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In this study, PVP-gossypol complexes with different molecular weights and compositions were synthesized. UV and NMR spectra revealed the presence of hydrogen bonds in these complexes. The dissolution rates of various PVP-gossypol complexes in water at 37 degrees C were determined. The results showed that the presence of PVP in the complex enhanced the dissolution rate of gossypol in water greatly. In addition, the in vitro spermicidal activity on human semen, antifertility effect on male rats, and the toxic reaction of male mice by taking large dosage were preliminarily studied. The experimental results indicated that the PVP-gossypol complexes not only possessed the similar antifertility effect and acute toxicity to male mice as gossypol-acetic acid, but also reduced the irreversibility of the fertility as well. Thus, certain species of PVP-gossypol complex may have potential as new and better male oral contraceptive with recoverability in fertility.