Hydrocortisone preparations

Nonprescription hydrocortisone preparations Temporary relief of itching associated with minor skin irritations, inflammation, and rashes caused by eczema, insect bites, poison ivy, poison oak, poison sumac, soaps, detergents, cosmetics, jewelry, seborrheic dermatitis, psoriasis, and external genital and anal itching. 

Hydrocortisone preparations BP PC All subject to limit on particle size of Hydrocortisone or Hydrocortisone Acetate. See Hydrocortisone Acetate Ointment BP, Hydrocortisone Cream BPC, Hydrocortisone and Neomycin Cream BPC, Hydrocortisone and Neomycin Ear Drops and Eye Drops BPC, Hydrocortisone Eye Ointment BPC, Hydrocortisone Lotion BPC and Hydrocortisone Suppositories BPC... 

With respect to the mechanism of side effects not much has been added in the period under review except the observation of decreased catabolism of exogenous corticosteroids as a factor in the development of side effects (96, 78 ). It has also been found that plasma cortisol showed little or no increase after intramuscular administration of cortisone-acetate, whereas a pronounced increase was observed after equimolar intramuscular administration of a hydrocortisone preparation (70 ). Whether this also applies to other 11-ketone corticosteroids as compared to the biologically active 11-hydroxy-compounds is not known. It seems, however, that patients with decreased hepatic function may have impaired ability to convert prednisone to the biologically active prednisolone (72, 93 ). For these patients prednisolone should be used. 

I60C-Hydroxy Derivatives of Gorticoids and their Acetonides. The preparation of 16a-hydroxy-9a-fluoroprednisolone (48) from the 3,20-bisethylene ketal of hydrocortisone acetate (49) has been reported (73). The latter was dehydrated with thionyl chloride in pyridine to yield the 4,9(11),16-triene (50). The 16,17-unsaturated linkage was selectively hydroxylated with OsO /pyridine to yield the 16a,17a-diol (51), which was converted... 

Methylation of hydrocortisone/prednisolone ia positions C-4, C-7, C-12, and C-21 failed to give useful products. Methylation at C-16, ia contrast, led to 16a- and 16P-methyl-9a- uoroprednisolones which were exceptionally useful. Both series were prepared usiag 3a-acetoxy-5a-pregn-16-ene-ll,20-dione derived from desoxychoHc acid (80). A much shorter route was subsequentiy developed from... 

Crystallization and Purification Solvent. Dimethylacetamide is useful ia the purification by crystallization of aromatic dicarboxyHc acids such as terephthahc acid [100-21-0] and/vcarboxyphenylacetic acid [501-89-3]. These acids are not soluble ia the more common solvents. DMAC and dibasic acids form crystalline complexes containing two moles of the solvent for each mole of acid (16). Microcrystalline hydrocortisone acetate [50-03-3] having low settling rate is prepared by crystallization from an aqueous DMAC solution (17). 

The principal OTC pharmaceutical products include cold remedies, vitamins and mineral preparations, antacids, analgesics, topical antibiotics, antiftingals and antiseptics, and laxatives. Others include suntan products, ophthalmic solutions, hemorrhoidal products, sleep aids, and dermatological products for treatment of acne, dandmff, insect parasites, bums, dry skin, warts, and foot care products (11). More recent prescription-to-OTC switches have included hydrocortisone, antihistamine and decongestant products, antiftingal agents, and, as of 1995, several histamine H2-receptor antagonists. 

C22H24N2O, or trimethoprim [738-70-5] These preparations may also contain an antiinflammatory corticoid such as hydrocortisone... 

Many functional groups are stable to alkaline hydrogen peroxide. Acetate esters are usually hydrolyzed under the reaction conditions although methods have been developed to prevent hydrolysis.For the preparation of the 4,5-oxiranes of desoxycorticosterone, hydrocortisone, and cortisone, the alkali-sensitive ketol side chains must be protected with a base-resistant group, e.g., the tetrahydropyranyl ether or the ethylene ketal derivative. Sodium carbonate has been used successfully as a base with unprotected ketol side chains, but it should be noted that some ketols are sensitive to sodium carbonate in the absence of hydrogen peroxide. The spiroketal side chain of the sapogenins is stable to the basic reaction conditions. 

During the preparation of the dihalo-(usually dibromo) 20-ketopregnanes, other reactive sites must be protected (e.g., addition of bromine to the A -double bond, ketal formation with a 3-ketone). An elegant method which avoids such problems has been devised by the Upjohn group in their studies on the conversion of 11-ketoprogesterone to hydrocortisone. The former is reacted with ethyl oxalate at C-2 and C-21, then addition of three moles of bromine gives a 2,21,21-tribromide. Alkaline rearrangement produces the side chain unsaturated acid, and the bromine at C-2 is subsequently removed with zinc. 

A-norsteroids (59) of the cholestane, androstane, pregnane and hydrocortisone series have been prepared from the diols (61)." However, preparation of these 1,2-diols is complicated by concomitant formation of isomeric 4,5-diols, which are usually difficult to separate. The sequence (58) -> (59) appears to be the most practical route to A-norsteroids (59), provided that diosphenol (58) is readily available. 

Other Formulations. Neural networks have been applied to the modeling of pellet formulations to control the release of theophylline [63] and to control the rate of degradation of omeprazole [64]. They have also been applied to the preparation of acrylic microspheres [65] and to model the release of insulin from an implant [66]. In arecent study from Brazil, the release of hydrocortisone from a biodegradable matrix has been successfully modeled [67]. 

Oxytetracycline preparations for oral administration should contain not less than 90% or not more than 120% [i] or not less than 90% and not more than 110% [2], of the labeled amount. For ointment, the requirements are not less than 90.0% and not more than 115% (for oxytetracycline HC1 and Hydrocortisone ointment, or 120% for other ointment. For ophthalmic suspension mixture with hydrocortisone acetate, its content should contain not less than 90% and not more than 110% [1]. 

Galego and Arroyo [14] described a simultaneous spectrophotometric determination of OTC, hydrocortisone, and nystatin in the pharmaceutical preparations by using ratio spectrum-zero crossing derivate method. The calculation was performed by using multivariate methods such as partial least squares (PLS)-l, PLS-2, and principal component regression (PCR). This method can be used to resolve accurately overlapped absorption spectra of those mixtures. 

What is the percentage of ophthalmic hydrocortisone ointment prepared by mixing 10 grams of 2.5% hydrocortisone ointment, 8 g of 2% hydrocortisone ointment, and 14 g of ointment base (diluent) ... 

Materials Required Hydrocortisone acetate 0.350 g aldehyde-free absolute ethanol 100 ml triphenyltetrazolium chloride solution [a 0.5% w/v solution of 2,3,5, -triphenyltetrazolium chloride in aldehyde-free ethanol (96%)] 10 ml dilute tetramethylammonium hydroxide solution [Dilute 10 ml of tetramethylammonium hydroxide solution (10%) to 100 ml with aldehyde-free ethanol (96%). It contains about 1% w/v of C4H13NO. To be prepared immediately before use] 10 ml. 

Daktacort cream is a trade name for a preparation containing miconazole (imidazole antifungal) and hydrocortisone (corticosteroid). 

Triamcinolone is a corticosteroid that is more potent than hydrocortisone and has a longer duration of action. Triamcinolone has only slight mineralocorticoid activity, whereas hydrocortisone has high mineralocorticoid activity and therefore triamcinolone is unsuitable for disease suppression on a long-term basis. Triamcinolone is available as injection, dental paste, nasal spray and as cream or ointment preparations. Hydrocortisone is available as cream, tablets and injections. 

Docusate sodium is a preparation used for softening ear wax before removal. Hydrocortisone is a corticosteroid, whereas gentamicin, neomycin and clioquinol are antibacterial agents. Otitis externa may be managed by the use of antibacterial preparations used alone or in combination with topical corticosteroids. 

Proprietary preparations of hydrocortisone for skin administration present a low-potency corticosteroid for topical skin administration. 

Q7 A pharmacist is required to dispense 30 g of 0.5% hydrocortisone ointment. The pharmacist has available o hydrocortisone ointment 1%. Hov/ many grams of the 1% ointment could be diluted v/ith v/hite soft paraffin to prepare this order ... 

Excellent separations of corticosteroids can be achieved on an ODS column with a suitable ratio of methanol/water as an eluent. In this assay hydrocortisone is quantified using betamethasone as an internal standard. The structure of betamethasone is close to that of hydrocortisone but since it is more lipophilic it elutes from the ODS column after hydrocortisone (Fig. 12.12). The assay is a modification of the BP assay for hydrocortisone cream. In the assay described here the internal standard is added at the first extraction step rather than after extraction has been carried out in order to ensure that any losses in the course of sample preparation are fully compensated for. Extraction is necessary in the case of a cream because the large amount of oily excipients in the basis of the cream would soon clog up the column if no attempt was made to remove them. The corticosteroids are sufficiently polar to remain in the methanol/water layer as they have a low solubility in hexane, while the oily excipients are removed by extraction into hexane. The sodium chloride (NaCl) is included in the sample extraction solution to prevent the formation of an emulsion when the extract is shaken with hexane. Solution 2, where the internal standard is omitted, is prepared in order to check that there are no excipients in the sample which would interfere with the peak due to the internal standard. 

Stated content of hydrocortisone cream = 1% w/w Weight of hydrocortisone cream used to prepare solution 3 = 1.173 g Area of hydrocortisone peak in Solution 1 = 103 026 Area of betamethasone peak in Solution 1 = 92 449 Area of hydrocortisone peak in Solution 3=113 628 Area of betamethasone peak in Solution 3 = 82 920 Concentration of hydrocortisone in the solution used in the preparation of Solution 1 = 0.1008% w/v... 

Analysis Is carried out on a cream stated to contain 2% w/w of both miconazole and hydrocortisone. An ODS column is used with a mobile phase consisting of acetonitrile/ acetate buffer pH 4.0 (70 30) and the eluent is monitored at 220 nm. A narrow range calibration curve, within 20% of the expected concentration of each analyte in the sample extract was prepared for each analyte by plotting the ratio of the areas of the analyte peaks against fixed amounts of the internal standards for both analytes. The internal standards used were econazole and hydrocortisone 21-acetate for miconazole and hydrocortisone, respectively. 

The original synthesis of 9-fluorocorticoid by Fried involves the opening the 9, 11-epoxy hydrocortisone acetate by HF. This oxirane is prepared in two steps from hydrocortisone acetate. This synthesis still remains the only method to prepare 9-fluorocorticoids (Fig. 55) [130], To date, there is no alternative known method for this purpose [136],... 

This reaction was applied (with various modifications) to the estimation of corticosteroids in pharmaceutical preparations [78, 79], and also for the estimation of hydrocortisone and cortisone in admixtures of the two [80]. 

System (6) was recommended for the analysis of hydrocortisone, cortisone, and their acetates in pharmaceutical preparations, as well as their separation from a number of impurities and decomposition products [154]. The sample (creams, ointments, lotions, or suppositories) was extracted with hot ethanol prior to introduction into the HPLC system. 

Cream (Rectal) 1% (Nupercainal Hydrocortisone Cream, Cortizone-10, Preparation H Hydrocortisone, Proctocort, Procto-Kit 1%), 2.5%(Anusol-HC, Hemorrhoidal HC, Procto-Kit 2.5%, Proctosol-HC, Proctozone-HC). 

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