INFLAMMATORY... /CORTICOSTEROIDS/
EVEN IN INSTANCES IN WHICH NEARLY WHOLE BODY HAS BEEN COVERED BY CREAM CONTAINING CORTICOID, EVIDENCES OR SYSTEMIC SIDE EFFECTS ARE RARE. ... TOPICAL FLUOCINOLONE IS CONTRAINDICATED IN PRESENCE OF TUBERCULOSIS, FUNGAL INFECTIONS, & MOST VIRAL LESIONS OF SKIN (VACCINIA, VARICELLA, HERPES SIMPLEX, ETC).
...CAUTION SHOULD BE EXERCISED IF FLUORINATED PREPN ARE USED ON FACE OR OTHER COSMETICALLY IMPORTANT AREAS, SINCE PARADOXICAL SKIN ERUPTIONS MAY OCCUR WITH LONG-TERM USE.
VET: SOLN IN PROPYLENE GLYCOL USUALLY PRODUCES FAR MORE THAN "TRANSIENT STINGING SENSATION" DESCRIBED BY MFR & SHOULD BE AVOIDED ESP ON RAW OR DENUDED AREAS.
For more Drug Warnings (Complete) data for FLUOCINOLONE ACETONIDE (7 total), please visit the HSDB record page.

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Pharmacodynamics
Fluocinolone acetonide is a synthetic anti-inflammatory corticosteroid and thus, the effect of its interaction with the body produces vasoconstriction and suppression of membrane permeability, mitotic activity, immune response and release of inflammatory mediators. For its ophthalmic indications, fluocinolone acetonide is administered as intravitreal micro-insert. This preparation was observed in clinical trials to reduce the recurrence of uveitis flares by 2 fold when compared with the non treated patients even after six months after initial administration. As well the intraocular pressure seemed to increase slightly with the presence of the fluocinolone implant but it is important to monitor intraocular pressure.

C24H30F2O6

452.49

452.201

67-73-2

6215

White to off-white solid powder

1.4±0.1 g/cm3

578.5±50.0 °C at 760 mmHg

267-269 °C(lit.)

303.7±30.1 °C

0.0±3.6 mmHg at 25°C

1.577

2.24

93.06

2

8

2

32

960

9

C[C@]12C[C@@H]([C@]3([C@H]([C@@H]1C[C@@H]4[C@]2(OC(O4)(C)C)C(=O)CO)C[C@@H](C5=CC(=O)C=C[C@@]53C)F)F)O

FEBLZLNTKCEFIT-VSXGLTOVSA-N

InChI=1S/C24H30F2O6/c1-20(2)31-19-9-13-14-8-16(25)15-7-12(28)5-6-21(15,3)23(14,26)17(29)10-22(13,4)24(19,32-20)18(30)11-27/h5-7,13-14,16-17,19,27,29H,8-11H2,1-4H3/t13-,14-,16-,17-,19+,21-,22-,23-,24+/m0/s1

(1S,2S,4R,8S,9S,11S,12R,13S,19S)-12,19-difluoro-11-hydroxy-8-(2-hydroxyacetyl)-6,6,9,13-tetramethyl-5,7-dioxapentacyclo[10.8.0.02,9.04,8.013,18]icosa-14,17-dien-16-one

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

配方 1 中的溶解度: ≥ 2.08 mg/mL (4.60 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 20.8 mg/mL澄清DMSO储备液加入400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.08 mg/mL (4.60 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 20.8 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 2.08 mg/mL (4.60 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 20.8 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。